Methods of enhancing bioavailability of drugs

Methods of enhancing bioavailability of drugs

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  Methods of EnhancingBioavailability Of Drugs Presented By-Debasish Ghadei M.B.A. (Pharmaceutical Management) (2nd Sem) Roll No-21142 1
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  Contents: • Introduction toBioavailability • Enhancement of Bioavailability • Approaches used in overcoming Bioavailability Problems • Methods of Enhancing Bioavailability 2
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  Bioavailability • It isdefined as the rate and extent amount of absorption of unchanged drug from dosage form. 3
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  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
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  Biopaharmaceutics classification system(BCS) 5
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  Approaches used inovercoming Bioavailability Problems: • The pharmaceutical Approach • The pharmacokinetic Approach • The biological Approach
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  Methods of EnhancingBioavailability (The pharmaceutical Approach) • Enhancement of drug solubility or dissolution rate • Enhancement of drug permeability • Enhancement of drug stability • Enhancement of gastrointestinal retentions. 7
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  Enhancement of Drugstability 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
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  Enhancement of drugpermeability • Lipid technologies • Ion Pairing • Penetration enhancers 9
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  Enhancement of drugstability • Enteric coating • Complexation • Use of metabolism inhibitors 10
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  Enhancement of gastrointestinal retention •Increased contact with epithelial surface • Prolonged residence time in the stomach • Delaying intestinal transit 11
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  Enhancement of Drugstability 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 Enhancement of drugpermeability • Lipid technologies • Ion Pairing • Penetration enhancers
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  32 Enhancement of drugstability • Enteric coating • Complexation • Use of metabolism inhibitors
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  Enhancement of gastrointestinal retention 34
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