Design, in vitro release characterization and pharmacokinetics of novel controlled release pellets containing levodropropizine. (May 2014)

• Record Type: Journal Article
• Authors: Cao, Qing-Ri; Piao, Yong-Nan; Choi, Jae-Seung; Liu, Yan; Yang, Mingshi; Cui, Jing-Hao
• Is Part Of: Pharmaceutical development and technology. Volume 19:Number 3(2014)
• Page Start: 296
• Page End: 303
• Publication Date: 2014-05
• Subjects: Drug delivery systems -- Periodicals; Pharmaceutical technology -- Periodicals; Drugs -- Administration -- Research -- Periodicals; Drug Delivery Systems -- Periodicals; Pharmaceutical Preparations -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615
• DOI: 10.3109/10837450.2013.778871
• Languages: English
• ISSNs: 1083-7450

Abstract

<abstract> <title>Abstract</title> <p>This study was performed to investigate the <italic>in vitro</italic> 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 (<italic>C</italic>_max) and elimination rate (<italic>K</italic>) than the reference product (LEVOTUS® SYR) but the similar bioavailability (<italic>F</italic> = 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.</p> </abstract>