This document discusses various approaches to enhancing the bioavailability of drugs, including improving solubility, permeability, stability, and gastrointestinal retention. It introduces concepts like bioavailability, the biopharmaceutics classification system (BCS), and approaches through pharmaceutical, pharmacokinetic and biological means. Specific pharmaceutical methods covered are enhancing drug solubility/dissolution through techniques like micronization, use of surfactants, salt forms or eutectic mixtures, as well as enhancing permeability through lipid technologies, ion pairing or penetration enhancers.

1. BIOPHARMACEUTICS & PHARMACOKINETICS
Methods of Enhancing Bioavailability Of Drugs
NITIN LAXMAN THOMBRE
ROLL NO.95

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

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

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.

5. Biopaharmaceutics classification system (BCS)
CLASS SOLUBILITY PERMABILITTY ABSORPTION PATTERN EXAMPLE
1 HIGH HIGH WELL ABSORBED DILTIAZEM
PROPRANOLOL
METOPROLOL
2 LOW HIGH VARIABLE NIFEDIPINE
CARBAMEZAPINE
NAPROXEN
3 HIGH LOW VARIABLE INSULINE
METFORMIN
CIMETIDINE
4 LOW LOW POORLY ABSORB TAXOL
CHLORTHIAZIDE
FUROSEMIDE

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

8. Enhancement of Drug stability or
dissolution rate
1) Micronization
2) Nano suspension
3) Supercritical fluid process
4) Spray freezing into liquid (SFL)
5) Evaporate precipitation into aqueous solution (EPAS)
6) Use of surfactant
7) Use of salt forms
8) Eutectic mixture

9. Enhancement of drug permeability
 Lipid technologies
 lon Pairing
 Penetration enhancers

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

11. THANK YOU