关键词: 头孢克洛, 头孢克洛, 头孢克洛, 缓释, 缓释, 缓释, 微丸, 微丸, 微丸, 胶囊, 胶囊, 胶囊, 生物利用度, 生物利用度, 生物利用度

Abstract:

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 L30D-55 or Eudragit 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.

Key words: Cefaclor, Cefaclor, Modified-release, Modified-release, Pellets, Pellets, Capsules, Capsules, Bioavailability, Bioavailability