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A kind of ophthalmic nano micellar antifungal solution containing isavuconazole
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A nano-micelle and anti-fungal technology, applied in the field of medicine, can solve the problems of poor absorption effect, strong irritation, poor preparation stability, etc., and achieve good absorption, absorption promotion, and good anti-fungal effect
Active Publication Date: 2019-01-04
河南省立眼科医院
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Similar to other antifungal drugs, isavuconazole has strong hydrophobicity and is not easy to make aqueous solution eye drops. If it is administered as a suspension, the absorption effect is generally poor and the irritation is strong, and the stability of the preparation usually worse
There is no report on isavuconazole nanomicelle
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Embodiment 1
[0029] An ophthalmic nanomicelle antifungal solution containing isavuconazole, which is composed of the following raw materials in parts by weight: 0.01-0.5 parts of isavuconazole, 0.1-10 parts of solubilizer, and 2-10 parts of polyethylene glycol 400 , 90-99.8 parts of water, preferably: composed of the following raw materials in parts by weight: 0.1-0.3 parts of isavuconazole, 2-6 parts of solubilizer, 5-7 parts of polyethylene glycol 400, and 93-96 parts of water.
[0030] The solubilizer is polyethylene glycol 15-hydroxystearate (Kolliphor® HS 15, HS 15); or a combination of polyethylene glycol 15-hydroxystearate and Tween 80, 15-hydroxystearate Acid polyethylene glycol (HS-15) and Tween 80 in a mass ratio of (1.5-5.5):1; or a combination of 15-hydroxystearic acid polyethylene glycol and Poloxamer 407, 15-hydroxy The mass ratio of polyethylene glycol stearate to poloxamer 407 (Pluronic F127) is (2.5-6.5):1.
[0031] Polyethylene glycol 400 is used as a co-solvent without ...
Embodiment 2
[0042] An ophthalmic nanomicelle antifungal solution containing isavuconazole, which consists of the following raw materials: 0.2 g of isavuconazole, 5 g of HS-15, 5 g of polyethylene glycol 400, and 99.8 g of water, prepared according to the following steps :
[0043] ① Weigh each raw material according to the formula;
[0044] ② Add isavuconazole to polyethylene glycol 400 and heat to 100°C to dissolve completely;
[0045] ③ Add the solubilizer HS-15 to the polyethylene glycol 400 dissolved in isavuconazole, and stir evenly;
[0046] ④ Add water to the uniformly stirred solubilizer and polyethylene glycol 400, and stir until a stable, uniform and transparent micellar solution is obtained;
[0047] ⑤ Filtrate the above-prepared micellar solution with a sterile filter to obtain an ophthalmic antifungal nano-micelle solution containing isavuconazole, which is colorless and transparent, and has a pH of 5.86.
Embodiment 3
[0049] An ophthalmic nanomicelle antifungal solution containing isavuconazole, which is composed of the following raw materials: 0.2 g of isavuconazole, 5 g of HS-15, 2.5 g of Tween 80, 5 g of polyethylene glycol 400, and 99.8 g of water , the preparation method is the same as in Example 2.
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Abstract
The invention discloses an isavuconazole-containing nano-micelle antifungal solution for eyes. The isavuconazole-containing nano-micelle antifungal solution is prepared from the following raw materials in parts by weight: 0.01-0.5 part of isavuconazole, 0.1-10 parts of a solubilizer, 2-10 parts of polyethylene glycol 400 and 90-99.8 parts of water. According to the isavuconazole-containing nano-micelle antifungal solution for eyes, through simple mixing of the isavuconazole, the polyethylene glycol 400, the solubilizer and the water, the isavuconazole nano-micelle is formed by self aggregation of the solubilizer; the average particle size of the isavuconazole nano micelle is smaller than 20nm; the isavuconazole nano micelle is stable in physical and chemical properties; the absorption of the isavuconazole nano micelle in cornea can be significantly promoted; through better absorption of the isavuconazole nano micelle in the cornea, the antifungal effect is better. The polyethylene glycol 400 is used as a co-solvent; other organic solvents are not needed; the nano micelle is not required to be specially treated after the nano micelle is prepared, namely the prepared nano micelle can be directly used; the preparation steps of the micelle are greatly simplified.
Description
technical field [0001] The invention relates to the field of medicine, in particular to an isavuconazole micelle solution for eye drops, in particular to a low-molecular nano-micelle solution capable of promoting isavuconazole corneal absorption and a preparation method thereof. Background technique [0002] Fungal keratitis is a kind of infectious eye disease that seriously threatens the vision of patients. It occurs mostly in developing countries and has become the leading cause of corneal blindness in my country, especially in our province with a large agricultural population. The rate has remained high. However, there are very few ocular anti-true drug preparations on the market, and currently only natamycin suspension has a relatively definite curative effect and can be used by patients. Isavuconazole is a new triazole antifungal drug, which exhibits strong antifungal activity in vivo and in vitro, especially against Aspergillus and Mucormyces. Similar to other antifun...
Claims
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Application Information
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