论文部分内容阅读
目的利用热熔挤出技术制备难溶性药物硝苯地平固体分散体,提高其溶出度,并进一步制成控释片剂。方法以丙烯酸树脂Ⅳ号、醋酸羟丙甲基纤维素琥珀酸酯、聚乙烯吡咯烷酮共聚物、高取代羟丙基纤维素为载体,采用同向双螺杆热熔挤出机制备硝苯地平固体分散体,考察不同载体挤出物在不同介质中的累积溶出度,为筛选合适的固体分散体,进一步制备控释片做准备。结果利用热熔挤出技术制备的固体分散体均显著提高了硝苯地平的溶出度,通过羟丙基甲基纤维素骨架材料的控制作用,制成了符合零级释放的控释制剂。结论热熔挤出技术制备固体分散体能够提高难溶性药物硝苯地平的溶出度,并能进一步制成符合零级释放的控释片。
OBJECTIVE To prepare a solid dispersion of nifedipine, a poorly soluble drug, by hot melt extrusion to improve its dissolution rate and to make a controlled release tablet. Methods Nifedipine solid dispersion was prepared by using a co-rotating twin-screw hot melt extruder with Acrylic Resin IV, hydroxypropylmethylcellulose acetate succinate, polyvinylpyrrolidone copolymer and highly substituted hydroxypropylcellulose as carriers. The cumulative dissolution rates of different carrier extrudates in different media were investigated to prepare for the preparation of controlled release tablets for screening suitable solid dispersions. Results The solid dispersions prepared by hot melt extrusion significantly increased the dissolution of nifedipine. The controlled release of zymoprofen was achieved through the control of hydroxypropylmethyl cellulose matrix. Conclusion Hot-melt extrusion technology to prepare solid dispersions can improve the dissolution of nifedipine, a poorly soluble drug, and can be further prepared into controlled release tablets in line with zero-order release.