Methods of enhancing bioavailability of drugs

For pharma students

1. Methods of Enhancing Bioavailability Of Drugs Presented By-Debasish Ghadei M.B.A. (Pharmaceutical Management) (2 nd Sem ) Roll No-21142 1

2. Contents: Introduction to Bioavailability Enhancement of Bioavailability Approaches used in overcoming Bioavailability Problems Methods of Enhancing Bioavailability 2

3. Bioavailability It is defined as the rate and extent amount of absorption of unchanged drug from dosage form. 3

4. Enhancement of Bioavailability As far as the bioavailability is concerned, a drug with poor bioavailability is the one with : Poor aqueous solubility or slow dissolution rate in biological fluid. Poor permeability through the bio membrane owing to inadequate partition coefficient or lipophilicity or large molecular size such as that of protein or peptide drug like insulin. 4

5. Biopaharmaceutics classification system (BCS) 5

6. Approaches used in overcoming Bioavailability Problems: The pharmaceutical Approach The pharmacokinetic Approach The biological Approach

7. Methods of Enhancing Bioavailability ( The pharmaceutical Approach) Enhancement of drug solubility or dissolution rate Enhancement of drug permeability Enhancement of drug stability Enhancement of gastrointestinal retentions. 7

8. Enhancement of Drug stability or dissolution rate Micronization Nano suspension Supercritical fluid process Spray freezing into liquid(SFL) Evaporate precipitation into aqueous solution(EPAS) Use of surfactant Use of salt forms Use of precipitation inhibitors Alteration of pH of drug microenvironment Use of amorphs,anhydrates,solvetes & metastable polymorphs Solvent deposition Precipitation Selective absorption on insoluble carriers Solid solutions Eutectic mixture Solid dispersions Molecular encapsulation with cyclodextrins 8

9. Enhancement of drug permeability Lipid technologies Ion Pairing Penetration enhancers 9

10. Enhancement of drug stability Enteric coating Complexation Use of metabolism inhibitors 10

11. Enhancement of gastrointestinal retention Increased contact with epithelial surface Prolonged residence time in the stomach Delaying intestinal transit 11

12. Enhancement of Drug stability or dissolution rate Micronization Nano suspension Supercritical fluid process Spray freezing into liquid(SFL) Evaporate precipitation into aqueous solution(EPAS) Use of surfactant Use of salt forms Use of precipitation inhibitors Alteration of pH of drug microenvironment Use of amorphs,anhydrates,solvetes & metastable polymorphs Solvent deposition Precipitation Selective absorption on insoluble carriers Solid solutions Eutectic mixture Solid dispersions Molecular encapsulation with cyclodextrins 12

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26. 26 Enhancement of drug permeability Lipid technologies Ion Pairing Penetration enhancers

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32. 32 Enhancement of drug stability Enteric coating Complexation Use of metabolism inhibitors

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34. Enhancement of gastrointestinal retention 34

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