双氯芬酸钠微胶囊的制备及体外释药性能研究  

Preparation and In Vitro Drug Release of Diclofenac Sodium Microcapsules

作　　者：郭洪辉 谢全灵 洪专 张怡评 GUO Honghui;XIE Quanling;HONG Zhuan;ZHANG Yiping(Technology Innovation Center for Exploitation of Marine Biological Resources,Third Institute of Oceanography,Ministry of Natural Resources,Xiamen 361005,China;Xiamen Ocean Vocational College,School of Marine Biology,Xiamen 361102,China)

机构地区：[1]自然资源部第三海洋研究所,海洋生物资源开发利用工程技术创新中心,福建厦门361005 [2]厦门海洋职业技术学院海洋生物学院,福建厦门361102

出　　处：《中国药学杂志》2023年第19期1752-1758,共7页Chinese Pharmaceutical Journal

基　　金：福建省科技计划项目资助(2023N0037);厦门市2022年公共技术服务平台项目资助(3502Z20221036);厦门南方海洋研究中心项目资助(22CZP008HJ10)。

摘　　要：目的制备双氯芬酸钠肠溶微胶囊,并进行体外释药性能研究。方法以双氯芬酸钠为模型药物,酪蛋白酸钠/明胶作为复合载体材料,采用喷雾干燥技术制备双氯芬酸钠微胶囊,通过单因素正交试验确定了最佳制备条件。利用扫描电镜、浊度法、红外光谱对微胶囊的形貌特性进行了表征,用紫外可见分光光度计对微胶囊的包埋率、载药量以及在模拟消化条件中的释放行为进行了测试和分析。结果在酪蛋白酸钠质量浓度为10 g·L^(-1),酪蛋白酸钠/明胶的质量比为1∶1,双氯芬酸钠质量浓度为15 g·L^(-1)的最佳制备条件下,制备的双氯芬酸钠微胶囊粒径分布主要在10~20μm区间,平均包埋率为96.0%,平均载药量为35.8%。红外光谱分析表明双氯芬酸钠成功地包埋于酪蛋白酸钠/明胶微胶囊中。双氯芬酸钠微胶囊在模拟消化条件下的释放曲线显示微胶囊经0.1 mol·L^(-1)盐酸溶液处理2 h后,释放率仅为4.5%,而在pH 6.8磷酸盐缓冲液中4 h内可完全释放,累积释放率达99.5%,并具有一定的缓释效果。结论以酪蛋白酸钠/明胶为壁材,采用喷雾干燥工艺,可以制备包埋率高、具有肠溶性能的双氯芬酸钠微胶囊。OBJECTIVE To study the preparation and in vitro release properties of diclofenac sodium enteric microcapsules.METHODS With diclofenac sodium as model drug and sodium caseinate/gelatin as composite carrier material,diclofenac sodium microcapsules were prepared by spray drying technology.The optimum preparation conditions were determined by single factor orthogonal test.The morphology and characteristics of microcapsules were characterized by scanning electron microscopy,turbidimetry and infrared spectroscopy.The encapsulation efficiency,drug loading capacity and release behavior in simulated digestive conditions of microcapsules were measured and analyzed by UV-vis spectrophotometer.RESULTS The optimal preparation conditions were as follows:sodium caseinate concentration of 10 g·L^(-1),sodium caseinate/gelatin mass ratio of 1∶1,and sodium diclofenac concentration of 15 g·L^(-1).The particle size of as prepared diclofenac sodium microcapsules was mainly distributed in the range of 10-20μm,the average encapsulation efficiency was 96.0%,and the average drug loading capacity was 35.8%.Infrared spectrum analysis showed that diclofenac sodium was successfully embedded in sodium caseinate/gelatin microcapsules.The release curves of diclofenac sodium microcapsules in simulated digestive conditions showed that the release rate of diclofenac sodium microcapsules was only 4.5%after 2 h treatment in 0.1 mol·L^(-1) hydrochloric acid solution,but 99.5%in pH 6.8 phosphate buffer for 4 h.And the diclofenac sodium microcapsules have a certain sustained release effect.CONCLUSION With sodium caseinate/gelatin as wall material,diclofenac sodium microcapsules with high encapsulation efficiency and enteric performance can be prepared by spray drying process.

关 键 词：肠溶微胶囊 喷雾干燥 酪蛋白酸钠 双氯芬酸钠 体外释放 

分 类 号：R944[医药卫生—药剂学]