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目的:研究大黄素固体脂质纳米粒在大鼠体内的药动学。方法:采用乳化蒸发-低温固化法制备大黄素固体脂质纳米粒,将12只SD大鼠,随机分成对照组和试验组,分别注射10 mg·kg~(-1)大黄素溶液和10 mg·kg~(-1)大黄素固体脂质纳米粒混悬液。HPLC法测定大鼠血浆中大黄素的浓度,3P97程序计算药动学参数。结果:大黄素固体脂质纳米粒消除速率较慢,其消除速率仅为大黄素溶液的0.533倍,生物利用度为大黄素溶液的1.874倍,半衰期为大黄素溶液的1.484倍,药物溶液和纳米混悬液在大鼠体内的药动学过程均符合二室模型。结论:与大黄素溶液相比,大黄素固体脂质纳米粒具有明显的缓释效果,同时提高了药物的生物利用度。
Objective: To study the pharmacokinetics of emodin solid lipid nanoparticles in rats. Methods: Emodin solid lipid nanoparticles were prepared by emulsion evaporation and low temperature solidification. Twelve SD rats were randomly divided into control group and experimental group. Erythromycin 10 mg / kg and 10 mg / · Kg ~ (-1) emodin solid lipid nanoparticles suspension. HPLC method for the determination of rat plasma emodin concentration, 3P97 program calculated pharmacokinetic parameters. Results: The elimination rate of emodin solid lipid nanoparticles was slower than that of emodin, its eradication rate was only 0.533 times that of emodin, its bioavailability was 1.874 times that of emodin, and its half-life was 1.484 times of that of emodin. The drug solution and nano- The pharmacokinetics of the suspension in rats are in accordance with the two-compartment model. Conclusion: Compared with emodin solution, emodin solid lipid nanoparticles have obvious sustained release effect and meanwhile improve the bioavailability of drug.