摘要
目的 制备头孢克洛缓释微丸，并研究其体外释放行为及人体药动学。方法 采用包衣锅滚丸法制备头孢克洛载药微丸， 以不同类型和比例的丙烯酸树脂及Surelease作为缓释包衣材料并以流化床对载药微丸进行包衣，对最终确定处方的成品进行体外释放和20例健康受试者的生物等效性研究，求算体内药动学参数。结果 以Surelease包衣增重15％，其体外释放行为符合一级释放方程，制备的头孢克洛缓释微丸和上市对照相比生物等效。结论 本方法适于制备较大剂量的缓释微丸，工艺可行，头孢克洛缓释微丸和市售对比体内生物等效。
Abstract
OBJECTIVE To prepare cefaclor sustained-release pellets(CSP)， and to study its release behavior in vitro as well as its pharmacokinetics in vivo. METHODS The core of CSP as the drug loading micro granule was prepared in the coating pan， and the outer layer as the controlled coating was prepared by acrylic resin (different ratio of Eudragit RS30D and Eudragit RL30D) and Surelease in the fluidized bed (mini-glatt). The pellets prepared according to the optimum coating formulations and technology were investigated on its release behavior in vitro and its pharmacokinetics in vivo when it was administered to 20 healthy subjects. RESULTS Surelease aqueous dispersions used with 15% coating level of the outer coating controlled layer proved to show a desirable release profile of cefaclor pellets which fit a first-order model. It obtained bioequivalence to the present commercial products. CONCLUSION The preparation procedure is feasible for a relatively large amount of sustained-release pellets, and the CSP prepared is bioequivalence in vivo.
关键词
头孢克洛 /
缓释微丸 /
体外释放
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Key words
cefaclor /
sustained-release pellets /
release in vitro /
pharmacokinetics
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谢晓燕 李战 赵全如 张自强.
头孢克洛缓释微丸制备、体外释放及人体药动学评价[J]. 中国药学杂志, 2010, 45(19): 1475-1478
XIE Xio-yn;LI zhn;ZHO Qun-ru;ZHNG Zi-qing.
Preparation， Release in Vitro and Pharmacokinetics of Cefaclor Sustained-Release Pellets[J]. Chinese Pharmaceutical Journal, 2010, 45(19): 1475-1478
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参考文献
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脚注
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