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目的 研究多剂量口服盐酸氨溴索缓释胶囊的人体药代动力学和相对生物利用度。方法 选择盐酸奎宁为定量内标物 ,采用反相高效液相色谱法测定了多剂量口服 75mg盐酸氨溴索国产缓释胶囊和进口缓释胶囊在健康人体内的盐酸氨溴索血药浓度 ,以考察盐酸氨溴索缓释胶囊多剂量口服达稳态过程和稳态药代动力学特征。结果 75mg盐酸氨溴索缓释胶囊连续口服d 4起 ,体内盐酸氨溴索血药浓度基本达稳态水平。国产缓释胶囊和进口缓释胶囊的稳态药代动力学参数Tmax分别为 (4 2± 0 7)h和 (4 1± 0 8)h ,Cmax分别为 (2 0 8 73± 31 91) μg·L-1和 (2 12 5 6± 2 9 6 4) μg·L-1,Cmin分别为 30 76± 10 47μg·L-1和 (2 9 80± 10 2 3)μg·L-1,AUCss分别为 (2 113 90± 430 6 0 ) μg·h·L-1和2 0 88 2 2± 40 2 5 2 μg·h·L-1,Cav分别为 (88 0 8± 17 94) μg·L-1和 (87 0 1± 16 77) μg·L-1,DF分别为 (2 0 7± 0 31)和(2 16± 0 37) ,多剂量口服 75mg国产盐酸氨溴索缓释胶囊的相对生物利用度为 10 1 10 %± 6 33 %。结论 盐酸氨溴索国产缓释胶囊和进口缓释胶囊的主要稳态药代动力学参数差异均无显著性 ,两种制剂具有生物等效性
Objective To study the pharmacokinetics and relative bioavailability of ambroxol hydrochloride extended-release capsules with multiple doses. Methods Quinine hydrochloride was selected as quantitative internal standard and the concentration of ambroxol hydrochloride hydrochloride in the healthy volunteers was determined by reversed-phase high-performance liquid chromatography with multiple doses of oral administration of ambroxol hydrochloride 75 mg domestic sustained-release capsules and imported sustained-release capsules In order to investigate the multi-dose oral ambroxol hydrochloride sustained-release process and steady-state pharmacokinetic characteristics. Results 75 mg ambroxol hydrochloride sustained-release capsules continuously oral d 4, in vivo ambroxol hydrochloride plasma concentration reached steady state level. The steady-state pharmacokinetic parameters Tmax of domestic sustained-release capsules and imported sustained-release capsules were (42 ± 0 7) h and (41 ± 0 8) h, respectively, with Cmax of (2 0 8 73 ± 31 91) μg · L-1 and (2 12 5 6 ± 2 9 6 4) μg · L-1, respectively, and Cmin was 30 76 ± 10 47 μg · L-1 and (2980 ± 10 23) μg · L -1 , And the AUCss were (2 113 90 ± 430 6 0) μg · h · L -1 and 2 0 88 2 2 ± 40 2 5 2 μg · h · L -1, respectively, and the values of Cav were (88 0 8 ± 17 94) μg · L-1 and (87 0 1 ± 16 77) μg · L-1, DF were (207 ± 0 31) and (2 16 ± 0 37) respectively.Multiple doses of oral ambroxol hydrochloride The relative bioavailability of release capsules was 10 1% ± 6 33%. Conclusion The main steady-state pharmacokinetic parameters of ambroxol hydrochloride domestic sustained release capsules and imported sustained release capsules were not significantly different. The two preparations were bioequivalent