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Oral mucosal preparation containing quercetin and preparation method thereof

An oral mucosa, quercetin technology, applied in the field of medicine, can solve the problems of high drug swallowing ratio, low efficiency, and reduced local treatment efficiency, etc.

Active Publication Date: 2022-05-20
SHENZHEN NYCRIST TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Dissolution of such solid dispersions is too rapid for topical treatment, and powdered formulations are not suitable for sustained release, easily dissolved and swallowed
[0009] In the disclosed patent CN102266311A, chitosan is used as a film-forming agent, and after being mixed and dissolved with quercetin, the film is obtained by solvent volatilization. This method takes a long time, is relatively low in efficiency, and has a single prescription and is a single layer. Membrane, in terms of drug release, the drug can be released to one side of the oral mucosa or to the other side, and the proportion of drugs swallowed by saliva is high, which reduces the efficiency of local treatment

Method used

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  • Oral mucosal preparation containing quercetin and preparation method thereof
  • Oral mucosal preparation containing quercetin and preparation method thereof
  • Oral mucosal preparation containing quercetin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Quercetin / polyvinylpyrrolidone monolayer film

[0062] 1. Preparation of drug-loaded layer solution

[0063] The film-forming agent polyvinylpyrrolidone (PVP) K60 was dissolved in N,N-dimethylamide, and stirred on a magnetic stirring table until a clear solution was obtained to obtain a 20% (20g / 100ml) PVP-K60 solution. Add quercetin with a purity of 98% and stir to obtain a 5% (5 g / 100 ml) quercetin clear solution (drug-loaded layer solution) for subsequent use.

[0064] 2. Film preparation of the drug-loaded layer

[0065] Pour the drug-loaded layer solution into a syringe and install it on the feed pump of the electrospinning machine. Select the appropriate voltage and use aluminum foil as the receiver to receive the drug-loaded spinning. After two hours, a smooth and soft white surface is obtained. Membrane (oromucosal formulation containing quercetin).

[0066] 3. Use 1.8×1.8cm 2 Cut the film into small square pieces with a special puncher, put it into an alumi...

Embodiment 2

[0070] Quercetin / borneol / polyvinylpyrrolidone monolayer film

[0071] 1. Preparation of drug-loaded layer solution

[0072] The film-forming agent polyvinylpyrrolidone (PVP) K60 was dissolved in N,N-dimethylamide, and stirred on a magnetic stirring table until a clear solution was obtained to obtain a 20% (20g / 100ml) PVP-K60 solution. After adding quercetin with a purity of 98% and stirring to obtain a 5% (5g / 100ml) clear and transparent solution, add borneol and stir to obtain a 1% (1g / 100ml) borneol clear and transparent solution (drug-loaded layer solution) for subsequent use .

[0073] 2. Film preparation of the drug-loaded layer

[0074] Pour the drug-loaded layer solution into a syringe and install it on the feed pump of the electrospinning machine. Select the appropriate voltage and use aluminum foil as the receiver to receive the drug-loaded spinning. After two hours, a smooth and soft white surface is obtained. Membrane (oromucosal formulation containing quercetin)...

Embodiment 3

[0079] Borneol / polyvinylpyrrolidone monolayer film

[0080] 1. Preparation of drug-loaded layer solution

[0081] The film-forming agent polyvinylpyrrolidone (PVP) K60 is dissolved in N, N-dimethylamide, and stirred until a clear solution is obtained on a magnetic stirring table to obtain a 20% (20g / 100ml) PVP-K60 solution, adding borneol and stirring, Obtain 1% (1g / 100ml) borneol clear and transparent solution (drug-loaded layer solution) for use.

[0082] 2. Film preparation of the drug-loaded layer

[0083] Pour the drug-loaded layer solution into a syringe and install it on the feed pump of the electrospinning machine. Select the appropriate voltage and use aluminum foil as the receiver to receive the drug-loaded spinning. After two hours, a smooth and soft white surface is obtained. membrane.

[0084] 3. Dissolution test: During the dissolution process, when the white film comes into contact with pH=6.8 phosphate dissolution medium, its disintegration time is 2s.

[0...

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Abstract

The invention discloses an oral mucosa agent containing quercetin and a preparation method thereof. The oral mucosal preparation containing quercetin includes a drug-loaded layer, and the drug-loaded layer contains 1-50 parts of quercetin, 0-5 parts of borneol, 0-3 parts of glycyrrhetinic acid and Polyvinylpyrrolidone 50‑95 parts. The invention solves the problem of poor water solubility of quercetin, borneol and glycyrrhetinic acid by optimizing formula and adopting electrospinning technology to prepare amorphous solid dispersion film. The dissolution and release of the drug is delayed by forming an adduct between the film-forming agent and quercetin. At the same time, in order to prevent the drug from dissolving in saliva and causing excessive loss, a protective film was added as the back film on the basis of the drug film loaded with quercetin, and the increase of the protective film would not have a great impact on the dissolution .

Description

Technical field: [0001] The invention belongs to the field of medicine, and in particular relates to an oral mucosal agent containing quercetin and a preparation method thereof. Background technique: [0002] Oral ulcers are a common oral disease, mostly in the tongue, lips, and buccal mucosa. When they attack, there is a strong sense of discomfort and pain. In severe cases, it even affects eating and speaking. The treatment of oral ulcers focuses on local anti-inflammatory, pain relief, and promotion of healing. The common watermelon cream, Bingbo powder and oral patch all have the disadvantages of low drug utilization and being easily eroded by saliva and swallowed. In contrast, the double-layer oral film of the present invention can improve drug availability. [0003] Quercetin (Quercetin), chemical formula: C 15 h 10 o 7 , molecular weight: 302, structure such as formula I is as follows: [0004] [0005] Quercetin, also known as quercetin and quercetin, is a po...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K31/56A61K31/352A61K31/045A61K47/32A61P1/02D04H1/728D01D5/00
Inventor 田芳安妮.齐默尔曼韩云凤
Owner SHENZHEN NYCRIST TECH CO LTD
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