Bioequivalence evaluation of two brands of aceclofenac 100mg tablets (Aceclofar and Bristaflam) in healthy human volunteers

Abstract

A randomized, two-way, crossover, bioequivalence study in 24 fasting, healthy, male volunteers was conducted to compare two brands of aceclofenac 100 mg tablets, Aceclofar (Julphar, UAE) as test and Bristaflam (Bristol Myers Squibb, Egypt) as the reference product. The drug was administered with 240 ml of water after a 10 h overnight fast on two treatment days separated by 1 week washout period. After dosing, serial blood samples were collected for a period of 24 h. Plasma harvested from blood was analysed for aceclofenac by a validated HPLC method with UV-visible detection capable of detecting aceclofenac in the range 0.2-8.0 microg/ml with the limit of quantitation as 0.2 microg/ml. Various pharmacokinetic parameters including AUC(0-t), AUC(0- infinity ), C(max), T(max), T(1/2), and lambda(Z) were determined from plasma concentrations for both formulations and found to be in good agreement with reported values. AUC(0-t), AUC(0- infinity), and C(max) were tested for bioequivalence after log-transformation of data. No significant difference was found based on ANOVA; 90% confidence interval (100.0%-106.4% for AUC(0-t), 100.2%-106.8% for AUC(0- infinity ); 83.3%-102.8% for C(max)) of test/reference ratio for these parameters were found to be within the bioequivalence acceptance range of 80%-125%. Based on these statistical inferences, it was concluded that Aceclofar is bioequivalent to Bristaflam.

Liquid chromatography–tandem MS/MS method for simultaneous quantification of paracetamol, chlorzoxazone and aceclofenac in human plasma: An application to a clinical pharmacokinetic study

“…All volunteers were fasting males with an average weight of 70 kg, average height of 166 and body mass index of 26.13. Figure shows the mean plasma concentration vs time curves for the studied drugs and the obtained results (Table ) were in good agreement with the pharmacokinetic profile of PAR (Borin & Ayres, ), CXZ (Frye & Stiff, ) and ACL (Najib et al, ) concentrations in human plasma.…”

Efficacy and Safety of Aceclofenac Controlled Release in Patients with Knee Osteoarthritis: A 4-week, Multicenter, Randomized, Comparative Clinical Study

“…Thus, once or twice daily administration is necessary to maintain the efficacy of aceclofenac and major metabolites, 4'-hydroxy-aceclofenac, 4'-hydroxydiclofenac, and diclofenac21,22).…”

Safety and effectiveness of 4-week therapy with aceclofenac controlled release once a day

“…A sustained-release formulation can improve adherence and clinical outcomes while benefiting from its fast-acting properties 15 . Aceclofenac CR is bioequivalent to conventional aceclofenac (100 mg twice daily) 15 – 17 . However, its safety in humans has not been well studided.…”