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在中国男性健康自愿者体内进行了国产盐酸纳曲酮片剂与进口盐酸纳曲酮片剂的相对生物利用度试验。１０名健康自愿者随机自身交叉服用５０ｍｇ国产盐酸纳曲酮片和进口盐酸纳曲酮片，应用高效液相色谱－电化学检测器测定盐酸纳曲酮及其主要代谢产物纳曲醇的血浆浓度。盐酸纳曲酮两种片剂在健康人体内的血药浓度－时间过程符合一级吸收二室模型。国产盐酸纳曲酮片剂的药代动力学参数分别为：Ｔ１／２β２．９７±０．６１ｈ，Ｔｐｅａｋ０．８１±０．０９ｈ，Ｃｍａｘ１７．２±２．６μｇ／Ｌ，ＡＵＣ６４．７±９．４μｇ．ｈ·Ｌ－１。进口盐酸纳曲酮片的药代动力学参数分别为：Ｔ１／２β３．３４±１．４９ｈ，Ｔｐｅａｋ１．０９±０．２５ｈ，Ｃｍａｘ１６．６±１．６μｇ·Ｌ－１，ＡＵＣ６６．２±８．４μｇ·ｈ·Ｌ－１。除了Ｔｐｅａｋ和Ｔ１／２α国产片稍快于进口片外，两种片剂的Ｔ１／２β、Ｃｍａｘ、ＡＵＣ等主要药代动力学参数之间经统计学检验均无显著性差异（Ｐ＞０．０５），国产与进口盐酸纳曲酮片剂的相对生物利用度为９８．６±１４％。口服国产和进口两种盐酸纳曲酮片剂后，血浆中主要代谢产物纳曲醇的药代动力学参数无显著性差异，Ｔ１／２β分别为９．９±１．８和７．６±?
The relative bioavailability of domestic naltrexone hydrochloride tablets and imported naltrexone hydrochloride tablets was tested in Chinese male health volunteers. Ten healthy volunteers were randomized to cross themselves with 50mg naltrexone hydrochloride tablets and imported naltrexone hydrochloride tablets. The plasma concentrations of naltrexone hydrochloride and its major metabolite naltrexol were determined by high performance liquid chromatography-electrochemical detector . Naltrexone hydrochloride tablets in healthy human blood concentration-time course in line with the absorption of two-compartment model. The pharmacokinetic parameters of domestic naltrexone hydrochloride tablets were: T1 / 2β2.97 ± 0.61h, Tpeak0.81 ± 0.09h, Cmax17.2 ± 2.6μg / L, AUC64.7 ± 9. 4 μg. h · L-1. The pharmacokinetic parameters of naltrexone hydrochloride tablets were T1 / 2β3.34 ± 1.49h, Tpeak1.09 ± 0.25h, Cmax16.6 ± 1.6μg · L-1, AUC66.2 ± 8 .4 μg · h · L-1. There was no significant difference in the main pharmacokinetic parameters of T1 / 2β, Cmax, AUC among the two tablets except the Tpeak and T1 / 2α domestic films were slightly higher than the imported ones (P> 0. 05). The relative bioavailability of domestic and imported naltrexone hydrochloride tablets was 98.6 ± 14%. After oral administration of naltrexone hydrochloride tablets, the pharmacokinetic parameters of naltrexol, a major metabolite in plasma, showed no significant difference. The T1 / 2β were 9.9 ± 1.8 and 7.6 ± ?