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Patient Related
Factors
Affecting drug absorption
Presented by,Presented by,
Hinglajia HetalHinglajia Hetal
RatilalRatilal
Patient Related Factors
Age
Age
Infants
• Gastric pH high
• Intestinal surface low
• Blood flow to GIT low
Elderly persons
 Altered gastric emptying
 Decreased intestinal surface area
& GI blood flow
 Higher incidents of achlorhydria
 Bacterial overgrowth
Altered Absorption
pattern
GastricGastric
emptyingemptying
Gastric emptying
Apart from dissolution of a drug & its permeation through the
bio membrane, the passage from stomach to the small
intestine, called as gastric emptying.
Rate limiting step, because the major site of drug absorption is
intestine.
It increases bioavailability of a drug.
It is first order process.
Rapid gastric emptyingRapid gastric emptying
advisable where,advisable where,
Delay gastric emptying
advisable where,
Gastric acid
quantifying parameters
• Gastric emptying rate is the speed at which the
stomach contents empty into the intestine.
• Gastric emptying time is the time required for the
gastric content to empty into the small intestine.
• Longer the gastric emptying time , lesser the gastric emptying
rate.
• Gastric emptying t1/2 is the time taken for half the
stomach contents to empty.
Factors affecting on
gastric emptying
Intestinal transiIntestinal transit
Intestinal transitIntestinal transit
Small intestine- major site for drug absorption,
long intestinal transit is desirable for complete
drug absorption
The residence time depends on the intestine that
occurs due to peristaltic contractions..
It promotes drug absorption by,
Increasing drug intestinal membrane contact,
Enhancing dissolution especially poorly soluble
drugs, through induced agitation.
 Delayed intestinal
transit is desirable for,
Intestinal transitIntestinal transit
 Promotes..
 Diarrhea
 Laxatives
 Drugs like metoclopramide
 Demotes..
 Food
 Pregnancy
 Anticholinergics
GastrointestinalGastrointestinal
pHpH
 107
fold difference in the H+
ion
concentration is observed
between the gastric & colon fluids.
Blood Flow To
The GIT
The GIT is extensively supplied by blood capillary network & the
lymphatic system.
The blood flow rate to the GIT is 500 to 1000 times (28% of
cardiac output) more than the lymph flow.
GI perfusion rate could be a rate limiting step in the absorption of
lipid soluble drugs.
The perfusion rate increases after meals but absorption is not
influenced significantly.
Disease States
Classes of diseases
states, can affect on
Bioavailability of drug
Gastrointestinal diseases
Cardiovascular diseases
Hepatic diseases
Gastrointestinal
diseases
Altered GI motility
GI diseases & infections
Achlorhydria – decreased gastric acid secretion &
increased stomach pH
Malabsorption syndrome
Celiac disease
Crohn’s disease
Infections like gastroenteritis, cholera, colitis,
amoeviasis & constipation
GI surgery
Cardiovascular diseases:
CHF influence bioavailability of drug viz.
oedema of intestine,
Decreased blood flow to the GIT & gastric
emptying rate,
Altered GI pH, secretion & microbial flora
Hepatic diseases:
Such as hepatic cirrhosis.
Presynaptic
metabolism
(First-pass effects)
 Before a drug reaches blood circulation, it has to pass for
the first time through organs of elimination namely the GIT
& liver.
 The loss of drug through biotransformation by such
eliminating organs during its passage to systemic
circulation is called as FIRST-PASS METABOLISM
 Following system affect on FIRST-PASS METABOLISM
 Luminal enzymes
 Digestive enzymes
 Bacterial enzymes
 Mucosal / Gut wall enzymes
 Hepatic enzymes
What is gastric emptying? Describe its
role in drug absorption
 Write a note on factors affecting drug
absorption.
QUESTIONSQUESTIONS
ASKEDASKED
For further reading regarding this topic,
please refer the books like Brahmankar,
Remington, Alton and another related
books…..!

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Patient related factors

  • 1. Patient Related Factors Affecting drug absorption Presented by,Presented by, Hinglajia HetalHinglajia Hetal RatilalRatilal
  • 3. Age
  • 4. Age Infants • Gastric pH high • Intestinal surface low • Blood flow to GIT low Elderly persons  Altered gastric emptying  Decreased intestinal surface area & GI blood flow  Higher incidents of achlorhydria  Bacterial overgrowth Altered Absorption pattern
  • 6. Gastric emptying Apart from dissolution of a drug & its permeation through the bio membrane, the passage from stomach to the small intestine, called as gastric emptying. Rate limiting step, because the major site of drug absorption is intestine. It increases bioavailability of a drug. It is first order process.
  • 7. Rapid gastric emptyingRapid gastric emptying advisable where,advisable where,
  • 9. Gastric acid quantifying parameters • Gastric emptying rate is the speed at which the stomach contents empty into the intestine. • Gastric emptying time is the time required for the gastric content to empty into the small intestine. • Longer the gastric emptying time , lesser the gastric emptying rate. • Gastric emptying t1/2 is the time taken for half the stomach contents to empty.
  • 11.
  • 13. Intestinal transitIntestinal transit Small intestine- major site for drug absorption, long intestinal transit is desirable for complete drug absorption The residence time depends on the intestine that occurs due to peristaltic contractions.. It promotes drug absorption by, Increasing drug intestinal membrane contact, Enhancing dissolution especially poorly soluble drugs, through induced agitation.
  • 14.  Delayed intestinal transit is desirable for,
  • 15. Intestinal transitIntestinal transit  Promotes..  Diarrhea  Laxatives  Drugs like metoclopramide  Demotes..  Food  Pregnancy  Anticholinergics
  • 17.  107 fold difference in the H+ ion concentration is observed between the gastric & colon fluids.
  • 19. The GIT is extensively supplied by blood capillary network & the lymphatic system. The blood flow rate to the GIT is 500 to 1000 times (28% of cardiac output) more than the lymph flow. GI perfusion rate could be a rate limiting step in the absorption of lipid soluble drugs. The perfusion rate increases after meals but absorption is not influenced significantly.
  • 21. Classes of diseases states, can affect on Bioavailability of drug Gastrointestinal diseases Cardiovascular diseases Hepatic diseases
  • 22. Gastrointestinal diseases Altered GI motility GI diseases & infections Achlorhydria – decreased gastric acid secretion & increased stomach pH Malabsorption syndrome Celiac disease Crohn’s disease Infections like gastroenteritis, cholera, colitis, amoeviasis & constipation GI surgery
  • 23. Cardiovascular diseases: CHF influence bioavailability of drug viz. oedema of intestine, Decreased blood flow to the GIT & gastric emptying rate, Altered GI pH, secretion & microbial flora Hepatic diseases: Such as hepatic cirrhosis.
  • 25.  Before a drug reaches blood circulation, it has to pass for the first time through organs of elimination namely the GIT & liver.  The loss of drug through biotransformation by such eliminating organs during its passage to systemic circulation is called as FIRST-PASS METABOLISM  Following system affect on FIRST-PASS METABOLISM  Luminal enzymes  Digestive enzymes  Bacterial enzymes  Mucosal / Gut wall enzymes  Hepatic enzymes
  • 26.
  • 27. What is gastric emptying? Describe its role in drug absorption  Write a note on factors affecting drug absorption. QUESTIONSQUESTIONS ASKEDASKED
  • 28. For further reading regarding this topic, please refer the books like Brahmankar, Remington, Alton and another related books…..!