Determinats of pharmacologic effects on Absorbtion
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Transcript of Determinats of pharmacologic effects on Absorbtion
Is the passage of drug from its site of
administration to its site of action through cell
membranes.
Drug orally given
GIT
Disintegration (to form granules ) into small molecules
Dissolution into the aqueous media
Absorption
Since oral route of drug administration is most
common for systemically acting drug and through
this route drugs mostly absorbed from GIT so here
we will discuss on oral administration of drug.
1. Passive diffusion
2. Carrier- mediated transport:
a) .Active diffusion
b). Facilitated diffusion
3. Pore Transport
4. Ionic or Electrochemical diffusion
5. Ion-pair transport
6. Endocytosis
The passage of drug
molecules occurring from
the side of high drug
concentration to low drug
concentration
x
CCDAk
dt
dQ lh )(
Q: is the net quantity of drug transferred across
the membrane, t: is the time
Ch: is the conc on one side (GIT) and Cl:
that on the other side (plasma)
x: is the thickness of the membrane
A: is surface area of membrane and D: is
the diffusion coefficient related to permeability
k: is the partition coefficient of the drug
Active Transport
The drug is transported against a concentration gradient .This
system is an ENERGY consuming system.
Example: Glucose and Amino acids transport.
A drug carrier is Required but no ENERGY is
necessary. e.g. vitamin B12 transport. Drug moves
along conc gradient (from high to low), downhill
but faster .
Pore Transport: In this process low mol. Wt. (less than 100) molecules passes the membrane by osmotic pressure.
Ion Pair Transports: Here the cationic drugs or anionic drugs penetrates the membranes by forming reversible neutral complexes. Such phenomena is called ion pair transport.
Endocytosis: It is a minor transport mechanism which involves engulfing extracellular materials with in a segment of cell membrane to form a vesicles which then pinched off intra cellularly.
Factors Related to Drugs :
1.Lipid water solubility:
Lipid soluble drug… absorption Water soluble drug… absorption
2. Molecular size:
Smaller mol. Size….rapid absorption large mol. Size… absorption
3. Particle size:
Large particle size… slower absorption small particle size… absorption
4. Degree of Ionization:
Acidic drug unionized….. Better absorption from acidic compartment
5. Physical Forms :
Solutions>Emulsions>Suspensions>Capsules> Tablets> Coated Tablets>Enteric
Coated Tablet>Sustain Release Tablet
6. Chemical Nature: Salt form of drug > organic compound
inorganic form > organic compound
7. Dosage Forms :
Rapid disintegration ……rapid absorption
Rapid dissolution…….. absorption
Factors Related to Body
1. Area of Absorptive Surface : stomach < intestine
2. Blood supply :
in which part blood supply is greater there absorption rate is high.
3. pH :
Acidic pH favors acidic drug absorption while basic pH is better for basic drugs.
4. Presence of other Substances :
Iron given with milk ……… absorption
Vitamin C…….. Absorption of iron
5. Motility of drug :
Drugs are better absorbed in normal GIT movement
6. Functional Integrity of Absorptive Surface :
Flattening and edema of mucosa……. Absorption
7. Diseases :
Diarrhea…. Absorption
Malabsorptive syndrome ……. absorption
Convenient - can be self- administered, pain free, easy to
take
Absorption - takes place along the whole length of the GI
tract
Inexpensive - compared to most other parenteral routes
vomiting/stomach distress
variability in dose
effect too slow for emergencies
unpleasant taste of some drugs
unable to use in unconscious patient
first pass metabolism