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[葛根素-川芎油亚微乳联合用药与佐剂]

[Puerarin-Chuanxiong oil submicron emulsion combining medicine and adjuvant].

作者信息

Fan Xiao-Yu, Zhang Yi, Huang Jia-Yi, Hong Ting-Ting, Bi Jia-Yao, Yang Qi-Lin, DU Shou-Ying, Li Peng-Yue

机构信息

School of Chinese Materia Medica, Beijing University of Chinese Medicine Beijing 102488, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2021 Sep;46(17):4410-4416. doi: 10.19540/j.cnki.cjcmm.20210412.303.

Abstract

This study was mainly based on the compatibility of Puerariae Lobatae Radix and Chuanxiong Rhizoma to prepare submicron emulsion and evaluated its physical and pharmaceutical properties. Firstly, pseudo-ternary phase diagrams were drawn by dripping method which took Chuanxiong oil as the oil phase and the area of microemulsion region as the index. On this basis, suitable emulsifier and co-emulsifier were screened for the preparation of Chuanxiong oil submicron emulsion. Then, the formula realizing the largest oil loading was selected. Finally, puerarin substituted part of emulsifier and co-emulsifier to lower their content, so as to form puerarin-Chuanxiong oil submicron emulsion featuring the combination of medicine and adjuvant. Its particle size, zeta potential, centrifugal stability and storage stability were determined, and the in vitro drug release behavior was investigated by dialysis bag method, based on which the quality of the as-prepared submicron emulsion was evaluated comprehensively. The proposed method was proved feasible for the preparation of Chuanxiong oil submicron emulsion, which adopted polyoxyethylene castor oil(EL-40) as the emulsifier and was free from co-emulsifier. The formula of the maximum oil loading was found as Chuanxiong oil∶EL-40∶water 3∶7∶90. Further, puera-rin successfully replaced up to 10% of the emulsifier in submicron emulsion. Eventually, the optimal drug-loading formula was determined as puerarin∶Chuanxiong oil∶EL-40∶water 7∶30∶63∶900. The quality evaluation results of the as-prepared submicron emulsion demonstrated that the average emulsion droplet size was 333.9 nm, the PDI 0.26, and the zeta potential-10.12 mV. The submicron emulsion had a good centrifugal stability and did not present any instable phenomena such as delamination and precipitation during its standing still for 50 days. The evaluation of in vitro drug release behavior indicated that the submicron emulsion was capable of releasing the drug completely. The puerarin-chuanxiong oil submicron emulsion prepared in this study possessed a stable quality and to some extent increased the solubility of puerarin along with a sustained-release effect. This study provided ideas for the clinical application of puerarin.

摘要

本研究主要基于葛根与川芎的配伍制备亚微乳,并对其物理和药学性质进行评价。首先,以川芎油为油相,采用滴加法绘制伪三元相图,以微乳区域面积为指标。在此基础上,筛选合适的乳化剂和助乳化剂制备川芎油亚微乳。然后,选择实现最大载油量的配方。最后,用葛根取代部分乳化剂和助乳化剂以降低其用量,从而形成具有药辅结合特点的葛根-川芎油亚微乳。测定其粒径、ζ电位、离心稳定性和储存稳定性,并采用透析袋法考察其体外释药行为,在此基础上对所制备的亚微乳的质量进行综合评价。结果表明,以聚氧乙烯蓖麻油(EL-40)为乳化剂、无需助乳化剂制备川芎油亚微乳的方法可行。发现最大载油量的配方为川芎油∶EL-40∶水3∶7∶90。此外,葛根成功取代了亚微乳中高达10%的乳化剂。最终,确定最佳载药配方为葛根∶川芎油∶EL-40∶水7∶30∶63∶900。所制备的亚微乳的质量评价结果表明,平均乳滴粒径为333.9 nm,PDI为0.26,ζ电位为-10.12 mV。该亚微乳具有良好的离心稳定性,静置50天未出现分层、沉淀等不稳定现象。体外释药行为评价表明,该亚微乳能够使药物完全释放。本研究制备的葛根-川芎油亚微乳质量稳定,在一定程度上提高了葛根的溶解度并具有缓释效果。本研究为葛根的临床应用提供了思路。

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