基于pH梯度法的盐酸普萘洛尔立方液晶纳米粒的制备  

Preparation of propranolol hydrochloride cubosomes by pH gradient method

作　　者：曾令军 陈旭 张灵娜 张佳良 宋洪涛 周欣 ZENG Lingjun;CHEN Xu;ZHANG Lingna;ZHANG Jialiang;SONG Hongtao;ZHOU Xin(Department of Pharmacy,No.900 Hospital of Joint Logistics Support Force of the PLA,Fuzhou 350025,China)

机构地区：[1]中国人民解放军联勤保障部队第九〇〇医院药剂科,福建福州350025

出　　处：《药学实践杂志》2021年第6期538-541,565,共5页Journal of Pharmaceutical Practice

基　　金：福建省自然科学基金项目(2019J01523)。

摘　　要：目的制备具有较高包封率的盐酸普萘洛尔立方液晶纳米粒(PPL-Cubs)。方法采用pH梯度法制备PPL-Cubs;以粒径、多分散指数为评价指标,优化空白立方液晶纳米粒(B-Cubs)制备的高压均质压力、高压均质次数、单油酸甘油酯用量及泊洛沙姆407用量;以包封率等为评价指标,优化外水相pH值、内水相pH值、载体/药物比、载药温度、载药时间、BCubs粒径和多分散指数、药物浓度等。结果高压均质压力为900 bar、均质次数为7次、单油酸甘油酯用量为25%、泊洛沙姆407用量为5%时,制得的B-Cubs具有较小的粒径和多分散指数。外水相pH值为8.5、内水相pH值为3.0、载体/药物比为6∶1、载药温度为20℃、载药时间为15 min、药物浓度为1%时,制得的PPL-Cubs包封率较高;B-Cubs粒径和多分散指数对制得的PPL-Cubs包封率无明显影响。结论pH梯度法能制得较高包封率的盐酸普萘洛尔立方液晶纳米粒。Objective To prepare propranolol hydrochloride loaded cubosomes(PPL-Cubs)with high entrapment efficiency.Methods PPL-Cubs was prepared by pH gradient method.Pressure and cycles of high pressure homogenization,dosage of glyceryl monooleate and poloxamer 407 were optimized to prepare blank cubosomes with particle size and polydispersity index as the indexes.The influences of various factors,including exterior pH values,internal pH values,the ratio of carrier to drug,particle size and polydispersity index of blank cubosomes,incubation temperature and time,and drug concentration on the entrapment efficiency were investigated.Results The blank cubosomes with small particle size and polydispersity index was prepared under homogenization conditions of 900 bar for 7 cycles,glyceryl monooleate dosage of 25%,and poloxamer 407 dosage of 5%.PPL-Cubs showed high entrapment efficiency with exterior pH value of 8.5,internal pH value of 3.0,ratio of carrier to drug of 6∶1,incubation temperature of 20℃,and incubation time of 15 min,and drug concentration of 1%.The particle size and polydispersity index of blank cubosomes showed no influence on entrapment efficiency.Conclusion PPL-Cubs with high entrapment efficiency could be prepared under the pH gradient method.

关 键 词：盐酸普萘洛尔 立方液晶 PH梯度法 

分 类 号：R94[医药卫生—药剂学]