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目的:研究吴茱萸碱的水包油型纳米乳(evodiamine nanoemulsion,EDN)在大鼠体内的药动学特征与生物等效性。方法:本试验将12只雄性大鼠随机分成2组,分别灌胃给予吴茱萸碱(evodiamine,ED)或EDN,并于给药后0、5、15、30、45 min、1、2、5、8、12、24、48、72 h时对大鼠眼底取血,用HPLC法测定ED的血药浓度,用DAS软件分析药动学参数,并经方差分析和双单侧检验进行生物等效性评价。结果:EDN的主要药动学参数:血药浓度-时间曲线下面积(area under concentration-time curve,AUC(0~72 h))、药峰浓度(peak concentration,Cmax)和药峰时间(peak time,Tmax)分别为(3 636.79±1 642.94)μg/L*h、(192.49±37.68)μg/L和(4.94±1.67)h。EDN的大鼠口服生物利用度约为ED的4.66倍。AUC(0~72 h)的90%置信区间超出所规定的生物等效性标准区间。结论:EDN明显提高了ED的口服生物利用度。ED和EDN的生物不等效性。
Objective: To study the pharmacokinetics and bioequivalence of evodiamine nanoemulsion (EDN) in rats. Methods: Twelve male rats were randomly divided into two groups. The rats were administered intragastrically with evodiamine (ED) or EDN respectively. The rats were sacrificed at 0, 5, 15, 30, 45 min, , 8,12,24,48,72 h when the blood collected from the fundus of rats, HPLC determination of plasma concentrations of ED, the use of DAS software analysis of pharmacokinetic parameters and analysis of variance by one-sided and two-sided test of biology Validity evaluation. Results: The main pharmacokinetic parameters of EDN were: area under concentration-time curve (AUC (0 ~ 72 h)), peak concentration (Cmax) and peak time time and Tmax were (3 636.79 ± 1 642.94) μg / L * h, (192.49 ± 37.68) μg / L and (4.94 ± 1.67) h, respectively. The oral bioavailability of EDN rats was about 4.66 times that of ED. The 90% confidence interval for AUC (0-72 h) exceeded the stated bioequivalence criteria interval. Conclusion: EDN significantly improves the oral bioavailability of ED. Bioequivalence of ED and EDN.