ketoconazole在中國人體內的藥物動力學特性   全文下載

Pharmacokinetic Behavior of Ketoconazole in Adult Chinese Males

口服投與含400 mg之ketoconazole錠於十四名健康男性獲得如次的藥物動力學參數：AUC∞ （51. 4 ± 17.9 mg.h ／ 1, mean ± SD）, Cmax （10.3 ± 2.8 mg ／ l）, Tmax （1.5 ± 0.3 h）, MRT （4.1 ± 0.7 h）, VRT （30.9 ± 11.2h2） , Cl ／ F ／ BW （ 0.138 ± 0.0631 ／ h ／ kg） 和k* （末端相斜率，0.330 ± 0.09 h-1）。倘若將十四名受試者之血漿中濃度使用傳統的一室體模式加以歸納，吸收速率常數為0.236 ± 0.136 h-1，而消失速率常數為0.172 ± 0.041 h-1。白種人和中國人間之Cl ／ F, k*, Cmax和AUC∞並無顯著差異。唯中國人的Tmax （1.5 ± 0.3 h）遠比白種人（2.6 ± 1.2 h, P < 0.01）為短，顯示吸收速率明顯地較快速。"

The pharmacokinetic behavior of ketoconazole (Nizoral-Janssen) in Chinese adults was studied in 14 male volunteers. The pharmacokinetic parameters of ketoconazole obtained after oral administration of 400 mg (two tablets) were AUC (51.4 ± 17.9 mg•h/l, mean ± SD), Cmax (10.3 ± 2.8 mg/l), Tmax (1.5 ± 0.3 h), MRT (4.1 ± 0.7 h), VRT (30.9 ± 11.2 h2), CI/F/BW (0.138 ± 0.063 l/h/kg) and k* (slope of terminal phase, 0.330 ± 0.09 h-1). When the plasma concentration data of 14 subjects were fitted to a conventional one-compartment body model, then the first order absorption rate constant was 0.236 ± 0.136 h-1, and the elimination rate constant was 0.172 ± 0.041 h-1. No statistical difference was observed for the parameters CL/F, k*, Cmax and AUC between Caucasians in a published study and Chinese in this study (p > 0.1). However, the T max in Chinese (1.5 ± 0.3 h) was significantly shorter than that in Caucasians (2.6 ± 1.2 h, p < 0.01). 口服投與含400 mg之ketoconazole錠於十四名健康男性獲得如次的藥物動力學參數：AUC∞ （51. 4 ± 17.9 mg.h ／ 1, mean ± SD）, Cmax （10.3 ± 2.8 mg ／ l）, Tmax （1.5 ± 0.3 h）, MRT （4.1 ± 0.7 h）, VRT （30.9 ± 11.2h2） , Cl ／ F ／ BW （ 0.138 ± 0.0631 ／ h ／ kg） 和k* （末端相斜率，0.330 ± 0.09 h-1）。倘若將十四名受試者之血漿中濃度使用傳統的一室體模式加以歸納，吸收速率常數為0.236 ± 0.136 h-1，而消失速率常數為0.172 ± 0.041 h-1。白種人和中國人間之Cl ／ F, k*, Cmax和AUC∞並無顯著差異。唯中國人的Tmax （1.5 ± 0.3 h）遠比白種人（2.6 ± 1.2 h, P < 0.01）為短，顯示吸收速率明顯地較快速。