头孢克洛缓释胶囊的研制及生物利用度研究

摘要

Aim To investigate whether modified-release cefaclor capsules could lead to a more suitable pharmacokinetic profile in the plasma. Methods Cefaclor pellets were prepared by extrusion/spheronization and coated by Eudragit(R) L30D-55 or Eudragit(R) NE30D, then the two sorts of pellets were filled to capsules in a 35 : 65 ratio to made a modified-release (MR) capsules. The bioavailability of the MR capsules was studied in 24 healthy volunteers after oral administration in a fast state using a commercially available immediate release (IR) capsule as a reference. Results The results showed that the MR formulation had a relatively good bioavailability compared with the commercial capsules, as well as a longer time keeping drug level above MIC than immediate release capsule. The relative bioavailability of the MR capsules was 97.4± 12.1%. Conclusion The data of the present study indicate that time of cefaclor plasma concentration above MIC can be substantially prolonged if cefaclor is administered as a modified-release product.%目的 与市售头孢克洛速释胶囊比较,探索头孢克洛缓释胶囊在人体内是否产生更合理的药物动力学特征.方法 用挤出滚圆法制备含药微丸,然后分别采用Eudragit(R) NE30D和Eudragit(R) L30D-55包衣,二类微丸按35:65比例填装胶囊,制成缓释胶囊,以市售速释胶囊作为参比制剂,在禁食状态下对24个健康志愿者进行生物利用度研究.结果 与市售胶囊相比,缓释胶囊有较好的生物利用度,相对生物利用度为97.4%±12.1%,并且血药浓度高于MIC的时间比速释胶囊更久.结论 本法制得的头孢克洛胶囊缓释作用较好,采用头孢克洛缓释胶囊给药,有效血药浓度保持时间可以大大延长.