Introduction to Pharmaceutics-1 PCT 2213rd Semester )8/14/15 1 IHS-Gaboronenit-1Po!ders and Granu"esnit-2 Semiso"id #osa$e %ormsnit-3 &mu"sions nit-4 Sus'ensions nit-5 Pharmaceutica" Ca"cu"ations Tota" Credit ( 3)ssessment ( 2C)s*+,-) . &nd o/ sem0 &1am*4,-)8/14/15 2 IHS-Gaborone2ecommended 3oo4s 10 Pharmaceutica" dosa$e /orms and dru$ de"i5er6 s6stems )nse" H0C7 Po'o5ich 20 Pharmaceutics7 The science o/ dosa$e /orm desi$n7 80& )u"ton 30 2emin$ton7 The science and 'ractice o/ Pharmac6 9o"-1 : 2 40 Pharmaceutica" Ca"cu"ations b6 Stoc4"osa : )nse"50 )n6 other handouts / 2e/erence materia" $i5en to the c"ass 8/14/15 3 IHS-Gaboronenit-1Po!ders and Granu"es8/14/15 4 IHS-Gaboronenit contents 10 Po!ders and $ranu"es as dosa$e /orms20 S'ecia" 'rob"ems in 'o!dered dosa$e /orms 30 %actors a;ectin$ dru$ a5ai"abi"it6 /rom 'o!dered dosa$e /orms 40 Pac4a$e and stora$e o/ 'o!ders8/14/15 5 IHS-GaboroneTe and si>e ana"6sis Ca"cu"ations8/14/15 + IHS-Gaborone#e=nitions 8icromeritics? Science o/ sma"" 'artic"es Po!ders? Is a mi1ture o/ =ne"6 di5ided dru$s and /or Chemica"s in a dr6 /orm )ccordin$ to 30P ( subdi5ided so"ids containin$ constituent 'artic"es !hich can ran$e 1025um @ 10Amm in diameter )s #% ( are /ormu"ations in !hich 'o!dered dru$ has been mi1ed !ith 'o!dered e1ci'ients to 'roduce =na" /ormu"ations &$0 ard o/ $eneration o/ to1ic dust7 !hich ma6 arise durin$ the hand"in$ o/ the 'o!ders0+0 8ateria"s7 !hich are s"i$ht"6 h6$rosco'e7 ma6 adhere : /orm a ca4e i/ stored as a 'o!der08/14/15 1, IHS-GaboroneSie5e Fumber ) number used to desi$nate the si>e o/ the Sie5e7 !hich corres'onds to the no0 o/ o'enin$s 'er "inear inch &0$00 Sie5e 2, !i"" ha5e 2, o'enin$s in 1 "inear inch Sie5e o'enin$ Its an a''ro1imate si>e o/ a'erture o/ a $i5en sie5e as $i5en in SP &0$0 sie5e no 2, !i"" ha5e 2, o'enin$ 'er "inear inch and each o'enin$ !i"" ha5e an a'erture si>e ( 85,Gm8/14/15 11 IHS-GaboroneSome common"6 used sie5e noSieve NumberSieve opening (m)2, 85,4, 425+, 25,8, 18,12, 1250 000 00H H4,, 388/14/15 12 IHS-Gaborone)n$"e o/ re'ose*I ( Tan-1 h/r) The ma1imum s"o'e measured in de$rees /rom the hori>on at !hich "oose so"id materia" !i"" remain in '"aceor)n$"e o/ re'ose o/ a $ranu"ar 'o!der is the stee'est an$"e o/ descent or di' re"ati5e to hori>onta" '"an to !hich a materia" can be 'i"ed u'0 I/IJ 5,unsatis/actor6 /"o!I( 25or "ess than 25 5er6 $ood /"o! 'ro'erties8/14/15 13 IHS-Gaborone8/14/15 14 IHS-GaboroneG"idents &1ci'ients that increase Do! 'ro'erties o/ $i5en materia" 36 correctin$ sur/ace irre$u"arit67 reducin$ /riction or b6 neutra"i>in$ sur/ace char$es b/! 'artic"es&0$07 8a$0 Stearate7 )erosi" *co""oida" si"icon dio1ide)7 Starch7 Ta"c8/14/15 15 IHS-GaboroneGeometric mi1in$/di"ution *doub"in$ u' method)8i1in$ o/ in$redients accordin$ to order o/ their increasin$ !ei$ht/5o"ume in eCua" 'ro'ortions &0$0Consider the /o""o!in$ master /ormu"a ) (1,$3 (5,$C (4,$# (E,$Bhat cou"d be the bene=ts K 8/14/15 1+ IHS-GaboronePo!der mi1in$ techniCues Spatulation isthecombiningofmaterials(2ormorepowders)intoa homogeneous mixture by continuously mixing them together &smoothingthemassoutonasmoothsurfacewitha spatula Trituration istheprocessforreducingtheparticlesizeofasubstance by grinding, eg grinding of powders in a mortar with a pestle Sifting relatestoputtingthroughasieveorstrainingdeviceto separate fine particles from coarse ones Tumbling8/14/15 IHS-Gaborone 1A)d5anta$e o/ 'o!ders/$ranu"es 10 Stabi"it6 So"id are more stab"e than "iCuids &0$0*)m'ici""in))ntibiotics 'o!ders dr6 /orm ( 2-3 6rs she"/ "i/eBhi"e "iCuid o/ same antibiotics ( 1-2 !ee4s20 8ore suitab"e/con5enient #% /or "ar$e dose&0$0 8a$0Trisi""icate )ntacid *1-5$)8/14/15 18 IHS-Gaborone30 %aster disso"ution rate/3ioa5ai"abi"it6 Increase S0) -------increase disso"ution 2a'id onset o/ action 40 Can be ta4en ora""6 b6 some 'atients !ho areunab"e to s!a""o! other so"id dosa$e /ormssuch as ca'su"es and tab"ets 8/14/15 1E IHS-Gaborone#isad5anta$es Incon5enient to carr6 / hand"e*e1ce't !hen 'resented as di5ided #%)n'"easant Taste Fot 5er6 suitab"e ##S /or 'otent dru$s #i5ided #% can be used ho!e5er Tabs are 're/erredFot suitab"e /or acid "abi"e / &n>6me 'rone dru$s*Coated $ranu"es ma6 be used)8/14/15 2, IHS-Gaborone#isad5anta$esHH0 *Cont0)Poor/8isunderstandin$ about correct method o/ useHi$her decom'osition rate incase o/ H6$rosco'ic7 de"iCuescent or aromatic in$redients3ecause o/ di;erent 'artic"e si>e/densit6 di;0 'o!der mi1 can be 'art"6 se'arated0 Fon uni/orm distribution 8/14/15 21 IHS-GaboronePo!ders 9S Granu"esPowdersGranules Com'arati5e"6 'oor Do! 'ro'erties %"o! !e"" com'ared to tab"ets7 $ood choice /or com'ressin$ tabs 2e"ati5e"6 "ess stab"e *'h6sica""6 and Chemica""6) due to inc0 S0) : )tm0 &;ect Has "ess sur/ace area7 more stab"e to atm0 e;ect 8ore "i4e"6 to hardenin$ / ca4e /ormation on "on$ stora$e Less "i4e"6 %or some 'o!ders7 dru$s Doat on the sur/ace7 diMcu"t to ma4e so"ution 8ore easi"6 !etted b6 the so"5ents7 $ood choice reconstitution "iCuids 2e"ati5e"6 'oor com'ressibi"it6 Good com'ressibi"it6 Chances o/ non uni/orm dosin$ are more 2e"ati5e"6 more uni/ormit6 o/ contents in case o/ $ranu"es 8ore dust due to sma"" '0s Generate "ess dust on hand"in$ Com'arati5e"6 "ess a''ea"in$ Ha5e a more e"e$ant a''earance 2e"ati5e"6 sim'"e method o/ 'rocessin$//ormu"ation It in5o"5es more 'rocessin$7 e1'osure to heat and contact !ith so"5ents8/14/15 22 IHS-GaboronePre'aration o/ Granu"es Bet method 8oistenin$ the desired 'o!der Passin$ 'aste "i4e mass thru sie5e no 4-140 Tra6 dr6 / o5en dr6 / 5acuum dr6Pac4ed and "abe"ed 8/14/15 IHS-Gaborone 23#r6 method Po!der materia" is 'assed throu$h a ro"" com'actor Granu"atin$ machine0 #ensi=ed sheets or Da4es The com'acted 'o!der is then $ranu"ated to uni/orm 'artic"e si>e b6 'assin$ throu$h a mechanica" $ranu"ator0 8/14/15 IHS-Gaborone 248/14/15 IHS-Gaborone 25Po!ders and $ranu"es as dosa$e /orm08/14/15 2+ IHS-GaboronePo!ders / Granu"esThera'eutic use?)s a true : 'ro'er 'harmaceutica" dosa$e /ormFon thera'eutic use?/or the 're'aration o/ other dosa$e /ormsTab"ets7 Ca'su"es7 Sus'ensions7 So"utions etc3u"4/di5ided/dustin$/insuNations/#PI/2econstitution)"" 'o!ders are stored at dr6 '"ace )!a6 /rom chi"dren8/14/15 2A IHS-Gaborone3u"4 Po!ders8i1ed in$redients are 'ac4ed suitab"e containers "i4e !ide mouthed bott"es or $"ass OarsConstituents are non to1ic / Less 'otent Lar$e doses can be dis'ensed sua""6 su''"ied !ith a measurin$ s'oonPro'er directions /or use shou"d be 'ro5ided8/14/15 28 IHS-Gaborone3u"4 Po!ders *ContH)&0$0 Com'ound 8a$ Trisi"icate 'o!der 2e/reshens sa"t *"a1ati5e) #ouch 'o!ders /or 5a$ina" irri$ation/ c"eansin$ #ietr6 su''"iments and /eedin$ /ormu"a0ST starch)Stora$e?C"osed Lid7 #r6 '"ace7 )!a6 /rom chi"dH00&1am'"es)nti/un$a"/ )ntibacteria" /oot 'o!ders0Qinc undec6"inate7 Ch"orohe1idineLubricatin$ dustin$ 'o!der7 Ta"c 8/14/15 35 IHS-Gaborone8/14/15 IHS-Gaborone 3+InsuNations )re medicated 'o!ders intended to be b"o!n into re$ions such as ear7 nose7 and throat !ith the he"' o/ an insuNators Fot 5er6 acce'tab"e7 In-e"e$ent and "ess con5enient to use7 8a6 sho! s6stemic e;ects *2a'id abosr'tion) Some dru$s are more ra'id"6 absorbed /rom "un$s than ora" use0 &0$0 Sodium Chromo$"6co"ateTraditiona" insuNator re'"aced b6 )d5ance de5ices7 Handiha"er7 )ccuha"er7 &tc08/14/15 3A IHS-Gaborone#r6 'o!ders /or inha"ation *#PIs)#PIs are used to de"i5er medicaments to "un$s in a dr6 'o!der /orm usin$ a hand-he"d de5ice7 as 6ou inha"e throu$h it0 It does not ha5e 'ro'e""ant "i4e 8#I do0 &0GSeretide )ccuha"er7 *Can 6ou "ist !hat does serretide contains) Handiha"er ses a ca'su"e in de5ice !hich is bro4en do!n as 6ou o'erate and than u inha"e medicaments0 8/14/15 38 IHS-Gaborone8/14/15 IHS-Gaborone 3E8/14/15 IHS-Gaborone 4,%#) a''ro5ed )/re>>a *Insu"in #PI)8/14/15 IHS-Gaborone 419ideo #emonstration8/14/15 IHS-Gaborone 42%or o'timum de"i5er6 and absor'tion into the "un$s77777777 Bhat shou"d be the Partic"e si>eKKKK8/14/15 43 IHS-Gaborone8/14/15 IHS-Gaborone 44I/ 'artic"e si>e is "ess than ,05 micron7 than dru$ ma6 be e1ha"ed out !ith breath !hen $i5en as 'o!dered #%H000e and Si>e distribution ana"6sis 8/14/15 IHS-Gaborone +4Partic"e si>e and Si>e distribution ana"6sis ) number o/ methods can be used inc"udin$ 10 8icrosco'6 Ca"ibrated $rid bac4$round20 Sie5in$30 Sedimentation rate Termina" sett"in$ 5e"ocit6 40 Li$ht ener$6 di;raction 2eduction o/ "i$ht reachin$ the sensor50 Laser ho"o$ra'h6 3# 'icture b6 ho"o$ra'h6 camera +0 Cascade im'act Stri4in$ sur/ace !ith air stream8/14/15 IHS-Gaborone +5Sie5in$ techniCueSie5e number KSie5e e or other meta"s 8/14/15 IHS-Gaborone +ASieve No. Sieve Opening (m)2, 85,4, 425+, 25,8, 18,12, 125H00 H04,, 38SP characteri>e Po!ders b6 /o""o!in$ descri'ti5e terms 8/14/15 IHS-Gaborone +8Type o powder !ll par"i#les pass "hru Sieve No No" more "han9er6 coarse 8 2,- thru +,Coarse2, 4,- thru +,8oderate"6 coarse4, 4,-thru 8,%ine+, 4,- thru 1,,9er6 =ne1,, Fo "imit8/14/15 IHS-Gaborone +EPo!ders ca"cu"ations 8/14/15 IHS-Gaborone A,Bhi"e dea"in$ 'o!ders ca"cu"ations )"!a6s ca"cu"ate /or at "east 1 e1tra 'o!der to com'ensate "oss o/ 'o!der durin$ mani'u"ations I/ amount o/ acti5e in$redient is "ess than minimum !ei$hab"e Ct6 than di"utions *triturations) are to be made8in0 !ei$hab"e Ct6 is di"uted o5er se5era" time to obtain reC0 dose8/14/15 IHS-Gaborone A1)0 #oub"in$ u' method / Trituration 30 Ca"cu"ations in5o"5in$ 'o!der 5o"umes8/14/15 IHS-Gaborone A2&0$021 H6oscine H3r3,, mc$mitte 4 'o!dersone to $i5en 3,minutes be/ore Oourne6*2emember? minimum 'o!der !ei$ht /or di5ided 'o!der ( 12,m$) Ca"cu"ate /or 5 doses)cti5e reC0( K#i"uent *"actose) reC0 ( K8/14/15 IHS-Gaborone A3Ste'-1H6oscine H3r(1,,m$#i"uent(E,,m$Ste'-2Triturate ) (1,,m$#i"uent (E,,m$Ste'-3Triturate 3 (K#i"uent(K8/14/15 IHS-Gaborone A4&1am'"e 21 Send 1, as'irin 'o!ders 2,,m$ /or a chi"do/ 3-6ears *144$)Is di"ution reCuiredK3,, m$ tabs are a5ai"ab"e in dis'ensar6 8/14/15 IHS-Gaborone A5&1am'"e Ca"cu"ate Cuantities reCuired to ma4e 8 'o!ders each containin$ 2,,mc$ o/ di$o1in 'er 12, m$ o/ 'o!der0se "actose as a di"uents 8in0 !ei$hab"e Ct6 ( 1,,m$ *c"ass 3 ba"ance)8/14/15 IHS-Gaborone A+Ca"cu"ation in5o"5in$ 'o!ders 5o"umePo!der dis'"acement&1am'"e a) Ca"cu"ate the 5o"ume o/ sus'ension occu'ied b6 amo1ici""in 'o!der 15,mL @ 111mL( 3EmL8/14/15 IHS-Gaborone AAb) Ruantit6 o/ amo1ici""in 'resent in entire bott"e 5mL contains(25,m$ 15,mL contains(A5,,m$c) 9o"ume o/ sus'ension that !i"" contains 5,,m$/5mL A5,,m$ /5,,m$/5mL(A5mLd) 9o"ume o/ 'uri=ed !ater reCuired A5mL-3EmL (3+mL o/ !ater to be added08/14/15 IHS-Gaborone A8I/ the 5o"ume o/ 25,m$ o/ ce/tria1one sodium *'o!dered) is ,01mL0 Ho! man6 mL o/ di"uents shou"d be added to 5,,m$ o/ ce/tria1one to ma4e 25,m$ / mL concentrated sus'ension0 9o"ume o/ ce/tria1one K%ina" 5o"ume o/ 'roduct0K9o"ume to be added0K8/14/15 IHS-Gaborone AE8/14/15 IHS-Gaborone 8,Some 'ractice 'rob"ems8/14/15 IHS-Gaborone 818/14/15 IHS-Gaborone 828/14/15 IHS-Gaborone 838/14/15 IHS-Gaborone 84