Formulation of a poorly water-soluble drug in sustained-release hollow granules with a high viscosity water-soluble polymer using a fluidized bed rotor granulator

Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Takumi Asada, Naoki Yoshihara, Yasushi Ochiai, Shin-ichiro Kimura, Yasunori Iwao, Shigeru Itai Water-soluble polymers with high viscosity are frequently used in the design of sustained-release formulations of poorly water-soluble drugs to enable complete release of the drug in the gastrointestinal tract. Tablets containing matrix granules with a water-soluble polymer are preferred because tablets are easier to handle and the multiple drug-release units of the matrix granules decreases the influences of the physiological environment on the drug. However, matrix granules with a particle size of over 800 μm sometimes cause a content uniformity problem in the tableting process because of the large particle size. An effective method of manufacturing controlled-release matrix granules with a smaller particle size is desired. The aim of this study was to develop tablets containing matrix granules with a smaller size and good controlled-release properties, using phenytoin as a model poorly water-soluble drug. We adapted the recently developed hollow spherical granule granulation technology, using water-soluble polymers with different viscosities. The prepared granules had an average particle size of 300 μm and sharp particle size distribution (relative width: 0.52–0.64). The values for the particle strength of the granules were 1.86–1.97 N/mm2, and th...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research