Lesson 4

Finished formulation of a drug
preparation designed to contain
a specific amount of a medication for ease and
accuracy of dosage administration

- HNO3, HCl, CH3COOH

▫ Particle size, size range and structure
▫ Photomicrographs

▫ The amount of heat absorbed when 1 g of a
liquid vaporizes

identity and PURITY

mixtures

Minimum melting point -

– factor for many physical
and chemical properties

– property of occurring in
several different forms.

▫ the time it takes for the drug to dissolve in
the fluids at the absorption site

Passive diffusion for lipid soluble drugs

- measures the lipophilic character of a molecule

– consider the lipophilic nature of biological membranes or
medium

– hygroscopic, deliquescent, efflorescent = cautious
handling and packaging

– for weak acids and bases = salts to enhance solubility

– for solubility, stability, resistance to degradation, design to prodrug
▫ Alcohol and acid

Capability of a particular
formulation in a specific container
or closure system to remain with
in its physical, chemical,
microbiological, therapeutic and
toxicological specifications

Refers to the duration of time during which a
drug preparation will remain physically,
chemically, therapeutically, toxicology and
microbiology stable (possessing NLT 90% of the labeled potency)

• Limits the time during which the product may
be dispensed by the pharmacist or used by the
patient

The description of drug concentration with respect to time

– loss of drug is concentration
independent, constant with time.

– loss of the drug is proportional to
the concentration remaining with respect to time.

The oxidative process is diverted, and the
stability of the drug is preserved by agents
called ———, which react with one or
more compounds in the drug to prevent
progress of the chain reaction.

CO2, DCDFM, DCTFE, carbon dioxide

Conducted under the usual / normal conditions
of the environment, transport and storage
expected during product distribution

It makes use of different “climatic zones”
also called _____ of exposure

Zone 1 –

Zone 2 –

Zone 3 –

Zone 4 A–

IVB

This involves the use of exaggerated conditions
of temperature, light, moisture, pH, humidity,
etc., to test the stability of drug formulations

The purpose is to determine kinetic
parameters, if possible and/or to predict
the tentative expiration dating period.

This is anything that goes into the formulation in
the preparation of the final dosage form

inactive substance used as a carrier for the active
ingredients of a medication. In addition, excipients
can be used to aid the process by which a product is manufactured

- Provide acidic medium for product stability

- Provide alkaline medium for product stability
- Ammonia solution, sodium borate, sodium
carbonate, trolamine

- Hold the molecules into its surface for moisture sensitive products
- Cellulose, activated charcoal

- Develops the pressure in the container and expels the product -

- Inhibits the process of oxidation for
possible cause of product deterioration

Butylated hydroxytoluene (BHT), sodium
bisulfite, ascorbic acid

- Prevents growth of fungi

- Paraben, benzoic acid, sodium benzoate

- Prevents growth of microorganism

- Benzalkonium chloride, benzyl alcohol, chlorobutanol, thimerosal, phenol

- Resist changes in pH

- Citrates, Acetates, Phosphates

- Used as stabilizers for heavy metals capable of
promoting instability

- Edetate disodium

- Impart color for improved aesthetic appeal - Dyes and Lakes

- Red ferric oxide, caramel, FD&C and D&C

- Used as filtering aid for the adsorbent properties

- Bentonite

Promote and maintains dispersion of finely divided particles of a liquid

- Acacia, spans and tweens, TEA, SLS, Cetyl pyridinium chloride

- Imparts pleasant flavor

- Prevents drying out of the preparation

- Glycerin, sorbitol, propylene glycol

- An intervening agent used to reduce the particle size

- Mineral oil, glycerin

- Semisolid vehicle for drug substances

- An agent used to dissolve another substance

- Water, alcohol, glycerin, mineral oil, Peanut oil, Sesame oil, Cottonseed oil, Castor oil

Agents that increase the thickness or hardness of the preparation

- Cetyl alcohol, paraffin, white wax, yellow wax

- A vehicle for drug substances formulated into suppositories

- Cocoa butter, witepsol, wecobee, PEG mixtures

- Agents which reduces interfacial tension

- Benzalkonium chloride, polysorbate 80, SLS

- Increases viscosity and reduces rate of sedimentation

- CMC, MC, bentonite, acacia

- Imparts sweetness

- Mannitol, saccharin, sorbitol, sucrose

– those that impart satisfactory characteristics to the formulation
(diluent, binders, disintegrants)

– those that impart satisfactory compression characteristics
(glidants, lubricants, and antiadherents)

– those that give additional desirable physical
characteristics to the finished tablets (colors,
flavors, sweetening agents, adsorbents)

Used more often on liquid dosage form than solid
dosage form

Observe congruity
• Correlated structures
• Taste of the drug itself
• Age of patient
• Types of the Flavors