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目的:以溶液剂为参比制剂,考察镰形棘豆总黄酮有效组分软膏剂经皮给药后在大鼠体内的药代动力学过程。方法:首先建立大鼠血浆中2’4’-二羟基查尔酮(TFC,指标性成份)的HPLC法的分析方法,然后测定大鼠经皮给药后不同时间点的TFC的浓度,并用3P97对结果进行药动学拟合。结果:镰形棘豆总黄酮有效组分软膏剂和溶液剂经皮给药后TFC的药动学分别符合二室模型和一室模型,镰形棘豆软膏剂的Cmax比溶液剂提高约3倍。结论:软膏剂具有明显的缓释特征,可长时间维持稳定有效的血药浓度,且生物利用度较溶液剂显著提高,有利于发挥其经皮给药后的镇痛抗炎活性。
OBJECTIVE: To study the pharmacokinetics of the active ingredient oatmeal solution of Oxytropis ochrocephala after transdermal administration in rats by using solution as reference preparation. Methods: Firstly, the HPLC method for the determination of 2’4’-dihydroxy chalcone (TFC) in rat plasma was established. Then the concentration of TFC at different time points after transdermal administration in rats was determined and compared with 3P97 The results of pharmacokinetic fit. Results: The pharmacokinetics of TFC after oral administration of effective component ointment and solution of Oxytropis ochrocephala were in compliance with two-compartment model and one-compartment model respectively. The Cmax of Oxytropis falcate ointment was increased by about 3 Times CONCLUSION: The ointment has obvious sustained-release characteristics and can maintain a stable and effective blood concentration for a long time. The bioavailability is significantly higher than that of the solution, which is beneficial to exert its analgesic and anti-inflammatory activity after transdermal administration.