Biopharmaceutical Classification System (BCS)

Presentation given by Divya Chauhan

1. BIOPHARMACEUTICAL CLASSIFICATION SYSTEM(BCS) Presented by- DIVYA CHAUHAN M.PHARM(PHARMACEUTICS)

2. BIOPHARMACEUTICAL CLASSIFICATION SYSTEM(BCS) INTRODUCTION:- Biopharmaceutical Classification System (BCS) system allows restricting the prediction using the parameters solubility and intestinal permeability. The tenets of biopharmaceutics, solubility and permeability, are of pivotal importance in new drug discovery and lead optimization.

3. Purpose of the BCS Guidance: Expands the regulatory application of the BCS and recommends methods for classifying drugs . Explains when a waiver for in vivo bioavailability and bioequivalence studies may be requested based on the approach of BCS.

4. Criteria for BCS based biowaiwers: Biowaiver are based on the Biopharmaceutics (BCS) classification of the active ingredient . Currently BCS class I and some class III compounds are eligible for biowaivers. The drug substance should be highly soluble and highly permeable.

5. COND….. An IR drug product should be rapidly dissolving. The drug should not be a narrow therapeutic index drug . Excipients used in the dosage form should have been used previously in FDA approved IR solid dosage forms.

6. FACTOR AFFECTING ON BCS The Biopharmaceutical Classification System has been developed to provide a scientific approach to allow for to prediction in vivo pharmacokinetics of oral immediate release (IR) drug product by classifying drug compound based on their , SOLUBILITY PERMEABILIT DISSOLUTION

7. SOLUBILITY The Maximum Amount of solute dissolved in a given solvent under standard conditions of temperature, pressure and pH . Solubility is the ability of the drug to be solution after dissolution. The higher single unit dose is completely soluble in 250 ml at pH 1- 6.8 ( 37˚C ).

8. PERMEABILITY Permeability of the drug to pass the biological membrane which is the lipophilic. Permeability is indirectly based on the extent of absorption of a drug substance. Drug substance is considered to be highly permeable, when the extent of absorption in human determined to be 90 %.

9. DISSOLUTION It is process in which solid substance solubilises in given solvent i.e mass transfer from solid surface to liquid phase . Using USP apparatus I at 100 rpm or USP apparatus II at 50 rpm. Dissolution Media [900 ml], 1. 0.1 N HCl or simulated gastric fluid (pH 1.2 ) without enzyme. 2. pH 4.5 buffer & pH 6.8 buffer. 3. Simulated intestinal fluid without enzyme.

10. BCS CLASSIFICATION CLASS SOLUBILITY PERMEABILITY EXAMPLES Class-I High High Metoprolol , Propranolol Class-II low High Nifedipine, naproxen Class-III High Low Cimitidine, Metformin Class-IV Low Low Taxol, Clorthiazole

11. CLASS - I Ideal for oral route administration. Drug absorbed rapidly. Drug dissolved rapidly. Rapid therapeutic action. Bioavailability problem not expected for immediate release drug product. e.g. Metoprolol , Propranolol, Diltiazem.

12. CLASS - II Oral route for administration. Drug absorb rapidly . Bioavailability is controlled by dosage form and rate of release of the drug substance . e. g. Nifedipine, naproxen.

13. CLASS - III Oral route for administration. Drug absorbance is limited. Drug dissolve rapidly. e. g. Cimitidine, Metformin , Insulin .

14. CLASS - IV Poorly absorbed by orally administration. Both solubility & permeability limitation . Low dissolution rate . Slow or low therapeutic action . e. g. Taxol, Chlorthiazole, Cefexime Trihydrate.

15. APPLICATION To use in biowaiver considerations . Aid in earliest stages of drug discovery research . Applications in both the preclinical and clinical drug development processes. To predict in vivo performance of drug product using solubility and permeability measurements.

16. Thank you all For Attention………….