Itraconazole drops and preparation method thereof

Abstract

The invention discloses itraconazole drops and a preparation method thereof. The itraconazole drops are prepared from components in parts by weight as follows: 1-3 parts of itraconazole, 80-120 partsof vitamin E acetate, 5-15 parts of vitamin A1 and 10-30 parts of PEG400. According to the itraconazole drops, itraconazole is in a dissolved state, has good stability, can be directly absorbed instead of being dissolved in gastrointestinal tracts and can improve the biocompatibility. Besides, the preparation technology is simple, auxiliary materials are high in safety, and the itraconazole dropscan be taken with milk or added to milk to be taken and are particularly applicable to treatment of infantile hemangioma.

Description

technical field

[0001] The invention relates to an itraconazole drop and a preparation method thereof. Background technique

[0002] Itraconazole is a triazole broad-spectrum antifungal drug, itraconazole can inhibit fungal cytochrome p450. Cytochrome p450 can catalyze the demethylation of lanosterol at the 14th position to ergosterol, and itraconazole inhibits sterol 14α-demethylase, leading to the accumulation of 14α-methylated sterol, which induces changes in cell membrane permeability, It can cause extravasation of fungal cell content and structural damage, and then cause fungal cell death. Itraconazole has been on the market for more than 20 years and is widely used in the treatment of fungal diseases in infants and young children, including tinea capitis, sporotrichosis, candidiasis, and aspergillosis. Mycosis, histoplasmosis, zygomycosis and other opportunistic fungal infections, etc., and itraconazole can effectively inhibit the proliferation and migration of hemang...

Examples

Embodiment 1

[0014] prescription:

[0015] Material composition

[0016] Preparation method: 1) Itraconazole is crushed through a 150-mesh sieve, and fully mixed with PEG400; 2) Vitamin E acetate and vitamin A1 are fully mixed; 3) The mixture of step 1) is slowly added to the mixture of step 2), Add while stirring on high speed until fully combined and dissolved. 4) Subpackaged as itraconazole 100mg / bottle.

Embodiment 2

[0018] prescription:

[0019]

[0020]

[0021] Preparation method: 1) Itraconazole is pulverized through a 100-mesh sieve, and fully mixed with PEG400; 2) Vitamin E acetate, vitamin A1 and butylated hydroxyanisole are fully mixed; 3) The mixture in step 1) is slowly added to step 2 ) mixture, add while stirring at high speed until completely mixed and dissolved. 4) Subpackaged as itraconazole 100mg / bottle.

Embodiment 3

[0023] prescription:

[0024] Material composition

[0025] Preparation method: 1) under a nitrogen-filled environment, itraconazole is pulverized through a 100-mesh sieve, and fully mixed with PEG400; 2) under a nitrogen-filled environment, vitamin E acetate, vitamin A1 and preservatives are fully mixed evenly; 3) filled with Under nitrogen environment, slowly add the mixture of step 1) into the mixture of step 2), and stir at high speed while adding, until completely mixed and dissolved. 4) Subpackaged as itraconazole 100mg / bottle.

technical field

[0001] The invention relates to an itraconazole drop and a preparation method thereof. Background technique

[0002] Itraconazole is a triazole broad-spectrum antifungal drug, itraconazole can inhibit fungal cytochrome p450. Cytochrome p450 can catalyze the demethylation of lanosterol at the 14th position to ergosterol, and itraconazole inhibits sterol 14α-demethylase, leading to the accumulation of 14α-methylated sterol, which induces changes in cell membrane permeability, It can cause extravasation of fungal cell content and structural damage, and then cause fungal cell death. Itraconazole has been on the market for more than 20 years and is widely used in the treatment of fungal diseases in infants and young children, including tinea capitis, sporotrichosis, candidiasis, and aspergillosis. Mycosis, histoplasmosis, zygomycosis and other opportunistic fungal infections, etc., and itraconazole can effectively inhibit the proliferation and migration of hemang...

Examples

Embodiment 1

[0014] prescription:

[0015] Material composition

[0016] Preparation method: 1) Itraconazole is crushed through a 150-mesh sieve, and fully mixed with PEG400; 2) Vitamin E acetate and vitamin A1 are fully mixed; 3) The mixture of step 1) is slowly added to the mixture of step 2), Add while stirring on high speed until fully combined and dissolved. 4) Subpackaged as itraconazole 100mg / bottle.

Embodiment 2

[0018] prescription:

[0019]

[0020]

[0021] Preparation method: 1) Itraconazole is pulverized through a 100-mesh sieve, and fully mixed with PEG400; 2) Vitamin E acetate, vitamin A1 and butylated hydroxyanisole are fully mixed; 3) The mixture in step 1) is slowly added to step 2 ) mixture, add while stirring at high speed until completely mixed and dissolved. 4) Subpackaged as itraconazole 100mg / bottle.

Embodiment 3

[0023] prescription:

[0024] Material composition

[0025] Preparation method: 1) under a nitrogen-filled environment, itraconazole is pulverized through a 100-mesh sieve, and fully mixed with PEG400; 2) under a nitrogen-filled environment, vitamin E acetate, vitamin A1 and preservatives are fully mixed evenly; 3) filled with Under nitrogen environment, slowly add the mixture of step 1) into the mixture of step 2), and stir at high speed while adding, until completely mixed and dissolved. 4) Subpackaged as itraconazole 100mg / bottle.

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