In vivo percutaneous absorption of capsaicin, nonivamide and sodium nonivamide acetate from ointment bases Pharmacokinetic analysis in rabbits英文电子书.pdf

international journal of pharmaceutics E L S E V I E R International Journal of Pharmaceutics 128 (1996) 169-177 In vivo percutaneous absorption of capsaicin, nonivamide and sodium nonivamide acetate from ointment bases Pharmacokinetic analysis in rabbits Jia-You Fang, Pao-Chu Wu, Yaw-Bin Huang, Yi-Hung Tsai* School of Pharmacy, Kaohsiung Medical College, Kaohsiung, Taiwan ROC Received 23 May 1995;accepted 24 July 1995 Abstract Nonivamide (NVA) and nonpungent sodium nonivamide acetate (SNA) are both synthetic derivatives of capsaicin. In this study, in vivo systemic drug plasma data of capsaicin, NVA and SNA following intravenous and transdermal ointment base administration in rabbits were performed to establish the pharmacokinetic analysis of these analogues. In order to describe the capsaicin, NVA and SNA plasma profiles observed, one-compartment pharmacokinetic open model for capsaicin and NVA, and two-compartment model for SNA was used in the i.v. plasma data. After the percutaneous administration, the plasma profiles between capsaicin and NVA were quite different although these two analogues showed similar physicochemical properties and intravenous pharmacokinetic parameters. The high plasma concentrations of SNA were obtained in the early period after transdermal ap