健康人口服国产洛美沙星片剂的药代动力学

The study of pharmacokinetics and bioavailability of lomefoxacin in normal volunteers

１２名健康男性志愿者，平均年龄２０ａ，分别交叉口服日本产胶囊和国产片剂盐酸洛美沙星３００ｍｇ。用微生物法测定服药后不同时间点取样的血、尿标本，进行药代动力学和相对生物利用度研究。结果表明：口服两药后均能迅速吸收，达峰时间（Ｔｍａｘ）分别为１．１２±０．２８和１．０８±０．５１ｈ；峰浓度（Ｃｍａｘ）为１．５３±０．５３和１．４９±０．３７ｍｇ·Ｌ－１，消除半衰期（Ｔ１／２β）为９．９２±２．４０和１０．４１±２．１７ｈ；二者的药时曲线下面积（ＡＵＣ）分别为１２．９７±２．８９和１１．８０±２．４８ｍｇ·Ｌ－１·ｈ，国产片剂对日本产胶囊洛美沙星的相对生物利用度为９２．５６±１６．１８％。

The clinical pharmacokinetics and the relative bioavailability of lomefloxacin were studied in 12 normal male volunteers with randomised crossover oral dose 300 mg capsule made in Japan and tablet made in China respectively.The blood and urine samples were taken at various time point after administration and measured by microbiological assay.Lomefloxacin capsule and tablet were rapidly absorbed.The serum concentration-time curves appeared two-compartment open model.The results showed that lag time were 0.17±0.12 and 0.15±0.08 h;Tmax 1.12±0.28 and 1.08±0.51h;Cmax 1.52±0.53 and 1.49±0.37 mg·L-1;T1/2β9.92±2.40 and 10.41±2.17 h;AUC 12.97±2.89and 11.80±2.48 mg·L-1·h-1.The relative bioavailability of lomefloxacin tablet made in China to capsule made in Japan is 92.56%±16.81%.This experiment suggested that the pharmacokinetics and bioavailability of lomefloxacin showed no difference between tablet made in China and capsule made in Japan.