Evaluation of injection moulding as a pharmaceutical technology to produce matrix tablets
Evaluation of injection moulding as a pharmaceutical technology to produce matrix tablets
复制标题
DOI：
10.1016/j.ejpb.2008.02.025
复制
发表时间：
2009-01-01
影响因子：
4.9
通讯作者：
Remon, Jean Paul
中科院分区：
文献类型：
--
作者：
Quinten, Thomas;De Beer, Thomas;Remon, Jean Paul
本研究的目的是通过注射成型开发缓释骨架片，并评估工艺温度、骨架成分（EC和HPMC浓度）以及乙基纤维素（EC）和羟丙基甲基纤维素（HPMC）的粘度等级对加工性能和药物释放的影响。分析药物释放数据以深入了解释放动力学和机制。将含有酒石酸伊奈托洛尔（30%，模型药物）、癸二酸二丁酯（基质形成剂和增塑剂）的 EC 和亲水性聚合物 HPMC 的制剂挤出，然后在 110 至 140 摄氏度的温度下注塑成片剂（375 mg，直径 10 mm，凸形）。含有 30% 美托洛尔和 70% 乙基纤维素的片剂（EC 4 mPa·s）显示24 小时（20 mPa s）和 HPMC（4000 和 10,000 mPa s）内药物释放不完全。片剂孔隙率低（
The aim of this study was to develop sustained-release matrix tablets by means of injection moulding and to evaluate the influence of process temperature, matrix composition (EC and HPMC concentration) and viscosity grade of ethylcellulose (EC) and hydroxypropylmethylcellulose (HPMC) on processability and drug release. The drug release data were analyzed to get insight in the release kinetics and mechanism. Formulations containing inetoprolol tartrate (30%, model drug), EC with dibutyl sebacate (matrix former and plasticizer) and hydrophilic polymer HPMC were extruded and subsequently injection moulded into tablets (375 mg, 10 mm diameter, convex-shaped) at temperatures ranging from 110 to 140 degrees C. Tablets containing 30% metoprolol and 70% ethylcellulose (EC 4 mPa s) showed an incomplete drug release within 24 h ( 20 mPa s) and HPMC (4000 and 10,000 mPa s). Tablet porosity was low (