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目的:采用熔融挤出技术制备难溶性药物穿心莲内酯的固体分散体,提高其溶出度。方法:以泊洛沙姆-188、聚乙二醇(PEG-6000)和羟丙甲基纤维素(HPMC)为载体,采用熔融挤出法制备不同质量比例的穿心莲内酯固体分散体,并比较熔融法和溶剂法固体分散体及市售普通片的溶出特性,从而判断熔融挤出法对提高穿心莲内酯溶出度的作用。通过差示热扫描法以及计算药物和载体的溶解度参数,验证药物与载体的互溶性。结果:泊洛沙姆-188为载体,载体-药物比例为4∶1,熔融挤出法制备的穿心莲内酯固体分散体溶出度最高,比原药提高2倍,比穿心莲片提高1倍。穿心莲内酯与泊洛沙姆-188溶解度参数相差最小,互溶性最好。结论:采用熔融挤出法制备的穿心莲内酯固体分散体可以显著提高穿心莲内酯的溶出度。
OBJECTIVE: To prepare a solid dispersion of andrographolide by melt extrusion to improve its dissolution. Methods: Solid dispersions of andrographolide with different mass ratios were prepared by melt extrusion using poloxamer-188, polyethylene glycol (PEG-6000) and hydroxypropyl methylcellulose (HPMC) The effects of melt extrusion on the dissolution of andrographolide were compared by comparing the dissolution characteristics of the melt dispersion method and the solvent dispersion and the commercial common tablets. The drug-carrier mutual solubility was verified by differential thermal scanning and by calculating the solubility parameters of the drug and carrier. Results: Poloxamer-188 was the carrier with carrier-drug ratio of 4:1. The dissolution of andrographolide solid dispersion prepared by melt-extrusion method had the highest dissolution rate, which was two times higher than the original drug and twice as high as that of Andrographolide. Andrographolide and poloxamer -188 solubility parameters of the smallest difference between the best mutual solubility. Conclusion: The solid dispersion of andrographolide prepared by melt extrusion method can significantly improve the dissolution of andrographolide.