5-氟尿嘧啶直肠温敏胶膜剂的制备

Preparation of 5-Fluorouracil Rectal Thermosensitive Gelling Film

目的：制备5-氟尿嘧啶（5-FU）直肠温敏胶膜剂。方法：以泊洛沙姆407（P407）和泊洛沙姆188（P188）为温敏材料制备5-FU直肠温敏胶膜剂,以溶液-凝胶的相变温度、凝胶强度、生物黏附力为指标,对温敏材料的比例、5-FU质量浓度、p H、生物黏附剂种类进行筛选。结果：以P407-P188（17∶2.5）为温敏材料,2%卡波姆940为生物黏附剂,p H为7.1,制得规格为500 mg/30 ml的5-FU温敏凝胶剂。所制凝胶在室温下为自由流动的液体,在生理条件下相变形成胶膜,相变温度为35-36.6℃,凝胶强度为20-60 g,生物黏附力为20-100 g,均符合直肠应用要求。结论：成功制得5-FU直肠温敏胶膜剂。

OBJECTIVE： To prepare 5-fluorouracil （5-FU） rectal thermosensitive gelling film. METHODS： Poloxamer 407 （P407） and Poloxamer 188 （P 188） were used as thermosensitive film matrix. Using solution-gelation phase-transition temperature, gel density and bioadhesive force as index, the proportion of thermosensitive material, 5-FU concentration, pH and type of biologi- cal adhesive were screened. RESULTS： Using P407-P188 （17：2.5）as thermosensitive material, 2% carbomer 940 as biological adhesive, setting pH at 7.1, 5-FU thermosensitive gel （500 rag/30 ml） was prepared. The prepared gel was free-flowing liquid at room temperature, and converted to glue film under physiological condition; phase-transition temperature was 35-36.6 ℃, gel density was 20-60 g and bioadhesive force was 20-100 g; all of these were in line with the requirements. CONCLUSIONS： 5-FU rectal thermosensitive gelling film is prepared successfully.