格拉司琼片人体生物利用度和药代动力学研究

PHARMACOKINETICS AND BIOAVAILABILITY OF DOMESTIC GRANISETRON TABLET IN HEALTHY VOLUNTEERS

９名男性健康志愿者，自身交叉口服单剂量（２ｍｇ）国产和进口格拉司琼片剂，用高效液相色谱荧光检测法测定血浆中格拉司琼浓度，进行药代动力学和相对生物利用度研究。试验结果表明，口服国产和进口格拉司琼的血药浓度－时间曲线均符合一房室模型，Ｔｍａｘ分别为１．２９±０．５２ｈ和１．４５±０．９８ｈ；Ｃｍａｘ为７．２３±１．９４μｇ·Ｌ－１和６．７８±２．８６μｇ·Ｌ－１；Ｔ１／２为５．３３±２．６５ｈ和５．４３±２．３２ｈ；ＡＵＣ为６８．０９±４２．６８μｇ·ｈ·Ｌ－１和７０．５５±５０．１９μｇ·ｈ·Ｌ－１；国产格拉司琼的相对生物利用度为１０２．４５±１６．９１％，其ＡＵＣ和Ｃｍａｘ值经对数转换后作方差分析，双单侧Ｔ检验证明两种制剂为生物等效制剂。

A single oral dose of 2 mg domestic and imported granisetron was given to 9 healthy volunteers in a randomized crossover study.Granisetron concentrations in plasma were determined by HPLC method. The pharmacokinetics and bioavailability were studied.The results showed that the plasma concentration-time curves of the two products were all fitted to one-compartment model.Tmax of domestic and imported tablets were 1.29±0.52 h and 1.45±0.98 h; Cmax were 7.23±1.94 μg·L-1 and 6.78±2.86 μg·L-1;T1/2 were 5.33±2.65 h and 5.43±2.32 h; AUC were 68.09±42.68 μg·h·L-1 and 70.55±50.19 μg·h·L-1 respectively. The relative bioavailability of domestic to imported tablets was 102.45±16.91%.There were no statistically singnificant difference between the two lnAUC values .The results demonstrated that two preparations were bioquivalent .