【摘要】 目的研究葛根总黄酮(TPF)生物黏附性缓释片和普通片在家犬体内的药动学与生物利用度,揭示葛根总黄酮生物黏附性缓释片在家犬体内的药动学变化规律,为临床合理运用该药提供实验依据。方法健康家犬6只,以自身前后交叉对照方式,单剂量分别给予葛根总黄酮生物黏附性缓释片和普通片600mg。葛根素血药浓度经时数据以3P87药动学程序处理,以对两种片剂在家犬体内的动态过程进行拟合。以非室模型统计矩方法,计算药时曲线下面积(AUC0→12),并由血药浓度数据读取Cmax,tmax,经统计分析比较普通片与缓释片的生物利用度。结果单剂量给予家犬TPF片及生物黏附片后,葛根素血药浓度变化符合一级吸收一室模型,Ke分别为(0.461±0.115)h-1,(0.238±0.042)h-1;Ka分别为(0.844±0.404)h-1,(0.446±0.100)h-1;t1/2ka分别为(0.954±0.352)h,(1.609±0.292)h,t1/2ke分别为(1.570±0.333)h,(2.995±0.617)h。普通片的AUC0-12,Cmax,tmax分别为(4430±998)ng·h·mL-1,(1241±247)ng·mL-1和(2.2±0.6)h。缓释片的AUC0→12,Cmax和tmax分别为(6459±738)ng·h·mL-1,(1040±134)ng·mL-1和(4.0±0.7)h。以普通片为参比制剂,缓释片的生物利用度为(151.4±37.6)%。结论葛根总黄酮缓释片在家犬体内表现出较好的缓释特性,主要药动学参数发?更多还原

【Abstract】 OBJECTIVE To study the pharmacokinetics and bioavailability of total puerariae flavones(TPF) bioadhesive sustained-release tablets in dogs. METHODS Blood samples were obtained at 0, 0.25, 1.0, 1.5, 2.0, 3.0, 4.0, 7.0, 9.0, 12 h after a single dose of 600 mg TPF tablets and TPF bioadhesive sustained-release of tablets. puerarin concentration was determined by HPLC. The pharmacokinetics of puerarin were analyzed by 3P87 program. RESULTS The concentration-time profile in dog plasma was discribed with a two-compartment model.The main pharmacokinetic parameters of puerarin in TPF tablets and TPF bioadhesive sustained-release of tablets were: Ke were (0.461 ±0.115)h-1 and (0.238 ± 0. 042)h-1 ,Ka were (0.844±0.404)h-1 and (0.446 ± 0.100) h-1, t1/2ka were (0.954 ± 0.352)h and (1.609±0.292) h, t1/2ke were (1.570±0.333)h and (2.995 ±0.617) h, respectively. AUC0→12, cmax and tmax were (4430±998) ng·h· mL-1,(1 241±247) ng·mL-1 ,(2.2±0.6) h and (6 459 ± 738) ng·h· mL--1 ,(1 040± 134) ng·mL-1,(3.40±0.7) h, respectively. The relative bioavailability of puerarin in PTF bioadhesive sustained-release of tablet were (151.4 ± 37.6) % compared with TPF tablets. CONCLUSION TPF bioadhesive sustained-release tablet was characterized with sustained-releasing profile, and the main pharmacokinetic parameters of puerarin in TPF bioadhesive sustained-release tablet were different from TPF tablet. The relative bioavaialability of puerarin in PTF bioadhesive sustained-release tablet was higher than that of TPF tablet.更多还原