Pharmacokinetics and bioequivalence of spironolactone tablets in healthy volunteers

AIM:To study the pharmacokinetics and bioequivalence of spironolactone in Chinese healthy people.METHODS:Two periods crossover randomized study was carried out in two groups with eighteen healthy male volunteers receiving a single dose of spironolactone 200 mg including two preparations, respectively.A sensitive and specific HPLC method was developed to quantitate the levels of canrenone in plasma,which was the metabolite of spironolactone.RESULTS:The concentration-time curves of canrenone coincided with a one-compartment open model.The main pharmacokinetic parameters of the trial and reference preparation weret t_(max)(4.2±s 1.2)and(4.7±1.6)h,c_(max)(160±47)and(150±43)μg·L-~(-1),t_(1/2ke)(18±5)and(19±4)h,AUC_(0-72)(3168±688)and(3267±627)μg·h·L~(-1),AUC_(0_∞)(3611±768)and(3759±642),respectively.The relative bioavailability of the trial preparation was(106±26)%.CONCLUSION: The HPLC method is suitable for the pharmacokinetie study of spironolaetone.Two one-sided t test and analysis of variance were performed in bioequivalent assessment,proving the two preparations of spironolactone are bioequivalent.