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本文建立了一个对环磷酰胺(cyclophosphamide以下简称CP)具有较高包封率、制备过程中CP水解程度最小、其重建型(冻干态)能长期贮存的CPL制备新工艺—SLV(sonication—lyo philization—vesicle)法。制备过程中CP的损失量为4.34%。CP的包封率达50%以上。MPVⅢ—TAS显微分光图象仪对重建的CPL(CPRL)的粒度测定表明,平均粒径为0.689μm。CPRL的LD_(50)以及对S_(180),EAC,LL三个瘤株的抑瘤结果显示,CPRL降低了CP的毒性、提高了其抑瘤活性。
In this paper, we established a new process of CPL preparation with high entrapment efficiency for cyclophosphamide (CP) and CP hydrolysis in the preparation process, and long-term storage in reconstructed (lyophilized) -SLV (sonication- lyo philization-vesicle) method. The loss of CP during preparation was 4.34%. CP encapsulation rate of 50% or more. The particle size determination of the reconstructed CPL (CPRL) by the MPV III-TAS microscope showed that the average particle size was 0.689 μm. The LD50 of CPRL and the antitumor effects on S 180, EAC and LL tumor strains showed that CPRL reduced CP toxicity and increased its antitumor activity.