Evaluation and Optimization of Preparative Variables for Controlled-Release Floatable Microspheres Prepared by Poor Solvent Addition Method |
| |
Authors: | Yasunori Miyazaki Shigeru Yakou Fumiki Yanagawa Kozo Takayama |
| |
Affiliation: | 1. Department of Pharmacy, Tokyo Women's Medical University Medical Center East, Nishiogu, Arakawa-ku, Tokyo, Japanmyph@dnh.twmu.ac.jp;3. Department of Pharmacy, Tokyo Women's Medical University Medical Center East, Nishiogu, Arakawa-ku, Tokyo, Japan;4. Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Hoshi University, Ebara, Shinagawa-ku, Tokyo, Japan |
| |
Abstract: | The aim of this study was to evaluate and optimize preparative parameters for floatable theophylline microspheres prepared by the emulsion–solvent evaporation method. A three-factor three-level Box–Behnken design was employed using amount of poor solvent, temperature-increase rate and drug loading as independent factors, and percentage floating at 3 h and time required for 50% drug release as dependent variables. Simultaneous optimization of the parameters for maximum buoyancy and desirable drug release was conducted using a partitioned artificial neural network. A microsphere using 27.6% of drug loading, 0.29°C/min of temperature-increase rate, and 1.7 mL of poor solvent was identified for maximizing buoyancy and sustaining drug release. |
| |
Keywords: | floatable microsphere sustained release solvent evaporation poor solvent addition optimization theophylline |
|
|