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目的:降钙素(一个由32个氨基酸组成的多肽)是治疗骨质疏松的首选药之一。降钙素的劣势是其半衰期过短,需要一天一次注射给药,本实验旨在制备突释小,药物释放浓度稳定的降钙素微球制剂。方法:制备降钙素羧酸葡聚糖颗粒和降钙素硫酸葡聚糖颗粒组合物,分别将其包裹于PLGA微球内,制备成降钙素组合微球,采用C18反相色谱柱研究药物的包封率和体外释放行为。结果:所制得的降钙素葡聚糖颗粒缓释微球体外释放一个月,释放曲线比较完美,接近零级释放。结论:本研究制得的降钙素葡聚糖颗粒缓释组合微球能实现理想的体外缓释效果,为后期药动学实验提供基础。
Objective: Calcitonin (a polypeptide of 32 amino acids) is one of the preferred drugs for the treatment of osteoporosis. The disadvantage of calcitonin is its half-life is too short, need injection once a day, the purpose of this experiment is to prepare a small burst release, drug release concentration stable calcitonin microsphere preparation. METHODS: Calcitonin and dextran sulfate particles were prepared and encapsulated in PLGA microspheres respectively to prepare the calcitonin-loaded microspheres. C18 reversed-phase column Drug entrapment efficiency and in vitro release behavior. Results: The release of calcitonin-dextran granules sustained-release microspheres released in vitro for one month, the release curve is relatively perfect, close to zero-order release. Conclusion: The microspheres prepared by this study can achieve the desired sustained release effect in vitro and provide the basis for the later pharmacokinetic study.