熔融高速搅拌法制备缓释微丸的研究
发布时间：2018-07-28 08:27
【摘要】：熔融高速搅拌法制备缓释微丸是一个全新的制备微丸的方法,以其高效的生产方式,近年来受到人们越来越多的关注。以物料混合这种最简单的方式并辅以加热,固体粘合剂熔融成为液体,最后通过充分的混合碰撞形成微丸。关于熔融高速搅拌法制备微丸已有国外文献报道,为了给生产提供依据、提高药物制剂的生产水平,本文以自制的带加热套的高速搅拌制粒机对三种不同类型药物微丸的制备工艺、处方进行了较为全面的考察和研究。选取水溶性药物盐酸二甲双胍为模型药物,采用先制备含药骨架丸,再包缓释衣层的方法,最后得到缓释微丸。对其制备工艺、处方进行了优化,得出了最佳的参数。粘合剂用量20%、包衣材料为硬脂酸、包衣量为15%、制丸时间25min、制丸温度49℃℃,制备出了释放度较好的缓释微丸。对释药曲线进行药物动力学拟合,结果表明药物释放机制为non-Fickian扩散,所以药物的释放是扩散和溶蚀协同的作用机制。初步稳定性实验结果表明熔融法制备的缓释微丸在高温、高湿、强光照条件下基本稳定。选取脂溶性药物格列齐特为模型药,根据药物性质,先制备空白丸芯,对其包含药衣层后再包蜡质衣层。对其影响因素进行考察,最后确定乳糖用量40%,包衣材料为硬脂酸与硫酸钙,比例为1：1,包衣量40%,搅桨转速200rpm、搅拌时间25min、水浴温度50℃C、升温速率0.5℃/min。重复性实验结果表明以上处方、工艺可行可靠。参考前两章的研究结果,制备了酒石酸美托洛尔缓释微丸,通过正交设计对处方、工艺进行优化。最佳主要参数如下：包衣量15%、包衣比例2：1、制丸温度48℃、制丸时间15min,通过验证,该法制备的酒石酸美托洛尔缓释微丸工艺可靠,质量可控。本次实验制备了三种不同药物的缓释微丸,均达到了预期要求。可以看出,熔融高速搅拌法制备缓释微丸效果良好,为将来的工业化大生产提供了可行的参考。
[Abstract]:The preparation of sustained-release pellets by melt high speed agitation is a new method for the preparation of pellets. In recent years, more and more attention has been paid to the preparation of sustained-release pellets because of their high efficiency. The simplest way of mixing materials and heating, the solid binder melts into a liquid, and finally the pellets are formed by fully mixing and colliding. The preparation of pellets by melting high speed agitation has been reported in foreign literature. In order to provide the basis for production and improve the production level of pharmaceutical preparations, In this paper, the preparation process of three different kinds of drug pellets was investigated and studied with a self-made high speed agitating granulator with a heating sleeve. The water-soluble metformin hydrochloride was used as the model drug. The drug skeleton pill was prepared first and then the sustained-release layer was encapsulated. Finally, the sustained-release pellets were obtained. The preparation process was optimized and the optimum parameters were obtained. The coating material was stearic acid, the coating amount was 15%, the preparation time was 25 min, the preparation temperature was 49 鈩，
本文编号：2149501
[Abstract]:The preparation of sustained-release pellets by melt high speed agitation is a new method for the preparation of pellets. In recent years, more and more attention has been paid to the preparation of sustained-release pellets because of their high efficiency. The simplest way of mixing materials and heating, the solid binder melts into a liquid, and finally the pellets are formed by fully mixing and colliding. The preparation of pellets by melting high speed agitation has been reported in foreign literature. In order to provide the basis for production and improve the production level of pharmaceutical preparations, In this paper, the preparation process of three different kinds of drug pellets was investigated and studied with a self-made high speed agitating granulator with a heating sleeve. The water-soluble metformin hydrochloride was used as the model drug. The drug skeleton pill was prepared first and then the sustained-release layer was encapsulated. Finally, the sustained-release pellets were obtained. The preparation process was optimized and the optimum parameters were obtained. The coating material was stearic acid, the coating amount was 15%, the preparation time was 25 min, the preparation temperature was 49 鈩，
本文编号：2149501
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