国产盐酸西替利嗪片的人体药代动力学及相对生物利用度

Pharmacokinetics and relative bioavailability of domestic cetirizine hydrochloride tablet in healthy volunteers

目的 :研究国产盐酸西替利嗪片的人体药代动力学和相对生物利用度。 方法 :选择 8名男性健康志愿者 ,采用反相高效液相色谱法 ,以紫外 2 2 9nm为检测波长 ,测定了单剂量 (10 mg)口服国产盐酸西替利嗪片和进口盐酸西替利嗪片在人体内的西替利嗪浓度。 结果 :盐酸西替利嗪的体内动态过程呈一级吸收的二房室开放模型 ,国产片和进口片的 cmax分别为(316 .71± 39.6 6 )和 (314.80± 31.79) ng/ ml,tmax分别为 (0 .72± 0 .0 9)和 (0 .72± 0 .0 9) h,t1 /2β分别为 (10 .71± 3.0 6 )和(9.95± 2 .41) h,AU C0～∞ 分别为 (2 72 8.5 2± 35 6 .0 6 )和 (2 75 3.0 1± 36 0 .33) ng· h/ ml。结论 :国产盐酸西替利嗪片剂的相对生物利用度为 (99.5 0± 8.89) % ;选择 cmax和 AU C0～∞ 进行三因素方差分析与双单侧 t检验 ,结果表明国产片和进口片两种制剂具有生物等效性。

Objective: To study the pharmacokinetics and relative bioavailability of domestic cetirizine hydrochloride tablet in healthy volunteers. Methods: A reversed phase high performance liquid chromatography (RP HPLC )method was used for the determination of cetirizine in plasma after a single oral dose of 10 mg domestic cetirizine hydrochloride tablet and imported cetirizine hydrochloride (Zyrtec)tablet in a crossover design. The detector was operated at UV 229 nm. Results: The dynamic course of cetirizine plasma concentrations conformed to a two compartment open model and the pharmacokinetic parameters after a single oral dose of 10 mg domestic tablet and Zyrtec tablet were as follows: c max were (316.71±39.66) and (314.80±31.79) ng/ml, t max were(0.72±0.09) and (0.72±0.09) h, t 1/2β were (10.71±3.06) and (9.95±2 41) h, AUC 0～∞ were (2 728.52±356.06) and (2 753.01±360.33)ng·h/ml, respectively.Conclusion: The relative bioavailability of domestic cetirizine hydrochloride tablet is(99.50±8.89)%. The results of statistical analysis for c max and AUC 0～∞ show that domestic cetirizine hydrochloride tablet and imported Zyrtec tablet are bioequivalent.