title: Design, in vitro release characterization and pharmacokinetics of novel controlled release pellets containing levodropropizine.
abstract: 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.
authors.affiliation: College of Pharmaceutical Sciences, Soochow University , Suzhou , People's Republic of China .
authors.forename: Qing-Ri
authors.initials: QR
authors.lastname: Cao
authors.forename: Yong-Nan
authors.initials: YN
authors.lastname: Piao
authors.forename: Jae-Seung
authors.initials: JS
authors.lastname: Choi
authors.forename: Yan
authors.initials: Y
authors.lastname: Liu
authors.forename: Mingshi
authors.initials: M
authors.lastname: Yang
authors.forename: Jing-Hao
authors.initials: JH
authors.lastname: Cui
mesh_terms: D000328:Adult; D000996:Antitussive Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000737:chemistry*; D006801:Humans; D008297:Male; D011109:Polymethacrylic Acids / Q000737:chemistry; D011145:Polyvinyls / Q000737:chemistry; D011409:Propylene Glycols / Q000008:administration & dosage* / Q000493:pharmacokinetics
chemical_list: D000996:Antitussive Agents; D003692:Delayed-Action Preparations; D011109:Polymethacrylic Acids; D011145:Polyvinyls; D011409:Propylene Glycols; C038300:methylmethacrylate-methacrylic acid copolymer; C013215:polyvinyl acetate; C013517:ethyl cellulose; D002482:Cellulose; C035916:dipropizine