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Ophthalmic composition

A composition and ophthalmic technology, applied in the directions of drug combination, drug delivery, medical preparations of inactive ingredients, etc., can solve problems such as the reduction of the content rate, and achieve inhibition of adsorption, inhibition of the reduction of the content rate or concentration, and good stability. Effect

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

AI Technical Summary

Problems solved by technology

[0005] However, the ophthalmic composition containing geranylgeranyl acetone has the disadvantage that the content rate tends to decrease due to storage.

Method used

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Examples

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preparation example Construction

[0077] 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).

[0078]

[0079] 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.

[0080] A base or a carrier may be used alone or in combination of two or more.

[0081]

[0082] Examples of additives include surfactants, fragrances or refreshers, preservatives, bactericides or antibacterial agents, pH adjusters, isotonic agents, chelating agents, buffers, stabilizers, other antioxidants, thickeners, and the like. Intraocular injections may c...

Embodiment

[0157] Hereinafter, although an Example is given and this invention is demonstrated in more detail, this invention is not limited to these Examples.

[0158] (1) Preparation of geranylgeranyl acetone

[0159] Commercially available teprenone (Wako Pure Chemical Industries, Ltd.) (all-trans form: 5Z monocis form (weight ratio) = 6:4) was purchased, and the all-trans form was purified by silica gel column chromatography.

[0160] 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%).

[0161]

[0162] Chromatographic column: DB-1 (J&Wscientific, 0.53mm...

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Abstract

An ophthalmic composition comprising geranylgeranylacetone and a fat-soluble antioxidant has an advantage that adsorption of geranylgeranylacetone to a wall of a container is remarkably reduced and thereby the loss of the geranylgeranylacetone content or decrease in the geranylgeranylacetone concentration in the composition is remarkably reduced. Adsorption of the fat-soluble antioxidant to a wall of a container is also reduced due to combination with geranylgeranylacetone.

Description

technical field [0001] The present invention relates to ophthalmic compositions comprising geranylgeranylacetone. Background technique [0002] Teprenone (Eisai Co.) contains 5E, 9E, 13E geranyl geranyl acetone (hereinafter sometimes referred to as "all-trans body") and 5Z, 9E, 13E geranyl in a weight ratio of 3:2 A mixture of geranylacetone (hereinafter sometimes referred to as "5Z monocis-isomer"). 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. [0004] Furthermore, Patent Document 2 discloses a clear eye drop comprising teprenone, phospholipids, a synthetic surfactant, and water. [0005] However, an ophthalmic composition containing geranylgeranylac...

Claims

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Application Information

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IPC IPC(8): A61K31/121A61K9/06A61K9/08A61K47/04A61P27/02
CPCA61K47/10A61K47/14A61K9/08A61K47/44A61K47/22A61K31/121A61K9/06A61K9/0048A61P27/02A61P27/04
Inventor 宫野贵之黑濑孝弘
Owner ROHTO PHARM CO LTD
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