伊曲康唑自乳化液的制备及质量评价

Preparation and Quality Evaluation of Itraconazole Self-emulsifying Solution

目的:制备伊曲康唑自乳化液并对其进行质量评价。方法:通过溶解度试验,油相与各种乳化剂、助乳化剂的配伍选择筛选自乳化液的处方。考察该乳化液经水稀释后形成微乳的形态、粒径和Zeta电位,并测定载药量。结果:该自乳化液处方为油相维生素E醋酸酯,乳化剂TranscutolP,助乳化剂CremophorRH40,三者比例为3:12:5。微乳在透射电镜下呈球形,分布均匀,粒径为(296.1±90.7)nm,Zeta电位为(—13.2±1.6)mV,载药量为9.88%。结论:所制自乳化液质量稳定可靠。

OBJECTIVE： To prepare itraconazole self- emulsifying .solution and evaluate its quality. METHODS： Through equilibrium solubility experiment, the formulation of itraconazole self - emulsifying solution was obtained by optimizing the compatible ratio of oil phase with emulsifier and co - emulsifier. The morphology, particle size, zeta potential and drug loading content of the microemulsion were examined after being diluted by water. RESULTS： The formulation of the self- emulsifying solution was tocopherol acetate （oil phase） - Transcutol P （emulsifier） - Cremophor RH40 （co- emulsifier） （3 ： 12 ： 5）. The morphology of microemulsion was homogeneous small spherical drops observed under the electron microscope, with particle size and Zeta potential at （296.1 ±90.7） nm and （-13.2 ± 1.6） mV, respectively. The drug loading content was 9.88%. CONCLUSION： The itraconazole self-emulsifying solution was proved to be stable and reliable in quality.