LC-MS/MS法测定人血浆中盐酸克林霉素胶囊血药浓度及其对人体生物等效性研究  

Study on Plasma Concentration of Clindamycin Hydrochloride Capsules and Its Bioequivalence to Human Body by LC-MS/MS

作　　者：付海申 武德龚 FU Hai-shen;WU De-gong(Kaifeng Hospital of Traditional Chinese Medicine,Kaifeng Henan 475000,China)

机构地区：[1]开封市中医院,河南开封475000

出　　处：《抗感染药学》2018年第9期1477-1480,共4页Anti-infection Pharmacy

摘　　要：目的:以健康志愿者为试验对象,考察受试制剂(T)和参比制剂(R)的药动学和人体生物等效性。方法:选取10名健康志愿者,按交叉单剂量双周期试验设计,随机单剂量口服含0.15 g克林霉素的两种制剂;以LC-MS/MS法测定各时间点的血药浓度,计算两种制剂的药动学参数和相对生物利用度,并评价其生物等效性。结果:受试制剂(T)和参比制剂(R)中克林霉素的曲线下面积(AUC_(0～t))分别为(6 994±2 607)ng/h·mL^(-1)和(8 654±3 890)ng/h·mL^(-1),消除半衰期(t1/2)分别为(2.71±0.82)h和(3.02±1.12)h,达峰时间(t_(max))分别为(0.57±0.21)h和(0.59±0.21)h,达峰浓度为cmax分别为(2 255±616)ng/mL和(2531±917)ng/mL。结论:受试制剂(T)的百分标示含量较参比制剂(R)低3.9%,受试制剂(T)的AUC_(0～t)和AUC_(0～∞)的几何均值比参比制剂(R)低15%左右,生物等效的可能性很低,需继续完善处方。Objective： To investigate the pharmacokinetics and bioequivalence of test preparation（T）and reference preparation（R） in healthy volunteers. Methods： Ten healthy volunteers were designed in a single-dose, two-cycle trial with a single oral dose of 0.15 g of clindamycin. The plasma concentrations at each time point were determined by LC- MS/MS method, and the pharmacokinetic parameters and relative bioavaitability of the two preparations were calculat- ed, and the bioequivalence was evaluated. Results： The AUC0-t of the test preparation （T） and the reference preparation （R） ofclindamycin were （6 994±2607） ng/h·mL^-1 and （8 654±3 890） ng/h·mL^-1, respectively, and the elimination half- life t1/2 is （2.71±0.82） h and （3.02±1.12） h, and the peak time tmax is （0.57±0.21） h and （0.59±0.21） h, respectively, and thc peak concentration cmax, is （2 255±616） ng/mL and （2 531±917） ng/mL Conclusion： The percentage of the test prepara- tion is 3.9% lower than that of the reference preparation. The geometric mean ofAUC., and AUC. , of the test prepara- tion is about 15% less than that of the reference preparation, and the possibility of bioequivalence is very low and need to continue to improve the prescription.

关 键 词：受试制剂 参比制剂 克林霉素胶囊 生物等效 生物利用度 药动学 

分 类 号：R969.3[医药卫生—药理学]