Academician Workstation, Changsha Medical University, Changsha, 410219, China.
Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, 410013, China.
J Mater Sci Mater Med. 2021 Aug 30;32(9):116. doi: 10.1007/s10856-021-06594-8.
L-glutamate is an important component of protein. It can prevent gastrointestinal damage caused by NSAIDs. We constructed two-phase enteric-coated granules of aspirin and L-glutamate compound by extrusion spheronization method and fluidized bed coating. The subliminal effective dose of L-glutamate is 100 mg/kg tested by model of gastric ulcer of rats induced by aspirin and drug administration. HPLC-UV and UV-Vis methods were adopted to determine content and cumulative release of aspirin and L-glutamate as quality analysis method indexes. The prescription and process optimization were carried out with yield, sphericity and dissolution. The two-phase compound granules have good sphericity of 0.93 ± 0.05 (aspirin pellets) and 0.94 ± 0.02 (L-glutamate pellets), content of salicylic acid (0.24 ± 0.03)%, dissolution of aspirin (2.36 ± 0.11)%. Quality evaluation and preliminary stability meet the commercial requirements. The stored environment of compound preparation should be sealed in a cool and dark place.
L-谷氨酸是蛋白质的重要组成部分。它可以预防 NSAIDs 引起的胃肠道损伤。我们通过挤出滚圆法和流化床包衣法构建了阿司匹林和 L-谷氨酸复合物的双层肠溶颗粒。通过阿司匹林和药物给药诱导的大鼠胃溃疡模型测试，L-谷氨酸的亚有效剂量为 100mg/kg。采用 HPLC-UV 和 UV-Vis 方法作为质量分析方法指标，测定阿司匹林和 L-谷氨酸的含量和累积释放。通过收率、球形度和溶出度对处方和工艺进行优化。双层复方颗粒具有良好的球形度，阿司匹林颗粒为 0.93±0.05，L-谷氨酸颗粒为 0.94±0.02，水杨酸含量（0.24±0.03）%，阿司匹林溶出度（2.36±0.11）%。质量评价和初步稳定性符合商业要求。复方制剂的贮存环境应密封于阴凉黑暗处。
