壬苯醇醚栓的研制及体外溶出度的测定

 目的：为延长避孕有效时间研制一种新型壬苯醇醚栓，对其进行理化性质、稳定性及溶出度考察，并与市售的两种壬苯醇醚栓比较。方法：参考中国药典1990年版溶出度测定法项下条件，进行3种栓的体外溶出实验。采用UV三阶导数光谱法测定样品液浓度，计算累积溶出量。HPLC测定栓中壬苯醇醚的含量。室温留样法及加速实验法进行稳定性考察。结果：研制栓的T₅₀为99．30min，6h释放75％。国内市售栓T₅₀为7．85min，Encare栓T₅₀为15．31min，两者1h释放均达90％。壬苯醇醚栓室温存放一年，或37℃、相对湿度75％存放6个月，理化性质及含量无明显变化。结论：研制的壬苯醇醚栓有较好的稳定性，在有效时间方面优于Encare栓及国产市售栓。

Preparation and dissolution of novel nonoxynol－9 suppository

OBJECTIVE: Novel nonoxynol-9 contraceptive suppositories were prepared for prolonging effectiveness. The stability of the nonoxynol-9 suppositories was examined. The dissolution rate of prepared suppository was compared with two commercial nonoxynol-9 suppositories. METHODS: The dissolution rate of the suppositories was tested according to the experimental condition of dissolution rate test in China Pharmacopoeia (1990 a edition) by UV spectrophotometry and the content of the suppository was determined by HPLC. RESULTS: T₅₀ of dissolution rat for commercial suppositories were 7.85 min and 15.31 min respectively. 75% of the novel suppository was dissolved within 6 hours, but commercial suppositories were dissolved by 90% within 1 hour. The content and physicochemical quality were not changed significantly after storing up to one year under room temperature. CONCLUSION: The effective duration of novel suppository is longer than commercial suppositories and the novel suppositories are stable.