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目的:考察鸦胆子油胃内滞留海藻酸钙凝胶微球的制备工艺及影响微球成型与功能的因素。方法:考察海藻酸钠G/M比、浓度,钙离子浓度,致孔剂用量,起漂剂用量,交联时间,交联剂酸度对微球形态、释药、载药量和包封率的影响,并以油酸和亚油酸为指标考察微球的体外释放度。结果:所制备的海藻酸钙凝胶微球外观圆整光滑、分散性好、粒径均匀;鸦胆子油海藻酸钙凝胶微球的载药量达到40%以上,包封率在70%以上。结论:该海藻酸钙凝胶微球具有良好的缓释作用,体外研究表明具有良好的漂浮能力,可延长药物在局部作用的时间,可提高鸦胆子油对胃癌及胃溃疡的局部治疗作用,为解决现有上市剂型不足提供一定参考。
OBJECTIVE: To investigate the preparation process of the alginate gel microspheres retained in the stomach of Brucea javanica oil and the factors influencing the formation and function of the microspheres. Methods: The morphology, drug release, drug loading and entrapment efficiency of microspheres were investigated with G / M ratio of sodium alginate, concentration, calcium ion concentration, porogen dosage, initiator dosage, crosslinking time and acidity of crosslinker The effects of oleic acid and linoleic acid on the in vitro release of microspheres were investigated. Results: The prepared calcium alginate gel microspheres were round and smooth with good dispersibility and uniform particle size. The drug loading volume of Brucea javanica alginate gel microspheres was more than 40%, and the entrapment efficiency was 70% the above. CONCLUSION: The calcium alginate gel microspheres have a good sustained-release effect. In vitro studies show that the microspheres have a good floating ability, can prolong the local time of the drug, improve the local therapeutic effect of Brucea javanica oil on gastric cancer and gastric ulcer, To solve the existing listing of available formulations to provide some reference.