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Novel triamcinolone acetonide high-polymer medicinal long-acting slow-release membrane and preparation method thereof

A polymer and slow-release film technology, applied in the fields of polymer materials, biomedicine, and organic chemistry, can solve the problems of drug washing and dilution, difficulties in local administration and repeated administration, and impact on bile duct healing, etc., to achieve Avoid systemic hormone side effects, reduce the risk of reoperation, good physical and chemical properties and biological properties

Inactive Publication Date: 2018-10-12
昆明医科大学第二附属医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The location of the bile duct is deep, and the commonly used methods for the treatment of skin scars are difficult to apply to bile duct scars. Local administration and repeated administration are difficult, and the drug cannot stay in the repaired part of the bile duct for a long time. , drugs can be washed out and diluted by bile and are difficult to work, and some drugs that inhibit scarring may affect the healing of bile ducts

Method used

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  • Novel triamcinolone acetonide high-polymer medicinal long-acting slow-release membrane and preparation method thereof
  • Novel triamcinolone acetonide high-polymer medicinal long-acting slow-release membrane and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0047] A preparation method of a novel triamcinolone acetonide macromolecule drug long-acting slow-release membrane, comprising the steps of:

[0048] Step (1), purification of chitosan raw material:

[0049] Chitosan was added to an aqueous sodium hydroxide solution with a concentration of 40 g / L, stirred at 70° C. to decolorize and deproteinize, and then separated from solid and liquid, and the solid was taken to obtain purified chitosan;

[0050] Wherein, the add-on ratio of chitosan and sodium hydroxide aqueous solution is 20g: 100ml;

[0051] Step (2), screening chitosan with high degree of deacetylation:

[0052] Place the purified chitosan obtained in step (1) in a mass concentration of 1% dilute hydrochloric acid and stir until dissolved, filter, take the filtrate, slowly add 1mol / L sodium hydroxide solution to the filtrate until the pH value is 7.6, Filtrate, get filter residue, wash to neutrality, obtain chitosan with high degree of acetylation;

[0053] The quali...

Embodiment 2

[0068] A preparation method of a novel triamcinolone acetonide macromolecule drug long-acting slow-release membrane, comprising the steps of:

[0069] Step (1), purification of chitosan raw material:

[0070] Chitosan was added to an aqueous sodium hydroxide solution with a concentration of 40 g / L, stirred at 70°C for 2 hours to decolorize and deproteinize, and then separated from solid and liquid, and the solid was taken to obtain purified chitosan;

[0071] Wherein, the add-on ratio of chitosan and sodium hydroxide aqueous solution is 20g: 100ml;

[0072] Step (2), screening chitosan with high degree of deacetylation:

[0073] Put the purified chitosan obtained in step (1) in dilute hydrochloric acid with a mass concentration of 1% and stir for 2 hours, filter, take the filtrate, slowly add 1mol / L sodium hydroxide solution to the filtrate until the pH value is 7.9, filter , take filter residue, wash to neutrality, obtain chitosan with high degree of acetylation;

[0074] ...

Embodiment 3

[0090] A preparation method of a novel triamcinolone acetonide macromolecule drug long-acting slow-release membrane, comprising the steps of:

[0091] Step (1), purification of chitosan raw material:

[0092] Chitosan was added to an aqueous sodium hydroxide solution with a concentration of 40 g / L, stirred at 70°C for 2 hours to decolorize and deproteinize, and then separated from solid and liquid, and the solid was taken to obtain purified chitosan;

[0093] Wherein, the add-on ratio of chitosan and sodium hydroxide aqueous solution is 20g: 100ml;

[0094] Step (2), screening chitosan with high degree of deacetylation:

[0095] Put the purified chitosan obtained in step (1) in dilute hydrochloric acid with a mass concentration of 1% and stir for 2 hours, filter, take the filtrate, slowly add 1mol / L sodium hydroxide solution to the filtrate until the pH value is 7.8, filter , take filter residue, wash to neutrality, obtain chitosan with high degree of acetylation;

[0096] ...

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Abstract

The invention relates to a novel triamcinolone acetonide high-polymer medicinal long-acting slow-release membrane and a preparation method of the novel triamcinolone acetonide high-polymer medicinal long-acting slow-release membrane. The method comprises the following steps: carrying out decoloration on chitosan, carrying out deproteinization, carrying out purifying, and carrying out screening toobtain deacetylated chitosan with high deacetylation degree; carrying out alkalization freeze thawing, and carrying out unimolecule nucleophilic substitution reaction with 2-chlorohydrin after the molecules completely swell; enabling the obtained hydroxyethyl chitosan and succinic anhydride to have ring-opening substitution reaction, carrying out dialysis on the reaction liquid, and carrying out purifying, by adopting DMAP / EDC as a catalytic system, carrying out esterification reaction with triamcinolone acetonide in the water phase, wherein ester bonds realize covalent binding, the end-product triamcinolone acetonide-N-succinyl hydroxyethyl chitosan high-polymer medicinal polymer is synthesized, and finally, carrying out BDDGE cross-linking reaction, and carrying out drying for membrane formation in a polytetrafluoroethylene mold. The prepared product is stable in physicochemical properties, is non-toxic, is good in biocompatibility, and can realize difference release of medicines inthe in-vitro simulated body fluid environment.

Description

technical field [0001] The invention belongs to the technical fields of organic chemistry, polymer materials and biomedicine, and in particular relates to a novel triamcinolone acetonide macromolecule drug long-acting slow-release membrane and its preparation method and application, in particular to N-succinyl hydroxyl with a carboxyl group Ethyl chitosan is esterified with triamcinolone acetonide with hydroxyl to form a high molecular drug polymer film. Background technique [0002] The management of benign bile duct scars has always been a major problem in the field of biliary surgery. Especially in recent years, with the popularity of biliary surgery and the promotion of laparoscopic technology, this problem has become more prominent and severe. The biliary tract is a closed and continuous pipeline system, which can be narrowed in the event of calculus, inflammation, trauma, iatrogenic injury, and parasites, and the biliary stenosis will aggravate the above-mentioned pat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/58A61K31/722A61K47/61A61P7/04A61P29/00A61P31/04A61P1/16C08B37/08
CPCA61K9/7007A61K31/58A61K31/722A61K47/61A61P1/16A61P7/04A61P29/00A61P31/04C08B37/003A61K2300/00
Inventor 王滔张小文邹浩
Owner 昆明医科大学第二附属医院
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