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目的:研制具有较好生物黏附性能和药物缓释效果的克拉霉素(Cla)-乙基纤维素(EC)-卡波姆(Cb)微球。方法:使用乳化-溶剂挥发法制备克拉霉素生物黏附微球(Cla-EC-Cb),以高效液相色谱法测定Cla-EC-Cb微球中克拉霉素的含量;以体外释药速率评价EC与Cb不同配比、不同EC黏度对微球缓释效果的影响;以大鼠体内胃黏膜表面滞留程度,考察EC与Cb不同配比、不同EC黏度对微球生物黏附能力的影响。结果:黏附材料Cb的加入有助于提高微球的载药量;EC(20cp)与Cb配比为2∶1的微球体外药物释放度明显高于同EC黏度其他比例组和EC组;EC与Cb配比为4∶1时,EC(10cp)组体外释放参数明显高于EC(20cp)与EC(45cp)组;不同比例、不同EC黏度的Cla-EC-Cb微球在大鼠胃黏膜的滞留率均明显高于Cla-EC微球,Cla-EC(20cp)-Cb微球的胃黏膜滞留率随着Cb比例的提高有增大的趋势,但差异无显著性。结论:处方配比为EC(10cp)-Cb为4∶1,粒径为450～1 000μm的Cla-EC-Cb微球具有较好的体外药物缓释效果和胃黏膜黏附特性。
OBJECTIVE: To develop clarithromycin (EC) -carbomer (Cb) microspheres with good bioadhesive properties and sustained drug release. Methods: Clarithromycin bioadhesive microspheres (Cla-EC-Cb) were prepared by emulsion-solvent evaporation method. Clarithromycin content in Cla-EC-Cb microspheres was determined by high performance liquid chromatography To evaluate the effect of EC and Cb at different ratios and different EC viscosities on the sustained release of microspheres. The effects of EC and Cb at different ratios and different EC viscosities on the bioadhesive ability of microspheres were investigated in vivo. Results: The drug release of microspheres with EC (20cp) to Cb ratio of 2:1 was significantly higher than that of other EC and EC groups with the addition of Cb. The release parameters of EC (10cp) were significantly higher than that of EC (20cp) and EC (45cp) when the ratio of EC to Cb was 4:1. Cla-EC-Cb microspheres with different ECV, Gastric mucosa retention rate was significantly higher than the Cla-EC microspheres, Cla-EC (20cp) -Cb microspheres gastric mucosa retention rate with the Cb ratio increased, but the difference was not significant. CONCLUSION: Cla-EC-Cb microspheres with EC (10cp) -Cb of 4:1 and particle size of 450-1000μm have better drug release in vitro and gastric mucosal adhesion characteristics.