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摘 要：研制有机酸丸芯，为制备药物微丸提供优质、便捷的母核。采用挤出滚圆法制备有机酸丸芯，分别对处方因素（控制有机酸丸芯的粒径分布，筛选粘合剂的种类和用量）和工艺因素（挤出筛网的直径、转速和时间及滚圆转速、时间和次数）进行考察，并对制得的有机酸丸芯进行质量评价（以粒度分布、圆整度和收率作为评价指标）；以MCC丸芯作为对照，采用流化床技术在有机酸丸芯和MCC丸芯的外部包裹活性成分API，制备得到含药微丸，并对制得的含药有机酸微丸与含药MCC微丸进行体外溶出实验，来验证制备有机酸丸芯的可行性。优化处方和工艺所制备的有机酸丸芯圆整度、粒径分布、收率等各项评价指标均符合要求，且工艺重现性良好。有机酸丸芯提供了一个酸性环境使含药微丸释药完全。有机酸丸芯制备工艺简便，适于工业化生产，挤出滚圆法制备有机酸丸芯是可行的。关键词： 有机酸丸芯；微丸；挤出滚圆法10241
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Studies on Preparation of organic acids pill core
Abstract: Objective: To study organic acids pill core used for providing quality and convenient nucleus for the preparation of pharmaceutical pellets. Methods: The organic acids pill core were prepared by extrusion-spheronization method. The formula agents, including controlling the particle size distribution of organic acids pill core, filtering the concentration and amount of adhesive and the technique agents, including extrusion mesh diameter, extrusion speed, extrusion time, spheronization speed, spheronization time and spheronization frequency, were investigated. Then, evaluation for the quality of obtained organic acids pill core included the size distribution, roundness and productive rate as evaluation index. The pellets were coated by fluid bed coating technology, their dissolution profiles were tested including organic acids pellets and MCC pellets to validate the feasibility of preparing organic acids pill core. Results: The organic acids pill core prepared via optimized formula and technique, of which all the evaluation index met the requirements, the preparation with optimized formula and technique could be well repeated. The organic acid pills core provided an acidic environment for complete release of the pellets. Conclusion: The preparation technique for organic acids pill core is simple, easy and suitable for industrial production, this method of preparing organic acids pill core is feasible.
Key Words: Organic acids pill core; Pellets; Extrusion spheronization
目录
1 前言 1
2 含药微丸的制备 4
2.1 丸芯的制备 4
2.1.1 试验仪器与材料 6
2.1.2 有机酸的预处理 6
2.1.3 有机酸丸芯的制备工艺 7
2.1.4 影响因素考察 7
2.1.5 有机酸丸芯质量评价 9
2.1.6 结论 11
2.2 含药微丸的制备 11
2.2.1 试验仪器与材料 12
2.2.2 含药包衣液的配制 12
2.2.3 丸芯上药 13
2.2.4 含药微丸的评价 13
2.2.5 结论 14
3 含药微丸的质量评价 15
3.1 试验仪器与材料 15
3.1.1 主要试剂 15
3.1.2 主要仪器 15
3.2 紫外扫描样品的配制 15
3.3 检测波长的确定 16
3.4 溶出方法 17
3.5 溶出度考察和比较 17
3.6 结论 18
4 全文结论 19
致 谢 20
参考文献 211 前言
微丸是指药物溶解、分散在球形或类球形骨架中或吸附在骨架上的实体小球，直径小于2.5mm，主要用于口服[1]。微丸流动性好，既可直接分装成剂量分散型小丸应用，也可填充于空心胶囊中成为一种剂量分散型胶囊剂或与适量填充剂混合压制成片应用[2]。微丸具有以下特点：①外形美观，流动性好；②含药量大，且服用剂量小；③释药稳定；④生物利用度高；⑤局部刺激性小；⑥能根据临床需要制成速释、缓释、控释制剂[3]。速释微丸可使药物迅速崩解和溶出，药物释放速度较快，一般在3min内释放药物不低于70%，如速释硝苯地平微丸[4]；缓（控）释微丸可使药物按一定规律缓慢地非恒速或恒速地释放，在服用的间隔时间（12小时或24小时）内累积释药应高于90%，如灯盏花素缓释微丸[5]。