Imiquimod micro emulsion gels for local skin and preparation method thereof

A technology of imiquimod micro, emulsion gel, applied in skin diseases, medical preparations containing active ingredients, antiviral agents, etc., can solve side effects, high transdermal absorption, and low local skin drug storage and other problems, to achieve the effect of enhancing compliance, good compatibility, and conducive to percutaneous penetration

Inactive Publication Date: 2010-06-30
HUAZHONG NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In EP.0 376 534 A1, it is mainly introduced that imiquimod is directly made into a medicament for transdermal administration, including cream, ointment, patch, etc. The disadvantage of the above dosage forms is that the amount of drug stored in the local skin is small , High transdermal absorption leads to side effects caused by systemic absorption

Method used

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  • Imiquimod micro emulsion gels for local skin and preparation method thereof
  • Imiquimod micro emulsion gels for local skin and preparation method thereof
  • Imiquimod micro emulsion gels for local skin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Take 100g of imiquimod, 1.5kg of oleic acid and stir to dissolve, then add 3.0kg of castor oil polyoxyethylene ether EL60 and 1kg of isopropanol, mix and stir evenly, add about 60kg of water to the container containing the above solution under constant stirring Gently stir in the homogenizer to form a light yellow to bluish transparent oil-in-water microemulsion A with an average particle size of 30nm; another 1.5kg of Carbomer 934 powder is weighed and evenly sprinkled in 50kg of distilled water. Fully swell, prepare carbomer water swelling solution B containing 3% carbomer 934 for later use; weigh 33.4kg of B and add it to A, stir while adding, add about 1kg of triethanolamine to adjust the pH value, and obtain 100kg of transparent Imiquimod microemulsion gel, that is, 0.1% imiquimod microemulsion gel.

Embodiment 2

[0025] Take 100g of imiquimod, 1.5kg of oleic acid and stir to dissolve, then add 1.5kg of castor oil polyoxyethylene ether EL60 and 1kg of isopropanol, mix and stir evenly, add about 10kg of water to the container containing the above solution under constant stirring Gently stir in the homogenizer to form a light yellow to bluish transparent bicontinuous microemulsion A with an average particle size of 30nm; another 300g of Carbomer 934 powder is weighed, evenly sprinkled in 10kg of distilled water, fully Swell, prepare carbomer water swelling solution B containing 3% carbomer 934 for later use; weigh 5.78g of B and add it to A, stir while adding, add about 120g of triethanolamine to adjust the pH value, and obtain 20kg of transparent rice Quinomod microemulsion gel, that is, 0.5% imiquimod microemulsion gel.

Embodiment 3

[0027] Take 100g of imiquimod, 1.5g of oleic acid and stir to dissolve, then add 1.5kg of castor oil polyoxyethylene ether EL60 and 1.0kg of isopropanol, mix and stir evenly, add about 3.0kg of water to the The solution was slightly stirred in a homogenizer to form a light yellow transparent water-in-oil microemulsion A with an average particle size of 30nm; another 300g of Carbomer 934 powder was weighed, evenly sprinkled in 10kg of distilled water, fully swelled, and prepared Prepare carbomer water swelling solution B containing 3% carbomer 934 for later use; weigh 2.84kg of B and add it to A, stir while adding, add about 60g of triethanolamine to adjust the pH value, and prepare 10kg milky white imiquimod Microemulsion gel, namely 1% imiquimod microemulsion gel.

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Abstract

The invention relates to imiquimod micro emulsion gels for local skin, at least comprising the following ingredients by mass percent: 0.1-2.5 percent of imiquimod, 1-24 percent of solvent, 1-16 percent of surface active agent, 1-12 percent of cosurfactant, 1-20 percent of gelatinizing agent and the remaining water; wherein the imiquimod is 1-isobutyl-1H-imidazole(4,5-C) quinoline-4-amine; the preparation method comprises the following steps: the imiquimod is dissolved in the solvent, the surface active agent and the cosurfactant are added in the solvent dissolved with the imiquimod, and the mixture is dispersed uniformly; water with [roper amount is added in the mixture to form micro emulsion; the gelatinizing agent is swelled by water, so as to prepare the solution with a certain concentration, the gelatinizing agent solution is dropped in the imiquimod micro emulsion dropwise, the stirring is carried out while the gelatinizing agent solution is dropped, the pH value is adjusted by adding triethanolamine, so as to prepare the imiquimod micro emulsion gels; the invention has the advantages that: the thorough dispersity of the micro emulsion to medicines, adhesiveness of gels to the skin and deformation flowability thereof under external force are concentrated, so as to lead the medicine to be applied to the affected part and cause the medicine to pass into internal body and reach target spot through the skin; the medicine effect can act on continuously.

Description

Technical field: [0001] The invention relates to a microemulsion gel for local skin administration and a preparation method thereof, belonging to the field of external skin preparations. Background technique: [0002] Imiquimod, chemical name: 1-isobutyl-1H-imidazo[4,5-C]quinolin-4-amine, is an immunomodulator and an interferon inducer. It was originally developed by Riker Labs in the United States, and later transferred to 3M Corporation and Japan's Daiichi Pharmaceutical Company. In 1997, the new drug application proposed by 3M was approved by the U.S. FDA, and it was listed in the U.S. in October. The listed product is called Aldara, which is a 5% imiquimod cream in a 250mg single-dose package, which is used to treat viral infections and herpes simplex infections. and genital warts. The side effect that occurs during the use of this drug is erythema, which is toxic at high doses. In U.S. Pat No. 4,689,338 imiquimod is reported as an antiviral agent and an interferon in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/4745A61P31/12A61P31/20A61P31/22A61P17/00
Inventor 程靖郭小杰郭峰夏亚婷
Owner HUAZHONG NORMAL UNIV
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