Singh J, Robinson D H
Department of Pharmacy, University of Otago, New Zealand.
J Microencapsul. 1990 Jan-Mar;7(1):67-76. doi: 10.3109/02652049009028424.
Captopril microcapsules were prepared using four different viscosity grades of ethyl cellulose (core: wall ratios 1:1, 1:2 and 1:3) by temperature induced coacervation from cyclohexane. In vitro dissolution studies in 0.1 M hydrochloric acid showed that the drug release was dependent on the core to wall ratio, the viscosity grade of the ethyl cellulose and thus the total viscosity of the coacervation system. Viscosity grade of greater than 100 c.p. was unsuitable for microencapsulation by coacervation method at the concentration used. The surface characteristics of a 1:2 core to wall ratio were studied by scanning electron microscopy. The surface of the microcapsules prepared with 10 c.p. viscosity grade was comparatively more porous with larger size pores than 50 c.p. viscosity grade of ethyl cellulose. However, 300 c.p. viscosity grade showed incomplete wall formation. The microcapsules did not fragment during dissolution, alter in shape or size, or show evidence of enlargement of the surface pores. The tensile strength of tablets prepared at constant pressure from each batch of microcapsules (mean diameter 675 microns) increased as both the core to wall ratios and the viscosity of ethyl cellulose increased. The dissolution rate of the drug from tableted microcapsules was significantly delayed. The in vitro release gave best correlation with first order release kinetics when compared to zero-order and square-root-of-time equations.
采用温度诱导凝聚法,从环己烷中制备了四种不同粘度等级的乙基纤维素包衣的卡托普利微胶囊(芯材与壁材比例为1:1、1:2和1:3)。在0.1M盐酸中的体外溶出度研究表明,药物释放取决于芯材与壁材的比例、乙基纤维素的粘度等级,进而取决于凝聚体系的总粘度。在所使用的浓度下,粘度等级大于100厘泊不适合通过凝聚法进行微囊化。通过扫描电子显微镜研究了芯材与壁材比例为1:2的微胶囊的表面特性。与50厘泊粘度等级的乙基纤维素相比,用10厘泊粘度等级制备的微胶囊表面孔隙相对较多,孔隙尺寸较大。然而,300厘泊粘度等级显示壁材形成不完全。微胶囊在溶解过程中没有破碎,形状或尺寸没有改变,也没有表面孔隙增大的迹象。由每批微胶囊(平均直径675微米)在恒定压力下制备的片剂的抗张强度随着芯材与壁材比例以及乙基纤维素粘度的增加而增加。片剂化微胶囊中药物的溶出速率显著延迟。与零级和时间平方根方程相比,体外释放与一级释放动力学的相关性最好。