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Imiquimod vesicle gel and preparation method for same

A technology of imiquimod bubble and capsule gel, which is applied in the field of drug capsule gel and its preparation, can solve the problem of difficulty in increasing local drug concentration, achieve high-efficiency and low-toxicity treatment of related skin diseases, and reduce toxic and side effects , enhance the effect of curative effect

Active Publication Date: 2013-07-17
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, gels cannot form drug depots in the skin, making it difficult to increase local drug concentrations in the skin

Method used

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  • Imiquimod vesicle gel and preparation method for same
  • Imiquimod vesicle gel and preparation method for same
  • Imiquimod vesicle gel and preparation method for same

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preparation example Construction

[0030] The preparation process of the vesicle suspension in the vesicle gel of the present invention is to dissolve the nonionic surfactant in the organic solvent earlier, then add the medicine of the prescribed amount, and after the ultrasound, adopt the injection method to inject the water phase (buffer Solution) is introduced into the organic phase and mixed, and the vesicle suspension is formed by self-assembly, and then mixed with the gel matrix prepared in advance. The imiquimod contained in the vesicle suspension prepared by the present invention is a poorly soluble drug. After comparing some investigation items, it was found that the preparation method of drug-loaded vesicles according to the present invention has no specific requirements for model drugs, and the same prescription and the same preparation method can be used to pack drugs of different properties, such as retinoic acid, 5-Fu. The prepared vesicle suspension can be further made into vesicle gel.

[0031...

Embodiment 1

[0033] 1. Preparation of imiquimod vesicle suspension

[0034] Take the prescribed amount of 10mg Brij78 (HLB value 15.3), 10mg Span85 (HLB value 1.8), 20mg Span40 (HLB value 6.7), 20mg Poloxamer188 (HLB value 29) in vials, add organic solvents, at 60 Magnetic stirring (2000r / min) in a water bath at ℃ to dissolve completely, add 10 mg of imiquimod (≤80 mesh), stir evenly, and sonicate for 3 minutes in a water bath at 60 ℃ to obtain an organic phase. Pour the PBS (pH 7.3) previously kept at 60°C into the organic phase under stirring state and stir it tightly for 10 minutes, then transfer it to a water bath at 37°C, stir at 2000r / min for 3 hours, and evaporate the ethanol and ethyl acetate. ester to obtain imiquimod vesicle suspension (abbreviation: vesicle suspension).

[0035] Using the same preparation method without adding drugs, a blank vesicle suspension was prepared for the preparation of the control preparation.

[0036] 2. Preparation of imiquimod vesicle gel

[00...

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Abstract

The invention relates to an imiquimod vesicle gel and a preparation method for the same. The vesicle gel is obtained by preparing a vesicle suspension by using imiquimod and the nonionic surfactants of Brij, Span, Poloxamer and the like via self-assembly, then reacting with the mixed gel matrix of carbomer and povidone, and used for treating the diseases of exophytic genital warts, actinic keratosis, skin basal cancer, melanoma and the like via local application on the skin; and by adding povidone in the carbomer gel matrix, the in-vitro medicine release amount can be increased by 42.1%, thus being beneficial to promote the entrance of medicines in the skin to exert the functions. According to the imiquimod vesicle gel and the preparation method for the same disclosed by the invention, the intradermal retention volume of the medicines in 24 hours can be remarkably increased and is 2.1 times that of the commercially available emulsifiable pastes, and the dose of the medicines penetrating through the skin is reduced by 48.7%; and the equivalent intradermal retention volume can be achieved only by a half of the dose of the commercially available emulsifiable pastes, so that the effectiveness of the medicine effect of the medicated parts can be remarkably enhanced, the dose of the medicines entering in the body can be greatly reduced, and the toxic and side effects of the whole body can be reduced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a pharmaceutical vesicle gel and a preparation method thereof. Background technique [0002] Imiquimod (Imiquimod, S-26308 or R-837), chemical name 1-(2-methylpropyl)-1H-imidazo[4,5-C]quinolin-4-amine, is a A non-nucleoside isocyclic imidazoquinoline amine drug, white or off-white crystalline powder, odorless, tasteless, almost insoluble or insoluble in water or ether, very slightly soluble in ethanol, methanol or acetone, in ice Soluble in acetic acid, slightly soluble in 0.1mol / L hydrochloric acid solution, almost insoluble or insoluble in 0.1mol / L sodium hydroxide solution. Imiquimod was originally a new topical immunomodulatory drug for the treatment of external genital warts. It mainly plays an immunomodulatory role by inducing the body to produce interferon (IFN), tumor necrosis factor (TNF), interleukin (IL) and other cytokines. [0003] The current...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/4745A61K47/34A61K47/32A61P17/00A61K47/10
Inventor 杨红陈华兵吴秀凤刘洪月龚珠萍顾艳赵成龙姚枫枫
Owner SUZHOU UNIV
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