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目 的：建立测定多奈哌齐血浆药物浓度的ＨＰＬＣ－ＵＶ检测法，研究国产多奈派齐胶囊在人体的药代动力学和相对生物利用度。方法：２４名健康男性志愿受试者单剂量随机交叉口服５ｍｇ国产多奈派齐胶囊和进口多奈哌齐片，采用ＨＰＬＣ法测定给药后不同时间点血浆中多奈派齐浓度，运用３Ｐ９７程序拟合房室模型，技统计矩进行药代动力学参数计算，并作方差分析和双维侧ｔ检验。结果：国产和进口多奈派齐的血药浓度－时间曲线符合二室开放模型，其主要药代动力学参数：Ｃｍаｘ分别为 １１．８５± ２．４７与１１．４８±２．８５μｇ·Ｌ－１（Ｐ＞０．０５），ｔｍаｘ分别为２．４３±０．５８与２．４６±０．５７ ｈ（Ｐ＞０．０５），ｔ１／２β分别为 ５１．５２± １４．１９与５４．５５±１４．２９ｈ（Ｐ＞０．０５）；ＡＵＣ０－１分别为４１７．９７±９０．７１和３９４．０６±９１．４０μｇ·Ｌ－１（Ｐ＞０．０５）。国产胶囊对进口片剂的相对生物利用度（Ｆ）为１０８．７４％±２１．８７％，国产多奈哌齐胶囊和进口片剂主要药代动力学参数均无显著性差异（Ｐ＞０．０５）。结论：双单侧ｔ检验结果显示国产多奈哌齐胶囊和进口多奈哌齐片生物等效。
OBJECTIVE: To establish a HPLC-UV method for the determination of donepezil plasma concentration in order to study the pharmacokinetics and relative bioavailability of Donepezil in human. Methods: Twenty-four healthy male volunteers were randomized to receive Dopitazepine 5mg and imported donepezil tablets in a single-dose randomized crossover study. The plasma concentrations of Donepine at different time points after administration were determined by HPLC, and were fitted by 3P97 program Atrioventricular model, the statistical moment of pharmacokinetic parameters calculated, and analysis of variance and two-dimensional side t-test. Results: The plasma concentration-time curves of domestic and imported doe-pieche in accordance with the two-compartment open model, the main pharmacokinetic parameters: Cmаx were 11.85 ± 2.47 and 11.48 ± 2.85μg · L -1 (P> 0.05). The tm-y values were 2.43 ± 0.58 and 2.46 ± 0.57 h respectively (P> 0.05), and the t1 / 2β values were 51.52 ± 14.19 and 54.55 ± 14.29h (P> 0.05). AUC0-1 was 417.97 ± 90.71 and 394.06 ± 91.40μg · L-1, respectively (P> 0.05). The relative bioavailability (F) of domestically made capsules to imported tablets was 108.74% ± 21.87%, and the main pharmacokinetic parameters of donepezil capsules and imported tablets showed no significant difference (P> 0.05) . Conclusion: The double unilateral t-test showed that domestic donepezil capsules and imported donepezil tablets were bioequivalent.