米格列奈片在健康人体内的药动学和生物等效性评价

Pharmacokinetics and bioequivalence study of mitiglinide tablets in healthy volunteers by LC-MS/MS method

目的评价米格列奈片在健康人体内的生物等效性。方法 24名健康成年男性志愿者采用随机分组自身交叉对照试验设计,单剂量口服10 mg米格列奈片后,用LC-MS/MS法测定血浆中药物浓度。结果米格列奈片和米格列奈钙片的主要药动学参数:t1/2(1.69±0.16)和(1.65±0.28)h;tmax[0.25(0.17~0.5)]和[0.33(0.25~1.50)]h;ρmax(1 165.1±357.50)和(1 081.0±338.41)μg·L^(-1);AUC_(0→τ)(1 489.6±336.85)和(1 378.3±309.56)μg·h·L^(-1);AUC0→∞(1 497.2±339.73)和(1 386.1±311.58)μg·h·L^(-1);AUC_(0→12h)/AUC_(0→∞)(99.51±0.16)%和(99.44±0.24)%;以AUC_(0→12h)计算受试制剂的相对生物利用度为(108.6±10.9)%。结论 2种米格列奈制剂生物等效。

AIM To evaluate the bioequivalence of two kinds of mitiglinide preparations in healthy volunteers. METHODS A total of 20 healthy male volunteers were enrolled in a randomized crossover study in which the subjects were randomly assigned to receive single oral dose of 10 mg mitiglinide tablets. The plasma concentrations of mitiglinide were determined by LC-MS/MS. RESULTS The main pharmacokinetic parameters of test and reference preparations were as follows ： t1/2（1.69±0.16） and （1.65±0.28）h;tmax[0.25（0.17～0.5）] and [0.33（0.25～1.50）]h;ρmax（1165.1±357.50） and （1081.0±338.41）μg·L-1;AUC0→τ,（1489.6±336.85） and （1378.3±309.56）μg·h·L-1;AUC0→∞（1497.2±339.73） and （1386.1±311.58）μg·h·L-1;AUC0→12h/AUC0→∞（99.51±0.16）% and （99.44±0.24）%;The relative bioavailability of mitiglinide tables to reference preparation was （108.6±10.9）%. CONCLUSION Test preparation and reference preparation of mitiglinide are bioequivalent.