1.

Define the following terms:

a.) Pharmaceutics –
It is the study on the formulation, manufacture, stability, and effectiveness of
pharmaceutical dosage forms.
b.) Pharmaceutics ingredients or excipients –
It is the selective use of these non-medicinal agents.
c.) Master formula –
It is the formulation that best meets the goals of the product.
d.) Stability –
Extent a product retains within specified limits and through its period of storage
and use
e.) Dissolution rate –
It is the time for the drug to dissolve in the fluids at the absorption site (rate-
limiting step in absorption).
f.) Expiration date –
It limits the time during which the product may be dispensed by the pharmacist
or used by the patient.
g.) Partition coefficient –
It is the selection of appropriate extraction solvents, drug stability, use of
salting-out additives and environmental concerns.

2. Give the principal reason for the need of dosage forms and
some dosage forms for specific reasons.

 To protect the drug substance from the destructive influences of atmospheric

oxygen or humidity. (Coated tablets)
 To protect the drug substance from the destructive influence of gastric acid after
oral administration. (Enteric-coated)
 To conceal the bitter, salty or offensive taste or odor of a drug substance.
(Capsules, Flavored syrups)
 To conceal the bitter, salty or offensive taste or odor of a drug substance.
(Capsules, Flavored syrups)
 To provide clear liquid dosage forms of substances. (Syrups, Solutions)
 To provide rate-controlled drug action. (Controlled-release tablets)
 To provide optimal drug action from topical administration sites.
(Ointments,Creams, Transdermal patches)
 To provide for insertion of a drug into one of the body’s orifices
(Suppositories)
 To provide placement of drugs directly in the bloodstream or body tissues
(Injections)
 To provide for optimal drug action through inhalation therapy (Inhalants,
Inhalation aerosols)

3. Before medicinal substance is formulated, what factors related

to illness must be considered?

Following are the factors that must be considered before medicinal substance is
formulated:
 Therapeutic matters (nature of the illness)
 Manner it is treated (locally or through systemic action)
 Age and anticipated condition of the patient.

4. Give 3 ways by which a liquid drug could be given in solid form

to be given orally.

Liquid substance:

 Sealed in soft gelatine capsule

 Developed into a solid ester or salt form suitable for tablets or drug capsules
 Mixed with a solid or melted semisolid material
 melted mixture is poured into hard gelatine capsules to harden & capsules
sealed

5. Give the importance of the ff. to the drug substance/product:

a.) Microscopic examination of the raw drugs

indication of: particle size and size range of the raw material along with the
crystal structure.
information in formulation processing attributable to changes in particle or
crystal characteristics of the drug.

b.) Melting point depression

It determines the: purity of the substance and compatibility of various subs
before inclusion in the dosage form
- Pure substance : sharp melting point
- Impure substance : depressed melting point

c.) Phase rule

It is where phase diagrams are constructed to determine the existence & extent
of the presence of solid and liquid phases in binary, ternary & other mixtures.
d.) Rate reaction
It is the description of the drug concentration with respect to time.

e.) Extent of dissociation/ionization

It is the extent of ionization of drug - strong effect on formulation &
pharmacokinetic parameters of the drug. It is determined by potentiometric
titration.

f.) Fick’s Law (Law of Diffusion)

It describes the relationship of diffusion & dissolution of the active drug in the
dosage form & when administered in the body.
- 1st law
Relates to a steady state flow
- 2nd law
Relates to a change in conc. of drug with time, at any distance, or a non-
steady state of flow

6. Give the methods of determining the following:

a.) Dissolution rate –

The time it takes for the drug to dissolve in the fluids at the absorption site, is
the rate-limiting step in absorption.

Dissolution rates of chemical compounds are determined by 2 methods:

1. Constant-surface method – which provides the intrinsic dissolution rate
of the agent
2. Particulate dissolution – in which a suspension of the agent is added to
a fixed amount of solvent without exact control of surface area.

b.) Drug’s solubility –

It is usually determine by the equilibrium solubility method, by which an
excess of the drug is placed in a solvent and shaken at a constant temperature
over long period until equilibrium is obtained.

c.) Membrane permeability –

In order to produce a biologic response, the drug molecule must first cross a
biologic membrane. The biologic membrane acts as a lipid barrier to most
drugs and permits the absorption of lipid-soluble substances by passive
diffusion, while lipid insoluble substances can diffuse across the barrier only
with considerable difficulty if at all.
d.) Molecule’s lipophilic character
It is measured by the oil-water coefficient.

e.) pKa
It is determined by potentiometric titration. For the pharmacists, it is
important to predict the precipitation in admixtures and to calculate the
solubility of drugs at certain pH values.

f.) Shelf-life determination

It has to be estimated based on assay results of the drug characteristic from a
stability study usually conducted during the process of drug development.

7. How will these factors affect solubility of the drug’s substance? (NOT
SURE OF THE ANSWER)

If a drug is formulated to liquid product, adjustment of pH of solvent where drug is

dissolved to adjust solubility. Further, chemical analysis of the drug content in
solution is performed to determine degree of solubility.

8. Give ways by which dissolution rate is increased.

a.) The dissolution rate of drugs may be increased by decreasing the drug’s particle
size.
b.) It may also be increased by increasing its solubility in diffusion layer.
c.) The most effective means of obtaining higher dissolution rates is to use a highly
water soluble salt of the parent substance.

9. Enumerate and explain the 5 types of stability.

a.) Physical Stability means that the original physical properties like
appearance, palatability, viscosity, uniformity of color maintained until expiry
date.
b.) Chemical Stability means that the active ingredient retains its chemical
integrity and labeled potency are retained over extended period of time.
c.) Microbial Stability means that the activity or resistance to microbial growth
should still according to specified requirements. Preservatives must be added
to prevent the growth of microorganism.
d.) Therapeutic Stability means that the therapeutic effect maintained until
expiry date.
e.) Toxicological Stability means when no significant increase in toxicity has
occurred.
 10. What are the 5 processes by which a drug could be degraded?

a.) Polymerization
It is a reaction between two or more identical molecules with resultant
formation of new & generally larger molecule (Ex. formaldehyde)

b.) Decarboxylation
The decomposition of Carboxylic acid (R-COOH) and release of carbon dioxide
(CO2)

c.) Deamination
The removal of nitrogen containing group from organic amine (Ex. Insulin)

d.) Hydrolysis
The process in which drug molecule interact with water molecules to yield
breakdown products of different chemical constitution. (Ex. Aspirin)

e.) Oxidation
A destructive process occurring in pharmaceutical. Chemically, it involved the
change in the number of electrons from an atom or molecule.

11. Give ways to prevent decomposition of the drug substance by:

a.) Oxidation
Light is catalyst to oxidation reactions. Thus, preparation should be packaged in
light resistant or opaque containers.

b.) Hydrolysis
Water should be reduced or eliminated from the system. For water-liable drugs,
waterproof protective coating is applied in the tablet. In liquid formulation, water
is replaced by substitute liquids.

12. How drug instability be detected?

Drug instability can be detected if there are changes in physical appearance, color,
odor, taste or texture of the formulation.
 13. Differentiate long term stability studies with accelerated
stability studies according to:

Long term stability Accelerated stability

studies studies

Use of exaggerated
Product is subjected to
conditions of
different climatic zones
temperature,
(temperature &
humidity, light and
humidity) nationally
others
and internationally

Duration 12 months minimum 6 months study

Temperature Conducted at 25 o C 40 o C
+/- 2oC and at

Humidity a relative humidity of 75% relative

60% +/- 5% humidity

14. What are the FDA guidelines on stability for extemporaneous

compounding?

 Nonaqueous liquids & solid formulations

(Source of active ingredient)’s
Not later than 25% of the time remaining until the product’s expiration date
or 6 months, whichever is earlier

 Nonaqueous liquids & solid formulations in w/c USP or NF substance

(Source of ing)
Beyond-use not later than 14 days in storage at cold temperatures

 Other formulations beyond-use date of the intended duration of therapy or 30

days whichever is earlier

15. Tabulate some pharmaceutic ingredients, their uses and

common examples.
 Pharmaceutic
Uses
Ingredients
Used to dissolve the drug
Solvents
substance
Used to make the product
Flavors and sweeteners
more palatable
Colorants Added to enhance appeal
May be added to prevent
Preservatives
microbial growth
16. What is Delaney Clause
Delaney clauses states that no new food additives may be used if animal
studies/appropriate tests showed that it caused cancer.
17. Give examples of sweetening agents and their advantages and
disadvantages.
Sweetening Agents Advantages
helpful aid in weight loss
due to the fact that it
Stevia (Stevia rebaudiana contains no sugar, no
Bertoni) calories and has been
shown to reduce craving
for sweets and fatty foods.
metabolized and excreted
Saccharin by the kidneys virtually
unchanged
breaks down in the body
Aspartame into three basic
components: the amino
acids phenylalanine and
Common
Examples
alcohol
aspartame
dyes
Ophthalmic and
injectable
preparations
Disadvantages
it leaves some
unpleasant tastes such
as a bitter taste. In
other words, it is
undesirable for a
sweetening to contain
large amounts of
Stevioside.
may cause sulfa
allergies and has
possible carcinogenic
properties when
consumed in very large
amounts
the use of aspartame
by persons with
phenylketonuria
(PKU) is discourages,
 aspartic acid, and and diet foods and
methanol drinks must bear
appropriate label
warning

18. What is the origin of synthetic colorant?

The synthetic coloring agent comes mostly from coal tar (pix carbonis) black, viscid
liquid which is a byproduct in the destructive distillation of coal. Most
pharmaceutical colorants are synthetic origin; few are naturally occurring principles
obtained from mineral, plants and animal source

19. Classify color additives according to their approved uses.

Color Additives Approved Uses

FD & C dyes legally used in food, drugs and cosmetics

D & C dyes legally used in drugs and cosmetics

legally used only to color externally applied drugs

External D & C dyes
and cosmetics

20. Differentiate dyes from lake pigments.

Dyes are added to pharmaceutical prens in the form of diluted solutions while lakes
are commonly used in the form of fine dispersions or suspension.

21. Give some factors in selecting dyes for formulations.

 PHYSICAL AND CHEMICAL PROPERTIES

 Solubility of the dye should be the first to be studied – in the solvent or vehicle
used. Dyes may be grouped into water soluble or oil soluble.

 pH
Dyes can change color with a change of pH. The color must be chemically
stable in the environment of the other formulative ingredients for the shelf life;
dye must be photostable.

22. How is sterilization by physical methods done?

It can be done thru autoclaving, the process of high-pressure sterilization by steam

of media and equipment required for growing microorganisms and for cultures and waste
materials prior to disposal. The recommended autoclave cycle is 20 minutes at 15 lb.
pressure and 121°C, dry heat at 180°C for 1 hour.

Another physical method is through bacterial filtration.

23. Name some factors in selecting preservatives.

a) Prevents the growth of the type of microorganisms ( contaminants of the

preparations)
b) Soluble enough in water to achieve adequate concentrations in aqueous phase
with two or more phase systems
c) Proportion of preservative remaining undissociated at the pH of preparation
(can penetrate the microorganism & destroy its integrity).
d) Concentration of the preservative does not affect the safety/comfort of the
patient
e) With adequate stability and not reduced in concentration by chemical
decomposition/volatilization
f) Compatible with all other formulative ingredients and does not interfere with
them
g) Does not adversely affect the preparation’s container or closure.

24. What are the mechanisms of antibacterial action?

a) Modifications of cell membrane permeability and leakage of cell constituents

(partial lysis);
b) Lysis and cytoplasmic leakage;
c) Irreversible coagulation of cytoplasmic constituents;
d) Inhibition of cellular metabolism by interfering with enzyme systems/inhibition
of cell wall synthesis;
e) Oxidation of cellular constituents; and
f) Hydrolysis