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Freeze-Dried Highly Porous Matrix as a New Gastroretentive Dosage Form for Ecabet Sodium: In Vitro and In Vivo Characterizations
Institution:1. School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea;2. College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju 660-751;3. College of Pharmacy, Chungbuk National University, Cheongju 361-763, Republic of Korea;1. Department of Cardiology, Chonnam National University Hospital, Gwangju, Republic of Korea;2. Heart Research Center, Chonnam National University Hospital, Gwangju, Republic of Korea;3. Department of Molecular Medicine and Advanced Chemical & Engineering, Chonnam National University Graduate School, Gwangju, Republic of Korea;4. Center for Functional Nano Fine Chemicals & School of Applied Chemical Engineering, Chonnam National University, Gwangju, Republic of Korea;5. Institute of Interventional Medicine, M.I. Tech Co., Ltd., Pyeongtaek, Republic of Korea
Abstract:The aims of the present study were to prepare hydroxypropylmethyl cellulose-based matrix tablets prepared using the freeze-drying method for gastroretentive delivery of ecabet sodium (ECS), a locally acting antigastric ulcer drug, and to perform in vitro/in vivo characterizations.The freeze-dried gastroretentive tablets (FD-GRTs) had porous structures, while they had good friability as a pharmaceutical dosage form. The porous structures lowered the tablet density, allowing the tablet to float without any lag time. Buoyancy of FD-GRT was maintained until they were entirely disintegrated during an in vitro release study. Release rate of ECS could be controlled by the amount of ethylcellulose (EC) in FD-GRT. As amount of EC in the composition was increased, there was a decrease in both release rate and erosion rate of FD-GRT. When administered to a miniature pig, FD-GRT remained in the stomach for more than 12 h, which was significantly longer than a conventional sustained release tablet. The new FD-GRT do not contain any excipients for buoyancy and do not require any lag time for buoyancy, consequently it could be considered to be safer and more effective than conventional floating-type GRT.
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