Kaur Gurpreet, Jain Subheet, Tiwary Ashok K
Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, 147002, India.
Sci Pharm. 2010 Jan-Mar;78(1):57-78. doi: 10.3797/scipharm.0908-10. Epub 2009 Dec 3.
The present study was aimed at evaluating the possible use of inter polymer complexed (IPC) films of chitosan (CH) and carboxymethyl tamarind kernel powder (CMTKP) for colon release of budesonide. Viscosity analysis of the supernatant liquid obtained after reacting CH and CMTKP in different proportions revealed 40:60 to be the optimum stoichiometric ratio. The FTIR spectra of IPC films formed from 50:50 or 40:60 ratio of CH:CMTKP did not reveal any reduction in the peaks at 1560cm(â1) and 1407cm(â1) after exposure to pH 1.2, suggesting resistance of the interaction between âCOO(â) groups of CMTKP and âNH(3) (+) groups of CH to gastric pH. Tablets containing Avicel pH 102 as diluent and coated to a weight gain of 10%, w/w with aqueous solutions of 40:60 or 50:50 ratio of CH:CMTKP did not release budesonide in pH 1.2 buffer. Histopathology of the rat colon after oral administration of these IPC film coated tablets revealed significantly greater (p<0.05) reduction in TNBS-induced ulcerative colitis as compared to that after administration of uncoated tablets. The Cmax of budesonide achieved after oral administration of these IPC film coated tablets was comparable to that observed after administration of uncoated tablets. The results strongly indicate versatility of CH-CMTKP IPC films to deliver budesonide in the colon.
本研究旨在评估壳聚糖（CH）与羧甲基罗望子核粉（CMTKP）的聚合物间复合物（IPC）薄膜用于布地奈德结肠释放的可能性。对CH和CMTKP按不同比例反应后获得的上清液进行粘度分析，结果显示40:60为最佳化学计量比。由CH:CMTKP比例为50:50或40:60形成的IPC薄膜在暴露于pH 1.2后，其傅里叶变换红外光谱（FTIR）在1560cm⁻¹和1407cm⁻¹处的峰没有任何降低，这表明CMTKP的-COO⁻基团与CH的-NH₃⁺基团之间的相互作用对胃内pH具有抗性。含有微晶纤维素pH 102作为稀释剂且用CH:CMTKP比例为40:60或50:50的水溶液包衣至增重10%（w/w）的片剂在pH 1.2缓冲液中不释放布地奈德。口服这些IPC薄膜包衣片剂后大鼠结肠的组织病理学显示，与口服未包衣片剂相比，三硝基苯磺酸（TNBS）诱导的溃疡性结肠炎的减轻程度显著更大（p<0.05）。口服这些IPC薄膜包衣片剂后布地奈德达到的Cmax与口服未包衣片剂后观察到的相当。结果有力地表明CH-CMTKP IPC薄膜在结肠中递送布地奈德具有多功能性。
