美沙拉嗪温敏液体栓的制备及体外性质考察

Study on Preparation and in vitro Properties of Mesalazine Thermosensitive Liquid Suppositories

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 prepare mesalazine thermosensitive liquid suppositories and study the in vitro properties. Methods：Poloxamer 407 （P407） and poloxamer 188 （P188） were used as the temperature-sensitive materials, and mesalazine thermosensitive liquid suppositories were prepared by a cold method. The optimal ratio of P407 and P188 was screened using gel temperature as the in-dex. The gel strength and bioadhesive force of mesalazine thermosensitive liquid suppositories were studied, and the in vitro gel erosion and drug release were investigated as well. Results：The optimal ratio of P407 and P188 was 20%： 2. 5%, and the gel temperature was （36.9 ±0.2）℃, the gel strength was （115.1 ±3.2）s and the bioadhesive force was （130.7 ±5.8） ×102 dyne·cm-2. The drug release and gel erosion in vitro were both fitted first-order kinetics, and the two had promising linear relationship, suggesting good sustained-release property based on gel erosion mechanism of mesalazine liquid suppositories. Conclusion：The preparation of mesala-zine liquid suppositories is simple, and the gelation, bioadhesion and sustained-release of the suppositories are promising. Mesalazine liquid suppositories are valuable to be studied further.