College of Pharmaceutical Sciences, Soochow University , Suzhou , People's Republic of China .
Pharm Dev Technol. 2014 May;19(3):296-303. doi: 10.3109/10837450.2013.778871. Epub 2013 Mar 19.
This study was performed to investigate the in vitro release characteristics of levodropropizine (LDP) from novel dual-coated sustained release (SR) pellets, and evaluate the pharmacokinetics of a novel controlled release (CR) preparation composed of the dual-coated SR pellets and immediate release (IR) LDP pellets. The dual-coated SR pellets composed of a drug-loaded nonpareil core, a sub-coating layer (HPMC 6cps) and an SR-coating layer (Aquacoat® ECD, Eudragit® RS 30D or Kollicoat® SR 30D) were prepared by a bottom-spray fluidized bed-coating method. The drug release from the dual-coated SR pellets coated with Aquacoat® ECD followed a zero-order profile in water, and the drug release was not affected by the coating level of the sub-coating layer and stable under the accelerated storage condition (40 °C, 75% RH) for 6 months. The CR preparation showed significantly decreased values of maximum drug concentration (Cmax) and elimination rate (K) than the reference product (LEVOTUS® SYR) but the similar bioavailability (F = 95.43%). The novel CR preparation presents promising delivery of LDP with an immediate and sustained release manner, with similar clinical effect as the commercial IR product.
本研究旨在考察左旋丙哌嗪（LDP）新型双层控释（SR）微丸的体外释放特性，并评价由双层 SR 微丸和即刻释放（IR）LDP 微丸组成的新型控释（CR）制剂的药代动力学。新型双层 SR 微丸由载药素丸、次涂层（HPMC 6cps）和 SR 涂层（Aquacoat® ECD、Eudragit® RS 30D 或 Kollicoat® SR 30D）组成，采用底部喷雾流化床包衣法制备。Aquacoat® ECD 包衣的双层 SR 微丸在水中的药物释放遵循零级动力学，药物释放不受次涂层包衣水平的影响，在加速储存条件（40°C、75% RH）下稳定 6 个月。CR 制剂的最大药物浓度（Cmax）和消除率（K）值明显低于参比制剂（LEVOTUS® SYR），但生物利用度（F=95.43%）相似。新型 CR 制剂具有即刻和持续释放的 LDP 递药方式，具有与商业 IR 产品相似的临床效果。
