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A technology of ifluconazole microemulsion and ifluconazole microemulsion gel is applied in the field of biomedicine to achieve the effects of improving skin adhesion, reducing medication frequency and increasing skin retention
Active Publication Date: 2021-07-09
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, use a high-efficiency mechanical stirrer at a stirring speed of 1000 rpm, stir well, 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 efluconazole microemulsion composition, which is an efluconazole microemulsion solution or an efluconazole microemulsion gel, and the raw material formula of the efluconazole microemulsion solution includes: Azole 0.1%-1.0%, oil phase 5%-15%, emulsifier 15%-30%, co-emulsifier 15%-30%, water 30%-60%, oil phase selected from triacetin, oleic acid Glyceride and isopropyl myristate, the emulsifier is selected from Tween 80, Tween 60 and lecithin, and the co-emulsifier is selected from propylene glycol, ethanol and glycerin; the raw material formula of efluconazole microemulsion gel contains Efluconazole microemulsion solutions and gel materials. The efluconazole microemulsion solution of the present invention has good stability, has an ideal microemulsion particle size, and can effectively improve the skin permeability of the drug; Permeability and retention can improve the compliance of clinical treatment of onychomycosis and play a sustained release effect.
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...
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