Zhao Guowei, Zeng Qingyun, Zhang Shoude, Zhong Youquan, Wang Changhao, Chen Yashao, Ou Liquan, Liao Zhenggen
Key Laboratory of Applied Surface and Colloid Chemistry, Ministry of Education, School of Chemistry and Chemical Engineering, Shaanxi Normal University, Xi'an 710119, China.
Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.
Pharmaceutics. 2019 Feb 10;11(2):74. doi: 10.3390/pharmaceutics11020074.
Solid dispersion (SD) is a useful approach to improve the dissolution rate and bioavailability of poorly water-soluble drugs. This work investigated the effects of carrier material lipophilicity and preparation method on the properties of andrographolide (AG)⁻SD. The SDs of AG and the carrier materials, polyethylene glycol (PEG) and PEG grafted with carbon chains of different length (grafted PEG), have been prepared by spray-drying and vacuum-drying methods. In AG⁻SDs prepared by the different preparation methods with the same polymer as carrier material, the intermolecular interaction, 5% weight-loss temperature, the melting temperature (T), surface morphology, crystallinity, and dissolution behavior have significant differences. In the AG⁻SDs prepared by the same spray-drying method with different grafted PEG as carrier material, T, surface morphology, crystallinity, and dissolution behavior had little difference. In the AG⁻SDs prepared by the same vacuum-drying method with different grafted PEG as carrier material, the crystallinity and decreased, and the dissolution rate of AG increased with the increase of grafted PEG lipophilicity. The preparation method has an important effect on the properties of SD. The increase of carrier material lipophilicity is beneficial to the thermal stability of SD, the decrease of crystallinity and the increase of dissolution rate of a poorly water-soluble drug in the SD.
固体分散体（SD）是提高难溶性药物溶出速率和生物利用度的一种有效方法。本研究考察了载体材料亲脂性和制备方法对穿心莲内酯（AG）-固体分散体性质的影响。采用喷雾干燥法和真空干燥法制备了AG与载体材料聚乙二醇（PEG）以及接枝不同长度碳链的聚乙二醇（接枝PEG）的固体分散体。在以相同聚合物为载体材料通过不同制备方法制备的AG-固体分散体中，分子间相互作用、5%失重温度、熔点（T）、表面形态、结晶度和溶出行为存在显著差异。在以不同接枝PEG为载体材料通过相同喷雾干燥法制备的AG-固体分散体中，T、表面形态、结晶度和溶出行为差异不大。在以不同接枝PEG为载体材料通过相同真空干燥法制备的AG-固体分散体中，结晶度降低，AG的溶出速率随接枝PEG亲脂性的增加而提高。制备方法对固体分散体的性质有重要影响。载体材料亲脂性的增加有利于固体分散体的热稳定性、结晶度的降低以及难溶性药物在固体分散体中溶出速率的提高。
