缬沙坦/硅胶固体分散体的制备和物理稳定性研究

Preparation of valsartan/silica gel solid dispersion and its physical stability

目的制备缬沙坦（valsartan,VAL）/硅胶的固体分散体并进行性质研究。方法利用溶剂蒸发沉淀法制备VAL/硅胶固体分散体,通过溶出试验筛选确定制备方法,通过溶出试验、加速试验、差示扫描量热（DSC）和X-射线粉末衍射（XRD）等方法考察药物溶出行为、药物存在状态及物理稳定性。结果确定固体分散体的较优制备方法,载药量为23%~31%,30 min内药物的累计溶出超过90%,药物以非晶状态存在,加速试验证明VAL/硅胶固体分散体溶出和存在状态稳定。结论 VAL/硅胶固体分散体载药量较高,物理稳定性良好,明显提高了药物溶出速率。

Objective To prepare valsartan/silica gel solid dispersion and determine the basic characteristics of the solid dispersion. Methods The solid dispersions were prepared by solvent evaporation and precipitation method. A premium condition of preparing the solid dispersion was determined by screening dissolution of preparations. The dis- solution behaviors, drug state in the dispersion, and its stability were examined by dissolution test, acceleration test, differential scanning calorimetry and X-ray diffraction. Results The solid dispersion was prepared, the drug loading was about 23% -- 31%, the drug release within 30 min exceeded 90%, the dispersion was in amorphous state, and the stability of dissolution and state was proved by acceleration test. Conclusion The drug loading is high, valsartar/ silica gel solid dispersion is physically stable, and the dissolution is improved by solid dispersion.