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目的建立HPLC同时测定大鼠血浆中柚皮苷和新橙皮苷含量的方法,研究玳玳黄酮自微乳化微丸在大鼠体内的药物动力学和相对生物利用度。方法将随机分组的大鼠分别灌胃给药玳玳黄酮自微乳化微丸液及玳玳黄酮有效部位混悬液,剂量120 mg·kg-1(按玳玳总黄酮含量计),分别于0.083,0.167,0.333,0.5,0.667,1,2、4、6、8、10、12和24 h取血。采用HPLC同时测定血浆样品中柚皮苷和新橙皮苷的浓度,运用DAS 3.0药动学程序计算药动学参数。结果比较口服玳玳黄酮自微乳化微丸及玳玳黄酮有效部位混悬液的药动学参数,柚皮苷AUC0-24分别为(17.710±6.588)和(9.139±1.982)mg.h.L-1,ρmax分别为(4.816±1.329)和(1.575±0.324)mg.L-1,tmax分别为(0.611±0.086)和(0.917±0.204)h,t1/2分别为(13.078±6.382)和(11.678±6.919)h,新橙皮苷AUC0-24分别为(18.094±4.892)和(10.961±2.276)mg.h.L-1,ρmax分别为(5.657±1.391)和(2.096±0.512)mg.L-1,tmax分别为(0.583±0.091)和(0.806±0.222)h,t1/2分别为(14.606±7.562)和(10.985±6.963)h。以玳玳黄酮有效部位混悬液为参比,玳玳黄酮自微乳化微丸中柚皮苷和新橙皮苷的相对生物利用度分别为193.78%和165.08%。结论玳玳黄酮研制成玳玳黄酮自微乳化微丸制剂能提高其口服生物利用度和改善其药剂学性质。
OBJECTIVE To establish a method for the simultaneous determination of naringin and neohesperidin in rat plasma by HPLC and to study the pharmacokinetics and relative bioavailability of tortoise-warfarin microemulsified pellets in rats. Methods Randomly divided rats were intragastrically administered with emamectin and microemulsion of toe warfarin and the effective suspension of toparagine, at a dose of 120 mg · kg -1 (according to the total flavonoids of toadstool) 0.067, 0.333, 0.5, 0.667, 1, 2, 4, 6, 8, 10, 12 and 24 h. Plasma concentrations of naringin and neohesperidin in plasma samples were simultaneously determined by HPLC. Pharmacokinetic parameters were calculated using the DAS 3.0 pharmacokinetic program. Results The pharmacokinetic parameters of the eustachinoside AUC0-24 were (17.710 ± 6.588) and (9.139 ± 1.982) mg.hL-1, respectively (ρmax) were (4.816 ± 1.329) and (1.575 ± 0.324) mg.L-1 respectively, the tmax were (0.611 ± 0.086) and (0.917 ± 0.204) h respectively, and t1 / 2 were (13.078 ± 6.382) and ± 6.919) h, the values of AUC0-24 were (18.094 ± 4.892) and (10.961 ± 2.276) mg.hL-1, respectively, and the ρmax were (5.657 ± 1.391) and (2.096 ± 0.512) mg.L- , tmax were (0.583 ± 0.091) and (0.806 ± 0.222) h respectively, and t1 / 2 were (14.606 ± 7.562) and (10.985 ± 6.963) h, respectively. The relative bioavailability of naringin and neohesperidin in the test group was 193.78% and 165.08% respectively. Conclusion The study of the tortoise shell flavone made into the tortoise shell flavone self-microemulsifying pellet preparation can improve its oral bioavailability and improve its pharmacy properties.