5-氨基水杨酸结肠定位双层包衣微丸的制备

 目的 制备5-氨基水杨酸（5-ASA）果胶壳聚糖聚电解质复合物（PEC）-尤特奇结肠定位双层包衣微丸。方法 扩散实验考察PEC膜对传递系统释药速率的影响；考察PEC包衣微丸在大鼠盲肠内的生物降解性；考察膜溶胀性与阻滞释药能力和生物降解性的关系；制备双层包衣微丸并验证其结肠定位性能。结果 扩散实验表明，在模拟小肠液中阻滞释药能力较强的3种处方为：A、果胶-壳聚糖Ⅰ=3∶1， B、果胶-壳聚糖Ⅰ-HPMC=2∶1∶1，C、果胶-壳聚糖Ⅱ=2∶1；膜降解实验表明PEC包衣微丸能被结肠微生物菌群所降解；溶胀实验显示，膜溶胀比与包衣微丸的释药速率和降解性之间不存在线性关系；模拟胃肠道传输的体外释药实验显示，PEC-尤特奇双层包衣微丸有效地在小肠中阻滞药物释放，在结肠中释药较快，具备双模式的释药特征。结论 5-ASA果胶壳聚糖PEC-尤特奇结肠定位双层包衣具有双模式的释药特征，具有良好的结肠定位性能。

Preparation of 5-Aminosalicylic Acid Donble Coated Colon-specific Pellets

OBJECTIVE To investigate the in vitro and in vivo effects of α-anordrin（α-Ano）on androgen-dependent and androgen-independent human prostate cancer， and compare the effect difference between them. METHODS SRB staining was applied to investigate the suppression effect of α-Ano on androgen-dependent human prostate cancer cells(LNCaP， RV1 and L1A) and androgen-independent cells （DU145 and PC-3）. Athymic nude mice were subcutaneously inoculated with cells suspension to construct transplantation tumor model. After intragastric administration with α-Ano， the volume of tumor was measured and the suppression rate of the drug to the proliferation of solid tumor was calculated. RESULTS After being treated by α-Ano， the survival of LNCaP， RV1 and L1A were lower than that of DU145 and PC-3. α-Ano significantly inhibited the RV-1 xenografts tumor growth at high and low concentration， but retarded PC-3 xenografts tumor growth tenderly. α-Ano exhibited inhibition effect on PC-3 xenografts tumor at high concertration， whereas no effect at low concentration. CONCLUSION The suppression effects of α-Ano on androgen-dependent human prostate cancer is stronger than that androgen-independent cancer.