title: Evaluating tamsulosin hydrochloride-released microparticles prepared using single-step matrix coating.
abstract: The objective of the present study was to determine the optimum composition for sustained-release of tamsulosin hydrochloride from microparticles intended for orally disintegrating tablets. Microparticles were prepared from an aqueous ethylcellulose dispersion (Aquacoa®), and an aqueous copolymer based on ethyl acrylate and methyl methacrylate dispersion (Eudragit®) NE30D), with microcrystalline cellulose as core particles with a fluidized bed coating process. Prepared microparticles were about 200 μm diameter and spherical. The microparticles were evaluated for in vitro drug release and in vivo absorption to assess bioequivalence in a commercial product, Harnal® pellets. The optimum ratio of Aquacoat® and Eudragit® NE30D in the matrix was 9:1. We observed similar drug release profiles in microparticles and Harnal® pellets. Higuchi model analysis of the in vitro drug release from microparticles was linear up to 80% release, typical of Fickian diffusion sustained-release profile. The in vivo absorption properties from microparticles were comparable to Harnal® pellets, and there was a linear relationship between in vitro drug release and in vivo drug release. In conclusion, this development produces microparticles in single-step coating, that provided a sustained-release of tamsulosin hydrochloride comparable to Harnal® pellets.
authors.affiliation: Pharmaceutical Research and Technology Labs, Astellas Pharma Inc., 180 Ozumi, Yaizu, Shizuoka 425-0072, Japan. atsushi.maeda@jp.astellas.com
authors.forename: Atsushi
authors.initials: A
authors.lastname: Maeda
authors.forename: Tatsuki
authors.initials: T
authors.lastname: Shinoda
authors.forename: Naoki
authors.initials: N
authors.lastname: Ito
authors.forename: Keizo
authors.initials: K
authors.lastname: Baba
authors.forename: Naoto
authors.initials: N
authors.lastname: Oku
authors.forename: Takao
authors.initials: T
authors.lastname: Mizumoto
mesh_terms: D000284:Administration, Oral; D058668:Adrenergic alpha-1 Receptor Antagonists / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D002853:Chromatography, Liquid; D003692:Delayed-Action Preparations; D004285:Dogs; D004339:Drug Compounding / Q000379:methods*; D005079:Excipients / Q000737:chemistry*; D008297:Male; D008689:Methacrylates / Q000737:chemistry; D008863:Microspheres; D008956:Models, Chemical; D010316:Particle Size; D011108:Polymers / Q000737:chemistry; D012995:Solubility; D013449:Sulfonamides / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D013608:Tablets, Enteric-Coated; D000077409:Tamsulosin; D053719:Tandem Mass Spectrometry; D013810:Therapeutic Equivalency
chemical_list: D058668:Adrenergic alpha-1 Receptor Antagonists; D003692:Delayed-Action Preparations; C477853:Eudragit NE 30-D; D005079:Excipients; D008689:Methacrylates; D011108:Polymers; D013449:Sulfonamides; D013608:Tablets, Enteric-Coated; C013517:ethyl cellulose; D002482:Cellulose; D000077409:Tamsulosin; C109691:microcrystalline cellulose