JP2011213599A - Ophthalmic composition for soft contact lens - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an ophthalmic composition for a soft contact lens that ameliorates a dry feeling of eyes during wearing a soft contact lens.SOLUTION: The ophthalmic composition for a soft contact lens that ameliorates a dry feeling of eyes during wearing a soft contact lens comprises (A) vitamin A, (B) panthenol, and (C) a nonionic surfactant and a polyhydric alcohol.

Description

  The present invention relates to an ophthalmic composition that improves the dryness of the eye when a soft contact lens is mounted. Specifically, the present invention relates to an ophthalmic composition for soft contact lenses containing vitamin A and panthenol.

  Wearing contact lenses causes various problems such as dry eyes, tired eyes, itching, and hyperemia. In particular, in the case of a soft contact lens, since wearability is good, it can be worn for a long time and often complains of dryness of the eyes. Thus, an ophthalmic composition for improving dry feeling (see Patent Document 1) containing fat-soluble vitamins has been disclosed, but the effect was not sufficient.

  In addition, eye drops for contact lenses containing amino acids for the purpose of activating the cornea's physiological functions, and soft contacts that contain a refreshing agent for the purpose of improving lens wettability and eliminating foreign body sensations and itchiness. Although eye drops for lenses (see Patent Documents 2 and 3) and the like have been disclosed, they were not satisfactory with respect to dry eyes and fatigue that are peculiar to wearing soft contact lenses.

JP 2001-158734 A JP-A-11-130667 Japanese Patent Laid-Open No. 11-180858

  An object of the present invention is to provide an ophthalmic composition that improves the dryness of the eye when a soft contact lens is mounted.

  As a result of intensive studies to solve the above-mentioned problems, the inventors have (A) vitamin A, (B) panthenol, (C) a nonionic surfactant and a polyhydric alcohol. The present inventors have found that the dryness of the eye when the soft contact lens is worn is improved, and have completed the present invention.

Accordingly, the present invention provides the following ophthalmic composition for soft contact lenses.
[1]. An ophthalmic composition for soft contact lenses containing (A) vitamin A, (B) panthenol, (C) a nonionic surfactant and a polyhydric alcohol and substantially free of preservatives.
[2]. The ophthalmic composition for soft contact lenses according to claim 1, wherein the pH is 5.5-8.

  According to the present invention, it is possible to provide an ophthalmic composition for a soft contact lens that can improve the dryness of the eye when the soft contact lens is mounted.

Vitamin A used in the present invention includes vitamin A, retinol palmitate, retinol acetate, and vitamin A oil. Preferable examples include retinol palmitate. Retinol palmitic acid ester is usually commercially available containing 1 million to 1.8 million international units (hereinafter abbreviated as I.U.) in 1 g, specifically, retinol palmitic acid manufactured by DSM Nutrition Japan Co., Ltd. There is an ester.
Vitamin A can be used alone or in combination of two or more, and the content thereof is 0.001 to 0.5 w (mass) / v (volume)% with respect to the total amount of the ophthalmic composition. (Hereinafter referred to as w / v%), preferably 0.002 to 0.2 w / v%, more preferably 0.004 to 0.1 w / v%.

The panthenol and derivatives thereof used in the present invention include panthenol and derivatives thereof that can be used for ophthalmology. Specific examples include panthenol, pantethine, pantethein pantotenyl alcohol, and pantotenyl ethyl ether. Among the above, panthenol (for example, manufactured by Fuji Pharmaceutical Co., Ltd.) is particularly preferable with respect to stability. Pantothenic acid can also be contained as long as the stability is not impaired.
As for pantenol, 0.001-10 w / v% is preferable with respect to the ophthalmic composition whole quantity. More preferably, it is 0.01-5 w / v%.

The nonionic surfactant used in the present invention is blended as a component that suppresses solubilization of vitamin A and adsorption to a soft contact lens. Examples of the nonionic surfactant include polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan monooleate, polyoxyethylene (hereinafter also referred to as POE) and polyoxypropylene (hereinafter also referred to as POP) glycol. . Specifically, for example, polyoxyethylene hydrogenated castor oil is manufactured by Nikko Chemicals Co., Ltd. HCO-40, HCO-50, HCO-60, etc., and polyoxyethylene sorbitan monooleate is manufactured by Nikko Chemicals Co., Ltd. -10, TO-10MV and the like.
Polyoxyethylene polyoxypropylene glycol is not particularly limited, and those described in the standard for pharmaceutical additives (medicine regulations) can be used. The average degree of polymerization of ethylene oxide is preferably 4 to 200, more preferably 20 to 200, and the average degree of polymerization of propylene oxide is preferably 5 to 100, more preferably 20 to 70, and may be a block copolymer or a random polymer. Specifically, polyoxyethylene (200) polyoxypropylene (70) glycol such as Unilube 70DP-950B (manufactured by NOF Corporation), polyoxyethylene (196) polyoxypropylene (67) glycol (Pluronic F127, Polyoxyethylene (160) polyoxypropylene (30), such as polyoxyethylene (120) polyoxypropylene (40) glycol (Pluronic F-87), pronon # 188P (NOF Corporation), etc. Polyoxyethylenes such as glycol (Pluronic F-68, also known as Poloxamer 188), polyoxyethylene (42) polyoxypropylene (67) glycol (Pluronic P123, also known as Poloxamer 403), Pronon # 235P (Nippon Oil Co., Ltd.) 54) Polyoxypropylene (39) glycol (Pluronic P85), polyoxyethylene (20) polyoxypropylene (20) glycol (Pluronic L-44), Tetronic and the like. Of these, polyoxyethylene (200) polyoxypropylene (70) glycol, polyoxyethylene (160) polyoxypropylene (30) glycol, and polyoxyethylene (54) polyoxypropylene (39) glycol are preferred.
The compounding amount of the nonionic surfactant in the composition is usually 0.01 to 0.5 w / v%, preferably 0.05 for polyoxyethylene hydrogenated castor oil and polyoxyethylene sorbitan monooleate. ~ 0.3 w / v%.
Polyoxyethylene polyoxypropylene glycol is 0.4 to 5.0 w / v%, preferably 0.5 to 3 w / v%, and more preferably 1.0 to 2 w / v%.
If the blending amount of the nonionic surfactant in the composition is small, solubilization of vitamin A becomes difficult, and if it is large, the storage stability of vitamin A is lowered.

  The polyhydric alcohol used by this invention is mix | blended as a component which suppresses adsorption | suction to the soft contact lens of vitamin A. Examples of the polyhydric alcohol include glycerin, propylene glycol, 1,3-butanediol, and polyethylene glycol. Particularly preferred are propylene glycol and glycerin. The blending amount of the polyhydric alcohol in the composition is preferably 0.01 to 10 w / v%, more preferably 0.05 to 5.0 w / v%. If it is this range, adsorption | suction to the soft contact lens of vitamin A can be suppressed.

  The ophthalmic composition of the present invention can withstand secondary contamination without blending preservatives such as benzalkonium chloride and sorbic acid. In addition to the above components, various components blended in the ophthalmic composition , And can be blended within a range not impairing the effects of the present invention. These components include buffers, thickeners, pH adjusters, isotonic agents, stabilizers, cooling agents, drugs, water and the like. These can be used individually by 1 type or in combination of 2 or more types, respectively, and can mix | blend suitable amount.

  Examples of the buffer include boric acid or a salt thereof (such as borax), citric acid or a salt thereof (such as sodium citrate), phosphoric acid or a salt thereof (such as sodium monohydrogen phosphate), tartaric acid or a salt thereof (tartaric acid) Sodium, etc.), gluconic acid or salts thereof (sodium gluconate, etc.), acetic acid or salts thereof (sodium acetate, etc.), various amino acids, etc. (epsilon-aminocaproic acid, potassium aspartate, aminoethylsulfonic acid, glutamic acid, sodium glutamate, etc.) And trometamol. Of these, trometamol is preferred because it has a good antiseptic power. Furthermore, in order to improve the preservative power of trometamol, it is preferable to use boric acid and borax in combination. The content of the buffer is preferably 0.001 to 10 w / v% in the ophthalmic composition, and more preferably 0.01 to 5 w / v%.

  Examples of the thickener include hydroxyethyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, polyvinyl alcohol, sodium hyaluronate, polyacrylic acid, carboxyvinyl polymer, and the like. The compounding quantity of a thickener is 0.001-10 w / v%, for example, Preferably it is 0.001-5 w / v%, More preferably, it is 0.01-3 w / v%.

  As the pH adjuster, it is preferable to use an inorganic acid or an inorganic alkali agent. For example, (diluted) hydrochloric acid is mentioned as an inorganic acid. Examples of the inorganic alkaline agent include sodium hydroxide, potassium hydroxide, sodium carbonate, sodium hydrogen carbonate and the like. Among these, hydrochloric acid and sodium hydroxide are preferable. The pH (20 ° C.) of the ophthalmic composition of the present invention is preferably 4.0 to 9.0, more preferably 5.0 to 8.0, and still more preferably 5.5 to 8.0. The pH is measured at 20 ° C. using a pH osmometer (HOSM-1, Toa DKK Co.). The compounding quantity of a pH adjuster is 0.00001-10 w / v%, for example, Preferably it is 0.0001-5 w / v%, More preferably, it is 0.001-3 w / v%.

  Examples of the isotonic agent include sodium chloride and potassium chloride. The compounding quantity of an isotonizing agent is 0.001-5 consideration%, for example, Preferably it is 0.01-3 w / v%, More preferably, it is 0.1-2 w / v%.

  Examples of the stabilizer include edetic acid, sodium edetate hydrate, cyclodextrin, sulfite, dibutylhydroxytoluene and the like. In order to further improve the preservative power, it is preferable to contain edetic acid and / or a salt thereof. The compounding quantity of a stabilizer is 0.001-5 w / v%, for example, Preferably it is 0.01-3 w / v%, More preferably, it is 0.1-2 w / v%.

  Examples of the refreshing agent include menthol, camphor, borneol, geraniol, and the like. The content of the refreshing agent is preferably 0.0001 to 5 w / v%, more preferably 0.001 to 2 w / v%, and more preferably 0.005 to 1 w / v%, as the total amount of the compound in the ophthalmic composition. Further preferred is 0.007 to 0.8 w / v%.

  Examples of drugs (pharmaceutical active ingredients) include other vitamins (eg, pyridoxine hydrochloride, tocopherol acetate), decongestants (eg, naphazoline hydrochloride, tetrahydrozoline hydrochloride, phenylephrine hydrochloride, epinephrine, ephedrine hydrochloride, dl-methyl hydrochloride) Ephedrine, tetrahydrozoline nitrate, naphazoline nitrate, etc.), flame retardant / astringent (eg, neostigmine methyl sulfate, ε-aminocaproic acid, allantoin, berberine chloride, zinc sulfate, zinc lactate, lysozyme chloride, dipotassium glycyrrhizinate, ammonium glycyrrhizinate, glycyrrhetin) Acid, methyl salicylate, tranexamic acid, sodium azulene sulfonate, etc.), antihistamines (eg, iproheptin hydrochloride, diphenhydramine hydrochloride, diphenhydramine, hydrochloric acid) Sotipendil, chlorpheniramine maleate, etc.), amino acids (eg, potassium L-aspartate, magnesium L-aspartate, aminoethylsulfonic acid, etc.), sulfa drugs, fungicides (eg, sulfur, isopropylmethylphenol, hinokitiol, etc.), A local anesthetic (for example, lidocaine, lidocaine hydrochloride, procaine hydrochloride, dibucaine hydrochloride, etc.) and an antiallergic agent (for example, sodium cromoglycate, etc.) can be appropriately blended.

  The compounding amounts of these components in the ophthalmic composition are appropriately selected according to the type of preparation, the type of drug, and the like, and the compounding amounts of various components are known in the art. For example, it can be selected from a range of about 0.0001 to 30 w / v%, preferably about 0.001 to 10 w / v% with respect to the whole preparation. More specifically, the content of each component is, for example, as follows for the ophthalmic composition.

  If it is a decongestant, for example, it is 0.0001 to 0.5 w / v%, preferably 0.0005 to 0.3 w / v%, more preferably 0.001 to 0.1 w / v%. If it is a flame retardant / astringent, it is 0.0001-10 w / v%, for example, Preferably it is 0.0001-5 w / v%. If it is an antihistamine, it is 0.0001-10 w / v%, for example, Preferably it is 0.001-5 w / v%. If it is an amino acid, it is 0.0001-10 w / v%, Preferably it is 0.001-3 w / v%. If it is a sulfa agent and a disinfectant, it is 0.00001-10 w / v%, for example, Preferably, it is 0.0001-10 w / v%. If it is a local anesthetic, it is 0.001-1 w / v%, for example, Preferably it is 0.01-1 w / v%. If it is an antiallergic agent, it is 0.001-5 w / v%, for example, Preferably it is 0.01-3 w / v%.

  Specific examples of usage forms of the ophthalmic composition of the present invention include eye drops for soft contact lenses, soft contact lens mounting liquid, soft contact lens removal liquid, and the like.

  The ophthalmic composition of the present invention is liquid, and the viscosity of the ophthalmic composition is preferably 1 to 50 mPa · s, more preferably 1 to 20 mPa · s, and further preferably 1 to 5 mPa · s. The viscosity is measured at 20 ° C. using an E-type viscometer (VISCONIC ELD-R, Tokyo Keiki Co., Ltd.).

<Manufacturing method>
The method for preparing the ophthalmic composition of the present invention is not particularly limited. For example, in the case of eye drops, fat-soluble vitamins are first solubilized in sterilized purified water with a nonionic surfactant, and then polymer compounds. It can be obtained by adjusting the pH by adding each compounding component such as.
Thereafter, it can be aseptically filled into a suitable container such as a container made of polyethylene terephthalate.

Hereinafter, the present invention will be described in more detail using examples, but the present invention is not limited to these examples.

[Example 1 and Comparative Examples 1-2]
<Improved dryness of eyes by wearing soft contact lenses>
Eye drops were prepared by a conventional method according to the composition shown in Table 1.
For 6 subjects wearing soft contact lenses, the eye drops of Example 1 and the eye drops of Comparative Example 1 and Comparative Example 2 were instilled, and the degree of improvement in dryness of the eyes by wearing the soft contact lens was investigated for each. It was. The obtained results were evaluated according to the following evaluation criteria. The results are shown in Table 2.

(Evaluation criteria)
5 points: Dry feeling improved 4 points: Dry feeling slightly improved 3 points: Dry feeling did not change 2 points: Dry feeling became slightly worse 1 point: Dry feeling became worse

表２の結果から、レチノールパルミチン酸エステルを含有した比較例１を点眼した眼は乾燥感が改善されたが、これにパンテノールを配合した実施例１では、さらに乾燥感の改善が認められ、両成分を含まない比較例２を点眼した眼では乾燥感の改善はほとんど変化がなかった。これらのことより、レチノールパルミチン酸エステル及びパンテノールを含有する眼科組成物の点眼により、ソフトコンタクトレンズ装着による眼の乾燥感を改善することが確認された。

From the results in Table 2, the eye feeling of Comparative Example 1 containing retinol palmitic acid ester was improved in dryness, but in Example 1 in which panthenol was added thereto, further improvement in dryness was observed, The improvement in dryness was hardly changed in the eyes instilled with Comparative Example 2 containing neither component. From these facts, it was confirmed that the ophthalmic composition containing retinol palmitate and panthenol improved the dryness of the eye by wearing a soft contact lens.

<Raw materials>
The raw materials used in Examples and Comparative Examples are as follows.
Retinol palmitate (DSM Nutrition Japan Co., Ltd., JP)
Panthenol (Daiichi Fine Chemical Co., Ltd.)
HCO-60 (Nippon Surfactant Kogyo Co., Ltd.)
Polysorbate 80 (Kao Corporation, JP Daily)
Propylene glycol (ADEKA Corporation, JP product)

[Examples 2 to 19]
Eye drops were prepared by a conventional method according to the compositions shown in Tables 3 to 6.

Also when Example 2 to Example 19 were instilled, the dryness of the eyes was improved.

Claims (2)

An ophthalmic composition for soft contact lenses containing (A) vitamin A, (B) panthenol, (C) a nonionic surfactant and a polyhydric alcohol and substantially free of preservatives. The ophthalmic composition for soft contact lenses according to claim 1, wherein the pH is 5.5-8.