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Drug absorption slideshare.pptx

  1. 1. TOPIC : DRUG ABSORBTION NAME- DEBABRATA DINDA ROLL NO- 20801920056 SUBJECT- BIOPHARMACEUTICS & PHARMACOKINETICS SUBJECT CODE- PT604
  2. 2. CONTENTS INTRODUCTION INTRODUCTION BIOLOGICAL MEMBRANE DRUG TRANSPORT ABSORPTION OF DRUG IN GIT FACTOR AFFECTING DRUG ABSORPTION EFFECT OF pH ON DRUG KINETICS BIOAVALABILITY FIRST PASS METABOLISM REFERENCE
  3. 3. INTRODUCTION DRUG ABSORBTION? Drug absorbtion is defined as the process of movement of unchanged form of drug from the site of administration to systemic circulation . - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - Minimum effective concentration (MEC) Subtherapeutic level Time Plasma Drug Concentration Therapeutic level Therapeutic success of a rapidly and completely absorbed drug Therapeutic failure of a slowly absorbed drug Fig- Plots showing significance of rate and extend of absorbtion in drug therapy
  4. 4. BIOLOGICAL MEMBRANE
  5. 5. DRUG TRANSPORT Drugs need to pass through one or more cell membrane to reach their site of action. Drugs transport by- (1) PASSIVE DIFFUTION - Drug transport in the direction of concentration gradient. More lipid soluble drug diffuse quickly. No energy and carrier required. (2) FILTRATION – trough paracellular space in membrane. (3) SPECIALIZED TRANSPORT – (a) Active transport- Drug movement against concentration gradient. Energy and carrier reguired Symport(cotransport) Antiport(Exchange transport) (b) Facilitated Diffusion- Transport of glucose across muscle cell membrane by a trans porter GLUT. Drug transport in the direction of concentration gradient. No energy and carrier required.
  6. 6. ABSORPTION ACIDIC AND BASIC DRUG IN GIT Weakly acidic drugs Unionised form Better absorbtion from stomach (Aspirin) Weakly basic drug (Morphine , Quinine) Unionised form Better absorbtion from stomach Acidic pH Basic pH So,acidic drug more readily absorbed from stomach and basic drug more readily absorbed from intestine.
  7. 7. FACTORS AFFECTING DRUG ABSORPTION Aquous solubility – Solution absorbed faster than solid. Concentration of drug – Concentrated solution absorbed faster than dilute solution. Area of absorption sueface – More area faster absorption. Blood flow – Increase blood flow removes the drug from the site of absorption so reduce absorption. Empty stomach – Increase absorption of drug. Presence of food – Retard drug absorption. Ionization of drug – Drug are absorbed in unionized state so ionization decreases drug absorption.
  8. 8. EFFECT OF pH ON DRUG KINETICS Most drugs are weak electrolytes, i.e. their ionization is pH dependent. The ionization of drug is given by: pH = pKa + log[A^-1]/[HA] pKa – Numerically equal to the pH at which the drug is ionized. [A^-1] – Concentration of ionized drug. [HA] – Concentration of unionized drug.
  9. 9. BIOAVALABILITY It is the fraction of a drug that reaches systemic circulation. eg – If 100 unit of a drug is administered by any route and 70% unit reaches In the systemic circulation , than bioavailability of the drug is 70%. Bioavailability is i.v. route is 100%. Disintegration time and dissolution rate – affect bioavailability. Calculated by relating area under curve plasma concentration – time for i.v. route and that particular route. Bioavailability= AUC oral AUC injected X 100
  10. 10. FIRST PASS METABOLISM When drugs are administered orally,they have to pass Gut Wall – Portal vein – Liver – Systemic Circulation. Drugs via high hepatic 1st pass metabolism are – Salbutamol,Verapamil,Propranolol, Lignocaine,Isoprenaline.
  11. 11. REFERENCE Brahmankar D M and Jaiswal .Sunil B,Drug absorbtion ,Biopharmaceutics and Pharmacokinetics.

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