结晶天花粉蛋白脂质体的物理性质与止孕活性

改良乳化法制备的天花粉蛋白脂质体(TPL)包封率为33.0～40.80%,药物回收率为95.15～99.58%。以650nm测定天花粉蛋白含量,可完全排除类脂吸收峰的干扰。TPL粒度多介于1～2μm之间(占96.9%)。首次采用γ射线辐射TPL样品,经4℃,⁶⁰Co照射90 min,可完全达到无菌。实验证实,在4℃,25℃与37℃下保存的TPL样品,具有较好的稳定性,室温贮存38 d的TPL样品,药物渗漏率为15.22%。过敏实验表明,TPL仍有一定的致敏性,但反应轻微。溶血与凝血试验显示,TPL用药较为安全。动物止孕实验证明,小鼠腹腔注入8μgTPL混悬液,其抗早孕率为83.3%,由此表明TPL有明显的抗早孕活性。本研究提示,TPL可望成为抗早孕药物新剂型。

THE PHYSICAL PROPERTIES, PHARMACOLOGY AND ANTIFERTILITY ACTION OF CRYSTAL TRICHOSANTHIN PROTEIN LIPOSOME

The crystal trichosanthin protein liposome (TPL) was prepared by an emulsionforming method. The rate of entrapment was 33. 0～44.8% and the rate of recovery was 95. 15～99. 58%. The determination of trichosanthin protein was accomplished by spectrophotometry at 650nm, thus eliminating completely the interference of lipids. The distribution of particle size of TPL was mainly in the range of 1～2 μm (96. 9% ). TPL was sterilized by ⁶⁰Co radiation at 4℃ for 90 min and was stable when stored at 4℃, 25℃ and 37℃. The seepage rate of trichosanthin from the liposome was 15.22% after storage for 38 days at room temperature. Experiments showed that TPL had a slight allergic reaction, but was safe by hemolysis and coagulation tests. When the mice were given TPL ip 8 μg per animal 6 days after pregnancy, the rate of termination of early pregnancy was 83. 3%. It thus appears that TPL can terminate early pregnancy in mice distinctly. This indicates that TPL may be expected to be developed into a new type of anti--early pregnancy preparation.