Study on Preparation and in vitro Properties of Mesalazine Thermosensitive Liquid Suppositories / 中国药师

ABSTRACT

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.