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Small-molecule gel, method for preparing same and gynecological solid-liquid mutual transformation type gel preparation

A molecular gel and gel preparation technology, applied in the field of gynecological pharmacy, can solve the problems of unsatisfactory stability of small molecule gel, uneven drug distribution, poor stability of raw materials, etc., and achieves good application prospects, solid- Strong liquid interconversion ability and good stability

Active Publication Date: 2019-01-04
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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  • Small-molecule gel, method for preparing same and gynecological solid-liquid mutual transformation type gel preparation
  • Small-molecule gel, method for preparing same and gynecological solid-liquid mutual transformation type gel preparation
  • Small-molecule gel, method for preparing same and gynecological solid-liquid mutual transformation type gel preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029]

[0030] 1. Etherification reaction

[0031] Add 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 tris The ether solution of boron fluoride (0.025mol) was refluxed at 34°C for 8 hours. After the reaction, 100mL of water was added to recover the ether, and petroleum ether was used as the eluent. The product was separated and purified by silica gel column chromatography to obtain 19.46g of compound 3 -1, yield 80%.

[0032] 2. Hydrolysis reaction

[0033] Add 100 mL of ethanol, 14.59 g (0.03 mol) of compound 3-1, 1.32 g (0.033 mol) of NaOH into a round bottom flask, reflux at 78°C for 4 hours, add 100 mL of water after the reaction, recover ether, and obtain 12.67 g of compound 4 -1, yield 95%.

[0034] 3. Bromination reaction

[0035] Add 50 mL of ether, 8.88 g (0.02 mol) of compound 4-1, 2.71 g (0.01 mol) of PBr into the round bottom flask 3 , reflux reaction at 3...

Embodiment 2

[0039] In step 4 of this example, the 7-hydroxycoumarin in step 4 of example 1 is replaced with equimolar 6-hydroxyflavone, and the other steps are the same as in example 1 to obtain 6.23 g of the small compound shown in formula 7-2. Molecular gelling agent, the yield is 90%, and the total yield is 65%.

[0040]

[0041] The structural characterization data of the obtained small molecule gel is: 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 ):176.9,162.1,154.8,149.3,140.8,131.5,131.3,129.1,128.8,126.1,124.2,123.0,120.0,107.4,105.8,72.0,65.1,56.4,42.7,40.1,331.5,361.3,37. 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 is replaced with equimolar β-sitosterol, and the other steps are the same as in example 2 to obtain the small molecule gelling agent shown in formula 7-3, with a total yield of 64%.

[0044]

[0045] The structural characterization data of the obtained small molecule gel is: 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 ):176.9,162.1,154.8,149.3,140.8,131.5,131.3,129.1,128.8,126.1,124.2,123.0,120.0,107.4,105.8,72.0,65.1,56.4,46.0,42.7,40,136.3,37. 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 small-molecule gel, a method for preparing the same and a gynecological solid-liquid mutual transformation type gel preparation. The structure of the small-molecule gel comprises structural units of sterol, flavone or coumarin and the like. The small-molecule gel is synthesized by means of classic reaction such as esterification reaction, etherification reaction and the like. The small-molecule gel, the method and the gynecological solid-liquid mutual transformation type gel preparation have the advantages that the small-molecule gel is good in stability and can stablyexist in acidic and alkaline environments; the small-molecule gel is high in gelling power and can be compounded with gynecological medicines, so that the gynecological solid-liquid mutual transformation type gel preparation can be prepared, can be uniformly distributed in integral tracts and is easy to prepare, good in safety and low in cost, medicine administration can be facilitated, and medicine liquid loss can be prevented.

Description

technical field [0001] The invention belongs to the technical field of gynecological medicaments, and in particular relates to a small-molecule gel, a preparation method of the small-molecule gel, and a gynecological solid-liquid interchanging gel preparation prepared by using the small-molecule 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 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 f...

Claims

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Application Information

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Patent Type & Authority Applications(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
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