ABSTRACT
Objective:To prepare thermosensitive liquid suppositories of mesalazine( MSZ) HP-β-CD complex and study the in vitro properties. Methods:Poloxamer 407 (P407) and poloxamer 188 (P188) were used as the thermosensitive polymers to load MSZ HP-β-CD complex to prepare the thermosensitive liquid suppositories. The viscosity, gel strength, bioadhesion,in vitro gel erosion and drug release of MSZ HP-β-CD complex were compared with those of MSZ liquid suppositories. Results: Compared with that of MSZ liquid suppositories, the gel temperature of MSZ HP-β-CD complex liquid suppositories was stable, while the viscosity, gel strength and bioadhesion of MSZ HP-β-CD complex liquid suppositories were increased significantly. The in vitro gel erosion was not affected by MSZ HP-β-CD complex, while the drug release was notably enhanced. The drug release and gel erosion showed a good linear relation-ship. Conclusion:MSZ HP-β-CD complex liquid suppositories show good gel temperature, viscosity, gel erosion and bioadhesion, and the in vitro release rate is faster than that of MSZ liquid suppositories.
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.