result and discussion 6
TRANSCRIPT
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Results
RESULT AND DISCUSSION
3.3 EVALUATION AND OPTIMIZATION OF FLOATING
TABLETS
3.3.1. Physical paa!"#"s
3.3.1.A Si$" a%& Shap": - The shape tablets were evaluated visually and the
size particularly thickness was measured with the help of screw gauge.
3.3.1.B '"i(h# Vaia#i)%: - The individual of 20 tabletss from each batch
were weighed accurately to determine the weight variations. As per the !" all the
tablets must within the the range of # $. The sample mean and standard deviation of
each batch of tablets were determined %table&.
3.3.1.C *a&%"ss: - The hardness individual '0 tablets from each batch were
determined with the help of "fizer hardness tester and the sample mean and standard
deviation were calculated for each batch %table&.
3.3.1.D Fia+ili#y, - (t was determined with )oche friabilator apparatus
%*icon+ (ndia&. ,ollowing formula was used to determination of friability:
,riability %(nitial wt - ,inal wt (nitial wt & / '00
Ta+l" 3., A/"a(" ha&%"ss a%& 0ia+ili#y
S.N). F)!la#i)% c)&" A/"a(" ha&%"ss 2(4c! 5 A/"a(" 0ia+ili#y 265
'. "' 2.$#0.$2 0.1# 0.0'$
2. "2 2.34#0.2' 0.14#0.002
5. "5 '.6#0.25 0.1#0.0'
3. "3 5.0'#0.3$ 0.10#0.025
$. "$ 5.5#0.'4 0.10#0.025
6. "6 5.'4#0.2$ 0.4$#0.0''
4. "4 2.15#0.52 0.1'#0.03
1. "* 5.#0.26 0.65#0.04
. * 3.2#0.3 0.$'#0.014'0. "' 2.'5#0.56 0.'#0.0'6
''. "2 2.26#0.'' 0.1#0.064
'2. "5 '.1#0.2 0.1#0.035
'5. "3 2.45#0.3 0.12#0.0'4
'3. "$ 5.0'#0.'' 0.12#0.0'
'$. "6 5.25#0.'$ 0.41#0.04$
'6. "4 2.45#0.32 0.15#0.0$'
'4. "* 3.'6#0.'$ 0.6$#0.063
'1. "7' 2.14#0.5' 0.41#0.0$5
'. "72 2.15#0.55 0.4'#0.01
20. "7' 5.25#0.2$ 0.15#0.05'
2'. "72 2.#0.2 0.4$#0.0'
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8ean # !+ n 5
Ta+l" 3.3, A/"a(" 7"i(h# a%& #hic%"ss
S.N). F)!la#i)% C)&" A/"a(" '"i(h# 2!(5
A/"a(" #hic%"ss 2!!5
'. "' 32.55#'.$5 $.$3# 0.452. "2 6'0.55#'.$5 $.64#0.'
5. "5 452#2.6$ 6.62#0.''
3. "3 45'.5#2.52 6.$3#0.'
$. "$ 412.36#'.52 6.$#0.'
6. "6 405.44#'.' 6.35#0.26
4. "4 463.44#2.5$ 6.$#0.'5
1. "*
455.35#2.36
6.31#0.54
. * 45'.14#'.51
6.3'#0.34
'0. "' 33#'.45$.$6#0.45
''. "2 6''#'.5
0.$.42#0.5'
'2. "5 452.6#5.'5
6.65#0.'$
'5. "3 42.'4#2.3'
6.$4#0.'5
'3. "$ 41'.14#'.5$
6.$'#0.'4
'$. "6 405.'#'.54
6.63#0.53
'6. "4 465.5#2.0$
6.6'#0.2'
'4. "* 455.'5#'.$
6.$#0.'1
'1. "7' 462.1#2.36
6.4#0.45
'. "72 42.''#'.33
6.'#0.63
20. "7' 465.05#'.$5
6.13#0.3
2'. "72 42.'#'.'$6.4#0.'3
8ean # !+ n 5
3.3.1.D Fl)a#i%( la( Ti!" a%& &a#i)% )0 0l)a#i%(, - The buoyancy lag time and
uration of floating were determined in the !" issolution apparatus (( in an acidic
environment %0.'9 *7+ 00 ml+ $0 )"8&. The time interval between introduction of
the tablets in to the dissolution medium and its buoyancy to the top of the dissolution
medium was taken as buoyancy lag time and duration of buoyancy was observed
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visually. The sample mean and standard deviation of each batch of tablets were
determined %n 5&.
3.3.1.E D"%si#y, - The apparent densities of the tablets were calculated from their
volumes and masses in triplicate. ;oth parameters were determined in 0.' 9 *7
after floating the tablets. The volumes < of the spherical tablets were calculated from
their radii %determine with a micrometer gauge i.e. screw gauge& using the
mathematical e=uation for a circle %3 5 >r 5&. The sample mean and standard deviation
of each batch of tablets were determined %n 5&.
3.3.1.F Di!"%si)%al S#a+ili#y, - The dimensional stability of formulation was studiedusing !" issolution Apparatus ((. The dissolution medium was 0.'9 *7 and the
volume being 00 ml. The temperature was maintained at 54 # $ 07. The rotation
speed was $0 rpm. The dimensional stability of the theophylline floating tablets was
observed visually. The sample mean and standard deviation of each batch of tablets
were determined %Table 5.5&.
3.3. C)%#"%# U%i0)!i#y, - The drug content of at least 6 tablets from each batch
was determined. The tablets were weighed collectively+ pulverized. The weight e=ual
to single tablet was weighted and dissolved in '00 ml of 0.'9 *7 solutions. The
drug solution was filtered. Ali=uots of filtrate was diluted suitably and analyzed
spectrophotometrically %!himadzu '400+ ?apan&at 240 nm. The sample mean and
standard deviation of each batch of tablets were determined. %Table 5.3&.
Ta+l" 3.8, Fl)a#i%( capa+ili#i"s )0 &i00""%# +a#ch"s )0 #h")phylli%" 0l)a#i%(
!a#i9 #a+l"#s
S.N). F)!la#i)%
c)&"
D"%si#y
2!(4c!35
Fl)a#i%( capa+ili#i"s
Fl)a#i%(
la( 2s"c5
Fl)a#i%(
&a#i)%2h)s5
Di!"%si)%al
s#a+ili#y
'. "' 0.4#.025 534# 1.6 ''.5 #0.2$ 9ote retain
2. "2 '.03 # 0.024 21#4.$' '4.#0.51 9ote )etain
5. "5 '.034# 0.023 '02#2.$6 @ 23 )etain
3. "3 0.41# 0.01$ 41#'.5 @ 23 )etain well
$. "$ '.02#0.0'' 4'#5 @ 23 )etain well
6. "6 '.025#0.06 1#2.$' 22 # 0.6' )etain
4. "4 0.6#0.02' 60.4#2.$2 @ 23 )etain well
1. "* 0.42#0.01$ 34.5#2.01 @ 23 )etain well
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Results
. * 0.$$#.023 '0.5#'.$5 @ 23 )etain well
'0. "' 0.51#0.0'$ 5$$#3.$1 '2.6 # 0.$6 9ote retain
''. "2 0.$#.0$ 23#3.$1 '#.16 9ote )etain+
'2. "5 '.006#.04$ '20#2.$2 @ 23 )etain
'5. "3 0.4$#0.0'1 1$.4#$.05 @ 23 )etain well
'3. "$ 0.31#0.015 4.5#'.$5 @ 23 )etain well
'$. "6 '.022#0.026 '0$#$.2 20.2# 0.1$ )etain
'6. "4 '.005#.024 6.4#2.01 @ 23 )etain well
'4. "* 0.33#0.033 $$#' @ 23 )etain well
'1. "7' 0.6#0.0'' $$.'#'.$5 @ 23 )etain well
'. "72 0.$#0.025 3$#2 @ 23 )etain well
20. "7' 0.64#0.56 6'.$#'.52 @ 23 )etain well
2'. "72 0.$#0.25 $0#'.65 @ 23 )etain well
8ean # !+ n 5
Ta+l" 3.:, D( c)%#"%# %i0)!i#y )0 &i00""%# +a#ch"s )0 #h")phylli%" 0l)a#i%(
!a#i9 #a+l"#s
S.N). F)!la#i)%
c)&"
La+"l"&
a!)%# )0
&( 2!(5 2;5
Ac#al a!)%#
)0 &(2!(5 25
'. "' 200 '1#0.56 .0
2. "2 200 '#'.$4 .$
5. "5 200 '1.5#0.1 .'2
3. "3 200 '.$#'.$4 .4$
$. "$ 200 '1.5#'.32 .'$
6. "6 200 '1.2#2.54 .'
4. "4 200 '6.2#'.0$ 1.'
1. "* 200 '4.3#2.$4 1.4
. * 200 '4.5#'.$$ 1.6$
'0. "' 200 '1.6#0.4$ .5
''. "2 200 '4.5#0.3$ 1.6$
'2. "5 200 '4.$#2.65 1.4$
'5. "3 200 '6.2#2.04 1.'
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'3. "$ 200 '4.3#'.4' 1.4
'$. "6 200 '4.'4#0.1$ 1.$1
'6. "4 200 '6.64#2.'$ 1.55
'4. "* 200 '.55#0.44 .66
'1. "7' 200 '.24#'.$4 .65
'. "72 200 '.02#'.5$ .$'
20. "7' 200 '.31#'.'1 .43
2'. "72 200 '1.5$#'.2' .'4
8ean # !+ n 5
3.3.3 In-Vitro R"l"as" S#&y: -The release of theophylline from the tablets was
studied using the !" dissolution apparatus (. The dissolution medium was 0.'9 *7
and the volume being 00 ml. The temperature was maintained at 54 #0. $ 07. The
rotation speed '00 rpm. ,ive ml of ali=uot was withdrawn at a predetermine intervals
of .'+2+5+3+$+6+4+1+'0+'2+hours. The medium was replenished with five ml of fresh
0.'9 *7 at each time. The drug solution was filtered. Ali=uots of filtrate was diluted
suitably and analyzed spectrophotometrically %!himadzu '400+ ?apan& at 240 nm. B
of drug released was calculated for each interval.
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3.3.3, B In -Vitro R"l"as" &a#a )0 Th")phylli%" 0)! Di00""%# F)!la#i)%s
P"pa"& 7i#h D"hs Psylli! *s i% >.1N *CL
Ta+l" 3.?, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch DP1 i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+. C)%c"%#a#i)% i% 2!(5 C!. &(
"l"as"
6 C!.
&( "l"as"
!l : !l @>> !l
'. 0.$ 0.'$0 0.0246 0.'51 23.16 23.16 '2.35
2. ' 0.503 0.0$$ 0.210 $0.5 $0.$5 2$.26
5. 2 0.326 0.041$ 0.52 40.6' 4'.05 5$.$'
3. 5 0.$'2 0.035 0.34' 13.16 1$.64 32.13
$. 3 0.$2 0'00 0.$3$ 1.'2 .30 3.40
6. $ 0.632 0.'110 0.$' '06.3 '01.25 $3.'2
4. 6 0.63 0.'241 0.65 ''$.05 ''4.33 $1.421. 4 0.43' 0.'56$ 0.615 '22.1$ '2$.6 62.1
. 1 0.411 0.'3$' 0.4$6 '50.$ '53.55 64.'6
'0. '0 0.143 0.'6'0 0.10$ '33.16 '3.55 43.66
''. '2 0.62 0.'442 0.116 '$.3$ '63.33 12.22
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
Fi( 3.1, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch DP1 i% >.1N *CL
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Ta+l" 3., In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch DP i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+. C)%c"%#a#i)% i% 2!(5 C!. &(
"l"as"
6 C!.
&( "l"as"
!l : !l @>> !l
'. 0.$ 0.'33 0.20 0.'0$ '1. '1.0 .3$
2. ' 0.223 0.03'5 0.206 54.'5 54.25 '1.62
5. 2 0.26 0.0$53 0.264 31.04 31.51 23.'
3. 5 0.513 0.0404 0.5$3 65.6$ 63.22 52.''
$. 3 0.332 0.01'3 0.3'0 45.26 43.' 54.0
6. $ 0.312 0.0114 0.351 4.1 10.16 30.35
4. 6 0.$'5 0.02' 0.360 12.14 13.2 32.'3
1. 4 0.$2' 0.06 0.313 14.'1 1.35 33.42
. 1 0.$36 0.03 0.34 1.$0 2.25 36.'2
'0. '0 0.662 0.'220 0.620 '0.42 ''2.$ $6.31
''. '2 0.446 0.'320 0.4'$ '21.62 '52.34 66.25
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
70
0 2 4 6 8 10 12 14
Time (hrs)
%
C u m . d r u g r e l e
a s e
Fi( 3., In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch DP i% >.1N *CL
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Ta+l" 3., In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch DP3 i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+. C)%c"%#a#i)% i% 2!(5 C!. D(
"l"as"
6 C!.
&( "l"as"
!l : !l @>> !l
'. 0.$ 0.'02 0.0'11 0.03 '6.0 '6.0 1.32
2. ' 0.'46 0.0523 0.'62 2.'4 2.24 '3.65
5. 2 0.221 0.03$4 0.221 3'.'0 3'.$ 20.4
3. 5 0.563 0.0640 0.55$ 60.55 60.12 50.3'
$. 3 0.512 0.0405 0.5$2 65.5' 63.56 52.'1
6. $ 0.3'2 0.04$1 0.54 61.2 6.36 53.42
4. 6 0.353 0.04 0.5 4'.5 45.31 56.43
1. 4 0.36 0.0165 0.352 44.45 4.61 5.13
. 1 0.311 0.01 0.33 10.11 15.26 3'.6
'0. '0 0.$'' 0.03' 0.34' 13.'0 14.$' 35.41
''. '2 0.$$1 0.'021 0.$'3 2.3 $.4 34.1
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
0 5 10 15
Ti!" 2hs5
6
C 1 ! . & 1 ( "
l " a s "
Fi( 3.3, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch DP3 i% >.1N *CL
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Ta+l" 3.@, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch DP8 i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% i% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.014 0.'60 0.010 '3.32 '3.32 4.2'
2. ' 0.'43 0.052 0.'60 21.15 21.2 '3.36
5. 2 0.232 0.03$ 0.225 30.'' 30.2 20.'3
3. 5 0.216 0.$26 0.265 34.3' 34.$4 25.5
$. 3 0.532 0.065 0.5'$ $0.6 $4.3' 21.4'
6. $ 0.541 0.66 0.513 62.6$ 65.6 5'.1$
4. 6 0.321 0.041 0.53 40.3 42.55 56.'6
1. 4 0.36' 0.01$ 0.323 46.3' 41.' 5.'
. 1 0.33 0.0' 0.3$$ 1'.11 13.0 32.03
'0. '0 0.$5' 0.01 0.31 11.0' 0.64 3$.53
''. '2 0.$41 0.''6 0.$52 $.10 1.$ 3.34
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
0 5 10 15
Time(hrs)
%
C u m .
d r u g r e l e a s e
Fi( 3.8: In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch DP8 i% >.1N *CL
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Results
Ta+l" 3.1>, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch DP: i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. D(
"l"as"
6 C!.
D(
"l"as"!l : !l @>> !l'. 0.$ 0.041 0.0'3 0.042 '2.5 '2.5 6.36
2. ' 0.'66 0.05' 0.'$5 24.$' 24.$1 '5.4
5. 2 0.223 0.03' 0.2'0 54.'5 54.32 '1.4'
3. 5 0.253 0.035 0.2'$ 51.4 5.22 '.6'
$. 3 0.24' 0.0$0 0.2$0 33.2 3$.$4 22.41
6. $ 0.523 0.0$ 0.21 $5.4 $3.60 24.50
4. 6 0.516 0.04' 0.5$$ 65.1 63.6 52.31
1. 4 0.322 0.044 0.51 6.3 4'.3 5$.4$
. 1 0.346 0.014 0.351 41.1 10.13 30.32
'0. '0 0.$51 0.0 0.3$ 1.'4 '..$$ 3$.41
''. '2 0.$11 0.'01 0.$3' 4.36 '00.55 $0.'4
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
0 5 10 15
Time(hrs)
%
C u m . d r u g r e l e a s
e
Fi( 3.:, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch DP: i% >.1N *CL
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Results
Ta+l" 3.11, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch DP? i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.04 0.0'1 0.01 '.01 '6.01 1.03
2. ' 0.'13 0.053 0.'6 50.$ 50.$ '$.2
5. 2 0.2$6 0.034 0.256 32.35 32.61 2'.53
3. 5 0.503 0.0$6 0.24 $0.5 $0.11 2$.33
$. 3 0.5$4 0.064 0.521 $.'4 $.$ 2.4
6. $ 0.546 0.06 0.531 62.64 65.44 5'.11
4. 6 0.322 0.041 0.51 6.3 4'.5 5$.6
1. 4 0.343 0.014 0.354 41.$6 10.30 30.2
. 1 0.31 0.02 0.3$ 12.$3 13.22 32.''
'0. '0 0.$54 0.0 0.33 1.0' '.3$ 3$.45
''. '2 0.605 0.''' 0.$$$ . '02.15 $'.32
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
0 0.2 0.4 0.6 0.8Time(hrs)
%
C u m .
d r u g r e l e a s e
Fi( 3.?, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch DP? i% >.1N *CL
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Results
Ta+l" 3.1, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch DP i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.016 0.0'4 0.015 '3.1$ '3.1$ 4.32
2. ' 0.'3 0.024 0.'54 23.66 23.43 '2.54
5. 2 0.2'6 0.05 0.' 5$.10 56.02 '1.0'
3. 5 0.266 0.031 0.23$ 33.01 33.$' 22.2$
$. 3 0.506 0.0$4 0.21$ $'.22 $'.11 2$.3
6. $ 0.554 0.62' 0.5'0 $$.1$ $6.1' 21.3'
4. 6 0.51 0.045 0.566 6$.4 64.25 55.62
1. 4 0.3'6 0.044 0.515 61.$ 40.$' 5$.2$
. 1 0.36 0.016 0.352 44.45 4.45 5.14
'0. '0 0.$02 0.02 0.362 1.40 1$.63 32.12
''. '2 0.$$ 0.'05 0.$'$ 2.6$ $.$3 34.44
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
0 0.2 0.4 0.6
Time(hrs)
%
C u m . d r u g r e l a s
e
Fi( 3., In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch DP i% >.1N *CL
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Results
3.3.3.B In-Vitro R"l"as" Da#a )0 Th")phylli%" 0)! Di00""%# F)!la#i)%s
P"pa"& 7i#h *s Psylli! i% >.1N *CL
Ta+l" 3.13, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch P1 i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l
'. 0.$ 0.'45 0.052 0.'$ 21.4 21.4 '3.5
2. ' 0.55' 0.06' 0.50$ $3.16 $$.02 24.$'
5. 2 0.3$3 0.013 0.320 4$.54 4$.15 54.2
3. 5 0.$' 0.06 0.341 16.03 16.2 35.36
$. 3 0.$ 0.''0 0.$$2 .5$ '00.4' $0.5$
6. $ 0.631 0.'' 0.$4 '04.30 '0.52 $3.6$4. 6 0.615 0.'26 0.650 ''5.24 ''$.44 $4.11
1. 4 0.43' 0.'56 0.612 '22.45 '2$.44 62.11
. 1 0.442 0.'32 0.4'' '24.$ '5'.63 6$.12
'0. '0 0.1$ 0.'$1 0.4' '32.51 '36.' 45.3$
''. '2 0.32 0.'43 0.164 '$6.'5 '6'.3$ 10.42
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
70
8090
0 5 10 15Time(hrs)
%
c u m .
d r u g r e l e a s e
Fi( 3., In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch P1 i% >.1N *CL
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Results
Ta+l" 3.18, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch P i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0'30 0.026 0.'5 25.2$ 25.2$ ''.65
2. ' 0.2$' 0.036 0.25 3'.46 3'.1 20.$
5. 2 0.5$2 0.06 0.55 $1.32 $1.41 2.5
3. 5 0.30 0.04$ 0.51 64.4 61.31 53.23
$. 3 0.366 0.016 0.35 44.5 41.54 5.'
6. $ 0.311 0.01 0.$3 10.12 12.52 3'.'6
4. 6 0.$02 0.02 0.36 15.20 1$.'$ 32.$4
1. 4 0.$' 0.6 0.31 16.02 11.33 33.25
. 1 0.$2$ 0.04 0.3 14.02 1.' 33.6
'0. '0 0.$4 0.'04 0.$5 $.4 .53 31.64
''. '2 0.64' 0.'23 0.62 '''.22 ''$.'' $4.$6
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
Fi( 3.@, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch P i% >.1N *CL
Dept. of Pharmaceutical Sciences S.S.I.T.M.46
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Results
Ta+l" 3.1:, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch P3 i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"
!l : !l @>> !l
'. 0.$ 0.''$ 0.02'2 0.'06 '.06 '.06 .$5
2. ' 0.'1 0.0560 0.'10 52.12 52.2 '6.36
5. 2 0.50$ 0.0$62 0.210 $0.$$ $0.13 2$.32
3. 5 0.53' 0.0621 0.5'3 $6.$2 $6.12 21.3'
$. 3 0.514 0.04'5 0.5$6 63.'3 6$.05 52.$'
6. $ 0.301 0.04$ 0.546 64.62 61.16 53.35
4. 6 0.350 0.04 0.56 4'.24 42.1 56.33
1. 4 0.3$$ 0.013 0.3' 4$.3' 44.35 51.4'
. 1 0.361 0.016 0.350 44.$4 4.6$ 5.12
'0. '0 0.3 0.02 0.360 12.'' 1$.30 32.6
''. '2 0.$50 0.01 311 14.1$ '.'4 3$.$1Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
0 5 10 15
Time(hrs)
% C u m . d r u g r e l e a s e
Fi( 3.1>, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch P3 i% >.1N *CL
Dept. of Pharmaceutical Sciences S.S.I.T.M.44
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Results
Ta+l" 3.1?, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch P8 i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.05 0.0'4' 0.016 '$.3' '3.3' 4.4'
2. ' 0.'15 0.0554 0.'6 50.55 50.32 '$.2'
5. 2 0.245 0.0$05 0.2$' 3$.24 3$.$2 22.46
3. 5 0.2' 0.0$30 0.261 31.25 31.43 23.54
$. 3 0.53 0.0630 0.52' $4.1$ $1.62 2.5'
6. $ 0.54' 0.0615 0.530 6'.3 62.$ 5'.2
4. 6 0.322 0.0444 0.51 6.3 4'.51 5$.6
1. 4 0.35 0.042 0.56 4'.24 45.0 56.$$
. 1 0.3$ 0.0121 0.3'3 43.$ 46.4 51.5
'0. '0 0.31' 0.010 0.335 4.42 12.43 3'.54
''. '2 0.$$' 0.'0'0 0.$0$ '.55 5.4 36.1
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
0 5 10 15Time(hrs)
% C u m . d r u g r e l e a s
e
Fi( 3.11, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch P8 i% >.1N *CL
Dept. of Pharmaceutical Sciences S.S.I.T.M.41
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Results
Ta+l" 3.1, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch P: i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.04 0.0'$6 0.045 '5.0 '5.0 6.$$
2. ' 0.'45 0.05' 0.'$ 21.64 21.4$ '3.54
5. 2 0.252 0.0324 0.2'3 51.3$ 51.61 '.53
3. 5 0.262 0.0315 0.230 35.20 35.6$ 2'.12
$. 3 0.503 0.0$$ 0.210 $0.30 $'.04 2$.$3
6. $ 0.514 0.04'5 0.5$6 63.'3 6$.'' 52.$$
4. 6 0.53 0.0426 0.560 6$.50 66.65 55.5'
1. 4 0.3'1 0.0461 0.51$ 6.21 40.6 5$.31
. 1 0.3$3 0.0136 0.3'1 4$.2$ 44.52 51.66
'0. '0 0.$03 0.052 0.340 15.34 16.5$ 35.'1
''. '2 0.$41 0.'06$ 0.$52 $.10 1.$2 3.26
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
0 5 10 15
Time(hrs)
%
C u m .
d r u g r e l e a s e
Fi(3.1, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch P: i% >.1N *CL
Dept. of Pharmaceutical Sciences S.S.I.T.M.4
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Results
Ta+l" 3.1, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch P? i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.'' 0.02' 0.'' '.42 '.42 .16
2. ' 0'1 0.0531 0.'4 5'.55 5'.33 '$.42
5. 2 0.216 0.0$26 0.20 34.3 33.61 25.13
3. 5 0.5'6 0.0$12 0.2 $2.51 $2.2 26.36
$. 3 0.530 0.0626 0.5' $6.5$ $4.'1 21.$
6. $ 0.541 0.066 05$ 62.63 65.41 5'.1
4. 6 0.5' 0.0420 0.56 63.1' 66.2 55.'$
1. 4 0.35$ 0.010' 03 42.' 45.$ 56.4
. 1 0.362 0.01$' 0.35 46.$4 41.12 5.3'
'0. '0 0.3$ 0.0'2 0.36 12.03 13.42 32.56
''. '2 0.$6$ 0.'03' 0.$2 5.6$ 6.4 31.5
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
0 5 10 15
Time(hrs)
%
C u m .
d r u g r e l e a s e
Fi( 3.13, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch P? i% >.1N *CL
Dept. of Pharmaceutical Sciences S.S.I.T.M.10
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Results
Ta+l" 3.1@, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch P i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.01 0.0'6 0.01 '3.4$ '3.4$ 4.54
2. ' 0.'$' 0.021 0.'3 2$.05 2$.'' '2.$$
5. 2 0234 0.036 0.25 30.3 3'.'6 20.$1
3. 5 0.246 0.0$' 02$ 3$.4$ 36.' 25.'0
$. 3 0.502 0.0$6 0.21 $0.06 $0.46 2$.51
6. $ 0.551 0.062 0.5' $6.02 $4.00 21.$0
4. 6 0.56 0.061 053 6'.2 62.3$ 5'.22
1. 4 0.3'$ 0.46 051 61.41 40.3' 5$.2'
. 1 0.354 0.010 030 42.35 43.35 54.22
'0. '0 0.313 0.1 0.3$ 10.22 12.65 3'.5'
''. '2 0.$53 0.01 0.3 11.$' '.0 3$.$$
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
0 5 10 15
Time(hrs)
% C u m . d r u g r e l e a s e
Fi( 3.18, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch P i% >.1N *CL
5.5.5.7. In-Vitro )elease ata of Theophylline from ifferent ,ormulations "repared
with *"87 C '00 8 alone and in combination with ehusk+ *usk "syllium in 0.'9
*7
Dept. of Pharmaceutical Sciences S.S.I.T.M.1'
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Results
Ta+l" 3.>, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch * i% >.1N *CL
S.N). Ti!"2hs5 A+s)+. C)%c"%#a#i)% 2!(5 C!. &("l"as" 6 C!.&(
"l"as"!l : !l @>> !l
'. 0.$ 0.01 0.'1 0.0 '6.23 '6.23 1.'2
2. ' 0.'46 0.52 0'6 2.'4 2.26 '3.6
5. 2 0.253 0.035 0.24 51.4 5.03 '.$2
3. 5 0.50' 0.0$3 0.21 $0.3 $0.14 2$.33
$. 3 0.5$1 0.66 0.55 $.53 60.'0 50.0$
6. $ 0.32' 0.41 0.511 6.41 40.16 5$.35
4. 6 0.36' 0.01$ 0.323 46.3' 44.11 51.3
1. 4 0.31 0.2 0.36 12.$3 13.33 32.22
. 1 0.$ 0.'' 0.$$ .00 '0'.5$ $0.61
'0. '0 0.641 0.'2$ 0.65 ''2.54 ''$.21 $4.65
''. '2 0.61 0.'2 0.63 ''$.6 ''1.3 $.34
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
70
0 5 10 15
Time(hrs)
%
C u m .
d r u g r e l e a s e
Fi( 3.1:, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch * i% >.1N *CL
Dept. of Pharmaceutical Sciences S.S.I.T.M.12
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Results
Ta+l" 3.1, In-Vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch DP* i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.'20 0.0'13 0.0 '6.6 '6.6 1.5
2. ' 0.20' 0.0540 0.' 55.5' 55.3' '6.4
5. 2 0.2$' 0.036' 0.25 3'.6 3'.11 20.5
3. 5 0.5'' 0.0$45 0.2 $'.$$ $2.0$ 26.05
$. 3 0.56 0.061 0.53 6'.'6 6'.$ 50.1
6. $ 0.355 0.04 0.5 4'.45 42.14 56.35
4. 6 034' 0.014 0.35 41.04 4.6 5.10
1. 4 0.$54 0.01 0.3 1.0' 0.3 3$.34
. 1 0.$6$ 0.'03 0.$2 5.6$ 6.'' 31.0$
'0. '0 0.$14 0.'01 0.$3 4.2 '00.21 $0.'3
''. '2 0.642 0.'53 0.62 '''.51 ''3.' $4.3$
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
70
0 5 10 15
Time(hrs)
%
C u m .
d r u g r e l e a s e
Fi( 3.1?, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch DP * i% >.1N
*CL
Dept. of Pharmaceutical Sciences S.S.I.T.M.15
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Results
Ta+l" 3., In-Vitro "l"as" Da#a )0 #h")phylli%" 0)! +a#ch P* i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.'04 0.0'4 0.0 '4.45 '4.45 1.16
2. ' 0.2'5 0.05 0.'6 5$.5 5$.3 '4.4
5. 2 0.212 0.0$2 0.26 36.43 34.03 25.$'
3. 5 0.5'' 0.0$4 0.2 $'.$$ $2.' 26.0$
$. 3 0.564 0.061 0.53 60.15 6'.64 50.15
6. $ 0.321 0.04 0.5 40.3 42.05 56.02
4. 6 033 0115 0.3' 43.35 4$. 51.
1. 4 0.$2$ 0.064 0.31 14.02 11.1 33.3$
. 1 0.$35 0.'00 0.$0 0.0 2.56 36.'1
'0. '0 0.$64 0.'03 0.$2 5.1 6.13 31.32
''. '2 0.6'1 0''3 0.$4 '02.35 '0$.1' $2.'
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
0 5 10 15
Tme(hrs)
%
C u m .
d r u g r e l e a
s e
Fi( 3.1, In-Vitro "l"as" )0 #h")phylli%" 0)! +a#ch P * i% >.1N *CL
5.5.5. In-Vitro )elease ata of Theophylline from ifferent ,ormulations "repared
with Ac-i-!ol in combination with ehusk+ and *usk "syllium in 0.'9 *7
Dept. of Pharmaceutical Sciences S.S.I.T.M.13
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Results
Ta+l" 3.3, In-vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch DPC1 i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.6 0.0'44 0.011 '$.' '$.' 4.$
2. ' 0.'13 0.055 0.'4 50.$0 50.$ '$.2
5. 2 0.2$$ 0.34'0 0.25$ 32.24 32.$2 2'.26
3. 5 0.5'4 0.0$13 0.22 $2.$3 $5.05 26.$2
$. 3 0.531 0.063 0.52 $4.61 $1.36 2.25
6. $ 0.53 0.045 0.565 6$.61 66.3' 55.2'
4. 6 0.32 0.04 0.5$ 4'.'0 42.$4 56.2
1. 4 0.3$2 0.015 0.3'6 43.3 46.6' 51.5'
. 1 0.$26 0.06 0.310 14.'1 1.25 33.6'
'0. '0 0.$4 0.'066 0.$55 $.4 1.45 3.56
''. '2 0.634 0.'' 0.$6 '04.23 ''0.$5 $$.24
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
0 5 10 15
Time(hrs)
%
C u m .
d r u g r e l e a s e
Fi( 3.1, In-vitro "l"as" )0 #h")phylli%" 0)! +a#ch DPC1 i% >.1N *CL
Dept. of Pharmaceutical Sciences S.S.I.T.M.1$
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Results
Ta+l" 3.8, In-vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch DPC i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.'0' 0.0'16 0.5 '6.43 '6.43 1.54
2. ' 0.'11 0.5$ 0.'45 5'.'6 5'.2$ '$.65
5. 2 0.24$ 0.0$' 0.2$5 3$.$1 3$.1$ 22.2
3. 5 0.526 0.06 0.5 $3.05 $3.$$ 24.21
$. 3 0.566 0.064 0.53 60.66 6'.31 50.43
6. $ 0.3'2 0.046 0.54 61.2 6.3$ 53.42
4. 6 0.363 0.01$ 0.324 46.' 41.33 5.22
1. 4 0.$'2 0.03 0.34 13.16 16.15 35.3'
. 1 0.$$2 0.'02 0.$01 '.3 5.5 36.6
'0. '0 0.631 0.'' 0.$4 '04.3 ''0.5$ $$.'4
''. '2 0.4'' 0.'5' 0.66 ''4.1$ '20.02 60.0'
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
70
0 5 10 15Time(hrs)
%
C u m . d r u g r e l e a s e
Fi(3.1@, In-vitro "l"as" )0 #h")phylli%" 0)! +a#ch DPC i% >.1N *CL
Dept. of Pharmaceutical Sciences S.S.I.T.M.16
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Results
Ta+l" .:, In-vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch PC1 i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.0' 0.0'4 0.01 '$.01 '$.01 4.$3
2. ' 0.'16 0.053 0.'4 50.14 50.$ '$.31
5. 2 0.24 0.0$' 0.26 36.23 36.3 25.2$
3. 5 0.52$ 0.060 0.50 $2.14 $3.51 24.'
$. 3 0.563 0.064 053 60.5' 6'.'2 50.$6
6. $ 0.30$ 0.04$ 0.54 64.'5 61.2 53.'3
4. 6 0.324 0.04 0.5 40.44 42.2 56.'3
1. 4 0.3$' 0.015 0.32 43.4$ 46.66 51.55
. 1 0.$'2 0.03 0.34 13.16 14.'1 35.$
'0. '0 0.$$2 0.'02 0.$2 '.12 3.62 34.5'
''. '2 0.601 0''2 0.$6 '00.44 '03.01 $2.03
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
0 5 10 15
Time(hrs)
%
C u m . d r u g r e l e a s e
Fi( 3.>, In-vitro "l"as" )0 #h")phylli%" 0)! +a#ch PC1 i% >.1N *CL
Dept. of Pharmaceutical Sciences S.S.I.T.M.14
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Results
Ta+l" 3.?, In-vitro "l"as" &a#a )0 #h")phylli%" 0)! +a#ch PC i% >.1N *CL
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l'. 0.$ 0.''2 0.02' 0.'5 '1.$6 '1.$6 .21
2. ' 0.'3 0.026 0.'1 52.'6 5'.26 '6.'5
5. 2 0.212 0.$20 0.24 36.43 34.02 25.$'
3. 5 0.552 0.6'0 0.5' $$.05 $$.$1 24.4
$. 3 0.562 0.064 0.55 60.00 60.16 50.35
6. $ 0.323 0.041 0.0.5 40.21 4'.34 5$.45
4. 6 00.54 0.01' 0.3 42.35 43.03 54.0'
1. 4 0.34 0.110 033 4.5 1'.56 30.6
. 1 0$55 0.01 0.3 11.53 0.46 3$.51
'0. '0 0.6'0 0.''2 0$6 '0'.'' '05.4$ $'.14
''. '2 0.616 0.'26 0.65 ''5.30 ''6.5 $1.'$
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
0
10
20
30
40
50
60
70
0 5 10 15
Time(hrs)
%
C u m . d r u g r e l e a s e
Fi( 3.1, In-vitro "l"as" )0 #h")phylli%" 0)! +a#ch PCi% >.1N *CL
3.3.8, D"#"!i%a#i)% )0 S7"lli%( I%&"9: - The swelling indeD of the tablets was
studied using the !" dissolution apparatus (. The dissolution medium was 0.'9 *7
and the volume being 00 ml. The temperature was maintained at 54 #0. $
0
7. The
Dept. of Pharmaceutical Sciences S.S.I.T.M.11
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Results
rotation speed '00 rpm. The tablets were withdrawn at predetermine intervals of '+ 2+
5+ 3+ $+ 6 E.'2 hrs. The tablets were blotted with tissue paper to remove the eDcess
0.'9 *7 and reweighed. The swelling indeD was calculated by the following
e=uation: '05+'03+'0$
!welling indeD % Ft - Fo Fo & / '00
Fhere: Ft is the weight of swelling matriD tablet after t times
Fo is the initial weight of matriD tablet
Ta+l" 3., S7"lli%( i%&"9 )0 #h")phylli%" 0l)a#i%( !a#i9 #a+l"#s 0)! &i00""%#
0)!la#i)%s i% >.1N *CL
S.N)
F)!la#i)
% c)&"
I%i#ial
7"i(h
#
2!(5
P"c"%#a(" )0 s7"lli%( i%&"9
Ti!" 2hs5
1 3 8 ?
1
'. "5 452 $4.' '5'.$$ 2''.3 240.3 506.2 553.
543.'4
2. "3 452 40. '5.2' 223.0 26.31 21.31 523.1
501.'
5. "5 452 36.05 ''4.43 '12.23 2$$.$ 5'1.'6 531.'$
5'4.25
3. "3 452 $1.3 '26.66 '1.31 231.1 24.1 55.5
506.'2
$. * 452 1$.2 '56.66 '40.34 22$.41 221.15 224.4
2'$.'5
6. "72 42 41.'3 '3$.'' 22$.0 24'.'' 501.0 53.''
5'2.$
4. "72 42 6$.'2 '50.6' 2'0.0 2$.' 5'.1 5$$.'
5'4.'1
% 1
Dept. of Pharmaceutical Sciences S.S.I.T.M.1
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Results
Fi( 3., S7"lli%( i%&"9 )0 #h")phylli%" 0l)a#i%( !a#i9 #a+l"#s 0)!
&i00""%# 0)!la#i)%s i% >.1N *CL
3.3.:. E)si)% S#&i"s, - Grosion studies of floating matriD tablets were performed as
reported by "aradkar et al. The preweighed tablets were placed in !" dissolution
Type ( dissolution test apparatus and were subHected to dissolution in 00 ml of 0.'9
*7 maintained at 54-7 # 0.$-7+ the speed of basket rotation was '00 rpm. The
matriD system were removed after '2 hrs from the dissolution vessels and dried to
constant weight in hot air oven %*icon+ (ndia& at $007 - 60 07. The percentage matriD
erosion at time '2 hrs was calculated by using following G=uation: '05+'03+'0$
"ercentage 8atriD Groded %wt of polymers eroded wt of initial matriD& /'00
Feight of polymers eroded total weight loss I amount of drug released
Dept. of Pharmaceutical Sciences S.S.I.T.M.0
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Results
Ta+l" 3., P"c"%#a(" !a#i9 ")&"& a0#" 1 hs 0)! &i00""%# 0)!la#i)% i%
>.1N *CL
S.N). F)!la#i)%
c)&"
Ta+l"# 7"i(h# 2!(5 T)#al7"i(h#
l)ss
2!(5
D("l"as"&
2!(5
Ma#i9")&"&
2!(5
P"c"%#a(")0 !a#i9
")&"&i%i#ial "!ai%i%(
&yi%( 7"i(h#
'. "5 45$ $16 '3 5.2 $$.01 4.3
2. "3 45' $' '30 6.1 35.02 $.14
5. * 455 $1$ '31 '5'.26 '6.43 2.21
3. "5 456 $41 '$1 1.11 61.'2 .2$
$. "3 452 $11 '33 2.2 $'.06 6.4
6. "72 40 654 '$4 '2'.5 5$.4 3.3
4. "72 43 6'6 '43 '53.3 5.6 $.0'
n '
Fi( 3.3, P"c"%#a(" !a#i9 ")&"& a0#" 1 hs 0)! &i00""%# 0)!la#i)%s
i% >.1 N *CL
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Results
Ta+l" 3.@, Chaac#"i$a#i)% )0 &i00""%# +a#ch"s
S.N) F)!la#i)%
c)&"
Fl)a#a#i)% +"ha/i)
'. "' Tablets floated with significant floating lag time good swelling but
not intact+ not release the drug up to 23 hrs.
2. "2 Tablets floated with significant floating lag time+ good swelling but
not intact+ not release the drug up to 23 hrs.
5. "5 Tablets floated with significant floating lag time+ good swelling+
remained intact throughout the study+ higher erosion+ release the drug
up to 23 hrs.
3. "3 Tablets showed good buoyancy with good swelling+ remained intactthroughout the study+ reduced erosion+ floating lag time
comparatively reduced+ release the drug up to 23 hrs.
$. "$ Tablets showed good buoyancy with good swelling+ remained intact
throughout the study+ reduced erosion+ floating lag time
comparatively reduced+ release the drug up to 23 hrs.
6. "6 Tablets floated with good swelling+ not remained intact throughout
the study and significant floating lag time.
4. "4 Tablets showed good buoyancy with good swelling+ remained intactthroughout the study+ floating lag time reduced.
1. "* Tablets showed good buoyancy with good swelling+ remained intact
throughout the study+ floating lag time comparatively reduced.
. * Tablets showed good buoyancy with good swelling+ remained intact
throughout the study+ floating lag time was lowest+ lowest erosion+
release the drug up to 23 hrs.
'0. "' Tablets floated with significant floating lag time+ good swelling but
not intact+ not release the drug up to 23 hrs.
''. "2 Tablets floated with significant floating lag time+ good swelling but
not intact+ not release the drug up to 23 hrs.
'2. "5 Tablets floated with significant floating lag time+ good swelling
remained intact+ highest erosionJ release the drug up to 23 hrs.
'5. "3 Tablets showed good buoyancy with good swelling+ remained intact
throughout the study+ reduced erosion+ floating lag time
comparatively reduced+ release the drug up to 23 hrs.
'3. "$ Tablets showed good buoyancy with good swelling+ remained intact
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Results
throughout the study reduced erosion+ floating lag time comparatively
reduced+ release the drug up to 23 hrs.
'$. "6 Tablets floated with good swelling+ not remained intact through the
study and and significant floating lag time.
'6. "4 Tablets showed good buoyancy with good swelling+ remained intact
throughout the study+ floating lag time reduced+ release the drug up to
23 hrs.
'4. "* Tablets showed good buoyancy with good swelling+ remained intact
throughout the study+ reduced erosion+ floating lag time reduced+
release the drug up to 23 hrs.
'1. "7' Tablets showed good buoyancy with good swelling+ remained intact
throughout the study+ floating lag time reduced+ release the drug up to23 hrs.
'. "72 Tablets showed good buoyancy with good swelling+ remained intact
through the study+ floating lag time reduced+ showed the release up to
the 23 hrs.
20. "7' Tablets showed good buoyancy with good swelling+ remained intact
throughout the study+ floating lag time reduced+ release the drug up to
23 hrs.
2'. "72 Tablets showed good buoyancy with good swelling+ remained intactthroughout the study+ floating lag time reduced+ showed the release up
to the re=uired period of time.
3.3.8. STUD< ON OPTIMIZED FORMULATIONS
3.3.8.A E00"c# )0 *a&%"ss )% B)ya%cy
Ta+l"3.3>, E00"c# )0 ha&%"ss )% +)ya%cy 0)! &i00""%# 0)!la#i)%s
S.N). Ba#ch c)&" *a&%"ss
2(4c!5
Fl)a#i%( capa+ili#i"s
Fl)a#i%( la(
Ti!" 2s"c.5
0l)a#i%(
&a#i)%2hs5
'. "72 2 3$#2 23
3 '0±5 23
6 9, -
2.
"72
2 $0 ±1.63 23
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Results
3 200±8 23
6 9, -
5. * 2 0 23
3 '0.5±1.53 23
6 0.4$ 23
9, note float+ 8ean ± SD, n = 3
3.3.8 B E00"c# )0 RPM )% In-vitro D( R"l"as"
Ta+l" 3.31, In-vitro "l"as" &a#a )0 &( "l"as" 0)! +a#ch DPC a# :> RPM
S.N). Ti!"
2hs5
A+s)+. C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&( "l"as"
!l : !l @>> !l
'. 0.$ 0.01 0.0'34 0.0454 '5.26 '5.26 6.65
2. ' 0.'66 0.050$ 0.'$2 24.$' 24.$1 '5.4
5. 2 0.253 0.035' 0.2'$$ 51.41 51.$ '.31
3. 5 0.524 0.0602 0.50'0 $3.2 $3.63 24.52
$. 3 0.555 0.06'5 0.5064 $$.'4 $$.66 21.$1
6. $ 0.3'' 0.04$4 0.5410 61.'2 61.4$ 53.54
4. 6 0.33' 0.01'2 0.306' 45.0 43.2$ 54.'5
1. 4 0.361 0.0162 0.35'0 44.$1 4.'3 5.$4
. 1 0.$'0 0.05 0.366 13.$5 16.$2 35.26
'0. '0 0.605 0.'''' 0.$$$$ . '02.'2 $'.06
''. '2 0.64' 0.'253 0564 '''.25 ''3.$2 $4.26
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
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Results
Fi( 3.8, In-vitro "l"as" )0 #h")phylli%" 0)! +a#ch DPC a# :> RPM
Ta+l" 3.3, In-vitro "l"as" &a#a )0 &( "l"as" 0)! +a#ch PC a# :> RPM
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as" !l : !l @>> !l
'. 0.$ 0.0 0.0'66 0.12 '3.2 '3.2 4.36
2. ' 0.'15 0.0533 0.'42 50.6 5'.03 '$.$2
5. 2 0.2$' 0.362 0.25' 3'.6 3'.16 20.5
3. 5 0.210 0.0$'6 0.2$1 36.3' 36.1 25.3$$. 3 0.535 0.0652 0.5'$1 $6.1$ $4.$ 21.4
6. $ 0.305 0.0432 0.54'' 66.4 64.16 55.5
4. 6 0.3'2 0.04$ 0.543 61.21 6.42 53.16
1. 4 0.342 0.016 0.35$ 41.2' 10.02 30.0'
. 1 0.$'0 0.05 0.366 13.$5 16.41 35.5
'0. '0 0.60' 0.''' 0.$$$$ .6' '0'.1 $0.$
''. '2 0.61. 0.'226 0.6'55 ''0.3' ''5.34 $6.4'
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
Fig3.25: In-vitro "l"as" )0 #h")phylli%" 0)! +a#ch PC a# :> RPM
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Results
Ta+l" 3.33, In-vitro "l"as" &a#a )0 &( "l"as" 0)! +a#ch * a# :> RPM
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&(
"l"as"!l : !l @>> !l
'. 0.$ 0.0 0.0'66 0.015 '3.2 '3.2 4.36
2. ' 0.'1$ 0.053' 0.'40 50.66 50.43 '$.5
5. 2 0.23' 0.0333 0.222 5.3 30.' 20.'
3. 5 0.26 0.0$3$ 0.245 3.06 3.$3 23.44
$. 3 0.562 0.6664 0.555 60.0 60.4$ 50.546. $ 0.3' 0.4420 0.51$ 6.3$ 40.$5 5$.26
4. 6 0.335 0.0120 0.301 45.35 43.1 54.3$
1. 4 0.312 0.1110 0.333 4.2 1'.4 30.1
. 1 0.$3' 0.06 0.31 1.64 2.54 31.'1
'0. '0 0.6'3 0.''5' 0.$6$ '0'.4 '03.6 $2.5
''. '2 0.612 0.'2$6 0.621 ''5.03 ''6.32 $1.2'
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
Fi(3.?, In-vitro "l"as" )0 #h")phylli%" 0)! +a#ch * a# :> RPM
3.3.8.C. I%#"ac#i)% S#&y 3.3.8.C.I Thi% lay" Ch)!a#)(aphy: - (t was concluded that there was no
significant changed in ) f value of theophylline alone and with polymer. The ) f was
found to be 0.66$+0.64 and 0.61$ for *+ "72 and "72 respectively.
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Results
3.3.8.C.II F)i" Ta%s0)! I%0a"& Sp"c#)sc)py: - () !pectroscopy is of
immense value in establishing drug polymer interaction in solid state. The origin of
any new sharp () peak or disappearance of any peak associated with a functional
group of the pure drug indicates the drug and polymer in solid state %Techibana and
9eekamura. '6$&.
() spectra of the pure drug and optimized formulations eDhibit the following
absorption band.
Ta+l"3.38, 'a/"l"%(#h /al"s )0 &( i% #h" IR sp"c#a
S.N).'a/"l"%(#h 2c!
-1
5Assi(%!"%#R"0""%c"
a%("
O+s"/"& /al/"
P" &( F)!la#i)%
'. 5500-5$00 5325 53$0 9-*%stretch&
2. '6$0-'4$0 '4'2 '4'2 7K%stretch&
5. '6$0-'64$ '666 '664 77%stretch&
3. '$$0-'$4$ '$65 '$63 79%stretch&
$. '300-'$00 '335 '335 7-*%bending&
6. '2$0-'500 '212 '216 7-9%vibration&
4. '200-'2$0 '230 '23' 7-K%vibration
1. 400-00 135 13' 7-* out plan bending
%A&
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Results
%;&
Fi( 3., I.R. Sp"c#a )0 2A5 Psylli! hs 2B5 Op#i!i$"& 0)!la#i)%
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Results
3.3.8. D R"l"as" i%"#ics
Ta+l" 3.3:, R"l"as" i%"#ics 0) 0)!la#i)% DPC
S.
N).
Ti!"
2hs5
Sa"
))#
#i!"
2hs5
L)(
#i!"
2hs 5
C!la#i/
"
6 &(
"l"as"
L)(
c!la#i/
" 6 &(
"l"as"
L)(
c!la#i/"
6 &(
"!ai%i%(
C+" ))#
c!la#i/"
6 &(
"!ai%i%(
' 0.$ 0.4' -0.50' 1.54 0.2 '.6 3.$'
2 '.0 ' 0 '$.65 '.' '.5 3.5
5 2.0 '.3' 0.50' 22.2 '.56 '.1 3.26
3 5.0 '.45 0.344 24.21 '.33 '.16 3.'4
$ 3.0 2 0.60 50.43 '.3 '.13 3.''
6 $.0 2.23 0.4 53.42 '.$3 '.12 3.05
4 6.0 2.3$ 0.41 5.22 '.$ '.41 5.5
1 4.0 2.6$ 0.1$ 35.3' '.63 '.4$ 5.13
1.0 2.15 0. 36.6 '.64 '.42 5.46
'0 '0 5.'6 ' $$.'4 '.43 '.6$ 5.$$
'' '2 5.36 '.' 60.0' '.41 '.6 5.3'
Ta+l" 3.3?, R"l"as" paa!"#"s )0 )p#i!i$"& 0)!la#i)% DPC
Z") )&" Fis# )&" *i(chi )s!"y"-
P"ppas
*i9s)%-
C)7"ll
>
2h-15
1
2h-15
*
2h-145
%
/al"
*C
2h-1435
0.3$ 3.24$' 0.$3 0.0402 0.4 '1.25 0.2' 0.$322 0.' 0.02
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Results
2A5 Z") )&" !)&"l
2B5Fis# )&" !)&"l
2C5 *i(chi !)&"l
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Results
2D5 *i9s)% C)7"ll !)&"l
2E5 )s!"y"-P"ppas !)&"l
Fi(3., R"l"as" i%"#ics 0) 0)!la#i)% DPC
Ta+l"3.3, R"l"as" i%"#ics )0 0)!la#i)% PC
S.
N).
Ti!"
2hs5
Sa"
))#
#i!"
2hs5
L)(
#i!"
2hs 5
C!la#i/
"
6 &(
"l"as"
L)(
c!la#i/
" 6 &(
"l"as"
L)(
c!la#i/"
6 &(
"!ai%i%(
C+" ))#
c!la#i/"
6 &(
"!ai%i%(
' 0.$ 0.4' -0.50' .21 0.4 '.6 3.32 '.0 ' 0 '6.'5 '.2' '.2 3.51
5 2.0 '.3' 0.50' 25.$' '.54 '.11 3.23
3 5.0 '.45 0.344 24.4 '.$1 '.16 3.'1
$ 3.0 2 0.60 50.35 '.31 '.13 3.''
6 $.0 2.23 0.4 5$.45 '.$$ '.1' 3.02
4 6.0 2.3$ 0.41 54.0' '.$4 '.1 5.1
1 4.0 2.6$ 0.1$ 30.6 '.6' '.44 5.
1.0 2.15 0. 3$.52 '.66 '.45 5.4
'0 '0 5.'6 ' $'.14 '.42 '.61 5.65
'' '2 5.36 '.' $1.'$ '.44 '.62 5.36
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Results
Ta+l" 3.3, R"l"as" paa!"#"s )0 )p#i!i$"& 0)!la#i)% PC
Z") O&" Fis# O&" *i(chi )s!"y"-
P"ppas
*i9s)%-
C)7"ll
>
2h-15
1
2h-15
*
2h-145
%
/al"
*C
2h-1435
0.406 5.601 0.116 0.065 0.0' '6.
'5
0.13 0.$'36 0.1 0.015$
2A5 Z") )&" !)&"l
2B5 Fis# )&" !)&"l
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Results
2C5 *i(chi !)&"l
2D5 *i9)% C)7"ll !)&"l
2E5 )s!"y"-P"ppas
Fi( 3.@, R"l"as" i%"#ics 0) 0)!la#i)% PC
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Results
Ta+l" 3.3@, R"l"as" i%"#ics )0 0)!la#i)% *
S.
N).
Ti!"
2hs5
Sa"
))#
#i!"
2hs5
L)(
#i!"
2hs 5
C!la#i/
"
6 &(
"l"as"
L)(
c!la#i/
" 6 &(
"l"as"
L)(
c!la#i/"
6 &(
"!ai%i%(
C+" ))#
c!la#i/"
6 &(
"!ai%i%(
' 0.$ 0.4' -0.50' 1.'2 0.' '.6 3.$'
2 '.0 ' 0 '3.65 '.'4 '.5 3.3
5 2.0 '.3' 0.50' '.$2 '.2 '.' 3.52
3 5.0 '.45 0.344 2$.33 '.30 '.14 3.2'
$ 3.0 2 0.60 50.0$ '.31 '.13 3.'2
6 $.0 2.23 0.4 5$.35 '.$$ '.1' 3.0'
4 6.0 2.3$ 0.41 51.3 '.$ '.41 5.3
1 4.0 2.6$ 0.1$ 32.22 '.62 '.46 5.16
1.0 2.15 0. $0.61 '.4 '.4 5.61
'0 '0 5.'6 ' $4.54 '.46 '.65 5.3
'' '2 5.36 '.' $.61 '.34 '.6' 5.35
Ta+l" 3.8>, R"l"as" paa!"#"s )0 )p#i!i$"& 0)!la#i)% *
Z") O&" Fis# O&" *i(chi )s!"y"-
P"ppas
*i9s)%-C)7"ll
>2h-15
12h-15
*2h-145
%
/al"
*C2h-1435
0.456 3.$$6 0.15 0.0424 0.' '.$61 0.21 0.6331 0.1$4 0.04$
2A5 Z") )&" !)&"l
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Results
2B5 Fis# )&" !)&"l
2C5 *i(chi !)&"l
2D5 *i9)% C)7"ll !)&"l
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Results
2E5 )s!"y"-P"ppas
Fi( 3.3>, R"l"as" i%"#ics 0) 0)!la#i)% *
3.3.8.E C)!paa#i/" in-Vitro D( "l"as" S#&y )0 Th")phylli%" a0#" 1 hs
0)! Op#i!i$"& F)!la#i)%s 7i#h #h" *"lp )0 S#a#is#ical A%alysis 2O%" 'ay
ANOVA5
Ta+l" 3.81, ANOVA
S)c" )0
i%0)!a#i)%
S! )0
sa"s
D"("" )0
0""&)!
M"a% s!
)0 sa"s
Calcla#"&
F /al"
Ta+l" /al"
)0 F
;etween the
formulation 5.2 2 '.6 '.'6
F ? $.'3
at $ B level
of
significance
Fith in the
formulation 4.01 6 '.'1
Total '' 1
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Results
I%#"p"#a#i)%, - The calculated , value %1.1?& is less than that of table value %:.185
a# : 6 level of significance %H >.>:5. !o 9ull hypothesis was accepted. There was
no significance difference between the B drug released from different optimized
formulations.
3.3.8.F. S#a+ili#y S#&y: - !tability study was conducted on only optimized
formulations. The formulation were packed in the aluminium foil and subHected to
stability studies at different temperature and humidity conditions as per the (7*
guidelines viz room temperature %2$0 760B )*& and 3007 4$B)*. The sample
was withdrawn at time intervals of 0+ '$+ 50 days. The sample was evaluated for
possible weight variation+ drug contents+ floating lag time and in vitro release profile.
Ta+l" 3.8, Physical chaac#"is#ics )0 #h")phylli%" 0l)a#i%( !a#i9 #a+l"# )0
+a#ch DPC "p# a# ))! #"!p"a#" 0) 3> &ays
Physical
paa!"#"s
Ba#ch c)&" DPC
> &ays 1: &ays 3> &ays
Feight gain %mg& 4'.25 # '.33 4'.22#'.'5 4'.23#'.3
"ercentage drug
content
1.3#0.$' .5#0.62 .1'#0.$2
Ta+l" 3.83, In-vitro "l"as" &a#a )0 #h")phylli%" 0)! 0l)a#i%( !a#i9 #a+l"#s )0
+a#ch DPC i% >.1N *CL "p# a# R))! #"!p"a#" 3> &ays
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&( "l"as"
!l : !l @>> !l
'. 0.$ 0.'04 0.0' 0.0 '4.' '4.' 1.$$
2. ' 0.'2 0.05$ 0.'4 5'.$ 5'.$ '$.10
5. 2 0.24' 0.03 0.23 33.' 33.54 22.'3. 5 0.5'2 0.0$4 0.21 $'.5 $'.12 2$.'
$. 3 0.564 0.061 0.53 6'.2 62.0 5'.0
6. $ 0.3'2 0.046 0.51 61.3 6.$3 53.46
4. 6 0.36' 0.013 0.32 4$.6 44.'2 51.$6
1. 4 0.$'3 0.0$ 0.3$ 1$.$ 14.33 35.42
. 1 0.$$ 0.'05 0.$' 2.4 $.'4 34.$6
'0. '0 0.635 0.''1 0.$ '06.2 '01.1 $3.3$
''. '2 0.4'5 0.'5' 0.6$ ''4. '2'.5 60.4
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
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Results
Ta+l" 3.88, Physical chaac#"is#ics )0 #h")phylli%" 0l)a#i%( !a#i9 #a+l"# )0
+a#ch PC "p# a# ))! #"!p"a#" 0) 3> &ays
Physical
paa!"#"s
Ba#ch c)&" PC
> &ays 1: &ays 3> &ays
Feight gain %mg& 42.5#2.'3 42.3'#2.' 42#2.36
"ercentage drug
content
.$'#'.62 .3'#'.6' .2#'.2'
Ta+l" 3.8:, In-vitro "l"as" &a#a )0 #h")phylli%" 0)! 0l)a#i%( !a#i9 #a+l"#s )0
+a#ch PC i% >.1N *CL "p# a# ))! #"!p"a#" 3> &ays
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&( "l"as"
!l : !l @>> !l
'. 0.$ 0.''3 0.02' 0.'0$ '1. '1. .3$
2. ' 0.'6 0.056 0.'10 52.3 52.$' '6.26
5. 2 0.251 0.0$2 0.262 36.1 34.0 25.$$
3. 5 0.55' 0.06' 0.50$ $3. $$.3$ 24.45
$. 3 0.563 0.064 0.55$ 60.$ 6'.'$ 50.$4
6. $ 0.35$ 0.010 0.300 42.2 45.24 56.63
4. 6 0.3$ 0.01$ 0.32$ 46.$ 41.01 5.03
1. 4 0.34' 0.0 0.35 44.33 4.3' 5.4
. 1 0.$51 0.016 0.3$ 1.' '.$3 3$.44
'0. '0 0.6'5 0.0''5 0.$6$ '0'.4 '0$.2 $2.60''. '2 0.61' 0.'2$ 0.62$ ''2.$ ''6.0 $1.0
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
Ta+l" 3.8?, Physical chaac#"is#ics )0 #h")phylli%" 0l)a#i%( !a#i9 #a+l"# )0
+a#ch * "p# a# ))! #"!p"a#" 0) 3> &ays
Physical
paa!"#"s
Ba#ch c)&" *
> &ays 1: &ays 3> &ays
Feight gain %mg& 42.'#2.'1 452.'5#2.2$ 452.''#2.''
"ercentage drug
content
.53#'.' .'4#'.2 .'5#'.54
Ta+l" 3.8, In-vitro "l"as" &a#a )0 #h")phylli%" 0)! 0l)a#i%( !a#i9 #a+l"#s )0
+a#ch * i% >.1N *CL "p# a# ))! #"!p"a#" 3> Days
S.N). Ti!"
2hs5
A+s)+. C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&( "l"as"
!l : !l @>> !l
'. 0.$ 0.05 0.0'4 0.01 '$.5 '$.1 4.6$
2. ' 0.'4' 0.05$ 0.'4 5'.$ 5'.$1 '$.6
5. 2 0.253 0.035 0.2' 51.4 51.6 '.31
3. 5 0.50$ 0.0$6 0.21 $0.3 $0.14 2$.35
$. 3 0.5$5 0.06$ 0.52 $1.$ $.2$ 2.65
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Results
6. $ 0.32$ 0.041 0.5 40.2 4'.21 5$.62
4. 6 0.36' 0.01$ 0.32 46.$ 44.4 51.1
1. 4 0.31 0.0' 0.3$ 1'. 15.4 3'.1
. 1 0.$ 0.''0 0.$$ .0 '0'.5$ $0.64
'0. '0 0.641 0.'2$ 0.65 ''2.$ ''$.3 $4.4
''. '2 0.403 0.'2 0.63 ''6.' ''.65 $.14
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
Ta+l" 3.8, Physical chaac#"is#ics )0 #h")phylli%" 0l)a#i%( !a#i9 #a+l"# )0
+a#ch DPC "p# a# 8>>C 4 : 6 R* 0) 3> &ays
Physical
paa!"#"s
Ba#ch c)&" DPC
> &ays 1: &ays 3> &ays
Feight gain %mg& 45.'6#'.4 43.'5#'.12 43.'#'.'5
"ercentage drug
content
1.2#0.2' 1.63#0.5 1.5'#0.61
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Results
Ta+l" 3.8@, In-vitro "l"as" &a#a )0 #h")phylli%" 0)! 0l)a#i%( !a#i9 #a+l"#s )0
+a#ch DPC i% >.1N *CL "p# a# 8>> C4 : 6R* 0) 3> Days
S.N). Ti!"
2hs5
A+s)+
.
C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&( "l"as"
!l : !l @>> !l
'. 0.$ 0.'0 0.02 0.' '1.0 '1
2. ' 0.'' 0.05$ 0.'4 5'.$ 5'.6 '$.1
5. 2 0.26 0.03 0.23 33.' 33.54 22.'1
3. 5 0.501 0.0$6 0.21 $0.3 $0.2 2$.36
$. 3 0.56' 0.066 0.55 $.3 60.' 50.0
6. $ 0.3'$ 0.046 0.51 61.1$ 6.1 53.
4. 6 0.364 0.016 0.35 44.3 4.1' 5.'
1. 4 0.$'3 0.0$ 0.34 1$.$ 14.33 35.42
. 1 0.$65 0.'03 0.$2 5.6 6.02 31.0'
'0. '0 0.63' 0.''1 0.$ '06.2 '0.'3 $3.$4
''. '2 0.4'$ 0.'52 0.66 ''1.1 '22.5 6'.'6Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
Ta+l" 3.:>, Physical chaac#"is#ics )0 #h")phylli%" 0l)a#i%( !a#i9 #a+l"# )0
+a#ch PC "p# a# 8>>C 4: 6 R* 0) 3> &ays
Physical
paa!"#"
Ba#ch c)&" PC
> &ays 1: &ays 3> &ays
Feight gain %mg& 42.36#'.25 45.''#'.'3 45.$1#'.3'
"ercentage drug
content
.63#0.'2 .$#0.5' .2#0.3
Ta+l" 3.:1, In-vitro "l"as" &a#a )0 #h")phylli%" 0)! 0l)a#i%( !a#i9 #a+l"#s )0
+a#ch PC i% >.1N *CL "p# a# 8>> C4 : 6 R* 0) 3> Days
S.N). Ti!"
2hs5
A+s)+. C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&( "l"as"!l : !l @>> !l
'. 0.$ 0.''2 0.02' 0.'' '1. '1. .3$
2. ' 0.'' 0.5$ 0.'4 5'.$ 5'.6' '$.1'
5. 2 0.21' 0.0$2 0.26 36. 34.01 25.$33. 5 0.524 0.060 0.50 $3.0 $3.$3 24.24
$. 3 0.56' 0.66 0.55 $.3 60.23 50.'2
6. $ 0.35' 0.04 0.5 4'.' 42.24 56.'3
4. 6 0.3$ 0.01$ 0.32 46.$ 41.04 5.05
1. 4 0.36$ 0.016 0.35 44.3 4.5 5.6
. 1 0.$5' 0.04 0.3 11.2 0.62 3$.5'
'0. '0 0.60' 0.''' 0.$$ . '02.1' $'.3
''. '2 0.61' 0.'26 0.65 ''5.3 ''6.16 $1.35
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
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Ta+l" 3.:, Physical chaac#"is#ics )0 #h")phylli%" 0l)a#i%( !a#i9 #a+l"# )0
+a#ch * "p# a# 8>>C : 6 R* 0) 3> &ays
Physical
paa!"#"
Ba#ch c)&" *
> &ays 1: &ays 3> &ays
Feight gain %mg& 453.'3#'.13 453.'3#'.1 45$#'.23
"ercentage drug
content
.'2#0.$ 1.'#0.$6 1.'2#0.$'
Ta+l" 3.:3, In-vitro "l"as" &a#a )0 #h")phylli%" 0)! 0l)a#i%( !a#i9 #a+l"#s )0
+a#ch * i% >.1N *CL "p# a# 8>> C4 : 6R* 0) 3> Days
S.N). Ti!"
2hs5
A+s)+. C)%c"%#a#i)% 2!(5 C!. &(
"l"as"
6 C!.
&( "l"as"!l : !l @>> !l
'. 0.$ 0.0' 0.0'4 0.01$ '$.5 '$.5 4.6$2. ' 0.'45 0.52 0.'6 21.1 21.11 '3.33
5. 2 0.253 0.035 0.22 51.4 51.$ '.34
3. 5 0.50$ 0.0$6 0.21 $0.3 $0.16 2$.35
$. 3 0.5$' 0.06$ 0.52 $1.$ $.23 2.62
6. $ 0.324 0.04 0.5 4'.' 42.'6 56.01
4. 6 0.3$4 0.013 0.32 4$.6 44.0$ 51.$5
1. 4 0.36 0.0' 0.3$ 1'.$ 12.44 3'.11
. 1 0.$6 0.'03 0.$2 5.$ $.3 34.43
'0. '0 0.64 0.'2$ 0.62 ''2.$ ''$.5$ $4.64
''. '2 0.404 0.'5 0.6$ ''4.0 '20.3' 60.23
Total amount of drug 200 mg+ dilution factor '0 slope 0.0$35
8.1. PREFORMULATION PARAMETRS
8.1.1. S#&y )% D(
Ta+l" 8.1, R"sl#s a%& &iscssi)% )0 p"0)!la#i)% paa!"#"s )0 &(
S.N). Paa!"#"s R"sl#s C)%clsi)%
'. "hysical characters 7rystalline powder+ white+
Kdorless+ ;itter2. (dentification
"hysical method
%a& Lanthine test
%b& 8elting "oint
%c& oss on drying
%d& *ygroscopicity
Analytical method
%a& MmaD
"ositive
24007
0.5 B
0.04 B%room temp&
0.'6 B%30074$B)* &
240 nm %0.' 9 *7&
265 nm %0.'9 8ethanolic *7&
243 nm %0.' 9 9aK*5
Kn the bases of
these tests it
could be confirm
that the drug
sample was pure
and authentic.
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Results
%b& ( ) spectra
%c& ) f%d& Assay
!howed all characteristics peaks
0.64
.'1$ B
5 !olubility Analysis
(n different solvents
%a& Fater
%b& 0.' 9 *7
%c& 0.' 9aK*
%d& Gthanol
(n different p*
%a& '.2 %0.'9 *7
%b& 5.$
%c& $
%d& 4
%e& 1
'20.1
54.5
20.
26.45
26.43 %mg ml5
25.4' %mg ml&
'4.0 2mg ml&
1.24 %mg ml&
'2.13 %mg ml&
!lightly soluble
!paringly soluble
!oluble
!lightly soluble
(ndicates
solubility slightly
increase as p*
increase+
otherwise it is
independent of
p*
3. 8icromeritics
%a& 7arrNs indeD
%b& Angle of repose
%c& *ausner )atio
24 B
5'0
'.56
"assable flow
$. "articles !ize )ange '0- '$0 micrometer ,ine and very
fine
6. "artition 7oefficient -0.666 %log p& (ndicates more
hydrophilicty
than lipohhilicity4. (onization 7onstant 1.4 and ''.34 (ndicates weak
acidic O weak
basic drug
1. rug "olymer (nteraction
!tudy
9o change in )f valve (ndicates no
interaction
8.1.. S#&y )% Psylli! *s
Ta+l" 8., R"sl#s a%& &iscssi)% )0 psylli! hs paa!"#"s
S.N). Paa!"#"s R"sl#s
*s psylli! D"hs psylli!
'. "hysical 7haracters "owder of psyllium
seed+ "ale buff color+
odorless+ Test less
"owder of psyllium
seed+ "ale buff color+
odorless+ Test less
2. Test for 8ucilaginous 8atter "ositive "ositive
5. p* %'B a=ueous !ol.& 6.1$ 6.1$
3. Ash
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$. GDtractive
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related to change in the porosity of the tablet. *owever as the porosity of the hydrated
matriD independent of initial porosity. Nih)&chi "# al.+ %'6& concluded the
compression force seem to have a little effect on the drug release.
All formulation was prepared with the help of "
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Results
8..? Fl)a#i%( Capa+ili#i"s, - The floating capabilities mainly concern here with
floating lag time and floating duration.
The floating duration should be at least 23 hrs and the floating lag time should be as
low as possible because compleD anatomy and physiology of P(T. The fasted state is
associated with various cyclic movement commonly referred as !i(a#i%( !)#)
c)!pl"9 %887&.The third phase of 887 %burst phase& is characterize by the large+
intense and regular contraction termed as house keeper waves that swept out the
particulate matter %undigested food particles& from the stomach and lasts to '0to 20
minutes. To prevent the formulation from the effect of this phase+ tablet should be
float as fast as possible after reaching in the stomach.
(n similar way the floating duration and dimensional stability are important in case of
once daily formulation obtain the continuous and constant drug release up to the 23
hrs.
(f physical integrity of the formulation is note maintain+ the tablet could break down
in to the small fragments and escape from the upper part of P(T.
8..?.A E00"c# )0 Psylli! *s )% Fl)a#i%( Capa+ili#i"s, - The floating lag time
of formulation "' containing 200 mg of dehusk psyllium was 534#1.6 seconds.This formulation was not able to maintain the dimensional stability upto the re=uire
time %23 hrs& and duration of floating was ''.5#0.2$ hrs. As the concentration of the
dehusk psyllium increased from 200 to 300%': 2 drug: polymer ratio& the floating lag
time reduced to '02. # 2.$6 %batch "5& and floating duration and dimensional
stability both were maintained more than 23 hrs.
!imilar effect were observed with husk psyllium in similar ratio of the drug and
polymer but the floating log time was more than that of dehusk psyllium formulation.The floating lag time of formulation "5 containing 300 mg %':2 drug: polymer& of
husk psyllium was '20 # 2.$2 seconds as compared to dehusk psyllium formulation
"5 %'02. #2.$6 seconds&.
This was due to grater particle size of husk psyllium as compared to dehusk psyllium
which hydrate at the slow rate and take more time to swell. This result in increasing
the floating lags time.
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8..?.B E00"c# )0 S)& CMC )% Fl)a#i%( Capa+ili#i"s: -The !odium 787 was
added to reduce the floating lag time. ,ormulation containing $0 mg sodium 787
had the floating lag time 41 # '.5 and the formulation containing '00 mg of sodium
787 had 4'# 5. The reduction of the floating lag time is due to sodium 787 is a
synthetics agent which hydrated at a faster rate than that of psyllium husk.
!imilar effect was observed with husk psyllium powder. The floating lag time
containing husk psyllium along with $0 mg %batch "3& and '00 mg %batch "$& was
found to be 1$.4#$.05+ 4.5#'.$5 respectively.
There was no measurable effect of concentration !od 787 on floating duration and
dimensional stability.
8..?.C E00"c# )0 S)&i! Bica+)%a#" )% Fl)a#i%( Capa+ili#i"s, - The floating lag
time reduced as the concentration of sodium ;icarbonate increased in both cases i.e.
dehusk and husk formulations.
Ta+l" 8.3, E00"c# )0 s)& +ica+)%a#" )% 0l)a#i%( la( #i!"
S.N) C)%c. )0 s)&i!
+ica+)%a#"
265
D"hs 0)!la#i)% *s 0)!la#i)%F C F L T F C F L T
'. '0 "6 1#2.$' "6 '0$#$.2
2. '$ "3 41#'.5 "3 1$.4#$.05
5. 20 "4 60.4#2.$2 "4 6.4#2.01
,7 ,ormulation code+ ,T ,loating lag time
The concentrations of sodium ;icarbonate effect the duration of floating in both cases
i.e. dehusk and husk formulation. The duration of floating was 22#0.6'hrs %batch
"6& with '0 B sodium ;icarbonate and 23 hrs %batch "3+ "4& when the
concentration of sodium ;icarbonate 7as '$ B %batch "3& and 20 B.% batch "4&.
(n case of husk the duration of floating was 20.2#0.1$hrs %batch "6& with '0 B
sodium ;icarbonat" and 23 hrs when the concentration of sodium ;icarbonate was '$
B %batch "3& and 20 B.% batch " 4&.This might de due to the gas generated by '0 B
sodium ;icarbonate might not be sufficient to keep the formulation in floating state
for prolonged period of time %23 hrs& where as the in case of '$ B+ 20 B sodium
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Results
;icarbonate sufficient gas produced to keep the formulation in floating state for 23
hrs.
The concentration of sodium ;icarbonate oppositely effect the dimensional stability
but this effect was not significant.
8..?.D E00"c# )0 Ac- Di S)l )% Fl)a#i%( Capa+ili#i"s, - Ac- i I!ol is a super
disintegrate when it come in contact with the medium swell rapidly at least two times
of its original volume. The psyllium husk and sodium ;icarbonate simultaneously
form the gel network due to which the swell mass of Ac-i-!ol is retaining in the gel
and tablet does note disintegrate.
The additional advantage of it+ the maDimum water uptake is achieved in short period
of time as the water reach in the deep in to the core of the tablet.
;eing a disintegrate Ac-i-!ol creates the pores and the 7K2 generated with the
reaction of !odium ;icarbonate and acidic medium was entrapped in the pores
resulting the floatation of the tablets i.e. the log time further reduced.
$ B and '0 B of Ac-i-!ol were used. The formulation containing '0 B Ac-i-!ol
%batch "72+ 3$# 2 seconds& take less time to float as compared to the formulation
containing $ B Ac-i-!ol %batch "7'+ $$.'# '.$5 seconds& in the case dehusk psyllium. !imilar effect was observed with formulation containing husk psyllium.
,ormulation containing *"87 C '00 8 showed very short lag time %batch *+ '0.5
#'.$5 seconds& without sod 787 and Ac-i-!ol.
8..?.E E00"c# )0 *a&%"ss )% Fl)a#i%( Capa+ili#i"s, - As the hardness increased
the floating lag time also increased. Kn immersion of tablets %batch "72+ "72+ * &
of hardness around 2 kg cm
2
in 0.' *7 solution floated immediately 3$.'#'.$5seconds for "72+ $0#'.65 seconds for "72+ zero for * & as compared to the
formulation 3 kg cm2 took more time % '0 # $ seconds for "72+ 200#1 seconds for
"72+'0.5 # '.$5 seconds *& to come up to the surface. The tablets hardness 6 kgcm2
showed the no floating in case of dehusk formulation and husk formulations while the
formulation containing *"87 ,loat in 0 # 4.$ seconds.
(n fact+ buoyancy of the tablet is governed by both the swelling the outer surface of
the tablets when it comes in the contact with the gastric fluids+ and the presence of the
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Results
internal void %"orosity& in the dry centre of the tablet. These two factors are essential
for the tablet to ac=uire bulk density less than that of the gastric fluid i.e. '.03 gmcm 5
which helps them to remain buoyant on gastric fluids %sheth and tossoumnian+ '4&
7ompression force of these tablets to high degree hardness may result in reduction of
porosity of the tablets and moreover+ the compressed hydrocolloids particle on the
surface of the tablets fail to hydrate rapidly when the tablets come in to contact with
the gastric fluid+ and as a result of this+ the capability of the tablets to float is
significantly reduced.
8.. D"%si#y, - The density of the formulation should be less than that of '.03
kgcm5
%7hues et. al. '0&.
The density of all the formulation was in the range of 0.42 # 0.01$ to '.034 # 0.023
for all formulation.
8.. S7"lli%( I%&"9, - ;aumgartner et al. 2'1& 7oncluded that tablets composed
of polymeric matrices build a gel layer around the tablet core when they come in
contact with water This gel govern the drug release. Cinetics of swelling is important
because the gel barrier is formed with water penetration. !welling is a vital factor toensure floating. To obtain floating+ the balance between the swelling and water must
be reported.
As shown in table the formulation containing psyllium husk %both grades dehusk and
husk psylluim& took about 6 to 1 hrs to complete swell as compared to the formulation
prepared with *"87 k'00 8 that took 3-$ hrs to complete swell.
(n the first hr of study+ the swelling indeD of formulation "5 was $4.' B %dehusk
psyllium&+ "5 was 36.05 B %husk psyllium&+ and * was 1$.2 B %*"87 C '00 8&The difference in the swelling indeD was because of the psyllium husk is a natural
agent took more time to hydrate as compared to synthetic agent *"87 C '00 8.
The difference in the swelling indeD between the formulation prepared with husk and
dehusk psyllium was due to the difference in the particle size. The particle size of
husk psyllium powder was grater than that of the dehusk psyllium resulting the
delayed the hydration.
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Results
After complete swelling the formulation prepared with husk psyllium %"5 531.'$ B&
showed the grater-swelling indeD than that of dehusk psyllium %;atch "5+ 553. B&+
this was due to presence of husk in husk psyllium+ which enhance the swelling indeD.
Addition of !od .787 enhanced the swelling indeD at initial stage %batch "3 40.
B+ batch "3 $1.B& due to faster rate of hydration as compared to psyllium powder.
The formulation prepared with sod .787 and Ac- i I!ol showed the swelling indeD
after first hr of study was 41.'3 B %batch "72&+ 6$.'2 B %batch "72& due to he
grater efficiency Ac- i I!ol for water and faster hydration.
8..@ E)si)% S#&y, -The tablets containing the husk psyllium showed the higher
erosion after '2 hrs %.2$B batch "5& than that of formulation prepared with dehusk psyllium %4.3B batch "5&. Addition of !od 787 reduced the erosion in both
formulation prepared with husk %6.4 B batch "3& and dehusk psylluim %$.14 B batch
"3&.
,ormulation containing Ac-i-!ol further reduced the percent erosion %3.$ B "72+
$.0' B batch "72& than that of formulation prepared with psyllium alone %4.3B
batch "5 .2$B batch "5& or in combination with sod 787 %$.14 B batch "3+
6.4 B batch "3&
The formulation containing pure *"87 C '00 8 showed the lowest erosion among
all the preparation.
8..1> In-Vitro R"l"as" S#&y
8..1>.A E00"c# )0 Psylli! *s )% In-Vitro R"l"as": - The formulation "'
%dehusk psylluim& and "'%husk psyllium& %200 mg psyllium husk+ ':' drug :polymer&
the burst release after 2 hrs was 55$.$'and 54.2 and final release after '2 hrs was
12.22 and 10.42 respectively. ;ut these formulations were not able to maintain the
dimensional stability and the drug release was note up to 23 hrs. !o the amount of
psyllium was increased to 500mg %':'.$ drug: polymer& and 300 mg %':2+ drug:
polymer&. The burst release after 2 hrs was 23.' %"2&+ 2.5 %"2& for the
formulation containing 500 mg of psyllium husk and 20.4 %"5&+ 2$.32 %"5& for the
formulation containing 300 mg of psyllium husk. ,inal B cumulative drug release
after '2 hrs 66.25 %"2&+ $4.$6 %"2& for the formulation containing 500 mg of
psyllium husk. and 34.1 %"5& and 3.$1 %"5& for the formulation containing 300 mg
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Results
of psyllium husk. This might be due to gelling property of psyllium husk. As the
concentration of psyllium husk incased resulting in increased the gel concentration+
which lead to increased the diffusion pathway and thus decreased the diffusion rate+
which decreased the release of the drug+ and complete release was obtained in 23 hrs.The burst release of formulation prepared with hush psyllium was slightly more than
that of dehusk .(t was due to larger particle size of husk psyllium than that of dehusk
psyllium which took more time to hydrate than that of dehusk.
The total B cumulative drug release after '2 hrs from dehusk psyllium formulation
was slightly more than that of husk psyllium formulation. (t was due to the presence
of husk in hush psyllium+ which provides an additive effect in swelling resulting
slightly reduction in drug release.
2A5 *s psylli!
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Results
2B5 D"hs psylli!
Fi( 8.1, E00"c# )0 psylli! hs )% In- vitro &( "l"as"
8..1>.B E00"c# )0 S)&i! CMC )% In-Vitro R"l"as", - Two =uantity of the
sodium 787 %$0 O'00 mg& were used in both grades of psyllum husk.
There was no significant effect on the drug release but the burst release after 2 hrs was
reduced. The reason behind it faster rate of hydration of sodium 787 than psyllium
husk..
The B burst release of after 2 hrs for formulation containing sodium 787 was 20.'3
%batch "3+ dehusk psylluim&+ 22.40 %batch "3+ husk psyllium& than that of the
formulation with out sodium 787 22.4 %batch "5& and 2$.32 %batch "5&.
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0
10
20
30
40
50
60
0 5 10 15Time (hrs)
% C u m . D r u
g r e l e a s e P3
P4
P5
2A5 *s psylli!
0
10
20
30
40
50
60
0 5 10 15
Time(hrs)
%
C u m .
D r u g r e l e a s e
DP3
DP4
DP5
2B5 D"hs psylli!
Fi( 8., E00"c# )0 S)&. CMC )% in- vitro &( "l"as"
8..1>.C R"l"as" 0)! #h" F)!la#i)% C)%#ai%i%( *PMC 1>> M, - Tocompare the release pattern of the psylluim %both grades&+ separate formulation
containing *"87 C '00 8 was prepared in ': 2 ratio of drug and polymer.
The initial B burst release after 2 hrs with *"87 C'00 8 was '.$2 %batch *& which
was less than that of preparation prepared with psyllium powder %batch "3 -20.'3
batch "3- 22.4&. The B cumulative drug release after '2 hrs was $.34 # %batch *&+
3.34 %batch "3& and 36.1 %batch "3&.
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(nitial burst release in case of *"87 C'00 8 was low than that of psyllium due to
faster rate of swelling of *"87 C'00 8. After '2 hrs release of drug from *"87
was more than that of formulation prepared with psyllium because the swelling indeD
of psyllium was more than that of *"87 C'00 8.
Fi( 8.3, Gffect of *"87 C '00 8 on in- vitro drug release
8..1>.D E00"c# )0 C)ss P)/i&)%" )% In-Vitro R"l"as", - In order to improve the
release profile of formulation prepared with psyllum husk as parallel to *"87 C'00
8 the cross povidone was used.
,ormulation containing 0 B of Ac-i-!ol showed the cumulative B drug release
3.34 %batch "3&+ 36.1 %batch "3& and formulation containing $B Ac-i-!ol
showed the cumulative B drug release was $$.24 %batch 7"'&+ $2.03 %batch "7'&.
,ormulation containing '0B Ac-i-!ol showed the cumulative B drug release was
60.0' %batch 7"2&+ $1. '$ %batch "72& which was comparable to formulation
prepared with *"87 C '00 8 %batch *+ $.34&.
The reason behind it Ac-i-!ol is a super disintegrate and creates pores in the net
work form by psyllium and sod.787.due to which the release of the drug increased
in the latter hrs.
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0
10
20
3040
50
60
70
0 5 10 15Time(hrs)
%
C u m .
D r u g
r e l e a s e
P4PC1PC2
2A5*s psylli!
0
10
20
30
40
50
60
70
0 5 10 15Time(hrs)
% C u m D r u g r e l e a s e
DP4DPC1DPC2
2B5 D"hs psylli!
Fi( 8.8: E00"c# )0 Ac-Di-S)l )% in- vitro &( "l"as"
8..1>.E E00"c# )0 S)& Bica+)%a#" )% In-Vitro R"l"as", - !odium bicarbonateshowed the opposite effect on percentage cumulative drug release. This might be due
to the alkaline nature of the sodium bicarbonate+ which create an alkaline environment
around the tablet. Theophylline was less soluble in the alkaline environment that
decreased the release of drug from the formulation. ,ormulation containing '0 B
9a*7K5 shown the drug release after '2 hrs was $'.32 %batch "6&+ 31.5 %batch
"6& as compared to formulation 20 B 9a*7K5 the drug release after '2 hrs was
34.44 %batch "4&+ 3$.$$ %batch "4&
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2A5 *s psylli!
2B5 D"hs psylli!
Fi( 8.:, E00"c# )0 s)&. +ica+)%a#" )% in- vitro &( "l"as"
8..1>.F E00"c# )0 A(i#a#i)% )% I%-/i#) D( R"l"as", -This study was conducted
only on optimized formulation like "72 %dehusk&+ "72 %husk&+ * %*"87 C '008&.
At $0 rpm cumulative percentage drug release after '2 hrs was formed to be $4.26
%"72&+ $6.4' %"72&+ $1.2' %*&.
At '00 rpm cumulative percentage drug release after '2 hrs was 60.0' # 0. %"72&+
$1.'$ %"72&+ $.34 %*&.
The release of drug was slightly higher at '00 rpm+ since the delivery by diffusion
mechanism occurred through the gel layer+ the system is mainly based on this release
mechanism get effected by stirring.%,(P. 3.6&
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Results
2A5 DPC
2B5 PC
2C5 *
Fi( 8.?, E00"c# )0 RPM )% in- vitro &( "l"as"
8..11. R"l"as" i%"#ics, - The In-vitro release data of optimized formulations were
treated with different kinetics models to eDplain the release kinetics of theophylline
from floating matriD tablets. These models were zero order+ first order+ higuchi model+
hiDon-crowel model and korsemayer peppas model. *iguchi model was considered as
the best fitted model with the highest value of correlation coefficient %r2&. The value
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r2 of different optimized formulation "72+ "72+ * were found to be 0.4+ 0.0'+
and 0.' respectively.
The release data were further treated by )itger-"eppas or power law to calculate the
value of n %release eDponent&. The values of n %release eDponent& for different
optimized formulations were found to be 0.$322 for "72 %dehusk psyllium&+ 0.$'36
for "72 %husk psyllium&+ and 0.6331 for *%*"87 C '00 8&. The value of n indicate
that the release mechanism from different formulation was the non-fickian diffusion
%anomalous type&+ controlled by the diffusion through swollen matriD.
8..1. D( P)ly!" I%#"ac#i)% S#&y )% Op#i!i$"& F)!la#i)%: - rug and
polymer interaction in the optimized formulation was checked with the help of T7
and ,T-() study.
T7 data showed that there was not a significance difference in the ) f value. ,T-()
data also showed that the characteristics peaks of drug of were observed in the ,T-()
!pectra of formulation prepared with "syllium husk %"72 O "72& and *"87 C
'00 8.
8..13. S#a#is#ical A%alysis, - Analysis of variance %A9K