Objective: In this study attempt was made to evaluate the effect of piperine on the bioavailability and pharmacokinetic of macrolides using experimental animals. Material and Methods: Albino Wistar rats (250-300 g body weight) were used for bioavailability study. All the rats were divided into four groups. First and third group of animals received only azithromycin (10mg/kg, p.o.) and erythromycin (50mg/kg, p.o.) respectively. Second and fourth group of animals received piperine (20mg/kg, p.o.) 30 minute before administration of drugs. About 2.5 ml of blood samples were collected at different time intervals from each rat. Plasma was separated from blood and plasma concentration of macrolides was measured by High performance liquid chromatography (HPLC). Pharmacokinetic parameters such as area under curve (AUC), peak plasma concentration (Cmax), time to occur peak plasma concentration (Tmax)were calculated and compared between macrolides with and without piperine. Results: Animals were treated with piperine followed by macrolides shown significantly (P<0.05) increased AUC as compared to animal administered only macrolides. The Cmax of azithromycin without and with piperine (20 mg/kg) was found to be 233.3±1.313 ng/l and 350.6±0.751ng/l respectively. Peak time at which maximum drug concentration of azithromycin in plasma without and with piperine (20mg/kg) was found to be 4 and 8 hrs respectively. The Cmax of erythromycin without and with piperine (20 mg/kg) was found to be 192.4±0.836 ng/l and 203.1±1.224 ng/l respectively. Peak time at which maximum drug concentration of erythromycin in plasma without and with piperine (20mg/kg) was found unchanged at 1.5 hrs.Conclusion: The result of present investigation shows that piperine significantly increased bioavailability of macrolides. Possible reason of increase in bioavailability by piperine may be due to inhibition of CYP3A4 enzyme drug metabolizing system.
Cite this article:
Samir Shah, Kintu Patel, Mohsin Pathan. Evaluation of the Effect of Piperine on Bioavailability and Pharmacokinetics of Macrolides in Rats. Asian J. Res. Pharm. Sci. 2018; 8(2):61-67. doi: 10.5958/2231-5659.2018.00013.9