title: Development and optimization of a novel oral controlled delivery system for tamsulosin hydrochloride using response surface methodology.
abstract: The purpose of this study was to develop and optimize oral controlled-release formulations for tamsulosin hydrochloride using a combination of two cellulose ester derivatives, hydroxypropyl methylcellulose (HPMC) and hydroxypropyl methylcellulose phthalate (HPMCP), with Surelease as a coating material. A three-factor, three-level Box-Behnken design was used to prepare systematic model formulations, which were composed of three formulation variables, the content of HPMC (X(1)) and HPMCP (X(2)) and the coating level (X(3)), as independent variables. The response surface methodology (RSM) and multiple response optimization utilizing the polynomial equation were used to search for the optimal coating formulation with a specific release rate at different time intervals. The drug release percentages at 2, 3 and 5h were the target responses and were restricted to 15-30% (Y(1)), 50-65% (Y(2)) and 80-95% (Y(3)), respectively. The optimal coating formulation was achieved with 10% HPMC and 20% HPMCP at a coating level of 25%, and the observed responses coincided well with the predicted values from the RSM optimization technique. The drug release from pellets coated with the optimized formulation showed a controlled-release pattern (zero-order), in comparison with a commercial product (Harunal capsule). In conclusion, a novel, oral, controlled-release delivery system for tamsulosin hydrochloride was successfully developed by incorporating HPMC and HPMCP as coating additives into Surelease aqueous ethylcellulose dispersion.
authors.affiliation: National Research Laboratory of Pharmaceutical Technology, College of Pharmacy, Chungnam National University, 220 Gung-dong, Yuseong-gu, Daejeon 305-764, Republic of Korea.
authors.forename: Min-Soo
authors.initials: MS
authors.lastname: Kim
authors.forename: Jeong-Soo
authors.initials: JS
authors.lastname: Kim
authors.forename: Yeon-Hee
authors.initials: YH
authors.lastname: You
authors.forename: Hee Jun
authors.initials: HJ
authors.lastname: Park
authors.forename: Sibeum
authors.initials: S
authors.lastname: Lee
authors.forename: Jeong-Sook
authors.initials: JS
authors.lastname: Park
authors.forename: Jong-Soo
authors.initials: JS
authors.lastname: Woo
authors.forename: Sung-Joo
authors.initials: SJ
authors.lastname: Hwang
mesh_terms: D000284:Administration, Oral; D000317:Adrenergic alpha-Antagonists / Q000008:administration & dosage / Q000737:chemistry*; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D005163:Factor Analysis, Statistical; D065347:Hypromellose Derivatives; D007700:Kinetics; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D008956:Models, Chemical; D012995:Solubility; D013449:Sulfonamides / Q000008:administration & dosage / Q000737:chemistry*; D000077409:Tamsulosin; D013678:Technology, Pharmaceutical / Q000379:methods*
chemical_list: D000317:Adrenergic alpha-Antagonists; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D013449:Sulfonamides; D065347:Hypromellose Derivatives; C013517:ethyl cellulose; D002482:Cellulose; D008747:Methylcellulose; C053309:hydroxypropyl methylcellulose phthalate; D000077409:Tamsulosin