Lin S Y, Yang J C
Department of Medical Research, Veterans General Hospital, Taipei, Taiwan, Republic of China.
J Microencapsul. 1985 Oct-Dec;2(4):315-25. doi: 10.3109/02652048509033843.
The effect of concentration of ethylene-vinyl acetate (EVA) copolymer, used as a coacervation-inducing agent, on the preparation of ethylcellulose microcapsules was studied with theophylline as the core material. The influence of EVA concentration on the micromeritic properties of the microcapsules and their drug release behaviour were investigated. Particle size distribution of the microcapsules obtained was dependent on the amount of EVA copolymer. As the EVA concentration increased the quantity of larger particles was reduced and that of the smaller particles was increased. Thus EVA might be used as a protective colloid to prevent aggregation of the microcapsules. The porosity of the microcapsules decreased with respect to EVA concentration, but the wall thickness of the microcapsules showed a corresponding increase. Zero-order release kinetics, from the resulting microcapsules in the initial dissolution phase was obtained. The apparent zero-order release rate in the initial steady-state decreased with the increase of EVA concentration, but T50 increased. The higher concentration of EVA causing a thick, compact wall lead to an effective prolongation of drug release.
以茶碱为核心材料,研究了用作凝聚诱导剂的乙烯 - 醋酸乙烯酯(EVA)共聚物浓度对乙基纤维素微胶囊制备的影响。研究了EVA浓度对微胶囊的粉体学性质及其药物释放行为的影响。所得微胶囊的粒度分布取决于EVA共聚物的用量。随着EVA浓度的增加,较大颗粒的数量减少,较小颗粒的数量增加。因此,EVA可作为保护胶体以防止微胶囊聚集。微胶囊的孔隙率随EVA浓度降低,但微胶囊的壁厚相应增加。在初始溶解阶段,所得微胶囊呈现零级释放动力学。初始稳态下的表观零级释放速率随EVA浓度的增加而降低,但T50增加。较高浓度的EVA导致形成厚而致密的壁,从而有效地延长了药物释放。