Biopharmaceutics: 1st Shifting
Current drug interpretations are empirical BIOPHARMACEUTICS
PHARMACOGENOMICS
- Mapping out drug effects to individuals
PHYSICOCHEMICAL FACTORS
- Alter drug bioavailability
- Particle size in solids
- Particle size in dispersed
- Tablet disintegration
- Tablet and capsule adjuncts
- Coatings
- Crystalline drug properties
Higher particle size = lower surface area covered
PHARMACEUTICS: reducing particle size to increase
surface area
DISSOLUTION MEDIUM: penetrates para mas maging
bioavalaible
Examples of drug products that were reduced in particle size
and lead to higher dissolution
1. Nitrofurantoin (macrocrystals)
- Modified in order to stay in the lumen
2. Spirinolactone
- Particles reduced to micro size (10^-6)
MICRONIZATION modern technique to
reduce particle size
METHODS OF REDUCING PARTICLE SIZE:
- Trituration
- Sieving (sieve # = higher means finer
squares)
- Micronization
- Sonication
DISSOLUTION
Depends on intrinsic solubility
Particle size is only a factor
EMULSIONS
Oil in water
- Oil globules
- Oil + water + emulsifier
Water in oil
- Water droplets
*EFFECTS OF DOSAGE FORMS ON THERAPEUTIC
SYSTEMS*
GABs NOTES
Area of study concerned with the formulation,
manufacture, stability and effectiveness of
pharmaceutical dosage forms.
Study of the factors (dosage form, formulation)
influencing the bioavailability (in vivo, in vitro
dissolution testing) of a drug in man and animals
and the use of this information to optimize
pharmaceutical or therapeutic activity of drug
products (vehicle) in clinical applications.
Interrelationship of the physicochemical
properties (solubility, etc) of the drug, the dosage
form in which the drug is given, and the route of
administration on the rate and extent of drug
absorption (bioavailability in the systemic
circulation)
Study of the relationship of the physicochemical
properties and in vitro behavior of the drug and
drug products on the delivery of the drug to the
body under normal conditions.
PHARMACOKINETICS drug movement in the body
A process of how the body deals with the drug
what your body does to your drug
PHARMACODYNAMICS - How drug changes your body
A process of how your drug deals with your body.
what your drug does to your body
LADMER
L biopharmaceutics
AD pharmacokinetics
ME drug elimination (liver and kidney)
PHARMACOKINETICS
Deals with the changes of drug concentration in a
drug product inside the human or animal body
following administration
500 mg IV bolus: 500 mg
500 mg Tab PO: <500 mg metabolized in the liver before
reaching the systemic circulation : first-pass effect
After 2 hours, lesser some are excreted
PHARMACODYNAMICS drug effect
Relationship between the drug concentration at
the site of action (Receptor- drug receptor
interaction may be good or bad) and
 pharmacologic response including the biochemical
and physiologic effects that influence their
interaction
Initiation of sequence of molecular events resulting
in pharmacologic or toxic response
Idiosyncracy- different effects to different people take
effect, no effect, adverse effect. (DRUG TO GENES)
DRUG PRODUCT
Finished dosage form that contains an active
ingredient, generally, but not necessarily, in
association with inactive ingredients (vehicle)
Formulation or matrix in which the drug is
contained
Term may also include a dosage form that does
not contain an active ingredient intended to be
used
o Placebo answers the question: if a
drug took effect by chance
Hepatic vein to inferior vena cava to heart
then to the systemic circulation
Bioavailable
DISTRIBUTION detour (on deposit sites or
storage) or to the target organ
o Deposit sites storage adipose,
muscles nerves, bones
peripheral tissues not the target
organ
- Difference in distribution different
affinity for tissue protein
- Can go back to systemic circulation from
the peripheral tissue when the drug in
the systemic circulation is eliminated.

DRUG DISPOSITION

Description of drug distribution and elimination

Tablet (oral)

No activity in esophagus
Disintegration in the stomach (liberation
/release)
Small intestine only accept the drug if its already
a solution
o Delay when not disintegrated)
o Absorption in the small intestine
Pass through a semi
permeable membrane
(involves diffusion) Ficks
Law of Diffusion
Should be lipid soluble,
nonionized, nonpolar, small
particle size fewer
absorption
Large surface area (villi), good
perfusion (good blood supply)
(should pass through veins)
Drain to portal vein
First-pass effect in the liver drug
metabolized before reaching the systemic
circulation
Deactivation efficacy may be reduced
(disadvantage)
Also known as first-pass metabolism or
presystemic elimination
Inactive (prodrug) active (ex. Aspirin,
prednisone methyl prednisolone)
Active parent (prolongs action of the drug in
the body) active metabolite (ex.
Diazepam oxazepam)