Imiquimod micro emulsion gels for local skin and preparation method thereof

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...

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

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