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Ophthalmic composition containing geranylgeranylacetone

一种基香叶基丙酮、组合物的技术，应用在眼科用组合物领域，能够解决视网膜疾病改善效果在实用不充分等问题，达到促进存活、抑制细胞死亡的效果

Inactive Publication Date: 2014-11-05
ROHTO PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, the ameliorating effect of retinal diseases produced by teprenone containing 5E, 9E, 13E geranylgeranyl acetone and 5Z, 9E, 13E geranyl geranyl acetone in a weight ratio of 3:2 was not confirmed in practice. not enough

Method used

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Examples

Experimental program
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preparation example Construction

[0118] Methods for the preparation of ophthalmic formulations are well known. It can be prepared by mixing GGA with a pharmaceutically acceptable base or carrier, pharmaceutically acceptable additives for ophthalmic preparations, and other active ingredients (physiologically active ingredients or pharmacologically active ingredients other than GGA).

[0119]

[0120] Examples of the base or carrier include water; aqueous solvents such as polar solvents; polyhydric alcohols; vegetable oils; Examples of bases or carriers for intraocular injections include distilled water for injection or physiological saline.

[0121] A base or a carrier may be used alone or in combination of two or more.

[0122]

[0123] Examples of additives include surfactants, fragrances or refreshing agents, preservatives, bactericides or antibacterial agents, pH adjusters, isotonic agents, chelating agents, buffers, stabilizers, antioxidants, thickeners, and the like. Intraocular injections may ...

Embodiment

[0227] Hereinafter, although an Example is given and this invention is demonstrated in more detail, this invention is not limited to these Examples.

[0228] (1) Preparation of geranylgeranyl acetone

[0229] Commercially available teprenone (all-trans body: 5Z monocis body = weight ratio 3:2) (Wako Pure Chemical Industries, Ltd.) was purchased, and the all-trans body was purified by silica gel column chromatography.

[0230] As specific conditions, silica gel (PSQ60B, manufactured by Fuji Silicon Chemical Co., Ltd.) was filled in a glass tube, and fractional purification was performed with a mobile phase (n-hexane:ethyl acetate=9:1). After fractionation, each fraction was concentrated and dried under reduced pressure, and then the purity and structure of the all-trans isomer were confirmed by GC and 1H-NMR (solvent: deuterated chloroform, internal standard: tetramethylsilane) (yield is about 20%).

[0231]

[0232] Chromatographic column: DB-1 (J&Wscientific, 0.53mm×30m...

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PUM

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Abstract

An ophthalmic composition comprising geranylgeranylacetone which (a) is a mixture of (5E,9E,13E)-geranylgeranylacetone and (5Z,9E,13E)-geranylgeranylacetone, the (5E,9E,13E)-geranylgeranylacetone content of the mixture being 80% by weight or more, (b) consists of (5E,9E,13E)-geranylgeranylacetone, or (c) consists of (5Z,9E,13E)-geranylgeranylacetone protects various types of retinal cells from degeneration, impairment or destruction, thereby remarkably promoting the survival. Consequently, the composition exhibits a remarkable effect of preventing, ameliorating or treating various retinal diseases. In addition, the composition hardly becomes white turbid during storage.

Description

technical field [0001] The present invention relates to ophthalmic compositions comprising geranylgeranylacetone. Background technique [0002] Teprenone (Eisai Co., Ltd.) is a mixture containing 5E, 9E, 13E geranylgeranyl acetone and 5Z, 9E, 13E geranyl geranyl acetone in a weight ratio of 3:2. Teprenone is widely used as a therapeutic agent for peptic ulcer for oral administration. [0003] In addition, a protocol for the use of teprenone in the field of ophthalmology has also been proposed. For example, Patent Document 1 teaches the use of teprenone as an active ingredient of a preventive or therapeutic agent for dry eye syndrome, eye fatigue, or dry eyes. Furthermore, Patent Document 2 discloses a clear eye drop comprising teprenone, phospholipids, a synthetic surfactant, and water. [0004] In addition, it is also known that geranylgeranylacetone (Eisai Co., Ltd.), whose cis-trans isomer ratio is not limited, is useful as an active ingredient of a therapeutic agent f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/121A61K9/06A61K9/08A61K47/04A61P27/02A61P27/04
CPCA61K47/26A61K47/44A61K47/02A61K31/121A61K9/0048A61P27/02A61P27/04
Inventor 宫野贵之黑濑孝弘加藤万里代高井良宏
Owner ROHTO PHARM CO LTD
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