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Antifungal composition and application thereof

A composition and antifungal technology, applied in the field of medicine, can solve the problems of poor treatment effect, greasy nails, easy to be washed off and the like

Inactive Publication Date: 2020-04-28
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its permeability is poor, and it is not effective in the treatment of fungal infections in nails and deeper parts of the skin.
At the same time, terbinafine oral preparations usually have adverse reactions such as systemic toxicity, liver toxicity, and gastrointestinal irritation, while general semi-solids such as creams contain oily bases, which are difficult to spread when applied to diseased parts, and are easily absorbed after administration. Rubbing off with clothing, leaving nails or surfaces with a greasy and uncomfortable feel; gels are not water resistant and tend to wash off when washing hands or bathing
The above reasons lead to poor patient compliance of these dosage forms

Method used

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  • Antifungal composition and application thereof
  • Antifungal composition and application thereof
  • Antifungal composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1. The synergistic antifungal effect of terbinafine hydrochloride and berberine hydrochloride

[0027] By comparing and judging the MIC values ​​of terbinafine hydrochloride and berberine hydrochloride and their combined use, the advantages of the combination of the two drugs in vitro are illustrated. This study was carried out with reference to the protocol and related literature formulated by the National Clinical Laboratory Standardization Institute (CLSI).

[0028] Experimental method: (1) Configuration of drug concentration: single-drug terbinafine hydrochloride TBH and berberine hydrochloride BRH were prepared with dimethyl sulfoxide to prepare mother solutions with concentrations of 50000 μg / mL and 10000 μg / mL, and then used RPMI1640 liquid medium was diluted 100-fold and 20-fold with the above mother liquid respectively to a maximum concentration of 500 μg / mL, and then diluted with RPMI1640 liquid medium to obtain 20 concentrations, and the final conc...

Embodiment 2

[0032] Embodiment 2. Treat the coating agent of onychomycosis infection disease

[0033] (1) The single drug composition (containing urea) of this embodiment includes the following raw materials by mass percentage:

[0034] Terbinafine Hydrochloride 1%

[0035] Eudragit ® RLPO 20%

[0036] Ethanol 55%

[0037] Urea 10%

[0038] water 14%

[0039] The preparation method of this embodiment composition:

[0040] A, according to the formula ratio, at room temperature, terbinafine hydrochloride and ethanol are mixed to form a transparent and clear solution;

[0041] B. Add RLPO to the solution described in A according to the formula ratio;

[0042] C. According to the formula ratio, at room temperature, urea is mixed with water and ultrasonicated at 25°C to form a uniform and clear urea solution, which is added to the solution described in step B to obtain C solution;

[0043] D. Stir the C solution continuously until the RLPO is dissolved to form a uniform, stable, transp...

Embodiment 4

[0086] Embodiment 4. the evaluation of the coating agent for the treatment of onychomycosis infection

[0087] 1. Film forming (drying time and appearance score) experiment

[0088] The combination composition (containing urea), single drug composition (containing urea), single drug composition (excluding urea) and the commercially available preparation (Lamisil Pedisan ® once) for film-forming experiments.

[0089] Test product: 0.2ml of the combined composition of the present invention (containing urea); terbinafine hydrochloride: 0.5%, berberine hydrochloride: 0.5%, and the properties are clear and transparent liquid; 0.2ml of the single drug composition of the present invention (containing urea ); Terbinafine hydrochloride: 1%, the properties are clear and transparent liquid; reference substance: 0.2ml composition (excluding urea), terbinafine hydrochloride: 1%, the properties are clear and transparent liquid; 0.2ml commercially available preparation (Lamisil Pedisan ®...

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Abstract

The invention relates to an antifungal composition. The composition includes as follows: a) terbinafine or a pharmaceutically acceptable salt thereof; b) berberine or a pharmaceutically acceptable salt thereof; and c) urea and applications thereof. An application of a drug composition in preparation of drugs for treating fungal infections is also related. The drug composition includes the terbinafine or the pharmaceutically acceptable salt thereof and the berberine or the pharmaceutically acceptable salt thereof; and fungi are selected from trichophyton, fusarium, candida and combinations thereof. The composition can enhance sterilization effects, reduce the using amount of the drugs, shorten the course of treatment or avoid drug resistance.

Description

technical field [0001] The invention belongs to the technical field of medicine, relates to a synergistic antifungal composition and its application, and also relates to the application of the pharmaceutical composition in preparing and treating fungal infection diseases. Background technique [0002] Fungal infectious diseases, that is, diseases caused by fungi. As a class of eukaryotic organisms that widely exist in nature, fungi can infect different parts of the human body. From the perspective of clinical pathogenicity, mycoses can be divided into two categories: superficial mycosis and deep mycosis. Many problems, such as the abuse of antibiotics, lead to the destruction of the normal flora symbiotic relationship between bacteria and fungi; secondly, in clinical application, more and more organ transplantation operations are carried out in clinical practice, and the use of immunosuppressants after surgery has affected the The normal immune function of the body reduces...

Claims

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Application Information

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IPC IPC(8): A61K31/4375A61K31/137A61K47/18A61P31/10
CPCA61K31/137A61K31/4375A61K47/18A61P17/00A61P31/10A61K2300/00
Inventor 徐月红杨凤蝶玉秀明
Owner SUN YAT SEN UNIV
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