Pharmaceutical formulation and Manufacturing of an Effervescent Tablet.

1. PHARMACEUTICAL EXCIPIENTS
AND FORMULATION OF A DOSAGE
FORM
Anwar Parvez, DIU
Pharmaceutical Technology II

2. I. POLYOXYLGLYCERIDES
 Nonproprietary Names
• Caprylocaproyl Macrogolglycerides(BP, PhEur)
• Lauroyl Macrogolglycerides(BP, PhEur)
• Lauroyl Polyoxylglycerides(USP-NF)
 Chemical Name:
• Caprylocaproyl polyoxylglycerides-Decanoic acid
• Lauroyl polyoxylglycerides-Lauric acid
 Structural Formula

3.  Functional Category:
• Used as a dissolution enhancer; nonionic surfactant; emulsifying agent;
penetration agent
 Applications in Pharmaceutical Formulation or Technology:
• used as self-emulsifying and solubilizing agents in oral and topical
pharmaceutical formulations. They are also used in cosmetic and food
products.
 Stability & Storage Conditions:
• Polyoxylglycerides are very stable and inert.
• It should be preserved in their original sealed containers
 Safety: Caprylocaproyl polyoxylglycerides:
LD50 (rat, oral): >22 ml/(kg day).
Lauroyl polyoxylglycerides:
LD50 (rat, oral): >2004 mg/(kg day).
 Handling Precautions
• To ensure stability during handling, and avoid the risk of oxidation or
hydrolysis

4. II. Polyvinyl Acetate Phthalate
 Nonproprietary Names:
• Polyvinyl Acetate Phthalate(USP-NF)
 Chemical Name: PVAP; Polyvinylacetate phthalate polymer
 Structural Formula:
 Functional Category: Coating agent.

5.  Applications in Pharmaceutical Formulation or Technology:
• Used in pharmaceutical formulations to produce enteric coatings for
products and for the core sealing of tablets prior to a sugar-coating
process.
 Stability & Storage Conditions:
• It is relatively stable to temperature and humidity, and does not age.
• Polyvinyl acetate phthalate should be stored in airtight containers.
 Incompatibilities:
• Polyvinyl acetate phthalate reacts with povidone to form an insoluble
• Benzocaine is also incompatible with polyvinyl acetate phthalate
 Safety:
• Nonirritant and nontoxic
 Handling Precautions
• Observe normal precautions appropriate to the circumstances and quantity
of material handled

6. III. Polyvinyl Alcohol
 Nonproprietary Names:
• Polyvinyl Alcohol (USP)
 Chemical Name: Ethenol, Vinyl alcohol
 Structural Formula:
 Functional Category:
• Lubricant, Coating agent
 Description:
• Polyvinyl alcohol (PVA), a colourless, water-soluble synthetic resin, white
to cream-colored granular powder.

7.  Applications in Pharmaceutical Formulation or Technology
• For oral administration used a lubricant & also used as a stabilizing agent
for emulsions (0.25–3.0% w/v)
 Stability and Storage Conditions:
• Polyvinyl alcohol is stable when stored in a tightly sealed container in a dry
and cool place.
• Aqueous solutions are stable in corrosion resistant sealed containers.
 Incompatibilities:
• Polyvinyl alcohol decomposes in strong acids, and at high concentration
with inorganic salts.
 Safety: Nonirritant and nontoxic
• LD50 (mouse, oral): 14.7 g/kg
• LD50 (rat, oral): >20 g/kg
 Handling Precautions:
• Use process enclosures, local exhaust ventilation, or other engineering
controls to keep airborne levels below recommended exposure limits

8. IV. Potassium Alginate
 Nonproprietary Names:
• USP-NF: Potassium Alginate
 Chemical Name: Potassium alginate (C6H7KO6)n
 Structural Formula:
 Functional Category: Emulsifying agent; stabilizing agent; suspending agent
 Applications in Pharmaceutical Formulation or Technology:
• Accelerate disintegration of tablet, helps retaining the color of lipstick

9.  Stability and Storage Conditions:
• In the solid state, potassium alginate is a stable material that is not prone
to microbial spoilage.
• Potassium alginate should be stored under cool, dry conditions in a well-
closed container.
 Incompatibilities:
• Strong oxidizers like oxygen, hydrogen peroxide and the halogens.
 Safety:
• Potassium alginate is widely used in food products. It is currently used as
an excipient only in experimental pharmaceutical formulations.
 Handling Precautions:
• Potassium alginate may be irritant to the skin, eyes and lungs. So gloves,
eye protection, suitable protective clothing, and respiratory equipment
should be worn.

10. V. Potassium Alum
 Nonproprietary Names:
• Alum (BP, PhEur) Potassium Alum(USP)
 Chemical Name: Aluminum potassium sulfate anhydrous
 Structural Formula:
 Functional Category:
• Cosmetic Astringent; Drug Astringent

11.  Applications in Pharmaceutical Formulation or Technology:
• Potassium alum precipitates proteins and is a powerful astringent
• Used as/in mouthwashes or gargles
 Stability and Storage Conditions:
• Stable under normal temperatures and pressures.
• Store in a cool, dry place in tightly closed containers.
 Incompatibilities:
• strong oxidizing agents, copper, aluminum, steel, and zinc.
 Safety:
• Large doses of potassium alum act as an irritant and may be corrosive;
gum necrosis and gastrointestinal hemorrhage have occurred.
 Handling Precautions:
• During a fire irritating and highly toxic gases may be generated by thermal
decomposition or combustion of potassium alum

12. VI. Potassium Benzoate
 Nonproprietary Names:
• USP-NF: Potassium Benzoate
 Chemical Name:
• Potassium benzoate, Benzoic acid potassium salt
 Structural Formula:
 Functional Category:
• Preservatives and Antioxidants, Food additives

13.  Applications in Pharmaceutical Formulation:
• Used as an antimicrobial preservative in a wide range of beverages, foods
and some pharmaceutical formulations.
• Therapeutically, potassium benzoate is used to treat hypokalemia.
 Stability and Storage Conditions:
• Potassium benzoate is stable at room temperature under normal storage
conditions.
• Should be stored in sealed containers.
 Incompatibilities: Strong oxidizing agents and strong acids.
 Safety:
• People with a history of allergies to potassium benzoate.
• Higher concentrations of it may cause irritation to mucous membranes.
 Handling Precautions:
• Exposure to heat, and when heated to decomposition, potassium benzoate
emits acrid smoke and irritating fumes.

14. VII. Potassium Bicarbonate
 Nonproprietary Names:
• Potassium Bicarbonate (BP, USP)
 Chemical Name: Potassium bicarbonate; Potassium hydrogen carbonate
 Structural Formula:
 Functional Category:
• Processing Aids and Additives, Disintegrant, Alkalizing agent

15.  Applications in Pharmaceutical Formulation or Technology:
• As an excipient, potassium bicarbonate is generally used in formulations as
a source of carbon dioxide in effervescent preparations.
• Often formulated with citric acid or tartaric acid in effervescent tablets or
granules.
 Stability and Storage Conditions:
• Potassium bicarbonate is stable in air at normal temperatures, but in
solution, it is gradually converted to potassium carbonate.
• Potassium bicarbonate should be stored in a well-closed container in a cool,
dry location.
 Incompatibilities: Acids and acidic salts
 Safety:
• relatively nontoxic and nonirritant material when used as an excipient.
 Handling Precautions:
• Observe normal precautions appropriate to the circumstances and quantity
of material handled.

16. VIII. Potassium Chloride
 Nonproprietary Names:
• Potassium Chloride(BP, USP)
 Chemical Name: Potassium chloride; Enseal.
 Structural Formula:
• Functional Category:
• Food Additives; Therapeutic agent; Tonicity agent

17.  Applications in Pharmaceutical Formulation:
• Used in a variety of parenteral and non-parenteral pharmaceutical
formulations.
• It is also used therapeutically in the treatment of hypokalemia.
 Stability and Storage Conditions:
• Usually stable and should be stored in a well-closed container in a cool, dry
place.
 tablets become increasingly hard on storage at low humidity.
 Incompatibilities:
• hydrochloric acid, sodium chloride, and magnesium chloride
 Safety:
 Parenterally, rapid injection of strong potassium chloride solutions can
cause cardiac arrest.
 Handling Precautions:
• Observe normal precautions appropriate to the circumstances and quantity
of material handled.

18. IX. Potassium Citrate
 Nonproprietary Names:
• Potassium Citrate(BP, USP, PhEur )
 Chemical Name: 2-Hydroxy-1,2,3-propane tricarboxylic acid tripotassium
salt anhydrous.
 Structural Formula:
 Functional Category:
• Alkalizing agent; buffering agent, sequestering agent.

19.  Applications in Pharmaceutical Formulation :
• Used in beverages, foods, and oral pharmaceutical formulations as a
buffering and alkalizing agent.
 Stability and Storage Conditions:
• Potassium citrate is a stable in normal conditions .
• Should be stored in an airtight container in a cool, dry place.
 Incompatibilities: Strong oxidizing agents, acidic substances.
 Safety:
• Regarded as a nontoxic and nonirritant material
 10 g may be administered daily, in divided doses is safe
 Handling Precautions:
• Observe normal precautions appropriate to the circumstances and quantity
of material handled.

20. Formulation of Vitamin C Effervescent tablet (500mg)
Name of the
Ingredient
Function Normal Conc.
(%)
Conc.
Used(%)
Calculated
amount(mg)
Vitamin C API Dose
dependent
33.78 500
Sucrose Diluent 5-90 22.62 335
PVP Binder 3-15 3 44.4
KHCO3 Effervescent Base 20-30 22 312
Citric Acid
Monohydrate
Effervescent Acid 10-20 18 266.4
Polyvinyl Alcohol Lubricant 1-2 1.5 22.2
Saffron Coloring Agent q.s.
Orange Oil Flavoring Agent q.s.
Total Wt. 1480