Comparative bioavailability cf two amlodipine formulation in healthy volunteers

Area of Science:

• Pharmacology and Pharmaceutical Sciences
• Clinical Pharmacy
• Drug Development

Background:

• Amlodipine is a widely prescribed calcium channel blocker for hypertension and angina.
• Ensuring bioequivalence between generic and reference formulations is crucial for therapeutic interchangeability.
• The CAS number for amlodipine is 88150-42-9.

Purpose of the Study:

• To assess the bioequivalence of a 10 mg amlodipine test tablet (Intervask) compared to a reference amlodipine formulation.
• To evaluate key pharmacokinetic parameters including AUCt, AUCinf, Cmax, Tmax, and t(1/2).

Main Methods:

• A randomized, single-blind, cross-over study involving 12 healthy volunteers under fasting conditions.
• Administration of single doses of test and reference amlodipine formulations in two study periods separated by a 3-week washout.
• Plasma amlodipine concentrations determined using a validated LC/MS method up to 144 hours post-dose.

Main Results:

• Mean pharmacokinetic parameters (AUCt, AUCinf, Cmax, t(1/2)) were comparable between the test and reference amlodipine formulations.
• Point estimators for AUCt, AUCinf, and Cmax ratios (test/reference) were 96.26%, 99.48%, and 97.03%, respectively.
• 90% confidence intervals for the mean ratios of In-transformed parameters fell within the accepted bioequivalence range (80-125%).

Conclusions:

• The Intervask 10 mg amlodipine tablet is bioequivalent to the reference formulation.
• Bioequivalence was demonstrated in terms of both the rate and extent of drug absorption.
• This supports the interchangeability of the test and reference amlodipine products.