甲砜霉素肠溶胶囊在健康人体的生物等效性

Study on the bioequivalence of thiamphenicol enteric-coated micro pills capsules in healthy volunteers

目的:研究甲砜霉素(广谱抗生素)肠溶胶囊在健康人体的药动学,并评价肠溶胶囊和肠溶片的生物等效性。方法:18名男性健康志愿者随机交叉单剂量口服试验胶囊(0.25g×2)或参比片(0.25g×2)。采用HPLC-UV法测定血浆中甲砜霉素浓度。运用DAS软件计算药代参数和生物等效性评价。结果:单剂量口服0.5g甲砜霉素试验胶囊或参比片,药动学参数如下:Tmax(实测)分别为(3.8±0.49)h、(4.3±1.0)h;T1/2分别为(5.4±1.2)h、(5.7±1.9)h。Cmax分别为(4.1±1.3)mg.L-1、(3.9±1.5)mg.L-1;AUC0→t分别为(28.7±8.1)μg.h.mL-1、(30.5±10.4)μg.h.mL-1;AUC0→∞分别为(30.7±8.7)μg.h.mL-1、(33.3±11.9)μg.h.mL-1。甲砜霉素肠溶胶囊的相对生物利用度为(98.7±26.2)%。结论:受试制剂与参比制剂生物等效。

OBJECtIVE To study the pharmacokinetics of thiamphenicol enteric-coated micro pills capsules in healthy volunteers and evaluate the bioequivalence of two different preparations of thiamphenicol. METHODS Single oral dose of 0. 5 g thiamphenicol enteric-coated micro pills capsules and tablets were given to 18 volunteers in an open randomized crossover way. The concentrations of thiamphenic-ol（TAP） in plasma were determined by high-performance liquid chromatography. The pharmaco-kinetic parameters were calculated and the bioequivalence of two formulations were evaluated by DAS program. RESULTS The main pharmacokinetic parameters of test and reference preparations obtained from single oral dose were as follows： tmax were （3.8 ± 0. 5）h,（4. 3 ± 1.0）h;t1/2 were（5. 4 ± 1.2）h, （5.7 ± 1.9）h. Cmax were（4. 1 ± 1.3）mg·L^- 1, （3.9 ± 1.5）mg·L^- 1 ; AUC0→t were（28. 7± 8. 1）mg·h·L^-1 ,（30. 5 ± 10. 4）mg·h·L^-1 ;AUC0→∞ were（30. 7 ± 8.7）mg·h·L^-1 , （33. 3 ± 11.9）mg·h·L^-1. The relative bioavailability of test formulation was（98. 7 ± 26. 2） %. CONCLUSION The two preparations are bioequivalent.