Preparation and Dissolution Characteristics of Captopril Microcapsule

Captopril微膠囊之製備與溶離特性

楊國明(Guo-Ming Yang) ； 郭人鳳(Jen-Feng Kuo)

《Journal of the Chinese Institute of Chemical Engineers》 34卷4期 (2003/07) Pp. 481-486

https://doi.org/10.6967/JCICE.200307.0481

摘要

本研究是captopril(CAP)和乙基纖維素(EC)和氫氧丙基纖維素(HPC)製備成微膠囊，以乳化劑溶劑蒸發法製備，探討影響微膠囊顆粒大小和大小分佈的因素，以Ｘ射線及接觸試驗和紫外線光譜鑑定微膠囊特性。用於研究藥物延遲施放的微膠囊平均直徑為337μm，其藥物與高分子比例為一比三，並有不同的EC/HPC組成。測定微膠囊的CAP施放行為，前0.7小時遵守一階段施放動力，而2到10小時期間則是零階動力。其一階及零階動力的速率常數與高分子組成關係呈線性，富HPC微膠囊呈較佳的延遲施放行為。釋放動力的變化可能由於微膠囊基體的形態(morphology)變化致使。

並列摘要

Sustained release of water-soluble captopril (CAP) from microcapsules composed of Ethylcellulose (EC) and Hydroxypropylcellulose (HPC) was studied. The microcapsules were prepared using the emulsion-solvent evaporation technique. Factors affecting the size and size distribution of microcapsules were investigated. The microcapsules were characterized using an x-ray diffractometer, static contact angle instrument and UV/visible spectrophotograph. The microcapsules for the sustained release study had an average diameter of 337 11m, a drug-to-polymer ratio of 1:3 by wt and various polymer compositions. The cumulative releases of CAP from the microcapsules at various times were measured. The results could be well described by a first order release kinetics for first 0.7 h and a zero order release behavior for the release time between 2 and 10 h. The rate coefficients of first and zero-order stages linearly depended upon the polymer composition. The microcapsules rich in HPC showed better sustained-release behaviors. The matrix changed from an anhydrate state to hydrogel may be the cause for the observed release kinetics change.

並列關鍵字

Captopril ； Microcapsules ； Ethylcellulose and hydroxypropylcellulose ； Sustained release ； Release kinetics