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目的:建立测定大鼠血浆中九里香叶总黄酮浓度的高效液相色谱法,并考察九里香叶总黄酮及其羟丙基-β-环糊精包合物在大鼠体内的药物动力学行为。方法:将大鼠分别灌胃给予九里香叶总黄酮及其包合物,剂量为200 mg·kg~(-1)。于不同时间点采血,检测药物主要成分5,7,3,4,四甲氧基黄酮(JA)和5,7,3,4,5,五甲氧基黄酮(JB)的浓度。采用DAS2.1.1软件计算药动学参数。结果:原药和包合物在体内的经时过程符合二室模型。包合后JA的生物利用度为原药的5.30倍,C_(MAX)为原药的3.42倍;JB的生物利用度为原药的4.96倍,C_(max)为原药的2.93倍。结论:九里香叶总黄酮经羟丙基-β-环糊精包合后,可以显著提高在大鼠体内的生物利用度。
OBJECTIVE: To establish a HPLC method for the determination of total flavonoids in JiLingXiang leaves in rat plasma, and to investigate the pharmacokinetics of the total flavonoids in JiLuxiang leaves and its hydroxypropyl-β-cyclodextrin inclusion complex in rats behavior. Methods: The rats were gavage given total flavonoids and its inclusion compound Jiulai, a dose of 200 mg · kg ~ (-1). Blood samples were taken at different time points and the concentrations of 5,7,3,4, tetramethoxyflavone (JA) and 5,7,3,4,5 and pentamethoxyflavone (JB) were detected. Pharmacokinetic parameters were calculated using DAS2.1.1 software. Results: The time course of the original drug and inclusion complex in the body conformed to the two-compartment model. The bioavailability of JA was 5.30 times that of the original drug and C_ (MAX) was 3.42 times of the original drug. The bioavailability of JB was 4.96 times that of the original drug, and the maximum value of C_ (max) was 2.93 times of the original drug. CONCLUSION: The total flavonoids of Grifola frondosa can be significantly increased in vivo after being encapsulated by hydroxypropyl-β-cyclodextrin.