基于环糊精包合技术提高冻干制剂中薄荷挥发油综合保留率研究  

Improving comprehensive retention rate of peppermint oil in freeze-dried preparation based on cyclodextrin inclusion technology

作　　者：石秀佳 程亚茹 龚燚婷 许铭珊 杨丽[1] 戴俊东[1] 董玲[1] SHI Xiu-jia;CHENG Ya-ru;GONG Yi-ting;XU Ming-shan;YANG Li;DAI Jun-dong;DONG Ling(School of Chinese Materia Medica,Beijing University of Chinese Medicine,Beijing 100029,China;School of Life Sciences,Beijing University of Chinese Medicine,Beijing 100029,China)

机构地区：[1]北京中医药大学中药学院,北京100029 [2]北京中医药大学生命科学学院,北京100029

出　　处：《中国中药杂志》2021年第22期5819-5824,共6页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81073056)。

摘　　要：冻干技术具有低温保留活性、吸收迅速等突出优势,尤其适用于挥发油等热不稳定药物。然而目前针对冻干制剂过程对于中药挥发油应用可行性研究较少。该研究拟利用冻干载体,以薄荷挥发油为代表,评价几种不同加入方式(吸附、乳化、固体分散、包合)对主要成分保留率的影响,从而探讨挥发油冻干制剂的应用可行性。首先通过比较不同冻干制剂中薄荷醇冻干保留率,确定薄荷挥发油加入方式;然后结合优选加入方式特点设计正交实验优选制剂工艺。结果表明,挥发油最佳冻干制剂形式为环糊精包合技术,薄荷醇冻干保留率达86.36%。根据挥发油经包合、冻干两步制剂成型过程,引入包合率、冻干保留率二者乘积——“综合保留率”这一指标设计正交实验考察所得薄荷油β-环糊精(beta-cyclodextrin,β-CD)包合物的最佳制备工艺为β-CD、油配比7∶1,包合温度40℃,包合时间2 h,由此工艺制得包合物为白色疏松粉末,综合保留率为68.41%,冻干保留率达92.53%,挥发油包合率达73.93%,溶解度显著增加。该研究所选取的薄荷油环糊精包合制备工艺稳定可靠,为挥发性成分在冻干制剂中的有效性与稳定性应用提供了一种新的思路和方法。The freeze-drying technique,characterized by low-temperature processing,is especially suitable for sensitive volatile oils with thermal instability.However,there are few studies focusing on the retention of volatile oils in the processing of freeze-dried preparations.This study evaluated the effects of different addition methods(adsorption,emulsification,solid dispersion,and inclusion)on the retention rate of the main components in peppermint oil,aiming to explore the application feasibility of freeze-dried preparations of volatile oils.Firstly,the addition method was determined based on the retention rates of menthol in four freeze-dried preparations.Secondly,an orthogonal test was designed to optimize the preparation process based on the characteristics of the preferred addition method.The results showed that the most suitable preparation form of peppermint oil was inclusion with beta-cyclodextrin(β-CD),and the retention rate of menthol in freeze-drying was 86.36%.According to the two-step preparation process of inclusion and freeze-drying,we introduced the product of inclusion rate and retention rate,i.e.,comprehensive retention rate,to determine the optimum processing parameters.The results showed thatβ-CD/oil ratio of 7∶1,inclusion temperature of 40℃,and inclusion time of 2 h were the optimum processing parameters.The product prepared with these parameter had the comprehensive retention rate of 68.41%,retention rate of 92.53%,and inclusion rate of 73.93%.The inclusion compound was white powder with significantly increased solubility.The pre-paration process based on cyclodextrin inclusion in this study is stable and reliable and provides a new idea for ensuring the efficacy and stability of volatile components in freeze-dried preparations.

关 键 词：薄荷挥发油 Β-环糊精 冻干制剂 综合保留率 

分 类 号：R283[医药卫生—中药学]