Pharmaceutical additives for liquid dosage form

Pharmaceutical additives for liquid dosage form

1. 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.

2. 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.
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3. 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.

4. 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.
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5. Pharmaceutical additives used Pharmaceutical additives used
in liquid dosage formin liquid dosage form
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Vehicles
Surfactants
Hydrocolloids
Antioxidants
Complexing agents
Preservatives Colouring
agents
Flavouring
agents
Sweetening
agentsBuffers
Tonicity
adjusters
Liquid Dosage Forms
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6. 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.
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7. 
WaterWater

CosolvencyCosolvency

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

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

8. 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 10
Tweens, spans ,SLS
o/w emulsifiers- 8 to 18
w/o emulsifiers-3 to 6
Glycol, glycerol esters, cetrimide.
HLB- 1.5 to 3
Castor oil, fatty acids.
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9. 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.
.
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10. 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.
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11. 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)
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12. 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 Mask discoloured, degraded ingredients and to maintain
appearance during shelp life.appearance 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.
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13. 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.
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14. 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
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15. 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.
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16. RefeRencesRefeRences

Pharmaceutics “The Science of Dosage Form Design” By Pharmaceutics “The Science of Dosage Form Design” By
M.E.Aulton, 1M.E.Aulton, 1
stst
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, 3
rdrd
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,3
rdrd
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, 4
thth
Edition, P.No.138-148. Edition, P.No.138-148.

www.google.com.www.google.com.
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