CAJ | 학술논문

目的采用单剂量交叉实验设计,考察30名健康受试者口服维 A 酸软胶囊受试制剂及其参比制剂20 mg 后的生物等效性研究.方法建立 LC-MS/MS 法测定血浆中维 A 酸的浓度.采用 C18柱,阿维 A 酸为内标,以多反应监测(MRM)模式监测.结果两种制剂的 Cmax、Tmax、AUC0→10和 AUC0→∞(均数±标准差)分别为:(142.52±34.09)和(141.75±31.64)ng·mL-1;(2.1±0.3)和(2.05±0.36)h;(352.67±121.78)和(343.95±100.70) ng·h·mL-1;(353.91±120.71)和(345.67±98.96)ng·h·mL-1.试验制剂对参比药物的相对生物利用度 F 为(101.6%±18.5%);校正后维 A 酸的主要药代动力学参数 Cmax、Tmax、AUC0→10和 AUC0→∞(均数±标准差)分别为:(141.59±34.09)和(140.79±31.64)ng·mL-1;(2.07±0.29)和(2.05±0.36)h;(343.19±121.56)和(334.11±100.32)ng·h·mL-1;(344.11±121.58)和(335.09±100.26)ng·h·mL-1.结论试验药物对参比药物的相对生物利用度 F 为(101.7%±19.1%)(以 AUC0→10作为评价依据),两者具有生物等效性.
목적채용단제량교차실험설계,고찰30명건강수시자구복유 A 산연효낭수시제제급기삼비제제20 mg 후적생물등효성연구.방법건립 LC-MS/MS 법측정혈장중유 A 산적농도.채용 C18주,아유 A 산위내표,이다반응감측(MRM)모식감측.결과량충제제적 Cmax、Tmax、AUC0→10화 AUC0→∞(균수±표준차)분별위:(142.52±34.09)화(141.75±31.64)ng·mL-1;(2.1±0.3)화(2.05±0.36)h;(352.67±121.78)화(343.95±100.70) ng·h·mL-1;(353.91±120.71)화(345.67±98.96)ng·h·mL-1.시험제제대삼비약물적상대생물이용도 F 위(101.6%±18.5%);교정후유 A 산적주요약대동역학삼수 Cmax、Tmax、AUC0→10화 AUC0→∞(균수±표준차)분별위:(141.59±34.09)화(140.79±31.64)ng·mL-1;(2.07±0.29)화(2.05±0.36)h;(343.19±121.56)화(334.11±100.32)ng·h·mL-1;(344.11±121.58)화(335.09±100.26)ng·h·mL-1.결론시험약물대삼비약물적상대생물이용도 F 위(101.7%±19.1%)(이 AUC0→10작위평개의거),량자구유생물등효성.
@@@@Objective The pharmacokinetics of tretinoin test and reference soft capsules which were orally administrated by 30 healthy volunteers was investigated. Methods A LC-MS/MS method was established for the determination of tretinoin in plasma. A C18 column was used with acitretin as the internal standard. The analytes were detected in the positive ion mode and multiple reactions monitoring (MRM). Results The Cmax, Tmax, AUC0→10 and AUC0→∞ (average ± SD) of test capsules and reference capsules were 142.52±34.09 ng·mL-1 and 141.75±31.64 ng·mL-1, 2.1±0.3 h and 2.05±0.36 h, 352.67± 121.78 ng·h·mL-1 and 343.95±100.70 ng·h·mL-1, 353.91±120.71 ng·h·mL-1 and 345.67±98.96 ng·h·mL-1, respectively. The relative bioavailability of tretinoin soft capsules was 101.6%±18.5%. The Cmax, Tmax, AUC0→10 and AUC0→∞ (aver-age±SD) of test capsules and reference capsules after baseline being corrected were 141.59±34.09 ng·mL-1 and 140.79± 31.64 ng·mL-1, 2.07±0.29 h and 2.05±0.36 h, 343.19±121.56 ng·h·mL-1 and 334.11±100.32 ng·h·mL-1, 344.11±121.58 ng·h·mL-1 and 335.09±100.26 ng·h·mL-1, respectively. Conclusion The relative bioavailability of tretinoin soft capsules was 101.7%±19.1%. No significant difference was observed in the rate and degree of absorption, which indicated that the two preparations were bioequivalent.