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A long-acting sustained-release film of triamcinolone acetonide macromolecule drug and preparation method thereof

A polymer and slow-release membrane 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 influence on bile duct healing, etc., to achieve Avoid the side effects of systemic hormones, reduce the risk of reoperation, and reduce the effect of scar adhesion

Inactive Publication Date: 2021-07-30
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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  • A long-acting sustained-release film of triamcinolone acetonide macromolecule drug and preparation method thereof
  • A long-acting sustained-release film of triamcinolone acetonide macromolecule drug and preparation method thereof

Examples

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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 macromolecule drug long-acting slow-release membrane and a preparation method thereof. Firstly, chitosan is decolorized and deproteinized, and then deacetylated chitosan with high degree of deacetylation is purified and screened out. Then it is alkalized and freeze-thawed, and after the molecule is fully swollen, a single-molecule nucleophilic substitution reaction occurs with 2-chloroethanol. The obtained hydroxyethyl chitosan and succinic anhydride undergo a ring-opening substitution reaction, and the reaction liquid undergoes dialysis and purification, and uses DMAP / EDC as a catalyst system to undergo an esterification reaction with triamcinolone acetonide in the water phase, and the ester bond co- Valence combination, the final product triamcinolone acetonide-N-succinyl hydroxyethyl chitosan high molecular drug polymer was synthesized, and finally after BDDGE cross-linking reaction, it was dried in a polytetrafluoroethylene mold to form a film. The prepared product has stable physical and chemical properties, is non-toxic and has good biocompatibility, and can release drugs differentially in a simulated body fluid environment in vitro.

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 Patents(China)
IPC IPC(8): A61K47/61A61K9/70A61K31/58A61K31/722A61P7/04A61P29/00A61P31/04A61P1/16C08B37/08
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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