复方二甲双胍胶囊在健康受试者体内的药物动力学和相对生物利用度

目的 研究复方二甲双胍胶囊在健康受试者体内的药物动力学和相对生物利用度。 方法 20 名男性志愿者随机交叉口服复方二甲双胍胶囊(试验药) 或合用二甲双胍片 格列本脲片(参比药), HPLC-紫外法和LC-MS 法测定人血浆中二甲双胍和格列本脲浓度, 计算药动学参数和相对生物利用度。 结果 口服试验药和参比药后二甲双胍的C_max 分别为1.87 ±0.36 和1.77 ±0.35 mg·L^-1;T_max 为1.7 ±0.6和1.8 ±0.5 h;AUC_0-∞ 为8.13 ±1.32 和8.62 ±1.47 mg·L^-1·h^-1 , 格列本脲的C_max 分别为129.2 ±51.4 和123.9 ±50.7 μg·L^-1;T_max 为2.3 ±0.7 和2.6 ±0.9 h;AUC_0-∞为0.690 ±0.228 和0.632 ±0.211 mg·L^-1 ·h^-1, 以上参数在试验药和参比药之间皆无显著性差异。试验片中二甲双胍和格列本脲相对于参比药的生物利用度分别为95.0 % ±11.5 % 和109.6 %±8.8 %。 结论 复方二甲双胍胶囊中二甲双胍和格列本脲与参比药相比皆生物等效。

Pharmacokinetics and relative bioavailability of compound metformin hydrochloride and glibenclamide capsule in healthy Chinese volunteers

AIM: To compare pharmacokinetics and relative bioavailability of metformin and glibenclamide in compound metformin hydrochloride and glibenclamide capsule (CMGC) with the reference preparations metformin tablet (MT) and glibenclamide tabet (GT). METHODS: Twenty male healthy volunteers were enrolled in a randomized two-way crossover design with a single-oral dose study.The plasma metformin and glibenclamide concentrations were determined by high performance liquid chromatography (HPLC) and liquid chromatography-mass spectrography (LC-MS), respectively.Pharmacokinetics parameters were calculated and bioequivalability was analyzed by two one-side t-test. RESULTS: The pharmacokinetics parameters of metformin in CMGC and co-administration of metformin glinbenclamide were as following, respectively:C_max (1.87 ± 0.36 and 1.77 ±0.35) mg·L ^-1;Tmax (1.7 ±0.6 and 1.8 ±0.5) h;AUC_0-∞ (8.13 ±1.32 and 8.62 ±1.47) mg·L ^-1·h ^-1, while those of glinbenclamide were as following, respectively: C_max (129.2 ±51.4 and 123.9 ±50.7) μg·L ^-1;T_max(2.3 ±0.7 and 2.6 ±0.9) h;AUC_0-∞ (0.690 ±0.228 and 0.632 ±0.211) mg·L ^-1·h ^-1.Relative bioavailability of metformin and glibenclamide in CGMC were 95.0 % ±11.5 % and 109.6 %±8.8 %, respectively. CONCLUSION: The main components of CMGC, metformin and glibenclamide, are bioequivalent to the reference tablets, MT and GT.