Professional Documents
Culture Documents
&
PHARMACOKINETICS
• Bio – life
• Pharmaceutics
– general area of study concerned with
the formulation, manufacture, stability
and effectiveness of pharmaceutical
dosage forms.
Biopharmaceutics
• study of the factors
influencing the
bioavailability of a drug
in man and animals and
the use of this
information to optimize
pharmacological or
therapeutic activity of
drug products in clinical
application.
Biopharmaceutics
Generic equivalency
Drug availability
Therapeutic efficacy
Drug substitution
BIOPHARMACEUTICS
&
PHARMACOKINETICS
Effects of Biopharmaceutics
Drug product selection
*drug product should be
cost-effective
By selective control
of the physical
parameters of a
drug, biologic
response may be
optimized.
b. dosage form
- delivery system the drug could be
available or administered.
b. dosage form
Biopharmaceutic
studies must be
performed to ensure
that the dosage form
does not irritate,
cause an allergic
response or allow
systemic drug
absorption.
The dosage of a drug intended for
systemic absorption is given on the basis
of absolute amount, such as mg or g.
c. route of administration
The design of a
vaginal tablet
formulation for the
treatment of a
fungus infection
must consider
ingredients
compatible with
vaginal anatomy and
physiology.
Example
Bioavailability
Drug in solution
buccal tablets
sublingual tablets
USP Specifications
Excipients
– added to the active ingredient to
form a dosage form that is convenient for
control purposes.
- it should be inert, inactive, neither
enhances nor diminishes the therapeutic
effect of the drug
Roles/Effects of Excipients
3. Lubricant
– helps to have an easier transfer from one
stage of manufacture to another
- assist the smooth tableting process.
Ex. Mag. Stearate, stearic acid, talc,
hydrogenated vegetable oil
excessive magnesium stearate (a hydrophobic
lubricant) in the formulation may retard drug
dissolution and cause slower drug absorption.
5. Tablet Coating
protection
uneven coating can cause uneven release of
active ingredient
Example:
a. enteric coatings – employed to permit safe
passage of tablet thru the acid environment of
the stomach where certain drugs may be
destroyed, to the more suitable juices of the
intestines where tablet dissolution safely takes
place. ( shellac, cellulose acetate phthalate)
b. film-coatings
– employed to protect the drug substance
from the destructive influences of moisture, light
and air throughout their period of storage or to
conceal a bad or bitter taste from the taste buds
of the patient. (hydroxypropylmethylcellulose)
Hydrates
Drug + H2O = crystal
In general, the crystalline form of drugs are more
rigid and thermodynamically more stable than
the amorphous form. The crystal form with the
lowest free energy is the most stable polymorph.
A change in crystal form may cause problems in
manufacturing the product. For example, a
change in crystal structure of the drug may
cause cracking in a tablet or even inability for a
granulation to be compressed to form a tablet.
Example
Determined by:
Inherent potency of the drug
Dosing strengths
Dependent on:
1. Clearance of the drug (elimination)
2. Target plasma drug concentration
(MEC)
e.g. Drug with a short half-life or rapid
clearance how frequent is the
dosing?
Sustained release (SR) tablets