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Imiquimod vesicle gel and preparation method thereof

A technology of imiquimod vesicles and vesicles gels, applied in the directions of antiviral agents, pharmaceutical formulations, aerosol delivery, etc. To avoid skin problems, reduce patient damage, and reduce systemic toxicity

Inactive Publication Date: 2019-12-13
湖北科益药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the deficiencies of the prior art, the present invention provides an imiquimod vesicle gel and a preparation method thereof, which solves the problem that the imiquimod vesicle gel is not effective and cannot protect the patient's skin to a certain extent. question

Method used

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  • Imiquimod vesicle gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] S1. Put 10 parts of poloxamer, 5 parts of polyethylene glycol and 4 parts of Span into the reaction vessel, and then magnetically stir it in a water bath at 60°C to dissolve it completely. The stirring speed is 2000r / min. After stirring for 20 minutes, 15 parts of imiquimod were added;

[0026] S2, after adding imiquimod in S1, make the reaction vessel rotate under reduced pressure, then evaporate and remove the internal organic solvent, at this time, a thin film layer is formed on the inner wall of the reaction vessel, then add 12 parts of phosphate buffer solution while stirring, statically After a period of time, self-assemble into multi-chambered vesicles;

[0027] S3. Add 15 parts of PVP and 2 parts of CP-940 to another reaction vessel, add an appropriate amount of deionized water, let it stand to make it fully swell, then add 3 parts of pH regulator to adjust the pH of the solution to 5-8, and obtain Gel base, and then placed for later use;

[0028] S4. Rapidly ...

Embodiment 2

[0031] S1. Put 20 parts of poloxamer, 8 parts of polyethylene glycol and 8 parts of Span into the reaction vessel, and then magnetically stir it in a water bath at 60°C to dissolve it completely. The stirring speed is 2000r / min. After stirring for 20 minutes, add 20 parts of imiquimod;

[0032] S2, after adding imiquimod in S1, make the reaction vessel rotate under reduced pressure, then evaporate and remove the internal organic solvent, at this time, a thin film layer is formed on the inner wall of the reaction vessel, then add 15 parts of phosphate buffer solution while stirring, statically After a period of time, self-assemble into multi-chambered vesicles;

[0033] S3. Add 10 parts of PVP and 2 parts of CP-940 to another reaction vessel, add an appropriate amount of deionized water, let it stand to make it fully swell, and then add 3 parts of pH regulator to adjust the pH of the solution to 5-8 to obtain Gel base, and then placed for later use;

[0034] S4, 5 parts of gl...

Embodiment 3

[0037] S1. Put 15 parts of poloxamer, 6 parts of polyethylene glycol and 6 parts of Span into the reaction vessel, and then magnetically stir it in a water bath at 60°C to dissolve it completely. The stirring speed is 2000r / min. After stirring for 20 minutes, add 10 parts of imiquimod;

[0038] S2, after adding imiquimod in S1, make the reaction vessel rotate under reduced pressure, then evaporate and remove the internal organic solvent, at this time, a thin film layer is formed on the inner wall of the reaction vessel, then add 13 parts of phosphate buffer solution while stirring, statically After a period of time, self-assemble into multi-chambered vesicles;

[0039] S3. Add 11 parts of PVP and 2 parts of CP-940 to another reaction vessel, add an appropriate amount of deionized water, let it stand to make it fully swell, and then add 5 parts of pH regulator to adjust the pH of the solution to 5-8 to obtain Gel base, and then placed for later use;

[0040] S4, 7 parts of gl...

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PUM

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Abstract

The invention discloses an imiquimod vesicle gel and a preparation method of the imiquimod vesicle gel. The imiquimod vesicle gel comprises the following components in parts by weight: 10 to 20 partsof imiquimod, 10 to 20 parts of poloxamer, 5 to 8 parts of polyethylene glycol, 12 to 15 parts of a phosphate buffer solution, 4 to 8 parts of Span, 10 to 12 parts of PVP, 2 to 4 parts of CP-940, 5 to10 parts of glycerin, 5 to 8 parts of dexamethasone and 3 to 5 parts of a pH regulator. The phosphate buffer solution is prepared by adding deionized water into potassium dihydrogen phosphate, disodium hydrogen phosphate, sodium chloride and potassium chloride and mixing and stirring the materials. The invention relates to the technical field of imiquimod. The invention discloses the imiquimod vesicle gel and the preparation method thereof. The whole medicine effect is strong, and the medicine is concentrated after use, and the imiquimod vesicle gel has low toxicity to the whole body, has noskin redness and swelling phenomenon and no skin itch phenomenon, has low side effects, improves the overall applicability, reduces the damage to patients, ensures the quality of the imiquimod vesiclegel, has a certain protection effect on the skins of the patients, avoids some skin problems occurring after the patients use the imiquimod vesicle gel, and is safe and reliable.

Description

technical field [0001] The invention relates to the technical field of imiquimod, in particular to an imiquimod vesicle gel and a preparation method thereof. Background technique [0002] Imiquimod is an imidazoquinoline compound, which is a small molecule immunomodulator. Its mechanism of action in the treatment of external genital and perianal warts is not clear, and it has no direct antiviral activity, nor does it cause direct and non-specific Cytolytic destruction, but preclinical studies suggest that this product may produce antiviral activity by inducing cytokines including INF-α in vivo, and the clinical relevance of these findings is unclear. At present, the drug concentration of clinical preparations at the skin application site is low, but the dosage is large, and a considerable part of the drug is absorbed into the body through the skin, so there are local toxic and side effects such as itching, erythema, burning sensation, tenderness, ulcers, erosion, pain, etc.,...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K9/127A61K31/4745A61K31/573A61K47/10A61K47/32A61P37/02A61P31/12A61P17/00
CPCA61K9/06A61K9/1273A61K31/4745A61K31/573A61K47/10A61K47/32A61P17/00A61P31/12A61P37/02A61K2300/00
Inventor 李志丹刘毅凌宏飞王虎余致维李旭雯凌济操
Owner 湖北科益药业股份有限公司
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