波生坦片的制备

Preparation of Bosentan Tablet

目的优化波生坦片的制剂处方,以解决波生坦溶出度不高,制剂不稳定的共性难题。方法采用湿法制粒后压片的工艺,以片剂的性状、溶出度、有关物质、晶型稳定性等为评价指标,比较不同处方制得的波生坦片,并与原研药相比较。结果优化后的处方制得的波生坦片,片面光洁美观,溶出效果好,晶型稳定,有关物质符合要求,且溶出行为和质量与原研药一致。结论该新处方增加了波生坦的溶出度,提高了制剂晶型的稳定性,制剂质量与原研药一致,且制备方法简单、可行、易于实现产业化大生产,值得推广。

OBJECTIVE To optimize the prescription of bosentan tablet, and in order to solve the common problem of dissolution and chemical stability. METHODS Tablets characters, dissolution, related substance and stability of crystal was used as the research index to compare the methods of preparating Bosentan tablet including original drugs, so as to get optimized method. RESULTS The tablets made by the best method （as tabletting after wet granulation after optimization） were one sided smooth and had beautiful appearance, high solubility, stable crystal and related substance according to requirement, especially the solubility activity and quality being compliant with original drug. CONCLUSION The new method can solve the problem of dissolution and chemical stability, can get tablets excellent quality of original drug, being simple and feasible to realize industrial production.