磷酸川芎嗪缓释滴丸在兔体内的药动学和相对生物利用度研究  

Study on the pharmacokinetics and relative bioavailability of tetramethylpyrazine phosphate sustained-release dropping pills in rabbits

作　　者：吴声振[1] 雷凯君[1] 霍钻云[1] 

机构地区：[1]佛山市中医院药剂科,广东佛山528000

出　　处：《广东药学院学报》2013年第3期233-236,共4页Academic Journal of Guangdong College of Pharmacy

摘　　要：目的研究磷酸川芎嗪自制缓释滴丸与市售普通片在兔体内的药动学与相对生物利用度。方法取12只新西兰兔随机分为2组,自身交叉对照、单剂量口服150 mg磷酸川芎嗪自制缓释滴丸与市售普通片,采用高效液相色谱法测定血浆中磷酸川芎嗪的浓度,应用DAS 2.1软件计算药动学参数和相对生物利用度。结果磷酸川芎嗪自制缓释滴丸与市售普通片的药动学参数t_(mat)分别为(4.17±0.41)h和(1.08±0.49)h,C_(max)分别为(3.240±0.471)mg·L^(-1)和(6.125±0.298)mg·L^(-1);AUC_(0-∞)分别为(38.549±2.408)mg·L^(-1)·h和(33.067±2.214)mg·L^(-1)·h;与市售普通片相比,缓释滴丸的相对生物利用度为(116.58±10.24)%。结论磷酸川芎嗪缓释滴丸较市售普通片t_(max)明显延长,AUC_(0-∞)较高,说明缓释滴丸能提高药物的生物利用度。Objective To study the pharmacokinetics and relative bioavailability of tetramethylpyrazine phosphate（TMPP） sustained-release dropping pills and MPP conventional tablets in rabbits. Methods Single dose of 150 mg TMPP sustained-release dropping pills or conventional tablets were orally given to 12 rabbits in a randomized crossover study. The TMPP concentration in plasma was determined by high performance liquid chromatography, and the pharmacokinetic parameters and relative bioavailability were calculated by DAS 2.1 software. Results The main pharmacokinetic parameters [or TMPP sustained-release dropping pills and conventional tablets were as follows ： tm^x （ 4.17v 0.41 ） h and （ 1.08 ± 0.49 ） h ; Cmax （3. 240±0.471） mg· L^-1and（6.125±0.298） mg· L^-1;AUC0~ （38.549 ＋2.408） mg· L^-1· h and （33. 067 ±2. 214） mg· L^-1· h;The relative bioavailability of TMPP sustained-release dropping pills to conventional tablets was （ 116.58± 10.24） %. Conclusion The pharmacokinetics of TMPP in rabbits was in accord with the two compartment models and with the first absorption after TMPP sustained-release dropping pills or conventional tablets administration. AUCo_~ and t of TMPP sustained-release dropping pills were all higher than those of conventional tablets, and TMPP sustained-release dropping pills had a higher bioavailability.

关 键 词：磷酸川芎嗪 缓释 滴丸 药动学 相对生物利用度 

分 类 号：R965[医药卫生—药理学]