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Bioavailability and bioequivalence testing

This document discusses bioavailability and bioequivalence testing. It defines bioavailability as the relative amount of an administered dose that reaches systemic circulation. Bioavailability can be measured using pharmacokinetic methods like plasma level time studies and urinary excretion studies. Factors that affect bioavailability include formulation factors, excipients, drug properties, and physiological factors. Bioequivalence refers to two drug products containing the same active ingredient reaching systemic circulation at the same rate and to the same extent. Statistical tests are used to determine bioequivalence based on pharmacokinetic parameters. Methods to enhance bioavailability include altering particle size, adding surfactants, changing pH, and using solubilizing formulations like solid dispersions.

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BIOAVAILABILITY AND BIOEQUIVALENCE TESTING Presented by N.Lakshmi Priya Pharmaceutics M.Pharmacy
INTRODUCTION Introduced in 1945. Studies of relative absorption of vitamins. Referred as physiologic availability.
CONCEPT OF BIOAVAILABILITY? Increased prescriptions. Formulary systems. Extending the laws of pharmacist’s role. By US federal government.
DEFINITION: Relative amount of an administered dose that reaches the systemic circulation. OR Rate and extent of absorption of unchanged drug from its dosage form. bioavailable dose administered dose F =
OBJECTIVES:  suitable dosage form.  efficiency of absorption. New formulations. Control of quality
TYPES OF BIOAVAILABILITY 1.Absolute bioavailability Plasma concentration versus time data Urinary data
2.RELATIVE BIOAVAILABILITY Plasma concentration vs time data. Urinary data
FACTORS AFFECTING BIOAVAILABILITY FORMULATION FACTORS EXCIPIENTS NATURE OF THE DRUG PARTICLE SIZE FORM OF THE DRUG PHYSIOLOGICAL FACTORS GASTRIC EMPTYING INTESTINAL MOTILITY PH INTESTINAL WALL CHANGES
CRITERIA FOR BIOAVAILABILITY TESTING 12 subjects. Physical examination and laboratory testing. Cross over design.
MEASUREMENT OF BIOAVAILABILITY Pharmacokinetic methods Plasma level time studies Urinary excretion studies Pharmacodynamic methods Acute pharmacologic response Therapeutic response
PHARMACOKINETIC METHODS 1.Plasma level time studies 3 parameters are to be considered. Cmax. tmax. AUC
2.URINARY EXCRETION STUDIES. 3 parameters are to be considered. dXu/dt (tu)max XU
ACUTE PHARMACOLOGIC RESPONSE ECG or EEG, pupil diameter is related to time course of a given drug. time Dose
DISADVANTAGES Variable Difficulty in correlation Response is not due to the pharmacological effect.
2.THERAPEUTIC RESPONSE Clinical response to a given formulation. •Drawback: Quantitation is improper to assess the relative bioavailability.
OTHER MEASURES 1.DISSOLUTION RATE In-vitro dissolution testing models. Factors to be considered. Dissolution apparatus Dissolution fluid Process parameters
TYPES OF DISSOLUTION APPARATUS Closed -compartment Open-compartment Dialysis systems ROTATING BASKET ROTATING PADDLE
IN VITRO-IN VIVO CORRELATION Objectives Batch to batch consistency  developing a new dosage form Basic approaches By linear relations ship By using previous data
QUANTITATIVE INVITRO-INVIVO CORRELATIONS Based on plasma level data Based on urinary excretion data Based on pharmacologic response
STATISTICAL TERMS Average ANOVA Bar over a letter Bioequivalence Confidence interval Control Cross over Distribution Formulation
Frequency distribution Logarithmic transformation Mean Median Period Sequence group Standard error washout
BIOEQUIVALENCE Drug substance in two or more identical dosage forms reaches the systemic circulation at same relative rate and extent. RELATED TERMS Pharmaceutical equivalence Chemical equivalence Therapeutic equivalence
MEASUREMENT OF BIOEQUIVALENCE Same route,equal doses,different times. Study in healthy, adult male volunteers. Latin square cross over design
ADVANTAGES Minimises intersubject variability. Minimises variations Minimises carry over effects. DRAWBACKS  Long time Dropout Rates are high
Statistical interpretation of analysis data. ANOVA CLINICALLY SIGNIFICANT
METHODS FOR ENHANCMENT OF BIOAVAILABILITY Micronization Use of surfactants Use of salt forms Alteration of pH of the drug micro environment Use of metastable polymorph Solute-solvent complexation Solvent deposition
Selective adsorption on insoluble carriers Solid solutions Eutectic mixtures Solid dispersions Molecular encapsulation with cyclodextrins
REFERENCES Biopharmaceutics and pharmacokinetics- D.M BRAHMANKAR. Page no:282-302 Biopharmaceutics and pharmacokinetics- P L MADHAN Page no:125-178 Basic pharmacokinetics-SUNIL S JAMBHEKAR AND PHILIP J BREEN page no:458-470