两层基质性质不同的阿司匹林上下双层栓剂的制备工艺探讨

STUDY ON THE PREPARATION OF ASPIRIN DOUBLE-LAYER SUPPOSITORY WITH DIFFERENT UPPER AND LOWER SUBSTRATE

目的为了有效阻止传统阿司匹林肛门栓剂所释放药物向上扩散,避免部分药物经门肝系统吸收,提高阿司匹林的生物利用度,研制了阿司匹林上下双层栓剂,并考察其上下两层基质性质不同时的制备工艺。方法用脂溶性基质混合脂肪酸甘油脂制备阿司匹林双层栓剂的下层含药层,用水溶性基质制备阿司匹林双层栓剂上层空白层。考察了空白层处方对空白层的融变时限、成栓性能与两层结合处牢固程度的影响。结果空白层处方为PEG4000(1.4 g),PEG1000(2.6 g),CMC-Na(1 g),Tween-80(0.5m L),胭脂红(适量),水(0.5 m L)。制备的双层栓融变时限合格、成栓性能良好、两层结合处牢固。结论所研制的双层栓的外观美观,工艺简单易行。

Objective： In order to effectively prevent the drug released by the traditional aspirin suppository to spread upward, and avoid the hepatic portal system absorbing part of the drug, improve the bioavailability of aspirin, aspirin suppository with double layer were prepared, and the preperation process was investigated for two layer substrates with different nature.Methods：Under drug layerofaspirin double-layer suppository was prepared by using fat soluble substrates mixed with fatty acid glyceride, and upper space layer was prepared by using water soluble substrates. The effects of the prescription of blank layer on its melting time, forming plug performance and the fastness degree of two layers were explored.Results：The prescriptionof blank layer included PEG4000（1.4 g）, PEG1000（2.6 g）, CMC-Na （1 g）, tween-80（0.5 mL）, carmine （moderate）, water （0.5 mL）.Conclusion： The prepared double-deck has beautiful appearance, simple and easy process.