替米考星固体分散体的制备与物相鉴定

Preparation and phase identification of tilmicosin solid dispersion

关键词:  替米考星  联合载体  固体分散体  溶出度

Key words:  Tilmicosin  Combined carrier  Solid dispersion  Dissolution

摘要:

为改善替米考星的水溶性，提高其生物利用度，试验选用聚乙二醇6000和泊洛沙姆188作为载体，采用熔融法制备替米考星固体分散体。以体外累积溶出度为评价指标，通过正交试验筛选最佳制备工艺，选用X-射线衍射法、傅里叶红外光谱法、扫描电镜法进行物相鉴定。结果显示，替米考星固体分散体最佳制备工艺为联合载体PEG6000：P188=20:1、药载比1:3、搅拌时间1 h、固化时间12 h；物相鉴定表明，替米考星为非晶态，固体分散体为晶体结构，替米考星以无定形态分散于载体中；替米考星固体分散体在2 min时溶出度达到71.8%，15 min时完全溶解，显著提高了替米考星的溶出速率。该制备工艺简单，选用联合载体制备替米考星固体分散体，能够有效避免单一载体制备替米考星固体分散体出现的缺陷，有效提高溶出度，方便临床饮水用药。

Abstract:

In order to improve the water solubility and bioavailability of tilmicosin, the solid dispersion of tilmicosin was prepared by melting method using PEG6000 and P188 as the carrier. Taking the accumulated dissolution in vitro as the evaluation index, the optimum preparation process was screened by orthogonal test. X-ray diffraction method, Fourier transform infrared spectroscopy and Scanning electron microscopy were used to identify the solid dispersion.The results showed that optimal preparation process of solid dispersion of tilmicosin were combined carrier PEG6000:P188=20:1, tilmicosin:carrier =1:3, the stirring time was one hour and the curing time was 12 hours.The phase identification showed that tilmicosin was amorphous and the solid dispersion was crystal structure.Tilmicosin was dispersed in the carrier in an amorphous form.The dissolution rate of tilmicosin solid dispersion reached 71.8% at 2 min.It was completely dissolved at 15 min, which significantly improved the dissolution rate of tilmicosin.The preparation process is simple, and the combined carrier is used to prepare the solid dispersion of tilmicosin, which can effectively avoid the defects of the solid dispersion of tilmicosin prepared by a single carrier, effectively improve the dissolution and facilitate the clinical use of drinking water.