Solid dispersion (SD) is the effective approach to improve the dissolution rate and bioavailability of class II drugs with low water solubility and high tissue permeability in the Biopharmaceutics Classification System. This study investigated the effects of polyethylene glycol (PEG) molecular weight in carrier material PEG palmitate on the properties of andrographolide (AG)-SD. We prepared SDs containing the poorly water-soluble drug AG by the freeze-drying method. The SDs were manufactured from two different polymers, PEG4000 palmitate and PEG8000 palmitate. The physicochemical properties of the AG-SDs were characterized by Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, dissolution testing, and so on. We found that AG-PEG4000 palmitate-SD and AG-PEG8000 palmitate-SD were similar in the surface morphology, specific surface area, and pore volume. Compared with the AG-PEG4000 palmitate-SD, the intermolecular interaction between PEG8000 palmitate and AG was stronger, and the thermal stability of AG-PEG8000 palmitate-SD was better. In the meanwhile, the AG relative crystallinity was lower and the AG dissolution rate was faster in AG-PEG8000 palmitate-SD. The results demonstrate that the increasing PEG molecular weight in the PEG palmitate can improve the compatibility between the poorly water-soluble drug and carrier material, which is beneficial to improve the SD thermal stability and increases the dissolution rate of poorly water-soluble drug in the SD.

中文翻译：

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水溶性差的药物穿心莲内酯PEG4000棕榈酸酯/PEG8000棕榈酸酯固体分散体的制备与表征

固体分散体 (SD) 是提高生物药剂学分类系统中低水溶性和高组织渗透性 II 类药物的溶出度和生物利用度的有效方法。本研究调查了载体材料 PEG 棕榈酸酯中的聚乙二醇 (PEG) 分子量对穿心莲内酯 (AG)-SD 性质的影响。我们通过冷冻干燥方法制备了含有难溶于水的药物 AG 的 SD。SD 由两种不同的聚合物制成，即 PEG4000 棕榈酸酯和 PEG8000 棕榈酸酯。AG-SDs的理化性质通过傅里叶变换红外光谱、热重分析、差示扫描量热法、粉末X射线衍射、扫描电子显微镜、溶出度测试等表征。我们发现 AG-PEG4000 棕榈酸酯-SD 和 AG-PEG8000 棕榈酸酯-SD 在表面形态、比表面积和孔体积方面相似。与AG-PEG4000棕榈酸酯-SD相比，PEG8000棕榈酸酯与AG的分子间相互作用更强，AG-PEG8000棕榈酸酯-SD的热稳定性更好。同时，AG-PEG8000棕榈酸酯-SD中AG相对结晶度较低，AG溶解速度较快。结果表明，增加 PEG 棕榈酸酯中的 PEG 分子量可以提高难溶性药物与载体材料的相容性，有利于提高 SD 热稳定性，增加难溶性药物在难溶性药物中的溶出度。标清。和孔隙体积。与AG-PEG4000棕榈酸酯-SD相比，PEG8000棕榈酸酯与AG的分子间相互作用更强，AG-PEG8000棕榈酸酯-SD的热稳定性更好。同时，AG-PEG8000棕榈酸酯-SD中AG相对结晶度较低，AG溶解速度较快。结果表明，增加 PEG 棕榈酸酯中的 PEG 分子量可以提高难溶性药物与载体材料的相容性，有利于提高 SD 热稳定性，增加难溶性药物在难溶性药物中的溶出度。标清。和孔隙体积。与AG-PEG4000棕榈酸酯-SD相比，PEG8000棕榈酸酯与AG的分子间相互作用更强，AG-PEG8000棕榈酸酯-SD的热稳定性更好。同时，AG-PEG8000棕榈酸酯-SD中AG相对结晶度较低，AG溶解速度较快。结果表明，增加 PEG 棕榈酸酯中的 PEG 分子量可以提高难溶性药物与载体材料的相容性，有利于提高 SD 热稳定性，增加难溶性药物在难溶性药物中的溶出度。标清。AG-PEG8000棕榈酸酯-SD中AG相对结晶度较低，AG溶解速率较快。结果表明，增加 PEG 棕榈酸酯中的 PEG 分子量可以提高难溶性药物与载体材料的相容性，有利于提高 SD 热稳定性，增加难溶性药物在难溶性药物中的溶出度。标清。AG-PEG8000棕榈酸酯-SD中AG相对结晶度较低，AG溶解速率较快。结果表明，增加 PEG 棕榈酸酯中的 PEG 分子量可以提高难溶性药物与载体材料的相容性，有利于提高 SD 热稳定性，增加难溶性药物在难溶性药物中的溶出度。标清。