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目的:建立高效液相色谱法测定血浆中茚地那韦2种制剂的浓度,并比较相对生物利用度。方法:采用反相高效液相色谱法测定18名男性健康受试者单剂量交叉口服800 mg两种茚地那韦胶囊后不同时间血浆中的药物浓度。萃取溶剂为乙腈。色谱条件:Hypersil ODS C18,流动相为乙腈∶0.01 mol.L-1磷酸盐缓冲液(pH 5.5)=43∶57。检测波长为210 nm。线性范围为0.03~16.38 mg.L-1。结果:两者药-时曲线均符合一房室模型。试验制剂和参比制剂的药动学参数如下:cmax分别为(10.6±s2.4)mg.L-1和(9.8±2.2)mg.L-1;tmax分别为(0.71±0.19)h和(0.8±0.3)h;t12ke分别为(1.30±0.24)h和(1.31±0.23)h;AUC0~10分别为(23±6)mg.h.L-1和(22±5)mg.h.L-1;AUC0~∞分别为(24±6)mg.h.L-1和(22±5)mg.h.L-1。双向单侧t检验证明,两制剂的主要药动学参数无明显差异。结论:所建立的HPLC法适用于测定人血浆中茚地那韦的浓度,试验制剂与参比制剂具有生物等效性。
OBJECTIVE: To establish a HPLC method for the determination of indinavir in plasma and to compare the relative bioavailability. Methods: The plasma concentrations of two indinavir capsules of 18 male volunteers were measured by reversed-phase high performance liquid chromatography (RP-HPLC) at different time intervals. The extraction solvent is acetonitrile. Chromatographic conditions: Hypersil ODS C18, mobile phase acetonitrile: 0.01 mol. L-1 phosphate buffer (pH 5.5) = 43:57. The detection wavelength is 210 nm. The linear range was 0.03 ~ 16.38 mg.L-1. Results: The two drug-time curves are in line with a room model. The pharmacokinetic parameters of the test and reference preparations were as follows: cmax were (10.6 ± s2.4) mg.L-1 and (9.8 ± 2.2) mg.L-1, respectively; tmax was (0.71 ± 0.19) (0.8 ± 0.3) h and (1.30 ± 0.24) h and (1.31 ± 0.23) h respectively for t12ke and (23 ± 6) mg.hL-1 and (22 ± 5) mg.hL-1 for AUC0-10 ; AUC0 ~ ∞ were (24 ± 6) mg.hL-1 and (22 ± 5) mg.hL-1, respectively. Two-way unilateral t test showed that there was no significant difference in the main pharmacokinetic parameters between the two preparations. Conclusion: The established HPLC method is suitable for the determination of indinavir in human plasma, and the bioequivalence of the test preparation with the reference preparation.