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目的 :研制一种具有较好生物粘附能力和药物缓释效果的阿昔洛韦 (Acv) 卡波姆 (Cb) 乙基纤维素 (Ec)微球。方法 :通过油包水乳剂的溶媒蒸发法制备Acv Cb Ec微球 ;以动物体内外胃粘膜表面滞留程度 ,考察Cb与Ec不同配比、Acv含量、微球粒径对Acv Cb Ec微球生物粘附能力的影响 ;以体外释药速率评价Cb与Ec不同配比、Acv含量、微球粒径和介质 pH对Acv Cb Ec微球缓释效果影响。结果 :Cb配比增加 ,Acv Cb Ec微球生物粘附能力增强 ,药物缓释效果降低 ,表现为负相关性 ;Acv含量增加 ,Acv Cb Ec微球生物粘附能力和药物缓释效果均降低 ,但Acv含量≤ 2 0 %时 ,缓释效果基本接近 ;粒径增大 ,Acv Cb Ec微球生物粘附能力有所减小 ,但在 5 0 0～ 12 0 0 μm时 ,药物缓释效果显著提高 (12h) ,而粘附性变化不明显 ;Acv Cb Ec微球在酸性介质中的释药速率明显快于中性或近中性介质。结论 :载药量≤ 2 0 % ,粒径为 5 0 0～ 12 0 0 μm ,Cb与Ec配比为1∶9的Acv Cb Ec微球在胃粘膜表面具有良好粘附特性 ,且药物缓释可达 12h ,近中性pH条件下的缓释效果更佳。
OBJECTIVE: To develop acv carbazole (Cb) ethylcellulose (Ec) microspheres with good bioadhesion and drug release. Methods: Acv Cb Ec microspheres were prepared by solvent evaporation of water-in-oil emulsions. The degree of gastric mucosal retention in vivo and in vitro were investigated. The effects of different concentrations of Cb and Ec, Acv content and microsphere diameter on Acv Cb Ec microspheres The effects of different ratio of Cb to Ec, Acv content, microsphere size and pH on the sustained release of Acv Cb Ec microspheres were evaluated by in vitro drug release rate. Results: The results showed that Acb Cb Ec microspheres had higher bioadhesive ability and lower drug release rate, which showed negative correlation. Acv Cb Ec microsphere bioadhesion and drug release were decreased , But the Acv Cb Ec microspheres had a smaller bioadhesive capacity when the Acv content was less than 20%, but the Acb Cb Ec microspheres decreased slightly. However, The effect of Acv Cb Ec microspheres in acid medium was obviously faster than that in neutral or near neutral medium. CONCLUSION: Acv Cb Ec microspheres with drug loading ≤20%, particle size of 500 ~ 1200 μm and ratio of Cb to Ec of 1: 9 have good adhesion properties on gastric mucosa, Release up to 12h, near-neutral pH conditions better sustained release.