Abstract P100: Bioavailability of Arginine versus Erbumine Formulations of Perindopril in Healthy Subjects [Session Title: Onsite Poster Competition I With Reception]

Perindopril is an angiotensin converting-enzyme inhibitor with a proven track record in cardiovascular clinical trials. Traditionally formulated as the t-butyl amine (“erbumine”) salt, perindopril’s arginine salt has been FDA-approved in combination with amlodipine besylate. The arginine salt has the advantage of being more stable at higher temperatures or humidity.To demonstrate bioequivalence (using the standard FDA definition of 90% confidence intervals that are within 80-125% of the values seen with the reference product), the bioavailability of the two perindopril formulations was compared. After screening 121 healthy subjects, 30 (73% male, 38.9±9.5 years of age, 67% African American, BMI of 26.6±2.7 kg/m2) signed informed consent, and were studied in a randomized, single-center, single-dose, open-label, 2-period, 2-way cross-over design with a 14-day washout period. After an overnight fast, perindopril was administered orally with 240 mL of water, and blood samples taken at defined time points.After dose-normalization (the arginine salt has a molecular weight 1.43-fold greater than that of the erbumine salt), all pharmacokinetic parameters for perindopril plasma concentrations were similar between treatments. Mixed model analysis of these parameters demonstrated bioequivalence (e.g., area under the time-plasma concentration curve: 10.2 vs. 10.5 hr•ng/mL/mg, P = 0.54). Very similar results with non-significant differences were also seen for the pharmacokinetic...

Source: Hypertension - September 14, 2017 Category: Cardiology Authors: Andrew Bishop Tags: Poster Abstract Presentations Source Type: research