羟乙基纤维素对用尤特奇RS 30 D包衣的茶碱微丸药物释放性能的影响。

Influence of hydroxyethylcellulose on the drug release properties of theophylline pellets coated with Eudragit RS 30 D.

作者信息

Zheng Weijia, Sauer Dorothea, McGinity James W

机构信息

College of Pharmacy, The University of Texas at Austin, Austin, TX 78712, USA.

出版信息

Eur J Pharm Biopharm. 2005 Jan;59(1):147-54. doi: 10.1016/j.ejpb.2004.06.002.

DOI:10.1016/j.ejpb.2004.06.002

PMID:15567312

Abstract

The objective of this study was to investigate the influence of a hydrophilic polymer, hydroxyethylcellulose (HEC), on the release properties of theophylline from pellets coated with Eudragit RS 30 D, and the physicochemical properties of Eudragit RS 30 D cast films. The release rate of theophylline from Eudragit RS 30 D coated pellets decreased during storage at 25 degrees C/60% RH due to the further coalescence of colloidal acrylic particles. In addition, water-vapor permeability and tensile strength of Eudragit RS 30 D cast film decreased after 1-month storage at 25 degrees C/60% RH. The presence of 10% hydroxyethylcellulose in the coating formulation was shown to stabilize the drug release rate from coated pellets, the water-vapor permeability and the tensile strength of free films. Atomic force microscopy and scanning electronic microscopy were used to demonstrate that the HEC was immiscible with Eudragit RS 30 D in the cast films. The stabilization effect of HEC was investigated and determined to be due to the formation of an incompatible phase between the latex particles which impaired further coalescence of the colloidal acrylic particles.

摘要

本研究的目的是考察亲水性聚合物羟乙基纤维素（HEC）对茶碱从包衣有尤特奇RS 30 D的微丸中的释放特性以及尤特奇RS 30 D流延膜的物理化学性质的影响。在25℃/60%相对湿度条件下储存期间，由于胶体丙烯酸颗粒的进一步聚结，茶碱从包衣有尤特奇RS 30 D的微丸中的释放速率降低。此外，尤特奇RS 30 D流延膜在25℃/60%相对湿度条件下储存1个月后，其水蒸气透过率和拉伸强度降低。结果表明，包衣配方中10%羟乙基纤维素的存在可稳定包衣微丸的药物释放速率、游离膜的水蒸气透过率和拉伸强度。利用原子力显微镜和扫描电子显微镜证明，在流延膜中HEC与尤特奇RS 30 D不混溶。对HEC的稳定作用进行了研究，确定其原因是在乳胶颗粒之间形成了不相容相，从而阻碍了胶体丙烯酸颗粒的进一步聚结。