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A technology of efluconazole microemulsion and efluconazole microemulsion gel, which is applied in the field of biomedicine to achieve good stability, improve therapeutic effect, and increase skin surface adhesion
Active Publication Date: 2018-11-02
SUZHOU VIGONVITA LIFE SCIENCES CO LTD
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Problems solved by technology
For a specific drug, it is unpredictable whether a microemulsion formulation with excellent stability and significantly improved efficacy can be obtained
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Embodiment 1-1
[0030] Example 1-1: Preparation of Efluconazole Microemulsion Solution
[0031] Prepare efluconazole microemulsion solution according to the formula composition in Table 1 and the following preparation steps:
[0032] 1) At room temperature, take glyceryl triacetate, Tween 80, and propylene glycol, and use a high-efficiency mechanical stirrer at a stirring speed of 1000 rpm to stir evenly, add efluconazole, and continue stirring until dissolved;
[0033] 2) Under the condition of continuous stirring, continuously add purified water to the oil phase, continuously stir until it becomes clear, and wait for the bubbles to disappear to obtain a yellow, clear and transparent solution.
[0034] Table 1
[0035]
[0036] The average particle size of the obtained microemulsion solution was 87.9±2.3 nm, and the polydispersity index (PDI) was 1.53.
Embodiment 1-2
[0037] Example 1-2: Preparation of Efluconazole Microemulsion Solution
[0038] This example is basically the same as Example 1-1, except that Tween 80 is replaced by Tween 60, and propylene glycol is replaced by ethanol. The average particle size of the obtained microemulsion solution is 93.4±4.7 nm, and PDI=1.33.
Embodiment 1-3
[0039] Embodiment 1-3: Preparation of efluconazole microemulsion solution
[0040]This example is basically the same as Example 1-1, except that Tween 80 is replaced by lecithin, propylene glycol is replaced by glycerin, the average particle size of the obtained microemulsion solution is 103.2±1.9 nm, and PDI=1.43.
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Abstract
The invention discloses an efinaconazole microemulsion composition. The efinaconazole microemulsion composition is an efinaconazole microemulsion solution or efinaconazole microemulsion gel. The efinaconazole microemulsion solution is prepared from the following raw materials: 0.01 to 1.0 percent of efinaconazole, 5 to 15 percent of oil phase, 15 to 30 percent of emulsifier, 15 to 30 percent of co-emulsifier and 30 to 60 percent of water; the oil phase is selected from glyceryl triacetate, triolein and isopropyl myristate; the emulsifier is selected from Tween 80, Tween 60 and lecithin; the co-emulsifier is selected from propylene glycol, ethanol and glycerol. The efinaconazole microemulsion gel comprises the efinaconazole microemulsion solution and a gel material. The efinaconazole microemulsion solution disclosed by the invention has the advantages of good stability, ideal microemulsion particle size and capability of effectively improving the skin permeability of drugs. Compared with the efinaconazole microemulsion solution, the efinaconazole microemulsion gel has the advantages that the skin permeability and retention volume can be further improved, the compliance of onychomycosis in clinical treatment can be improved and a slow release effect is achieved.
Description
technical field [0001] The invention belongs to the field of biomedicine, and specifically relates to an efluconazole microemulsion solution, a microemulsion gel and a preparation method thereof. Characterized by permeability and high skin drug retention, it is mainly used in the treatment of onychomycosis. Background technique [0002] Onychomycosis (Onychomycosis), commonly known as onychomycosis. Lesions caused by invasion of the nail plate and / or nail bed by dermatophytes, yeasts, and nondermatophyte molds. Dermatophytes are the most important pathogens. Divided into 3 genera: Trichophyton, Microsporum and Epidermophyton, among them, Trichophyton rubrum, Trichophyton interdigita, and Epidermophyton flocculum are the most common in most areas at home and abroad Three dermatophytes that cause onychomycosis. [0003] The incidence of onychomycosis is age-related. Epidemiological surveys show that the prevalence rate of people aged 60 to 79 is 18.2%, while those under th...
Claims
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