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A kind of 5-hydroxymethyl tolterodine liposome gel preparation and preparation method thereof

A technology of hydroxymethyltolterodine and catalyst, which is applied in the field of medicine and pharmacy, can solve the problems such as the absence of 5-hydroxymethyltolterodine liposome gel preparation, achieve good clinical application prospects, and reduce systemic absorption , to avoid the effect of toxic side effects

Inactive Publication Date: 2017-10-20
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although there are studies on this 5-hydroxymethyltolterodine hydrogel formulation, there is no relevant research on the 5-hydroxymethyltolterodine liposome gel formulation.

Method used

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  • A kind of 5-hydroxymethyl tolterodine liposome gel preparation and preparation method thereof
  • A kind of 5-hydroxymethyl tolterodine liposome gel preparation and preparation method thereof
  • A kind of 5-hydroxymethyl tolterodine liposome gel preparation and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0045] Refluxing p-hydroxyazobenzoic acid, 2,2'-dibromodiethyl ether, Na2CO3, and 18-crown-6 in a polar organic solvent at a molar ratio of 5:10:2:0.3 at 80-120°C for 12 hours, the product 1 was obtained. At room temperature, product 1, cholesterol, dicycloethylcarbodiimide (DCC) and 4-dimethylaminopyridine (DMAP) were reacted at a molar ratio of 1:1:1:0.1 for 24 hours. Compound 5 and diethylamine were refluxed in chloroform at a molar ratio of 1:10 for 48 hours, washed with chloroform, and separated by column chromatography to obtain the final product cholesterol derivative (CDEEA).

Embodiment 2

[0047]Refluxing p-hydroxyazobenzoic acid, 2,2'-dibromodiethyl ether, Na2CO3, and 18-crown-6 in a polar organic solvent at a molar ratio of 8:15:1:0.5 at 80-120°C for 48 hours, the product 1 was obtained. At room temperature, product 1, cholesterol, dicycloethylcarbodiimide (DCC) and 4-dimethylaminopyridine (DMAP) were reacted at a molar ratio of 2:2:1:0.05 for 36 hours. Compound 5 and diethylamine were refluxed in chloroform for 48 hours at a molar ratio of 1:20, washed with chloroform, and separated by column chromatography to obtain the final product cholesterol derivative (CDEEA).

Embodiment 3

[0049] Refluxing p-hydroxyazobenzoic acid, 2,2'-dibromodiethyl ether, Na2CO3, and 18-crown-6 in a polar organic solvent at a molar ratio of 5:15:0.5:0.01 at 80-120°C for 36 hours, the product 1 was obtained. At room temperature, product 1, cholesterol, dicycloethylcarbodiimide (DCC) and 4-dimethylaminopyridine (DMAP) were reacted at a molar ratio of 1.5:1.5:1.5:0.1 for 24 hours. Compound 5 and diethylamine were refluxed for 72 hours in chloroform at a molar ratio of 1:30, washed with chloroform, and separated by column chromatography to obtain the final product cholesterol derivative (CDEEA).

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Abstract

The invention provides a 5-hydroxyl tolterodine gel preparation and a preparation method thereof, and further provides a novel cholesterol derivative. One end of the molecular formula of the cholesterol derivative is provided with an uncharged diethylamine group, and cholesterol is replaced by the cholesterol derivative. As compared with lipidosome added with cholesterol, lipidosome added with cholesterol derivative has higher long-term stability and higher encapsulation efficiency. The 5-hydroxyl tolterodine gel preparation which can be absorbed percutaneously is good in drug stability and high in bioavailability; toxic and side effects caused by oral administration and suffering and discomfort to patients caused by medicine injection are both avoided. The 5-hydroxyl tolterodine lipidosome, which is prepared by ethanol injection, is easy to produce and can be prepared for use on site, is convenient in quality control, low in cost, and low in environmental pollution. Stability of the 5-hydroxyl tolterodine lipidosome can be improved by uniformly dispersing the same in gel. Compared with common gel preparations, the lipidosome gel preparation has the advantages of effectively prolonging medicine release time, reducing systematic absorption of medicines, reducing toxic and side effect of medicines, enhancing compliance of patients, and accordingly has good clinical application prospect.

Description

Technical field: [0001] The present invention is the improvement to the dosage form of tolterodine precursor compound 5-hydroxymethyl tolterodine, and further discloses a kind of 5-hydroxymethyl tolterodine liposome gel preparation, the present invention also A preparation method of the preparation is provided, which belongs to the technical field of medicine and pharmacy. Background technique: [0002] Clinical studies have shown that after oral administration, tolterodine is converted into different metabolites by the enzyme CYP2D6 in the liver, among which 5-hydroxymethyl tolterodine plays the main pharmacodynamic role. Due to individual differences in liver metabolic enzymes, oral administration of tolterodine causes individual metabolite content to vary, which is not conducive to drug dosage control, resulting in low drug efficacy and increased side effects, such as dry mouth, constipation, indigestion, headache, dizziness, etc. Although it can be administered by ordin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J9/00A61K31/137A61K9/70A61K9/127A61K9/06A61K47/38A61K47/28A61P13/10
CPCA61K9/0014A61K9/06A61K9/127A61K9/7015A61K31/137A61K47/28A61K47/38C07J9/00
Inventor 刘文华刘佳欣郑舒婷孙凤英滕利荣李又欣
Owner JILIN UNIV
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