Preparation and stability evaluation of artemether-loaded mixed micelles composed of the sodium glycocholate and soybean lecithin
10.16438/j.0513-4870.2021-0003
- VernacularTitle:载蒿甲醚甘氨胆酸钠/大豆磷脂混合胶束的制备与稳定性评价
- Author:
Guang-qing XIAO
1
;
Li WU
2
;
Ting XIONG
3
;
Hai-yan LI
2
;
Wei-feng ZHU
4
;
Dong-xun LI
4
;
Ji-wen ZHANG
3
Author Information
1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; Key laboratory of Modern Preparation Chinese Materia Medica of Ministry of Education, Jiangxi University of Chinese Medicine, Nanchang 330004, China; Guangdong Food and Drug Vocational-Technical School, Guangzhou 510663, China
2. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
3. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; Key laboratory of Modern Preparation Chinese Materia Medica of Ministry of Education, Jiangxi University of Chinese Medicine, Nanchang 330004, China
4. Key laboratory of Modern Preparation Chinese Materia Medica of Ministry of Education, Jiangxi University of Chinese Medicine, Nanchang 330004, China
- Publication Type:Research Article
- Keywords:
artemether;
sodium glycocholate;
soybean lecithin;
mixed micelle;
solubility;
stability
- From:
Acta Pharmaceutica Sinica
2021;56(6):1704-1711
- CountryChina
- Language:Chinese
-
Abstract:
In this study, artemether (ARM)-loaded mixed micelles (MM) composed of the sodium glycocholate (SGC) and soybean lecithin (SL) were prepared by film dispersion method. The effects of hydration medium, SL mass ratio and total concentration of excipients on the solubilization of ARM were investigated and the stability of MM was evaluated. Results showed that the particle size distribution of SGC-SL-MM prepared by phosphate buffer solution (PBS, pH 7.4, 0.05 mol·L-1) was uniform, with an average size of 3.58 ± 0.14 nm and the polydispersity index (PDI) value was 0.16 ± 0.04. The solubility of ARM increased significantly from 0.64 ± 0.04 mg·mL-1 to 13.7 ± 0.13 mg·mL-1 along with the concentration of total excipient increasing from 1.0% to 30.0% (w/w). The calculated results of Arrhenius parameter and storage stability showed that the degradation rate constant of ARM in MM was smaller than that in acetonitrile-PBS (pH 7.4) at either 37 ℃ or 60 ℃. The experimental ARM-MM was clear after storing for two months at 25 ℃ and the degradation of ARM was less than 7.0%. In conclusion, the SGC-SL-MM can not only improve the solubility of ARM in aqueous solution, but also improve its chemical stability in aqueous solution at low temperature.
