ABSTRACT
Objective:To study the effect of mesalazine hydroxyl-propyl-β-cyclodextrin inclusion compound ( MSZ-HP-β-CD) liq-uid suppositories on ulcerative colitis ( UC) in rats. Methods:Dextran sulfate sodium was used to induce UC in rats. The marketed MSZ suppositories were applied as the positive control, and the changes in morphology and histopathology of the UC rats were observed after the treatment with MSZ-HP-β-CD liquid suppositories. Results:The results of morphology study showed that CMDI was decreased in the two MSZ preparation groups when compared with that in the model group (P<0. 01), and that in MSZ-HP-β-CD liquid supposi-tories group was the lowest (P<0. 05). The results of histopathology study showed that with the treatment of the marketed MSZ sup-positories and MSZ-HP-β-CD liquid suppositories, the ulcer and damage were improved, and the improvement in the MSZ-HP-β-CD liquid suppositories group was more significant. Conclusion: MSZ-HP-β-CD liquid suppositories exhibit better effect on UC in rats when compared with the marketed MSZ suppositories, which is worthy of further studies.
ABSTRACT
Objective:To prepare mesalazine hydroxypropyl-β-cyclodextrin ( MSZ-HP-β-CD) inclusion complexes and observe the properties. Methods:The inclusion complexes were prepared by a stirring method and the content of MSZ was determined by HPLC. The preparation technology was optimized by orthogonal test with the inclusion rate and the yield of inclusion complexes as the indices. The inclusion complexes were identified respectively by ultraviolet ( UV) spectrometry, X-ray diffraction ( XRD) and solubility. The dissolution rate was investigated. Results: Using the stirring method, the optimum preparation process was as follows: the inclusion temperature was 35 ℃, the ratio of MSZ to HP-β-CD was 1∶ 4 ( mg/g) , and the inclusion time was 3 h. The average inclusion rate of the complexes was 96. 28%, and the yield was 97. 87%. The identification results showed that the freeze-dried powder was inclusion complexes. Compared with that of MSZ, the dissolution of MSZ- HP-β-CD inclusion complexes was notably enhanced. Conclusion:The prepared MSZ-HP-β-CD with optimized technology has good reproducibility and stable technology, which can obviously improve the dissolution of MSZ.
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.