Lanosterol compound preparation for eyes

An ophthalmic preparation, technology of lanosterol, applied in the field of treatment or prevention of cataracts, ophthalmic preparations of lanosterol compounds, which can solve problems such as difficult to cure cataracts, difficult to dissolve in water, etc.

Inactive Publication Date: 2017-01-25
BIOTOOL LLC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Lanosterol is easily soluble in organic solvents, such as DMSO, etc., but extremely difficult to dissolve in water, which makes it difficult to achieve the purpose of curing cataract in the form of eye drops alone when it is used as the main active ingredient of eye medicine (Makley, McMenimenet al. 2015, Shanmugam PM, Barigali A et al. 2015)

Method used

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  • Lanosterol compound preparation for eyes
  • Lanosterol compound preparation for eyes
  • Lanosterol compound preparation for eyes

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0141] Preparation of Ophthalmic Preparations

[0142] The ophthalmic preparation of the present invention can be prepared with conventional equipment and methods according to the pharmaceutical components and proportions provided by the method of the present invention. Including the following methods:

[0143] Method 1: (a) a pharmaceutically acceptable carrier; and (b) a lanosterol compound as the first active ingredient are mixed to form the ophthalmic preparation of the present invention.

[0144] Method 2: mixing (a) a pharmaceutically acceptable carrier; and (b) a lanosterol compound as the first active ingredient and (c) the second active ingredient to form the ophthalmic preparation of the present invention .

[0145] Method 3:

[0146] (i) dispersing the lanosterol compound as the first active ingredient and the optional second active ingredient in the polyol to form a first dispersion;

[0147] (ii) mixing the first dispersion with the rest of the pharmaceuticall...

Embodiment 1

[0163] According to the literature (Zhao, Chen et al.2015), the eye drops were prepared according to the formula, and the therapeutic effect of lanosterol eye drops alone on cataract in dogs was evaluated without simultaneous intravitreal injection. 25mM lanosterol eye drops contain 12.5g lanosterol (Tokyo Chemical Industry, Japan), 200ml medical ethanol and 1.1g (EDTA) 2 Na and 0.55 g of benzalkonium chloride, the whole solution was prepared with triple distilled water and dissolved in 1.1 L. Incompletely dissolved lanosterol particles can be clearly seen inside the prepared solution.

[0164] The above-mentioned 25mM lanosterol eye drops are administered three times a day in the morning, noon and evening, with an interval of at least 5 hours between administrations. The subjects of the administration were dogs with cataract caused by various reasons. A total of 7 cataract-affected eyes participated in the test. The administration method was to drop directly into the eyes to...

Embodiment 2

[0166] The eye drop of the present invention is uniform, non-suspended, white liquid, completely water phase, the cosolvent is cyclodextrin, preferably hydroxypropyl-β-cyclodextrin, the concentration of lanosterol is 25mM, and the whole eye drop has no See white particles that are insoluble in the aqueous phase.

[0167] Eye Drops Formula:

[0168]

[0169] Note: During the preparation process, physical dissolution methods such as conventional ultrasound and heating can be used.

[0170] Administration method:

[0171] The above pharmaceutical preparations are administered three times a day in the morning, noon and evening, with an interval of at least 5 hours between administrations. The administration objects are dogs with cataract caused by various reasons, and the administration method is to drop directly into the eyes to ensure that the medicine is completely instilled into the eyes. One drop, about 50 microliters, was administered to each affected eye of each treat...

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Abstract

The invention discloses a lanosterol compound preparation for eyes, particularly a pharmaceutical composition comprising 5-250mM lanosterol compounds and a preparation method of the pharmaceutical composition, and application of the pharmaceutical composition in the aspects of prevention and treatment of ophthalmic diseases.

Description

technical field [0001] The invention relates to the field of ophthalmic medicines, in particular, the invention discloses an ophthalmic preparation form of lanosterol compound and its use for treating or preventing cataract. Background technique [0002] Cataract is a common blinding eye disease with blurred vision and vision loss as the main symptoms. Among the 40 million to 45 million blind people in the world, cataract blindness accounts for 60%. Cataracts occur on the lens of the eye. Due to factors such as aging, genetics, local nutritional disorders, immune and metabolic abnormalities, trauma, radiation and other factors, the individual patient's crystal metabolism is disordered, resulting in lens protein denaturation and wrong accumulation, thereby affecting the light entering the eye. Retina, eventually manifested as symptoms of blurred vision or even complete loss of vision (Bloemendal, de Jong et al. 2004). [0003] The incidence of cataract is not limited to huma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61K31/4174A61K9/08A61K47/10A61K47/40A61K47/26A61K47/36A61P27/12
CPCA61K9/08A61K31/4174A61K31/575A61K47/10A61K47/26A61K47/36A61K47/40A61P27/12A61K9/0048A61K2300/00
Inventor 郑钦元责祎旦·加帕尔
Owner BIOTOOL LLC
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