国产与进口羟丙甲纤维素用作缓释骨架材料相关特性的比较研究

A comparative study on related characteristics of domestic and imported hydroxypropyl methyl cellulose used as sustained release matrix material

目的基于凝胶材料的吸水膨胀、溶蚀及凝胶对药物扩散的阻滞等影响亲水凝胶骨架片药物释放的关键因素,对国产和进口羟丙甲纤维素进行系统的比较研究。方法采用称重法,考察不同来源羟丙甲纤维素的吸水膨胀、溶蚀等特性的异同;以盐酸二甲双胍、托拉塞米、布洛芬为模型药物,考察不同来源羟丙甲纤维素在不同浓度下对药物扩散所起的阻滞作用的差异。结果国产羟丙甲纤维素吸水膨胀速率大于进口羟丙甲纤维素,而溶蚀速率小于进口羟丙甲纤维素;羟丙甲纤维素溶液对药物扩散的阻滞作用与溶液中羟丙甲纤维素浓度呈正相关,在较低浓度(5 mg/m L)时,国产羟丙甲纤维素与进口羟丙甲纤维素对3种模型药物的阻滞率相当,而在中等浓度(15 mg/m L)及高浓度(25 mg/m L)时,进口羟丙甲纤维素对3种模型药物的阻滞作用均小于国产羟丙甲纤维素。结论相同型号的国产和进口羟丙甲纤维素的吸水膨胀、溶蚀及对药物扩散的阻滞等性质并不完全一致。

Objective To investigate the water absorption, swelling, erosion of the gel material, and the blocking effect of it on drug diffusion, domestic and imported hydroxypropyl methyl cellulose （HPMC） were systematically compared by the key factor of affecting hydrophilic matrix tablets drug release. Methods A gravimetric method was employed for studying their swelling, erosion, and other characteristics of different sources of HPMC. Metformin hydrochloride, torasemide, and ibuprofen were used as representative drugs to investigate the blocking effect of different HPMC on drug diffusion under different concentration. Results The water absorption and swelling rate of domestic HPMC were more than those of imports HPMC, while the erosion rate of it was less than imports HPMC; The blocking effect of HPMC on drug diffusion was positively correlated with the concentration of HPMC, in addition, the blocking effect of domestic and imports HPMC on three model drugs was basically the same at low concentration （5 mg/mL）,while the blocking effect of imports HPMC on three model drugs was lower at a moderate concentration （15 mg/mL） and a high concentration （25 mg/mL）. Conclusion The water absorption, swelling, and erosion of HPMC with different models are not entirely consistent, the same as the blocking effect of them on drug diffusion.