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Eye antifungal nano-micelle solution containing terbinafine hydrochloride

A technology of terbinafine hydrochloride and nanomicelle solution, applied in the field of medicine, can solve the problems of sticking, difficult to clean, strong eye irritation, etc., and achieves stable physical and chemical properties, good antifungal effect, and good eye absorption. Effect

Active Publication Date: 2015-11-04
河南省眼科研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But terbinafine hydrochloride is very poor in water solubility, and it is difficult to be formulated into aqueous solution type eye drops. Most of the relevant researches at present use vegetable oil as a solvent to be formulated into eye drops. Oily solutions have shown that 0.25% terbinafine hydrochloride oil solution It can obtain antibacterial spectrum and antifungal activity similar to natamycin preparations, and has a good therapeutic effect on ocular fungal infections
However, the oil is inconvenient to use, the eyes are highly irritating, sticky, blurred and difficult to clean up, and the eye absorption is not ideal. Therefore, the clinical application of terbinafine hydrochloride ophthalmic oil is not very extensive.
However, the current situation of ocular antifungal drug treatment is not optimistic. At present, there is only "natamycin eye drops" which is an antifungal eye drop with good therapeutic effect in the market. antifungal drugs
The anti-fungal effects of terbinafine hydrochloride in vivo and in vitro are very ideal, but the unfavorable factors of the dosage form and the earth limit the application of terbinafine hydrochloride in the treatment of fungal eye diseases, so a new dosage form of terbinafine hydrochloride is developed becomes more important

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0025] An ophthalmic antifungal nano-micelle solution containing terbinafine hydrochloride, which mainly consists of the following raw materials in parts by weight: 0.05-1 part of terbinafine hydrochloride, 0.5-10 parts of solubilizer, 0.5-10 parts of glycerin, Bacteriostat 0.003~0.05 parts, thickener 0.05~0.2 parts, water 90~99.8 parts.

[0026] The solubilizer is one or a combination of polyethylene glycol 15-hydroxystearate (HS 15) and polyoxyethylene ether (40) hydrogenated castor oil (RH 40); the pH The bacterial agent is one of benzalkonium chloride, benzalkonium bromide and ethylparaben; the thickener is hyaluronic acid and its salt, hydroxypropylmethylcellulose, polyvinyl alcohol and hydroxypropylcellulose one or a combination of several.

[0027] The preparation method of the above-mentioned ophthalmic antifungal nano-micelle solution containing terbinafine hydrochloride comprises the following steps:

[0028] ① Weigh each raw material according to the formula;

[...

Embodiment 2

[0035] An ophthalmic antifungal nano-micelle solution containing terbinafine hydrochloride, which mainly consists of the following raw materials in parts by weight: 0.2-0.5 parts of terbinafine hydrochloride, 1-4 parts of solubilizer, 1-4 parts of glycerin, Bacteriostat 0.01~0.03 parts, thickener 0.1~0.15 parts, water 92~96 parts.

[0036] The solubilizer is one or a combination of polyethylene glycol 15-hydroxystearate (HS 15) and polyoxyethylene ether (40) hydrogenated castor oil (RH 40); the pH The bacterial agent is one of benzalkonium chloride, benzalkonium bromide or ethylparaben; the thickener is hyaluronic acid and its salt, hydroxypropyl methylcellulose, polyvinyl alcohol or hydroxypropyl fiber One or a combination of several elements.

[0037] The preparation method of the above-mentioned ophthalmic antifungal nano-micelle solution containing terbinafine hydrochloride comprises the following steps:

[0038] ① Weigh each raw material according to the formula;

[00...

Embodiment 3

[0045] An ophthalmic antifungal nano-micelle solution containing terbinafine hydrochloride, which mainly consists of the following raw materials in parts by weight: 0.5 g of terbinafine hydrochloride, 5 g of polyoxyethylene ether (40) hydrogenated castor oil, and 3.125 g of glycerin , 0.04 g of bacteriostatic agent benzalkonium chloride, 0.2 g of hydroxypropyl methylcellulose, and 99 g of water.

[0046] The preparation method of the above-mentioned ophthalmic antifungal nano-micelle solution containing terbinafine hydrochloride comprises the following steps:

[0047] ① Weigh each raw material according to the formula;

[0048] ② Add terbinafine hydrochloride to glycerin and heat to dissolve completely;

[0049] ③ Add the solubilizer to the glycerin dissolved in terbinafine hydrochloride, and stir evenly;

[0050] ④ Dissolve the thickener and antibacterial agent in hot water at 80°C;

[0051] ⑤ Add the hot water with thickener and antibacterial agent into the uniformly stirre...

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Abstract

The invention discloses an eye antifungal nano-micelle solution containing terbinafine hydrochloride. The eye antifungal nano-micelle solution consists of the following raw materials in parts by weight: 0.05-1 part of terbinafine hydrochloride, 0.5-10 parts of a solubilizer, 0.5-10 parts of glycerinum, 0.003-0.05 part of a bacteriostatic agent, 0.05-0.2 part of a thickening agent and 90-99.8 parts of water. According to the eye terbinafine hydrochloride antifungal nano-micelle solution disclosed by the invention, terbinafine hydrochloride nano-micelle is prepared from the solubilizer by self aggregation, the average particle size of the terbinafine hydrochloride nano-micelle is smaller than 30nm, the characters are not greatly changed after the terbinafine hydrochloride nano-micelle is subjected to freezing redissolution and boiling sterilization for 30 minutes and then cooled to room temperature, and the physicochemical properties are also stable. Water is taken as a solvent of the eye antifungal nano-micelle solution, and no organic solvent is used in the preparation process, so that the eye antifungal nano-micelle solution is small in irritation, relatively convenient to drop into eyes, free of phenomenon of adhesion or fuzziness, relatively long in eye acting time, relatively good in absorption by eyes, and relatively good in antifungal effect, and use comfort degree of patients can be greatly increased.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an ophthalmic antifungal nano-micelle solution containing terbinafine hydrochloride and a preparation method thereof. Background technique [0002] Terbinafine hydrochloride (TH) belongs to the allylamine antifungal drug, which mainly exerts strong antibacterial and bactericidal effects by inhibiting squalene cyclooxygenase. It has a wide antibacterial spectrum and strong bactericidal power, and is particularly sensitive to dermatophytes , The clinical application is very extensive, recent studies have found that TH has a high sensitivity to most ocular infection fungi. But terbinafine hydrochloride is very poor in water solubility, and it is difficult to be formulated into aqueous solution type eye drops. Most of the relevant researches at present use vegetable oil as a solvent to be formulated into eye drops. Oily solutions have shown that 0.25% terbinafine hydroch...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/137A61K47/44A61K47/38A61K47/36A61K47/34A61P27/02A61P31/10
Inventor 周天洋张俊杰王丽娅
Owner 河南省眼科研究所
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