pharmaceutical additives for liquid dosage form

Pharmaceutical Pharmaceutical Additives Used for Additives Used for

development of liquid development of liquid oral oral

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Presented By, Chetan M. Jain

First Year M.Pharm(Quality Assurance)

Government College of Pharmacy,Amaravati.

DrugDrug APIAPI A substance which has a therapeutic effect when A substance which has a therapeutic effect when

administered.administered. Drug is not administered as it is.Drug is not administered as it is.

CHETAN JAINCHETAN JAIN 22

Pharmaceutical Pharmaceutical AdditivesAdditives

Substances which are of little or no therapeutic value, but which Substances which are of little or no therapeutic value, but which are added to the formulation in order to,are added to the formulation in order to,

Help the productionHelp the production Maintain physicochemical stabilityMaintain physicochemical stability Improve patient acceptabilityImprove patient acceptability To improve the functioning of the dosage form as a DDSTo improve the functioning of the dosage form as a DDS

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Pharmaceutical aids, necessities, adjuvants or excipients.

Ideal PropertiesIdeal Properties Physiologically inertPhysiologically inert Physiologically stablePhysiologically stable Do not impart any undesired taste, colour and odourDo not impart any undesired taste, colour and odour Non-toxic, non-irritant and non-sensitizing.Non-toxic, non-irritant and non-sensitizing. Effective in low conc.Effective in low conc. Free from microorganismsFree from microorganisms Not interfere with bioavailability of the drug.Not interfere with bioavailability of the drug. Accepted by regulatory authorities.Accepted by regulatory authorities.


Pharmaceutical Additives used in Pharmaceutical Additives used in Liquid Dosage FormLiquid Dosage Form

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Vehicles

SurfactantsHydrocolloidsAntioxidants

Complexing agentsPreservatives Colouring

agents

Flavouring agents

Sweetening agentsBuffers

Tonicity adjusters

Liquid Dosage Forms

CHETAN JAINCHETAN JAIN

VehiclesVehicles Medium in which ingredients of a formulation are dissolve, Medium in which ingredients of a formulation are dissolve,

suspended or dispersed.suspended or dispersed. Pharmaceutical vehicles can be classified as underPharmaceutical vehicles can be classified as under

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Aqueous vehicles: Water, Aromatic Water, Alcohol,glycerin, Propylene Glycol.

Oily vehicles: Vegetable oils, mineral oils, organic oily bases or emulsified bases.


WaterWater

CosolvencyCosolvency


Lack of toxicity, Physiological compatibility,and its ability to dissolve a wide range of materials.Potable waterPurified water BP.Phenobarbitone, Aminophylline- Carbon dioxide.Apomorphine and Ergotamine - Oxidation

Water miscible solventsWater/ethanol blend, sorbitol , glycerol, propylene glycol and syrup. Propylene glycol and water for Co-trimoxazole.Paracetamol elixer- Alcohol,propylene glycol and syrup.

SurfactantsSurfactants Solubilising agents Solubilising agents

Wetting agentWetting agent

Emulsifying agentsEmulsifying agents

Antifoaming agentsAntifoaming agents

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HLB value- 15 to18.eg. Polysorbate 80.

HLB value 8 to 10Tweens, spans ,SLS

o/w emulsifiers- 8 to 18w/o emulsifiers-3 to 6Glycol, glycerol esters, cetrimide.

HLB- 1.5 to 3Castor oil, fatty acids.


Anti-oxidantsAnti-oxidants Effective when used in their soluble form.Effective when used in their soluble form. Conc. 0.01 to 1%Conc. 0.01 to 1%

True AntioxidantsTrue Antioxidants

Reducing agentReducing agent

Synergist antioxidantsSynergist antioxidants

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Act by suppressing the formation of free radical.Eg. Alphatocopherol, BHA, BHT, Methyl gallate.

These get preferentially oxidised over the drug.Eg. Sodium sulphide, Sodium bisulphide,sodium metabisulphide.Used in combination with above.Act by regeneration of antioxidant radical or by chelating metals.Eg. EDTA, Ascorbic acid, citric acid.. CHETAN JAINCHETAN JAIN

HydrocolloidsHydrocolloids

High mol. Wt. subs High mol. Wt. subs Produce highly viscous soln, suspension or gels.Produce highly viscous soln, suspension or gels. Natural : acacia, tragacanth, agar.Natural : acacia, tragacanth, agar. Semi-synthetic : methyl cellulose, sod.CMC, HEC.Semi-synthetic : methyl cellulose, sod.CMC, HEC. Synthetic : carbopols.Synthetic : carbopols.


Preservatives Preservatives Stop the multiplication of microbes.Stop the multiplication of microbes. Mainly included for fungistatic action.Mainly included for fungistatic action. For oral solution: For oral solution:

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Benzoic acid (0.1-0.2%)Sodium benzoate(0.1-0.2%)Alcohol (15-20%)Glycerin (45%)Methyl paraben and propyl paraben (10:1)


Colouring agentsColouring agents To give aesthetic appeal and impart pleasing appearance.To give aesthetic appeal and impart pleasing appearance. Mask discoloured, degraded ingredients and to maintain appearance Mask discoloured, degraded ingredients and to maintain appearance

during shelp life.during shelp life. For identification.For identification. Synthetic coloursSynthetic colours

Natural Colours:Natural Colours:

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Colours for FD&C

Colours for D&C

FD&C Red no.3(Erythrosine)FD&C Yellow no.5(Tartrazine)

D&C Blue no.5(indigo)D&C Red no.22(Eosine)D&C Yellow no 7 (fluorescein)Vegetable colours: Chlorophyll, carotene.

Animal colour: Cochineal.Mineral Colours: Titanium dioxide, ferric oxides.


Flavouring agentsFlavouring agents To mask unpleasant smell.To mask unpleasant smell. Vitamins with cherry, Strawbery or raspberry flavour.Vitamins with cherry, Strawbery or raspberry flavour. Paediatric drops fruity flavour.Paediatric drops fruity flavour. Volatile oils including cinnamon, clove, lemon, orange and Volatile oils including cinnamon, clove, lemon, orange and

peppermint flavour which activate olfactory cells.peppermint flavour which activate olfactory cells. Natural Sources: Pine-apple, Cardamom, ginger.Natural Sources: Pine-apple, Cardamom, ginger. Volatile oils- Clove, lemon, orange, rose.Volatile oils- Clove, lemon, orange, rose. Synthetic Chemicals: Alcohol, aldehydes, fatty acids, esters.Synthetic Chemicals: Alcohol, aldehydes, fatty acids, esters.


Sweetening agentsSweetening agents Are natural or synthetic agents.Are natural or synthetic agents. SugarsSugars::

Polyhydric alcohols:Polyhydric alcohols:

Artificial :Artificial :

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Sucrose, fructose, glucose, syrup.

Sorbitol, Mannitol, glycerin.

Saccharin, Aspartame


Buffers Buffers Resists any change in pH when acid or base is added.Resists any change in pH when acid or base is added. To encounter stability problem.To encounter stability problem. pH -7.4 to 8.4.pH -7.4 to 8.4. Eg. Monobasic sod. Acetate, sod. Citrate, pot.phosphate, Eg. Monobasic sod. Acetate, sod. Citrate, pot.phosphate, pot. Metaphosphates.pot. Metaphosphates.


ReferencesReferences Pharmaceutics “The Science of Dosage Form Design” By Pharmaceutics “The Science of Dosage Form Design” By

M.E.Aulton, 1M.E.Aulton, 1stst Edition (1996) P.No.254-290. Edition (1996) P.No.254-290. The Theory And Practice of Industrial Pharmacy By Leon The Theory And Practice of Industrial Pharmacy By Leon

Lachman and Herbert Lieberaman., Published By Varghes Lachman and Herbert Lieberaman., Published By Varghes Publishing House, 3Publishing House, 3rdrd Edition, P.No429,457. Edition, P.No429,457.

Modern Dispensing Pharmacy By Atmaram Pawar and R.S. Modern Dispensing Pharmacy By Atmaram Pawar and R.S. Gaud, Career Publication,3Gaud, Career Publication,3rdrd Edition(2009) P.No. 134-139. Edition(2009) P.No. 134-139.

Introduction To Pharmaceutics II By A.K. Gupta And S.S. Introduction To Pharmaceutics II By A.K. Gupta And S.S. Bajaj, CBS Publishers, 4Bajaj, CBS Publishers, 4thth Edition, P.No.138-148. Edition, P.No.138-148.

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