BIOEQUIVALENCE STUDIES

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Presentation Transcript

Seminar on : 

Seminar on BIOEQUIVALENCE STUDIES PRESENTED BY BINDU.R M.PHARM 1ST SEM INDUSTRIAL PHARMACY St. PETERS INSTITUTE OF PHARMACEUTICAL SCIENCES VIDYANAGAR, HANAMKONDA WARANGAL, 506001 ANDHRA PRADESH

Contents : 

Contents Bioavailability Bioavailability Study Protocol Methods To Assess Bioavailability Bioequivalence Statistical Analysis Of Data References

Bioavailability : 

Bioavailability The extent and rate at which its active moiety is delivered from pharmaceutical form and becomes available in the systemic circulation AUC Cmax Tmax

Slide 4: 

Absolute bioavailability (F): Relative bioavailability (Frel)

Bioavailability study protocol : 

Bioavailability study protocol A. Study objective B. Study design 1.Experimental design 2.Washout period 3.Drug products a)Test products b)Reference product 4.Dosage regimen 5.Sample collection schedule 6.Route of administration 7.single versus multiple-dose study design

Slide 6: 

8.Subjects a)Healthy subjects versus patients b)Subject selection i) Medical history ii) Physical examination iii) Laboratory tests 9. Analysis of biological fluids

Assessment of bioavailability : 

Assessment of bioavailability 1) Pharmacokinetic methods (indirect methods) a) Plasma data (i) Tp (ii) Cmax (iii) AUC b) Urine data (i) dXu/dt (Rate of drug excretion) (ii) Xu- ∞ (Cumulative drug excreted) (iii) Tu- ∞(time for max. urinary excretion) 2) Pharmacodynamic methods (direct methods) a) Acute pharmacological effect b) Clinical response

Plasma data : 

Plasma data Basic assumption is bioequivalent products produce super imposable plasma level – time curves Time of peak plasma concentration (tp) – indicates rate of drug absorption At tp, rate of drug absorption is equal to rate of drug elimination Units of tp are hr or min. Peak plasma concentration (Cmax) – indicates maximum drug concentration, shows whether drug is in therapeutic range or not Units of Cmax are mcg/ml or ng/ml

Slide 9: 

AUC represents extent of absorption or fraction of dose that reaches systemic circulation AUC0-∞ is sum of AUC0-t and AUCt- ∞ where t is last time point of plasma sample collection. AUC0-t is calculated by Trapezoidal method and AUCt- ∞ is obtained by equation C*/K, C* is concentration of drug in last plasma sample, K is overall elimination rate constant. AUC is independent of route of administration, Units are concentration-time/volume. (ng-h/ml)

Urine studies : 

Urine studies It involves non invasive method of sampling Concentration of drug in urine is greater than blood and easy to estimate Amount of drug excreted is obtained directly Drug should be eliminated unchanged in the urine Limitations Difficult to estimate absorption rate of rapidly absorbing drug Metabolites may be eliminated in urine and estimation may be difficult

Urinary Drug Excretion Data : 

Urinary Drug Excretion Data 1) dX u/dt. The rate of drug excretion. 2) X ∞u. The cumulative amount of drug excreted in the urine It is related directly to the total amount of drug absorbed. 3) t ∞ The total time for the drug to be excreted

Plots relating the plasma level–time curve and the rate of urinary drug excretion : 

Plots relating the plasma level–time curve and the rate of urinary drug excretion

Plot of cumulative urinary drug excretion versus time : 

Plot of cumulative urinary drug excretion versus time

Bioequivalence (BE): Definition : 

Bioequivalence (BE): Definition “the absence of a significant difference in the rate and extent to which the active ingredient or active moiety in pharmaceutical equivalents or pharmaceutical alternatives becomes available at the site of drug action when administered at the same molar dose under similar conditions in an appropriately designed study.” CDER U.S. Food & Drug Administration Two products are bioequivalent if they are pharmaceutically equivalent Bio availabilities (both rate and extent) after administration in the same molar dose are similar to such a degree that their effects can be expected to be essentially the same.

Bioequivalence : 

Bioequivalence

Types of designs : 

Types of designs Parallel design Crossover design In parallel design products are randomly administered to the volunteers Disadvantage is inter subject variability

TWO-WAY CROSSOVER : 

TWO-WAY CROSSOVER

FOUR-WAY CROSSOVER : 

FOUR-WAY CROSSOVER

BIBD FOR FOUR FORMULATIONS : 

BIBD FOR FOUR FORMULATIONS

Statistical Analysis of the data : 

Statistical Analysis of the data Due to the limitation in sampling techniques the resultant blood-level curve is influenced by both the number and duration of blood samples. Unfortunately, due to biological and experimental variations, some differences always exist. Statistical methods are used to evaluate the data in order to identify the different sources of variation. The analysis of variance (ANOVA), a statistical procedure used for a crossover design, is used widely in BA testing.

Statistical analysis using t-test : 

Statistical analysis using t-test Two types 1) Two independent sample t-test 2) Paired t-test

The formula to calculate t-value : 

The formula to calculate t-value

PAIRED T-TESTTo calculate variance : 

PAIRED T-TESTTo calculate variance To calculate t-value

REFERENCES : 

REFERENCES Fundamentals of Biopharmaceutics and Pharmacokinetics by V Venkateswarlu Biopharmaceutics and Pharmacokinetics by D.M Brahmankar & Sunil B. Jaiswal Applied Biopharmaceutics and Pharmacokinetics by Leon shargel , Susanna wu-pong, Andrew B.C yu

Slide 28: 

Thank You!