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RMACUTICAL FACTORS OF DRUG ABSORBTION.
Presented by y.d.n.satish
Reg no 121825101004
Mpharm 2 semester pharmacutics
.INTRODUCTION OF ABSORBTION
.TRANSPORT PROCESS
.FACTORS AFFECTING DRUG ABSORBTION
1.Physiological factors
2. physiochemical factors
3.pharmaceutical factors
ABSORBTION
.Defnition;the process of movement of unchanged drug from the
site of adminstration to systemic circulation.
CELL MEMBRANE
1.lipid layer
- phospholipid
- cholestrol
- glycolipids
2.proteins
. Integral membrane protein
.lipid ancored proteins
.peripheral proteins
TRANSPORT PROCESS
.passive diffusion
.pore transport
.facilitated diffusion
.active transport
.pinocytosis
1.PHYSIOLOGICAL FACTORS.
.age
.gastric emptying
.intestinal transist
.gastro intestinal pH
.diseased state
.gastro intestinal contents ..pre systamic metabolism
AGE; in childrens and infants gastric ph is high and intensional surface and
flow is low.
When in adults altered in gastric emptying,decrease intestinal surface
area;decrease gastric blood flow.in drug absorbtion
Gastric emptying.
.gastric emptying is the passage of drug from stomach to smaall intestine.
.gastric emptying is dealyed when co-adminstred with food.
.factors that influence g.e are valume of meal,composition of meal,temperature of
meal,body posture,exercise ,diseases state etc
Intestinal transist time.
Since intestine is the major site of absorbtion of most of drugs long intestinal
transit time is desirable for the complete absorbtion of drugs.
.dealyed intestinal transit is desirable for
-drugs that dissolve only in intestine (entric coated)
-drugs absorbed from specefic sites in the intestine.
Gastro intestinal pH;
A difference in ph is observed between gastric and colon fluids.the gi ph increases
gradually from the stomach to the colon and rectum.
The ph of gi fluids influence the drug absorbtion in sevral ways.
-dissolution
-stabity
DISEASE STATE
.gi disease;infection such as achlorhydria,malaabsorbtion and sugeries such as
gastrectonomy effect the absorbtion of drugs to grater extent.
.disorders such as hepatic cirrhosis influence the bioavalibility mainly of drugs that
undergoes considerable first pass hepatic metabolism e.g propranolol
PRESYSTAMIC METABOLISM;
The main reason for disease in bioavalibility of the drug are decresed absorbtion
or first pass metabolism
.various enzyme that effect presystamic metabolism of drugs’
-Gutwall enzyme’
-hepatic enzyme
-bacterial enzyme
2.physiochemical factors;
Drug solubity and dissolution rate
Particle size
Polymorphism and amorphism
Psudopolymorphism
Salt form of drug
Pka of drug
Particle size
.the absorbtion of the drug can be increased by increasing the particle surface
area by micronization...
Smaller
the drug
particle
Greater the
surface area
Polymorphism and amorphism;
.when substance exists in defferent crystaliine
forms it is polymorphism..
AMORPHISIM.
.they have greater aques solubility than the crytaline forms
because the energy required to transfer a molecule from
crystaline lattice is greater than required for the non crystalline
soild.
E.g novabacin
.the order of dissolution hence absorbtion for different soild
dosage forms is
amorphous>meta-stable>stable..
PH PARTION HYPOTHESIS;
UNIONIZED DRUG
HIGH ABSORBTION
IONISED DRUG
LOW ABSORBTION
SALTS FORMATION OF A DRUG.
.salt of weak acid and weak bases have much higher aqueos
solubility than free acid or base.
.therefore if a drug can be given as a salt ,the solubity can be
increased the dissolution can be improved.
3.pharmacutical factors.
Manufacturing variables
-method of granulation
-compression force
Nature and type of dosage form
Pharmacutical ingriedent and exipients
Storage conditions...
Manufacturing variables;
1.method of granulation; the method of dry granulation can
be used to produce tablets that dissolve at faster rate .
2.compression force;influence the hardness
density,porosity,disintegration dissolution of tablet.
Nature and type of dosage forms;
.bioavalibility of a drug from various dosage forms in the
following order
.solution >emulsion >suspension >capsules>tablets>coated
tablets>entric coated tablets>sustained release tablets
Pharmacutical excipients.
.product storage conditions.
Refrences.
TESTBOOK OF BIOPHARMACEUTICS AND
PHARMACOKINETICS ,BY D.M.BRAHMANKAR PG NO5-97

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Absorbtion presentation

  • 1. RMACUTICAL FACTORS OF DRUG ABSORBTION. Presented by y.d.n.satish Reg no 121825101004 Mpharm 2 semester pharmacutics
  • 2. .INTRODUCTION OF ABSORBTION .TRANSPORT PROCESS .FACTORS AFFECTING DRUG ABSORBTION 1.Physiological factors 2. physiochemical factors 3.pharmaceutical factors
  • 3. ABSORBTION .Defnition;the process of movement of unchanged drug from the site of adminstration to systemic circulation.
  • 4. CELL MEMBRANE 1.lipid layer - phospholipid - cholestrol - glycolipids
  • 5. 2.proteins . Integral membrane protein .lipid ancored proteins .peripheral proteins
  • 6. TRANSPORT PROCESS .passive diffusion .pore transport .facilitated diffusion .active transport .pinocytosis
  • 7. 1.PHYSIOLOGICAL FACTORS. .age .gastric emptying .intestinal transist .gastro intestinal pH .diseased state .gastro intestinal contents ..pre systamic metabolism
  • 8. AGE; in childrens and infants gastric ph is high and intensional surface and flow is low. When in adults altered in gastric emptying,decrease intestinal surface area;decrease gastric blood flow.in drug absorbtion
  • 9. Gastric emptying. .gastric emptying is the passage of drug from stomach to smaall intestine. .gastric emptying is dealyed when co-adminstred with food. .factors that influence g.e are valume of meal,composition of meal,temperature of meal,body posture,exercise ,diseases state etc
  • 10. Intestinal transist time. Since intestine is the major site of absorbtion of most of drugs long intestinal transit time is desirable for the complete absorbtion of drugs. .dealyed intestinal transit is desirable for -drugs that dissolve only in intestine (entric coated) -drugs absorbed from specefic sites in the intestine.
  • 11. Gastro intestinal pH; A difference in ph is observed between gastric and colon fluids.the gi ph increases gradually from the stomach to the colon and rectum. The ph of gi fluids influence the drug absorbtion in sevral ways. -dissolution -stabity
  • 12. DISEASE STATE .gi disease;infection such as achlorhydria,malaabsorbtion and sugeries such as gastrectonomy effect the absorbtion of drugs to grater extent. .disorders such as hepatic cirrhosis influence the bioavalibility mainly of drugs that undergoes considerable first pass hepatic metabolism e.g propranolol
  • 13. PRESYSTAMIC METABOLISM; The main reason for disease in bioavalibility of the drug are decresed absorbtion or first pass metabolism .various enzyme that effect presystamic metabolism of drugs’ -Gutwall enzyme’ -hepatic enzyme -bacterial enzyme
  • 14. 2.physiochemical factors; Drug solubity and dissolution rate Particle size Polymorphism and amorphism Psudopolymorphism Salt form of drug Pka of drug
  • 15. Particle size .the absorbtion of the drug can be increased by increasing the particle surface area by micronization... Smaller the drug particle Greater the surface area
  • 16. Polymorphism and amorphism; .when substance exists in defferent crystaliine forms it is polymorphism..
  • 17. AMORPHISIM. .they have greater aques solubility than the crytaline forms because the energy required to transfer a molecule from crystaline lattice is greater than required for the non crystalline soild. E.g novabacin .the order of dissolution hence absorbtion for different soild dosage forms is amorphous>meta-stable>stable..
  • 18. PH PARTION HYPOTHESIS; UNIONIZED DRUG HIGH ABSORBTION IONISED DRUG LOW ABSORBTION
  • 19. SALTS FORMATION OF A DRUG. .salt of weak acid and weak bases have much higher aqueos solubility than free acid or base. .therefore if a drug can be given as a salt ,the solubity can be increased the dissolution can be improved.
  • 20. 3.pharmacutical factors. Manufacturing variables -method of granulation -compression force Nature and type of dosage form Pharmacutical ingriedent and exipients Storage conditions...
  • 21. Manufacturing variables; 1.method of granulation; the method of dry granulation can be used to produce tablets that dissolve at faster rate . 2.compression force;influence the hardness density,porosity,disintegration dissolution of tablet.
  • 22. Nature and type of dosage forms; .bioavalibility of a drug from various dosage forms in the following order .solution >emulsion >suspension >capsules>tablets>coated tablets>entric coated tablets>sustained release tablets
  • 23.
  • 25. Refrences. TESTBOOK OF BIOPHARMACEUTICS AND PHARMACOKINETICS ,BY D.M.BRAHMANKAR PG NO5-97