高效液相色谱法测定吉非贝齐的人体药动学和相对生物利用度

目的:建立高效液相色谱(HPLC)法测定血浆中吉非贝齐浓度,并研究其药动学及相对生物利用度。方法:20名受试者随机分成2组,先后单剂量口服受试制剂或参比制剂后,采用HPLC法测定血药浓度,计算药动学参数并进行方差分析,以双单侧t检验进行生物等效性判定。结果:单次服用600mg受试制剂或参比制剂后的药动学参数AUC0～10,AUC0～∞,cmax,tmax及t1/2分别为(93±s17)和(93±18)mg·h·L-1,(95±17)和(96±19)mg·h·L-1,(31±8)和(31±8)mg·L-1,(1.6±0.4)和(1.5±0.5),(2.0±0.4)和(1.8±0.6)h。受试制剂对参比制剂的相对生物利用度为(100±11)%。2种制剂的药动学参数无明显差异。结论:HPLC法能快速、准确的测定人血浆中的吉非贝齐浓度,受试制剂与参比制剂具有生物等效性。

Pharmacokinetics and relative bioavailability of gemfibrozil by HPLC determined in human being

AIM: To determine gemfibrozil in human plasma by HPLC method, and study its pharmacokinetics and relative bioavailability. METHODS: Twenty volunteers were randomly divided into 2 groups. Group Ⅰ first received the trial preparation gemfibrozil capsules, and then followed by the reference preparation, while Group Ⅱ received the reference preparation first, and followed by the trial preparation. Plasma concentration of gemfibrozil was measured by high performance liquid chromatography (HPLC) method. ANOVA was used to check the difference of the means of the pharmacokinetic parameters between the two preparations. Bioequivalence was determined by two one-sided t-tests. RESULTS: The pharmacokinetic parameters, AUC 0-10, AUC 0-∞, c max, t max and t 1/2 of the volunteers after taking a single dose of 600 mg of the trial preparation or the comparison preparation were (93±17) and (93±18) mg·h·L -1, (95±17) and (96±19) mg·h·L -1, (31±8) and (31±8) mg·L -1, (1.6±0.4) and (1.5± 0.5) h, respectively. The relative bioavailability was(100±11)%. No significant differences were found among the main pharmacokinetic parameters after the ANOVA. CONCLUSION: The methods can determine gemflbrozil concentration in the human plasma quickly and correctly. The two preparations were equivalent.