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A kind of small molecule gel and preparation method and solid-liquid interconversion gel preparation for gynecology

A technology of molecular gels and gel preparations, applied in the field of gynecological pharmaceuticals, can solve the problems of unsatisfactory stability of small molecule gels, uneven distribution of drugs, poor stability of raw materials, etc., and achieve good application prospects, solid- Strong liquid interconversion ability and good stability

Active Publication Date: 2022-07-19
SHAANXI UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Vaginal administration is a very important route of administration for the treatment of gynecological diseases. Commonly used clinical dosage forms include gel preparations, solid dosage forms, and liquid preparations. The currently used vaginal gel preparations are composed of macromolecular gelling agents. After administration for a certain period of time, the matrix of the macromolecular gelling agent needs to be pulled out from the body, causing inconvenience; for solid dosage forms, such as vaginal suppositories, vaginal tablets, vaginal effervescent tablets, vaginal capsules, etc., the matrix of this type of dosage form needs to be Extracted from the body, it is also prone to the problem of uneven distribution of drugs; solutions, such as lotions, sprays, etc., such drugs are easy to distribute evenly, but they are easy to lose
[0003] In the invention patent application with the publication number CN 107417758A and the invention title "A small molecule gel for ear drops and its preparation method and application", a series of small molecule gels were prepared using cholesteryl chloroformate as raw material. Gel, but the stability of the raw materials used is poor, and the stability of the obtained small molecule gel is not ideal in alkaline environment, so that its application in alkaline environment is limited to a certain extent

Method used

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  • A kind of small molecule gel and preparation method and solid-liquid interconversion gel preparation for gynecology
  • A kind of small molecule gel and preparation method and solid-liquid interconversion gel preparation for gynecology
  • A kind of small molecule gel and preparation method and solid-liquid interconversion gel preparation for gynecology

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029]

[0030] 1. Etherification reaction

[0031] Into a round-bottomed flask were added 100 mL of ether, 19.32 g (0.05 mol) of cholesterol (compound 1-1), 6.49 g (0.055 mol) of propylene glycol monoacetate (compound 2-1), and 7.63 mL of 46.5% triacetate The ether solution of boron fluoride (0.025mol) was refluxed at 34°C for 8 hours. After the reaction, 100 mL of water was added, and ether was recovered. Using petroleum ether as the eluent, the product was separated and purified by silica gel column chromatography to obtain 19.46 g of compound 3. -1, 80% yield.

[0032] 2. Hydrolysis reaction

[0033] 100 mL of ethanol, 14.59 g (0.03 mol) of compound 3-1, 1.32 g (0.033 mol) of NaOH were added to the round-bottomed flask, and the reaction was carried out under reflux at 78°C for 4 hours. After the reaction, 100 mL of water was added, and ether was recovered to obtain 12.67 g of compound 4. -1, 95% yield.

[0034] 3. Bromination reaction

[0035] 50mL of ether, 8.88g (...

Embodiment 2

[0039] In step 4 of this example, equimolar 6-hydroxyflavone was used to replace the 7-hydroxycoumarin in step 4 of Example 1, and other steps were the same as in Example 1, and 6.23g of the small compound shown in formula 7-2 was obtained. Molecular gelling agent, yield 90%, total yield 65%.

[0040]

[0041] The structural characterization data of the obtained small molecule gelling agent are: 1 H NMR (CDCl 3 ,TMS):8.11-8.09(2H,d,J=6.11Hz),7.69(1H,d,J=8.05Hz),7.65(1H,s),7.61(3H,m),7.37-7.39(1H, d, J=3.05Hz), 7.30-7.27 (1H, dd, J=8.05Hz, J=3.05Hz), 5.37 (1H, s), 3.88-3.87 (2H, t), 3.50 (3H, m), 2.27-2.28(2H,m), 2.07-2.08(2H,m), 0.67-1.85(41H); 13C NMR (CDCl 3 ): 176.9,162.1,154.8,149.3,140.8,131.5,131.3,129.1,128.8,126.1,124.2,123.0,120.0,107.4,105.8,72.0,65.1,56.4,42.7,40.1,3,126.1,37.0 28.0, 24.4, 22.8, 21.0, 19.1, 18.5, 11.2.

Embodiment 3

[0043] In step 1 of this example, the cholesterol in step 1 of Example 2 was replaced with equimolar β-sitosterol, and other steps were the same as those of Example 2, to obtain a small molecule gelling agent represented by formula 7-3, and the total yield was 64%.

[0044]

[0045] The structural characterization data of the obtained small molecule gelling agent are: 1 H NMR (CDCl 3 ,TMS):8.11-8.09(2H,d,J=6.11Hz),7.69(1H,d,J=8.05Hz),7.65(1H,s),7.61(3H,m),7.37-7.39(1H, d, J=3.05Hz), 7.30-7.27 (1H, dd, J=8.05Hz, J=3.05Hz), 5.37 (1H, s), 3.88-3.87 (2H, t), 3.50 (3H, m), 2.27-2.28(2H,m), 2.07-2.08(2H,m), 0.67-1.85(45H); 13 C NMR (CDCl 3 ):176.9,162.1,154.8,149.3,140.8,131.5,131.3,129.1,128.8,126.1,124.2,123.0,120.0,107.4,105.8,72.0,65.1,56.4,46.0,42.7,4,1,1,37.0 28.0, 24.4, 23.4, 22.8, 21.0, 19.1, 18.5, 12.1, 11.2.

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Abstract

The invention discloses a small-molecule gel, a preparation method and a solid-liquid interconversion gel for gynecology. The small-molecule gel contains structural units such as sterols, flavonoids or coumarin in its structure, and undergoes an esterification reaction. , etherification reaction and other classical reaction synthesis. The small-molecule gel preparation of the invention has good stability, can exist stably in an acid-alkaline environment, and has strong gelling ability, and can be compounded with gynecological drugs to prepare a solid-liquid interconversion gel preparation for gynecology. The preparation can evenly distribute the entire cavity, and has the advantages of simple preparation, convenient administration, prevention of loss of medicinal liquid, good safety and low cost.

Description

technical field [0001] The invention belongs to the technical field of gynecological medicaments, in particular to a small molecular gel, a preparation method of the small molecular gel, and a gynecological solid-liquid interconversion gel preparation prepared by using the small molecular gel. Background technique [0002] Vaginal administration is a very important route of administration for the treatment of gynecological diseases. Commonly used clinical dosage forms include gel preparations, solid dosage forms, and liquid preparations. The currently used vaginal gel preparations are composed of macromolecular gelling agents. After a certain period of administration, the macromolecular gelling agent matrix needs to be pulled out from the body, causing inconvenience; for solid dosage forms, such as vaginal suppositories, vaginal tablets, vaginal effervescent tablets, vaginal capsules, etc. It is also prone to the problem of uneven distribution of drugs when extracted from th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K47/32A61P15/00A61P15/02C07J17/00
CPCA61K47/32A61P15/00A61P15/02A61K9/0034A61K9/06C07J17/00
Inventor 姜祎徐虹郭敏宋小妹邓翀张化为冯改利
Owner SHAANXI UNIV OF CHINESE MEDICINE