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目的:研制美沙拉嗪温敏液体栓,并对其体外性质进行考察。方法:以泊洛沙姆407和188为温敏材料,采用冷法制备美沙拉嗪温敏液体栓;以胶凝温度为评价指标,筛选出两种材料的最佳配比;对美沙拉嗪温敏液体栓的胶凝强度、生物黏附力等性质进行考察,并对其体外溶蚀行为及释药特性进行研究。结果:泊洛沙姆407及188的最佳配比为20%∶2.5%,此时胶凝温度为(36.9±0.2)℃,胶凝强度为(115.1±3.2)s,生物黏附力为(130.7±5.8)×102dyne·cm-2;体外释药特性及凝胶溶蚀特性均符合一级动力学特征,且两者相关性良好,显示美沙拉嗪液体栓具有较好的缓释性。结论:美沙拉嗪温敏液体栓制备工艺简单,且具有较好的胶凝性、生物黏附性及缓释性。
Objective: To develop mesalazine thermosensitive liquid suppository and study its in vitro properties. Methods: Poloxamers 407 and 188 were used as thermosensitive materials, and the mesalazine thermosensitive liquid suppositories were prepared by cold method. The optimal ratio of the two materials was screened with the gelation temperature as the evaluation index. Temperature-sensitive liquid plug the gel strength, bio-adhesion and other properties were investigated, and in vitro dissolution behavior and release characteristics of the study. Results: The optimal ratio of Poloxamer 407 and 188 was 20%: 2.5%, the gelling temperature was (36.9 ± 0.2) ℃, the gelling strength was (115.1 ± 3.2) s and the bioadhesive power was 130.7 ± 5.8) × 102dyne · cm-2. The in vitro drug release characteristics and gel erosion properties were consistent with the first-order kinetic characteristics, and the correlation between the two was good, which showed that the mesalazine liquid suppository had good sustained-release properties. Conclusion: Mesalazine thermosensitive liquid suppository has simple preparation process, good gelation, bioadhesion and sustained release.