Method for preparing Ftorafur-loaded vesicle
A technology of tegafur and vesicles, which is applied in the field of preparation of tegafur-loaded vesicles, can solve the problems of low bioavailability of oral preparations and increased difficulty in clinical application of tegafur, and achieve enhanced inhibition of cancer cell proliferation and differentiation ability, strong cell proliferation inhibition ability and cell cycle inhibition ability, and the effect of prolonging the biological half-life
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Embodiment 1
[0034] Example 1: Synthesis of single [6-deoxy-N-butylamino]-β-cyclodextrin
[0035] Add 2.578g (2mmol) of mono[6-p-toluenesulfonyl]-β-cyclodextrin to 40ml of anhydrous N-methylpyrrolidone at room temperature, stir until completely dissolved, then add 0.264g (3mmol) of 1 , 4-butanediamine, add 2 drops of triethylamine as a catalyst, the mixture was stirred at 70oC for 10 hours, and the reaction progress was detected by thin-layer chromatography. After the reaction is complete, cool the reaction solution to room temperature, pour the reaction solution into 50ml of acetone to produce a large number of white particles, filter with suction, wash the filter cake 3 times with acetone, and collect the mono[6-deoxy-N-butylamino ]-β-cyclodextrin crude product.
[0036] The above cyclodextrin derivatives were separated and purified by silica gel chromatography (eluents were isopropanol, water and 30% ammonia water, the volume ratio was 5:2:1), and mono[6-deoxy-N-butyl Amino]-β-cyclode...
Embodiment 2
[0040] Example 2: Preparation of tegafur-loaded vesicles
[0041] Dissolve 0.241 g of mono[6-deoxy-N-butylamino]-β-cyclodextrin in 100 ml of triple distilled water at room temperature and sonicate for 3 minutes to obtain 2×10 -3 mol / L mono[6-deoxy-N-butylamino]-β-cyclodextrin solution; 0.04g tegafur was dissolved in 100ml triple distilled water at room temperature, and ultrasonicated for 3 minutes to obtain 2×10 -3 mol / L tegafur solution.
[0042] Take 25ml2×10 -3 mol / L mono[6-deoxy-N-butylamino]-β-cyclodextrin solution and 25ml2×10 -3 The mol / L tegafur solution was prepared into a 50ml mixed solution, which was sonicated for 30 minutes to obtain an aqueous solution of tegafur-loaded supramolecular vesicles.
Embodiment 3
[0043] Example 3: Preparation of tegafur-loaded vesicles
[0044] According to the ratio of 1.1g:1L, the purified mono[6-deoxy-N-butylamino]-β-cyclodextrin was dissolved in three times distilled water, and ultrasonically mixed for 2 minutes to prepare mono[6-deoxy-N- -Butylamino]-β-cyclodextrin solution; Tegafur was dissolved in triple distilled water at a ratio of 0.1g:1L, and ultrasonically mixed for 2 minutes to prepare a Tegafur solution;
[0045] Mix the above tegafur solution with the mono[6-deoxy-N-butylamino]-β-cyclodextrin solution at a ratio of 1:1 by volume, and mix ultrasonically for 20 minutes at 25±1°C to obtain an average Tegafur-loaded vesicles with a diameter of 200 ± 10 nm.
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