Jian C H, Lin F H, Lee Y H
Department of Material Science Engineering, National Taiwan University.
Biomed Sci Instrum. 2000;36:391-6.
In the recent decade, the most useful drug for the therapy of colon cancer is 5-Fluorouracil(5-FU). It has been reported to have considerable toxicity administered by intravenous injections or via alimentary treat. Though many materials have developed for drug carrier of 5-FU, there was no clinically acceptable carrier for 5-FU till now. Montmorillonite, one of clay minerals, consists of hydrated aluminum silicates that are fined grained and usually have a large space between the layers. Isomorphous substitution of cations is common. We try to intercalate 5-FU into interlayer of montmorillonite through ion-exchange. Montmorillonite with 5-FU intercalation is expected to achieve in-situ release for colon cancer therapy. In the study, 5-FU was dissolved in 100 ml distilled water as 5-FU solution. Purified montmorillonite powder will soak in 5-FU solution for a period of time ad different pH value and temperature. The intercalated amount of 5-FU in montmorillonite is measured by scanning differential thermal (SDT) analysis and UV analysis. The results showed that 4 g purified montmorillonite soaked in 0.6% 5-FU solution for 2 hours had an optimum condition for intercalation. The total amount of 5-FU in montmorillonite is about 9.13 wt%.
在最近十年中，治疗结肠癌最有效的药物是5-氟尿嘧啶（5-FU）。据报道，通过静脉注射或经消化道给药时，它具有相当大的毒性。尽管已经开发出许多用于5-FU的药物载体材料，但迄今为止还没有临床上可接受的5-FU载体。蒙脱石是一种粘土矿物，由细颗粒的水合铝硅酸盐组成，层间通常有较大的空间。阳离子的同晶替代很常见。我们试图通过离子交换将5-FU插入蒙脱石的层间。含有5-FU插层的蒙脱石有望实现用于结肠癌治疗的原位释放。在该研究中，将5-FU溶解在100 ml蒸馏水中制成5-FU溶液。将纯化的蒙脱石粉末在不同pH值和温度下浸泡在5-FU溶液中一段时间。通过扫描差热（SDT）分析和紫外分析测定蒙脱石中5-FU的插层量。结果表明，4 g纯化的蒙脱石在0.6%的5-FU溶液中浸泡2小时具有最佳的插层条件。蒙脱石中5-FU的总量约为9.13 wt%。
