School of Pharmacy, China Pharmaceutical University, Nanjing, PR China.
Drug Dev Ind Pharm. 2011 Jan;37(1):33-40. doi: 10.3109/03639045.2010.489562. Epub 2010 Jun 14.
To reduce the frequency of administration and improve patient compliance, novel levofloxacin sustained-release capsules with suitable in vitro release profiles and good bioavailability were developed.
A fluidized bed was used to prepare levofloxacin pellets by spraying the drug solution onto blank pellets. Then the pellets were coated with either Surelease water dispersion or Eudragit® NE30D water dispersion to achieve sustained-release characteristics. The mixed pellets containing 15% of the uncoated pellets and 85% of the coated pellets were filled into the hard gelatin capsules. In vitro release test was performed with the capsules. A single-dose pharmacokinetic study of the capsules was carried out in beagle dogs.
Although Eudragit® NE30D-coated pellets and Surelease-coated pellets showed similar sustained-release profiles in vitro, their in vivo pharmacokinetic characteristics exhibited significant difference. Unsuccessful in vivo-in vitro correlation was shown in Eudragit® NE30D-coated pellets with a relative bioavailability of only 41.5%, whereas Surelease-coated pellets achieved best sustained-release feature both in vitro and in vivo with a relative bioavailability of 103.0%.
Statistical analysis indicated that the capsules containing Surelease-coated pellets had a satisfactory sustained-release behavior and a desired pharmacokinetic property.
为了减少给药频率并提高患者顺应性，开发了具有合适体外释放曲线和良好生物利用度的新型左氧氟沙星缓释胶囊。
采用流化床技术，将药物溶液喷到空白丸芯上制备左氧氟沙星丸芯。然后，用 Surelease 水分散体或 Eudragit® NE30D 水分散体对丸芯进行包衣，以实现缓释特性。将含有 15%未包衣丸芯和 85%包衣丸芯的混合丸芯填充入硬胶囊中。对胶囊进行体外释放试验。在比格犬中进行了胶囊的单剂量药代动力学研究。
尽管 Eudragit® NE30D 包衣丸芯和 Surelease 包衣丸芯在体外显示出相似的缓释曲线，但它们的体内药代动力学特征存在显著差异。Eudragit® NE30D 包衣丸芯的体内-体外相关性不理想，相对生物利用度仅为 41.5%，而 Surelease 包衣丸芯在体外和体内均表现出最佳的缓释特征，相对生物利用度为 103.0%。
统计分析表明，含有 Surelease 包衣丸芯的胶囊具有满意的缓释行为和理想的药代动力学特性。
