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Preparation method of seven-membered Cucurbit[n]uril and capecitabine supramolecular inclusion compound

A technology for capecitabine and seven-membered cucurbit rings, which is applied in the field of preparation of supramolecular inclusion complexes between seven-membered cucurbit rings and capecitabine, and no research on the interaction between capecitabine and cucurbit rings has been reported , Inability to effectively form clathrates between the seven-membered melon ring and capecitabine, and achieve the effects of low cost, easy operation, and mild reaction conditions

Active Publication Date: 2018-05-29
GUIZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, although it has been reported that the use of cucurbits in drugs can improve the sustained release control and stability of drugs and other applications, there is no report on the interaction between capecitabine and cucurbits.
Because the conditions required for the formation of inclusion complexes between different drug molecules and cucurbit rings are different, the seven-membered cucurbit rings and capecitabine cannot effectively form inclusion complexes according to general methods. Therefore, we specially designed a A method suitable for forming inclusion complexes between capecitabine drug molecules and cucurbit rings

Method used

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  • Preparation method of seven-membered Cucurbit[n]uril and capecitabine supramolecular inclusion compound
  • Preparation method of seven-membered Cucurbit[n]uril and capecitabine supramolecular inclusion compound
  • Preparation method of seven-membered Cucurbit[n]uril and capecitabine supramolecular inclusion compound

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Embodiment 1

[0034] Embodiment 1: A kind of preparation method of supramolecular inclusion compound of seven-membered cucurbit ring and capecitabine, the molecular formula of supramolecular inclusion compound is: C 57 h 64 N 31 o 20 F, the structural formula is attached figure 1 shown.

[0035] Its preparation method concrete steps are as follows:

[0036] 1) Mix the seven-membered melon ring and capecitabine at a molar ratio of 1:1, and then add distilled water to prepare a concentration of 4.0×10 -5 mol / L mixed solution to obtain product A;

[0037] 2) Heat product A to 50°C while stirring, and react for 3 hours to obtain product B;

[0038] 3) Cool product B to room temperature until a colorless and transparent solution is obtained, that is, the seven-membered cucurbitanyl-capecitabine supramolecular drug inclusion complex solution.

Embodiment 2

[0039] Embodiment 2: A kind of preparation method of seven-membered cucurbit ring and capecitabine supramolecular inclusion compound, the molecular formula of supramolecular inclusion compound is: C 57 h 64 N 31 o 20 F, the structural formula is attached figure 1 shown.

[0040] Its preparation method concrete steps are as follows:

[0041] 1) Mix the seven-membered melon ring and capecitabine at a molar ratio of 2:1, and then add distilled water to prepare a concentration of 4.0×10 -5 mol / L mixed solution to obtain product A;

[0042] 2) Heat product A to 45°C while stirring, and react for 4 hours to obtain product B;

[0043] 3) Cool product B to room temperature until a colorless and transparent solution is obtained, that is, the seven-membered cucurbitanyl-capecitabine supramolecular drug inclusion complex solution.

Embodiment 3

[0044] Embodiment 3: A kind of preparation method of supramolecular inclusion compound of seven-membered cucurbit ring and capecitabine, the molecular formula of supramolecular inclusion compound is: C 57 h 64 N 31 o 20 F, the structural formula is attached figure 1 shown.

[0045] Its preparation method concrete steps are as follows:

[0046] 1) Mix the seven-membered melon ring and capecitabine at a molar ratio of 5:1, and then add distilled water to prepare a concentration of 4.0×10 -5 mol / L mixed solution to obtain product A;

[0047] 2) Heat product A to 55°C while stirring, and react for 2 hours to obtain product B;

[0048] 3) Cool product B to room temperature until a colorless and transparent solution is obtained, that is, the seven-membered cucurbitanyl-capecitabine supramolecular drug inclusion complex solution.

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Abstract

The invention discloses a preparation method of a seven-membered Cucurbit[n]uril and capecitabine supramolecular inclusion compound. The method comprises steps as follows: seven-membered Cucurbit[n]uril and capecitabine are added to distilled water to be mixed, a mixed solution is prepared, the mixed solution is heated to 45-55 DEG C until reaction is complete, then cooling is performed, and the seven-membered Cucurbit[n]uril and capecitabine supramolecular inclusion compound is obtained. The seven-membered Cucurbit[n]uril and capecitabine supramolecular inclusion compound can be prepared withthe method, the controlled slow-release effect of capecitabine pharmaceutical molecules in a human body is improved, besides, the preparation method is simple, and cost is lower.

Description

technical field [0001] The invention relates to a preparation method of a supramolecular inclusion compound, in particular to a preparation method of a supramolecular inclusion compound of a seven-membered cucurbit ring and capecitabine. Background technique [0002] Cucurbit[n]uril, also known as cucurbit[n]uril, (abbreviated as CB[n] or Q[n], named for its structure resembling a pumpkin, is a macrocyclic compound following crown ether, cyclodextrin and calixarene. Another new type of cage-like host compound after that. From a structural point of view, the melon ring has a hydrophobic cavity and two ends are covered with polar carbonyl oxygen atoms. This structure is conducive to the melon ring in the solution state. Use electrostatic forces, hydrogen bonds, hydrophobic effects, π-π stacking or charge transfer interactions to selectively include organic small molecules of appropriate size, biomacromolecules, or interact with dipolar or ionic compounds at the port. Aqueous ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/7068A61P35/00
CPCA61K31/7068
Inventor 肖昕王海燕陈青
Owner GUIZHOU UNIV
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