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Pyrrolidinyl diaminopyrimidine oxide bata-cyclodextrin-based clathrate compound and preparation method thereof

A technology of pyrrolidinyl diaminopyrimidine and cyclodextrin, which is applied in the field of clathrates and their preparation, can solve problems that have not been reported in literature, and achieve the effects of no toxic side effects, improved solubility, and mild conditions

Inactive Publication Date: 2018-06-29
SHANGHAI INST OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are many cyclodextrin inclusion complex products on the market, but there are no literature reports and related patents on cyclodextrin inclusion complexes of pyrrolidinyl diaminopyrimidine oxides

Method used

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  • Pyrrolidinyl diaminopyrimidine oxide bata-cyclodextrin-based clathrate compound and preparation method thereof
  • Pyrrolidinyl diaminopyrimidine oxide bata-cyclodextrin-based clathrate compound and preparation method thereof
  • Pyrrolidinyl diaminopyrimidine oxide bata-cyclodextrin-based clathrate compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] (1) Preparation of hydroxypropyl-β-cyclodextrin (HP-β-cyclodextrin) aqueous solution: Weigh 6 grams of HP-β-cyclodextrin and 20 ml of deionized water to prepare HP-β-cyclodextrin aqueous solution , using a magnetic stirrer to stir at room temperature to obtain a clear HP-β-cyclodextrin aqueous solution.

[0039] (2) Weigh 0.7598 g of pyrrolidinyl diaminopyrimidine oxide and add it to HP-β-cyclodextrin aqueous solution, and under heating and vigorous stirring, obtain pyrrolidinyl diaminopyrimidine oxide HP-β-cyclodextrin Dextrin aqueous solution, add polyvinylpyrrolidone according to 1% of the mass of the above solution, add Kethon according to 0.02% of the mass of pyrrolidinyl diaminopyrimidine oxide HP-β-cyclodextrin aqueous solution, press pyrrolidinyl diamino 0.03% by mass of the pyrimidine oxide HP-β-cyclodextrin aqueous solution was added to iodopropynyl butyl carbamate, and mixed and stirred.

[0040] (3) Add acid regulator citric acid solution dropwise to adjust...

Embodiment 2

[0046] (1) Preparation of HP-β-cyclodextrin aqueous solution: 12 g of HP-β-cyclodextrin and 25 ml of deionized water were weighed and stirred at room temperature with a magnetic stirrer to obtain a clear HP-β-cyclodextrin aqueous solution.

[0047] 2) Weigh 0.7598 g of pyrrolidinyl diaminopyrimidine oxide, add it to HP-β-cyclodextrin aqueous solution, and obtain pyrrolidinyl diaminopyrimidine oxide HP-β-cyclodextrin under the condition of ultrasonic heating Aqueous solution, add polyvinyl alcohol according to 0.5% of the mass of the above mixed solution, add Kethon according to 0.04% of the mass of pyrrolidinyl diaminopyrimidine oxide HP-β-cyclodextrin aqueous solution, and oxidize according to pyrrolidinyl diaminopyrimidine Add iodopropynyl butyl carbamate to 0.03% of the mass of the HP-β-cyclodextrin aqueous solution, mix, heat and sonicate.

[0048] (3) Add acid regulator citric acid solution dropwise to adjust the pH value of the resulting solution.

[0049] (4) After the...

Embodiment 3

[0053] (1) Weigh 10 grams of HP-β-cyclodextrin and place it in a mortar, add an appropriate amount of deionized water, and stir with a mortar stick to make a paste.

[0054] (2) Weigh 0.3166 pyrrolidinyl diaminopyrimidine oxide, add polyvinylpyrrolidone according to 1% of pyrrolidinyl diaminopyrimidine oxide HP-β-cyclodextrin paste quality, press pyrrolidinyl diaminopyrimidine oxide Add 0.04% of the mass of aminopyrimidine oxide HP-β-cyclodextrin paste to Kethon, and add 0.03% of the mass of pyrrolidinyl diaminopyrimidine oxide HP-β-cyclodextrin paste to add iodopropyne Butyl butyl carbamate, pH adjuster citric acid solution was added to the paste.

[0055] (3) Grind the paste for 1 hour to obtain a uniformly mixed viscous paste.

[0056] (4) Put the obtained viscous paste into a drying oven to heat and dry to obtain a solid inclusion compound of pyrrolidinyl diaminopyrimidine oxide HP-β-cyclodextrin.

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Abstract

The invention relates to a pyrrolidinyl diaminopyrimidine oxide beta-cyclodextrin or / and beta-cyclodextrin derivative clathrate compound, and a preparation method thereof. The clathrate compound is prepared from beta-cyclodextrin or / and beta-cyclodextrin derivative, pyrrolidinyl diaminopyrimidine oxide, water-soluble polymer, pH adjuster, preservative, bacteriostatic agent and deionized water. The method comprises the steps: adding the beta-cyclodextrin or / and the beta-cyclodextrin derivative to the deionized water, then adding the pyrrolidinyl diaminopyrimidine oxide, the water-soluble polymer, the preservative and the bacteriostatic agent, stirring, ultrasonic mixing, adding the pH adjuster to adjust pH of a reaction solution obtain an aqueous solution of the pyrrolidinyl diaminopyrimidine oxide beta-cyclodextrin or / and beta-cyclodextrin derivative clathrate compound aqueous solution. According to the pyrrolidinyl diaminopyrimidine oxide beta-cyclodextrin or / and beta-cyclodextrin derivative clathrate compound, solubility of a water-insoluble and anti-off new hair pyrrolidinyl diaminopyrimidine oxide agent in an aqueous solution is improved, the clathrate compound has stable traits, has no toxic and side effects, and is mild in preparation conditions, simple in process and easy to control.

Description

technical field [0001] The present invention relates to an inclusion compound and its preparation method and application, especially a pyrrolidinyl diaminopyrimidine oxide β-cyclodextrin or / and β-cyclodextrin derivative inclusion compound and its preparation method and application. Background technique [0002] Pyrrolidinyl diaminopyrimidine oxide (Kopyrrol), chemical name 4-pyrrolidine 2,6-diaminopyrimidine 1-oxide. It is light white crystalline powder with a slight special smell, insoluble in water but easily soluble in propylene glycol solution. [0003] [0004] Pyrrolidinyl diaminopyrimidine oxide is a new type of hair growth promoter compound. By relaxing the blood vessels around the hair follicles, it provides the hair with the nutrients necessary for growth, thereby promoting the transformation of hair from the resting phase to the growing phase and keeping it longer growth phase, thereby promoting hair growth; as an active substance, it also has the effect of p...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/506A61P17/14
CPCA61K31/506
Inventor 张彦李星亮罗宽宽向迪袁军平
Owner SHANGHAI INST OF TECH
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