紫杉醇透明质酸注射用冻干制剂的研究

 目的 开发一种紫杉醇透明质酸的新型高效低毒注射剂。方法 对新型制剂的处方组成、制备工艺及稳定性进行了研究考察,制备了新的注射用固体制剂。并对该制剂的体内外活性进行了考察。结果 以透明质酸为基质的紫杉醇新制剂稳定性良好;对荷U14宫颈癌和S180肉瘤小鼠的抑瘤率、小鼠存活期、体重均优于原制剂。结论 以透明质酸为基质的紫杉醇新制剂可以降低原制剂的毒性,提高紫杉醇的治疗效果。

Study on the preparation of paclitaxel freeze-dried product for injection using hyaluronan as the base

OBJECTIVE To develop a new preparation of paclitaxel using hyaluronan as the base with high efficacy and low toxitci-ty.METHODS The new injections were prepared by freeze-drying.The optimal formultion and processing technology were chosen.The stability of the product was investigated by conventional stability study. The antitumor effect in vivo and increased life span (ILS) were observed . RESULTS The freeze-dried preparation was physically stable at ambient temperature. The inhibition of tumor-growth and ILS on S180 cell and U14 cervix cancer cell of the new preparation were significantly superior to those of the control preparation. CONCLUSION The adverse effect was reduced and the efficacy of the new paclitaxel preparation based on HA was obviously improved.