Tranilast在華人的藥物動力學   全文下載

Pharmacokinetic Properties of Tranilast in Chinese People

12名健康自願華人男性，以單劑量口服投予兩種Trani1ast膠囊製劑（Tranpro(R)和Rizaben(R)）之交叉試驗進行其藥物動力學及相對生體可用率之試驗。試驗前及試驗後適當時間之血液檢體收集至24小時，血漿中藥物濃度是以高效能液相層析儀進行分析。口服這二種不同處方膠囊製劑的藥動學參數並無顯著差異，故Trani1ast的藥動性質是將其合併起來計算Cmax, Tmax, t1／2及Cl／F分別為42.2 ± 5.92μg／ml，2.79 ± 1.14h, 7.58 ± 1.44h及8.12 ± 1.31mL／h／kg。口服Tranpro(R)和Rizaben(R)之AUC∞分別為431 ± 97和412 ± 60μg.h／mL，經統計分析之結果顯示二種Tranilast膠囊具生體相等性。"

The pharmacokinetics and relative bioavailability of two different formulated tranilast capsules were determined after single dosing in twelve healthy Chinese subjects in a two-way crossover study. Blood samples were obtained from predose until 24 h postdose. Plasma concentration of tranilast was determined by an HPLC method. Since no differences in pharmacokinetic parameters were found between the two distinctive tranilast products (Tranpro and Rizaben), the data were pooled together to characterize the pharmacokinetic property of tranilast. Mean peak plasma concentrations after dosing and the time at which it occurred (Tmax) were 42.2 ± 5.92 μg/mL and 2.79 ± 1.14 h, respectively. The elimination half-life and total body plasma clearance were 7.58 ± 1.44 h and 8.12 ± 1.31 mL/h/kg, respectively. The respective areas under the concentration-time curve from time 0 to infinity for Tranpro and Rizaben were 431 ± 97 and 412 ± 60 μg·h/mL. The results also indicated that the two tranilast products can be considered as bioequivalent. 12名健康自願華人男性，以單劑量口服投予兩種Trani1ast膠囊製劑（Tranpro(R)和Rizaben(R)）之交叉試驗進行其藥物動力學及相對生體可用率之試驗。試驗前及試驗後適當時間之血液檢體收集至24小時，血漿中藥物濃度是以高效能液相層析儀進行分析。口服這二種不同處方膠囊製劑的藥動學參數並無顯著差異，故Trani1ast的藥動性質是將其合併起來計算Cmax, Tmax, t1／2及Cl／F分別為42.2 ± 5.92μg／ml，2.79 ± 1.14h, 7.58 ± 1.44h及8.12 ± 1.31mL／h／kg。口服Tranpro(R)和Rizaben(R)之AUC∞分別為431 ± 97和412 ± 60μg.h／mL，經統計分析之結果顯示二種Tranilast膠囊具生體相等性。