盐酸丁螺环酮临床药代动力学及生物利用度研究

Studies on pharmacokinetics and bioavailability of buspirone hydrochloride in human

目的：在健康志愿者中进行国产与进口盐酸丁螺环酮片剂药代动力学及生物利用度的比较研究。方法：受试者随机分成２组，交叉口服国产与进口盐酸丁螺环酮片各１５ｍｇ，采用气－质联用选择离子色谱（ＧＣ－ＭＳ／ＳＩＭ）法测定血浆中药物浓度。结果：口服２种片剂的药－时曲线均符合二室模型，国产与进口片Ｔ１／２β分别为４．２５６±１．７９０与５．９９０±２．１０１ｈ；Ｔｍａｘ分别为０．８７９±０．６１０与０．５５９±０．２６３ｈ；Ｃｍａｘ分别为６．０００±２．８８１与８．８７１±４．５１６μｇ·Ｌ－１；ＡＵＣ分别为２５．７５６±４．７００与２４．５３２±２．８２７μｇ·ｈ·Ｌ－１。国产盐酸丁螺环酮片剂对进口盐酸丁螺环酮片剂的相对生物利用度为１０４．６９％。结论：２种片剂的各项动力学参数经统计学分析无显著性差异（Ｐ＞０．０５）。

Objective: The pharmacokinetics and relative bioavailability of buspirone hydrochloride were studied in 8 male healthy volunteers after the crossover oral administration of 15 mg tablet of both domestics and imports. Methods: Plasma concentration of buspirone hydrochloride was determined by GC MS method. Results: The concentration time curves of the two kinds of tablets were fitted to the two compartment model. The t 1/2 β of domestic and imported tablets were 4.256±1.790 and 5.990±2.101 h; the T max were 0.879±0.610 and 0.559±0.263 h; the C max were 6.000±2.881 and 8.871±4.516 μg·L -1 ; the AUC were 25.756±4.700 and 24.532±2.827 μg·h·L -1 respectively.The relative bioavailability of domestic to imported tablets was 104.69%. Conclusion: There was no significant difference in pharmacokinetic parameters between the two preparations (P>0.05). The bioavailability of domestic and imported tablets of buspirone hydrochloride was equivalent in human body.