摘要
目的研究两种丁苯酞(NBP)制剂在大鼠体内的药动学特点。方法将30只Wistar大鼠随机分为6组,分别尾静脉注射高、中、低剂量NBP胶束制剂和市售参比制剂,于0~8 h间隔采血,采用UPLC-MS法测定血浆中NBP的浓度,并用DAS2. 0软件计算其药动学参数。结果给予大鼠高、中、低剂量NBP后,受试制剂和参比制剂的主要药动学参数:Cmax分别为95. 73±11. 40、44. 93±7. 55、21. 25±2. 89μg·L-1和86. 83±26. 68、58. 57±6. 34、28. 70±8. 15μg·L-1; AUC0-t分别为59. 94±7. 87、24. 43±5. 57、14. 23±1. 79μg·L-1·h和41. 37±9. 18、20. 57±3. 85、11. 25±2. 07μg·L-1·h; t1/2分别为0. 51±0. 14、0. 36±0. 13、0. 48±0. 10 h和0. 40±0. 13、0. 25±0. 08、0. 38±0. 23 h。结论高剂量给药时,NBP受试制剂与参比制剂在大鼠体内的药动学参数具有显著性差异,且受试制剂较参比制剂提高了药物的生物利用度。
OBJECTIVE To investigate the pharmacokinetics of two kinds of 3-N-Butylphthalide( NBP) formulations in rats.METHODS 30 Wistar rats were randomly divided into six groups and administrated with NBP micelle or reference formulation at high,middle and low doses,respectively. Blood samples were collected at predetermined time intervals in 0-8 h after administration,then the concentration of NBP in plasma was determined by UPLC-MS method and pharmacokinetic parameters were calculated by DAS 2. 0. RESULTS The main pharmacokinetic parameters in rats after the administration of high,middle and low doses of test and reference formulations were as follows: Cmaxwere 95. 73 ± 11. 40,44. 93 ± 7. 55,21. 25 ± 2. 89 μg·L-1 and 86. 83 ± 26. 68,58. 57 ±6. 34,28. 70 ± 8. 15 μg·L-1; AUC0-twere 59. 94 ± 7. 87,24. 43 ± 5. 57,14. 23 ± 1. 79 μg·L-1·h and 41. 37 ± 9. 18,20. 57 ± 3. 85,11. 25 ± 2. 07 μg·L-1·h; t1/2 were 0. 51 ± 0. 14,0. 36 ± 0. 13,0. 48 ± 0. 10 h and 0. 40 ± 0. 13,0. 25 ± 0. 08,0. 38 ± 0. 23 h.CONCLUSION The pharmacokinetic parameters between test and reference formulations were significantly different in high dose group and the NBP micelle had higher bioavailability than reference formulation.
作者
游蓝
李燕飞
黄凌晶
叶利明
付春梅
YOU Lan;LI Yanfei;HUANG Lingjing;YE Liming;FU Chunmei(West China School of Pharmacy,Sichuan University,Chengdu,Sichuan,610041P.R.China)
出处
《华西药学杂志》
CAS
CSCD
2018年第6期604-607,共4页
West China Journal of Pharmaceutical Sciences
