Development and optimization of a novel oral controlled delivery system for tamsulosin hydrochloride using response surface methodology

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• 作者：Min-Soo Kim ; Jeong-Soo Kim ; Yeon-Hee You ; Hee Jun Park ; Sibeum Lee ; Jeong-Sook Park ; Jong-Soo Woo ; Sung-Joo Hwang
• 关键词：Tamsulosin hydrochloride ; HPMC ; HPMCP ; Surelease^® ; ; Box-Behnken design
• 刊名：International Journal of Pharmaceutics
• 出版年：2007
• 期刊代码：24_03785173
• 类别：pha
• 出版时间：16 August 2007
• 卷：341
• 期：1-2
• 页码：97-104
• 文件大小：712 K

摘要

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 (X₁) and HPMCP (X₂) and the coating level (X₃), 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 5 h were the target responses and were restricted to 15–30%(Y₁), 50–65%(Y₂) and 80–95%(Y₃), 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.