Assessment of sex differences in Pharmacokinetics of carvedilol in human

Abstract

Carvedilol is an anti-hypertensive agent capable of blocking both alph (α) and beta (β) receptors used to preclude cardiac arrhythmias and angina. The study was designed to evaluate the Pharmacokinetics of carvedilol in human male and female volunteers. Healthy male and female (twenty each) volunteers were finalized for the study after preliminarily clinical examination. Blood samples were collected at specific time intervals after giving an oral dose of 12.5mg carvedilol, separated the plasma and placed at -80°C until analysis. Estimation of carvedilol in human plasma was accomplished by High performance liquid chromatographic (HPLC) method using fluorescent detector. Plasma concentration-time curve was used for calculation of pharmacokinetic parameters using two-compartment open model.Mean (SD) values of AUC and Cmax 0.076±0.021µg.h/ml and 0.024±0.005µg/mL, respectively) in male differ significantly (P<0.05) from the female 0.197±0.042µg.h/ml and 0.048±0.02µg/mL, respectively). Overall, bioavailability of carvedilol was somewhat higher in females than in males, but these differences could be expounded by the lower body weight of female. Conversely, no significant differences were found for tmax, clearance and half-life in male and femaleMoreover the ethnicity had significant impact on the Pharmacokinetics of carvedilol in human.