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目的:制备胸腺肽α1结肠释放片(Tα1片),评价其体外释药性能。方法:将Tα1制成片芯,2次包衣,内层为壳聚糖盐酸盐,外层为尤特奇L100-55。高效液相色谱(HPLC)法进行含量及含量均匀度测定,扫描电镜法评价壳聚糖盐酸盐包衣膜在模拟大肠液中的降解作用。以荧光剂FD-4为模型化合物,同法制备模拟结肠片,荧光分光光度法检测其在pH 1.2盐酸溶液,pH 6.8磷酸盐缓冲液及模拟大肠液中的体外释放性能。结果:Tα1片的含量及含量均匀度符合《中国药典》相关规定;电镜扫描结果表明,壳聚糖盐酸盐包衣膜在模拟大肠液中具有显著降解作用;模拟结肠片在pH 1.2盐酸溶液和pH 6.8磷酸盐缓冲液中的累积释药量6 h内小于23％,而在模拟大肠液中4 h基本释药完全。结论:本研究所制备的Tα1结肠释放片具有潜在的结肠靶向释药效果。
Objective: To prepare thymosin α1 colon release tablets (Tα1 tablets) and evaluate its in vitro drug release properties. Methods: Tα1 was made into tablets and coated twice, the inner layer was chitosan hydrochloride, the outer layer was Eutech L100-55. Determination of content and content uniformity by high performance liquid chromatography (HPLC) method, scanning electron microscopy evaluation of degradation of chitosan hydrochloride coated membrane in simulated large intestinal fluid. Fluorescein FD-4 was used as a model compound to prepare simulated colon tablets in the same method. Fluorescence spectrophotometry was used to determine the in vitro release properties of the compound in pH 1.2 hydrochloric acid solution, pH 6.8 phosphate buffer solution and simulated colonic fluid. Results: The content and content uniformity of Tα1 tablets were in accordance with the relevant regulations of “Chinese Pharmacopoeia”. Scanning electron microscopy results showed that the chitosan hydrochloride coating film had a significant degradation effect in simulated large intestine fluid. And the cumulative release in phosphate buffered saline pH 6.8 was less than 23% within 6 h, whereas the basic release was complete within 4 h in simulated large intestinal fluid. Conclusion: The Tα1 colon release tablets prepared in this study have potential colon-targeted drug release.