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目的:优选甘草黄酮纳米结晶的制备工艺并对所得纳晶进行初步评价。方法:以超声辅助-反溶剂沉淀法制备纳米混悬液,采用正交试验L9(34),考察药物浓度、药物与表面活性剂的质量比、注入速度、超声时间对纳晶粒径及其分布的影响,并进一步优选稳定剂及冻干保护剂;比较所得纳晶与原药的平衡溶解度和体外溶出度。结果:最优处方工艺为:药物浓度20 mg·mL~(-1),稳定剂为10 mg·mL~(-1) SDS、5 mg·mL~(-1)PEG-400、0.2%PVA,注入速度0.5 mL·min-1,超声7 min,加入5%乳糖作为冻干保护剂;此条件下制得纳晶冻干前后粒径分别为(61.70±1.40)nm和(108.9±1.67)nm,呈电中性、粒径较均匀;冻干粉载药量31.04%,原料药和纳晶在pH6.8 PBS中的溶解度分别为3.41 mg·mL~(-1)和7.37 mg·mL~(-1),2 min时溶出率为8.33%和55.91%。结论:该纳米结晶制备工艺简便易行,可显著改善甘草黄酮的溶解度和溶出度。
Objective: To optimize the preparation of licorice flavonoids nanocrystals and make a preliminary evaluation of the obtained nanocrystals. Methods: Nanosuspension was prepared by ultrasonic assisted-anti-solvent precipitation method. The orthogonal experiment L9 (34) was used to investigate the effect of drug concentration, mass ratio of drug to surfactant, injection speed and ultrasonic time on the nanocrystalline particle size and its Distribution and further optimization of stabilizer and lyoprotectant; balance between the obtained crystal and the original drug solubility and dissolution in vitro. Results: The optimal prescription was as follows: drug concentration 20 mg · mL -1, stabilizer 10 mg · mL -1 SDS, 5 mg · mL -1 PEG-400, 0.2% PVA (61.70 ± 1.40) nm and (108.9 ± 1.67) nm, respectively, before and after freeze-drying under the conditions of injection speed of 0.5 mL · min-1 and sonication for 7 min and 5% lactose as the lyoprotectant. nm. The solubility of the drug substance and nanocrystal in pH6.8 PBS were 3.41 mg · mL -1 and 7.37 mg · mL -1, respectively. ~ (-1), the dissolution rate was 8.33% and 55.91% at 2 min. Conclusion: The nanocrystal preparation process is simple and easy, can significantly improve the solubility and dissolution of licorice flavonoids.