环磷酰胺微乳制剂的研制

Study on the preparation of cyclophosphamide microemulsion

目的 :研究环磷酰胺微乳的制备、稳定性及微乳中药物含量的测定方法。方法 :选用油酸正丁酯和肉豆蔻酸异丙酯作为油相 ,聚山梨醇酯作为表面活性剂 ,正丁醇和正戊醇作为助表面活性剂 ,在制备三元相图的基础上 ,考察微乳的组分对微乳形成的影响 ;用HPLC法测定微乳中环磷酰胺的含量。结果 :以聚山梨醇酯为乳化剂形成的微乳系统所需表面活性剂的量为 13.6 2 %～ 40 .5 2 % ;用HPLC法测定两种破乳剂对环磷酰胺微乳破乳后 ,环磷酰胺的含量分别为 (10 .6± 1.1)mg·L-1和(10 .4± 1.1)mg·L-1,两结果差异无显著性 (P >0 .0 5 )。结论 :采用微乳作为药物载体制备口服环磷酰胺微乳 ,为开发环磷酰胺新型口服制剂提供了依据。

OBJECTIVE To study the preparation process, stability determination method for oral microemulsion containing cyclophosphamide. METHODS On the basis of the triangular phase diagrams, the effect of various elements on the formation of the micromulsionswas investigated. HPLC method was chosed to determine the concentration of cyclophosphamide.RESULTS In the microemulsion of Tween-20 systems, the amount of emulsifier was 13.62%～ 40.52%.The content of cyclophosphamide, using two methods, were ( 10.58± 1.07) mg·L -1 and ( 10.43± 1.11) mg·L -1 respectively.CONCLUSIONS The cyclophosphamide microemulsion delivery could be prepared using tween-20/n-Butanol/n-Butyl oleate/water system and the tween-20/i-pentanol/IPM/water system. A new formulation for cyclophosphamide is developed.