JPH10155880A - Agent for contact lens - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an agent for contact lenses which has low toxicity to the eyes while having a sufficient sterilizing effect and is safely usable without exerting any influence at all on the properties of the contact lenses. SOLUTION: This agent for the contact lenses contains an alkyl amine compd. expressed by the formula [where, R1 is a 4 to 18C alkyl group, beef tallow alkyl or palm oil alkyl or R4 NHR5 - (where R4 is a 4 to 18C alkyl group, beef tallow alkyl or palm oil alkyl and R5 is a 1 to 3C alkylene group), R2 and R3 are each H or a 1 to 3C alkyl group] or its salt as the effective component for sterilization. This alkyl amine compd. or its salt is preferably incorporated into the agent in a range of 0.01 to 1000ppm.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a contact lens agent,
In particular, it has excellent antiseptic or bactericidal effects, is sufficiently safe for the eyes, and has no effect on the physical properties of contact lenses. The present invention relates to a contact lens agent which can be suitably used for the treatment of

[0002]

BACKGROUND ART In general, when a contact lens is worn, stains such as proteins and lipids derived from tears and eye oils,
Attaches to contact lenses. In addition, such dirt not only deteriorates a feeling of wearing, but also may cause a decrease in visual acuity and an eye disorder such as conjunctival congestion. In addition, when the contact lens is used continuously, microorganisms such as bacteria attached to the contact lens surface may grow while the contact lens is removed from the eyes and stored. In some cases, adverse effects such as infections may be caused on the eyes.

[0003] Therefore, in order to wear a contact lens safely and comfortably, it is necessary to periodically perform cleaning, disinfection, and the like. A general method of such contact lens cleaning is as follows. It looks like this:
First, the contact lens removed from the eyes is rubbed and washed with a detergent containing a surfactant, thereby removing lipid stains attached to the contact lens. When it is necessary to remove protein stains, the protein is removed by immersion in a detergent containing a protease. Then, after rinsing with a rinsing solution, immerse the contact lens in a case filled with a preservative solution and store it in that state.
That is. In addition, particularly in the case of care of a hydrated contact lens, microorganisms easily adhere to the surface of such a hydrated contact lens and are easily proliferated. It is necessary to use a device to perform boiling disinfection for each case containing contact lenses.

[0004] As described above, the maintenance work for the contact lens is complicated, and for the maintenance,
Several types of liquids and devices such as a cleaning solution, a preservation solution, and a boiling device had to be prepared, and the labor and cost involved in using and maintaining them would be a heavy burden for the contact lens user.

[0005] In order to solve such problems, in recent years, a simpler and less costly method for caring for contact lenses has been to use a surfactant, a protein removing agent,
There have been proposed several methods of using a contact lens liquid so that a single liquid can be used to perform all necessary care for a contact lens by adding a disinfectant. For such a disinfection treatment in a care method using a contact lens solution, a chemical disinfection method using a disinfectant is adopted instead of the heat disinfection method requiring a boiling device as described above. From there,
This eliminates the need for a boiling operation using a dedicated device as in the related art, thereby greatly improving the user's labor for maintaining the contact lens.

[0006] Such a contact lens solution which can be used as a germicidal solution having a chemical disinfecting effect and at the same time as a preservative solution has the following properties.
Not only is it necessary to have a high bactericidal effect, but also because the contact lens is immersed in the liquid for a long time, it has low toxicity to the eyes and physical properties of the contact lens It is also required that it does not affect

By the way, thimerosal, chlorhexidine, quaternary ammonium salts (eg, benzalkonium chloride) and the like are used as germicides used for the chemical disinfectants for contact lenses that are currently on the market. For example, in JP-A-52-109953, JP-A-62-153217 and JP-A-63-59960, benzalkonium chloride is added in an amount of 0.001.
A contact lens disinfectant and a contact lens disinfectant using chlorhexidine in an amount of 0.01 to 0.05% have been proposed. However, recently, it has been reported that such a bactericide acts as an allergic sensitizer and harms the eyes, and there is a need for a contact lens agent that is safer for the eyes. is there.

[0008]

Here, the present invention has been made in view of such circumstances, and it is an object of the present invention to solve the above problems, while having sufficient bactericidal efficacy, low toxicity to the eyes, and An object of the present invention is to provide a contact lens agent that can be used safely without affecting the physical properties of the contact lens at all.

[0009]

The present inventors have conducted intensive studies on a bactericide in a contact lens agent in order to solve the above-mentioned problems. As a result, the present inventors have heretofore been known as a corrosion inhibitor (rust inhibitor) or the like. It has been found that the specified alkylamine compounds or salts thereof have low toxicity to the eyes and are sufficiently safe to be used as an antiseptic / bactericidal component of contact lens agents, and have been further studied. As a result of this, if such an alkylamine compound or a salt thereof is included in a contact lens agent as an antiseptic / disinfectant, the agent has sufficient sterilizing effect and safety to be used as a contact lens agent. Thus, the present invention was completed.

That is, the present invention has been developed to solve the above-mentioned problems.

Embedded image [Where R ₁ is an alkyl group having 4 to 18 carbon atoms, tallow alkyl, coconut oil alkyl, or R ₄ NHR ₅ −
(Where R ₄ is an alkyl group having 4 to 18 carbon atoms, tallow alkyl or coconut oil alkyl, and R ₅ is an alkylene group having 1 to 3 carbon atoms), and R ₂ and R _2
3 is H or an alkyl group having 1 to 3 carbon atoms], a contact lens agent characterized by containing an alkylamine compound represented by the formula or a salt thereof as a bactericidal active ingredient; Is what you do.

As described above, the agent for contact lenses according to the present invention contains a predetermined alkylamine compound or a salt thereof as an active ingredient for preservation or disinfection, and is characterized by a broad antibacterial spectrum. It has a germicidal action, has low toxicity to the eyes, and does not affect the physical properties of contact lenses. It demonstrates.

In the contact lens agent according to the present invention, the alkylamine compound or a salt thereof is advantageously contained in the range of 0.01 to 1000 ppm.

[0013] In one preferred embodiment, the contact lens agent according to the present invention comprises:
In order to stabilize the hydrogen ion concentration of the contact lens agent in this range, a borate buffer is preferably added to adjust the pH to a range of 5 to 9. It will be included. By further containing this borate buffer, the pH stability can be improved.

[0014]

Briefly, the present invention relates to a method for preserving or disinfecting an agent for contact lenses, comprising an alkylamine compound having a predetermined structure (formula 2) or a salt thereof, which is excellent in bactericidal effect and eye safety. It is characterized in that it is used as a component, and it is another object of the present invention to obtain a contact lens agent that can easily perform such care for a contact lens.

By the way, the alkylamine compound represented by Chemical formula 2 used in the contact lens agent according to the present invention has been conventionally used as an anticorrosive (rust preventive) agent, a powder coating agent, an antistatic agent, an emulsifier, It has been used as an emulsifier, a flotation agent, and the like. In such an alkylamine compound represented by the above formula 2, R
₁ is an alkyl group having 4 to 18 carbon atoms, tallow alkyl,
It is coconut oil alkyl or R ₄ NHR ₅ —, in which the preferred carbon number is 6-14. Also, R ₂ and R ₃
Is H or an alkyl group having 1 to 3 carbon atoms, preferably H. R ₄ is an alkyl group having 4 to 18 carbon atoms, tallow alkyl or coconut oil alkyl, and preferably has 6 to 14 carbon atoms. R ₅ is an alkylene group having 1 to 3 carbon atoms. Further, examples of the salts of the alkylamine compound represented by Chemical Formula 2 include salts with organic acids such as acetic acid, lactic acid, and citric acid, and salts with inorganic acids such as hydrochloric acid, sulfuric acid, and nitric acid. Preferred among them are salts with acetic acid or hydrochloric acid. The alkylamine compound or salt thereof defined in this way is suitably used as a bactericidal component of the contact lens agent according to the present invention.

The alkylamine compound or a salt thereof is specifically, for example,
Wherein R ₁ is an alkyl group having 14 carbon atoms, and the salt thereof is an acetate;
Further, there is a laurylamine acetate in which R ₁ is an alkyl group having 12 carbon atoms and the salt is an acetate. Furthermore, in addition to them, laurylamine hydrochloride, stearylamine hydrochloride, oleylamine hydrochloride, octadecylamine hydrochloride, tallow alkylpropylenediamine acetate, coconut oil alkylpropylenediamine acetate and the like can be mentioned. In the present invention, one or more of these alkylamine compounds and salts thereof are used in combination.

Particularly preferred among such alkylamine compounds or salts thereof is tetradecylamine acetate. Products containing this tetradecylamine acetate are already commercially available. For example, under the name of “Nissan Cation MA”, a corrosion inhibitor (rust inhibitor), a bactericide, an algicide, a powder It is commercially available as body coating agents, antistatic agents, emulsifiers and the like.
In the present invention, such a product can be suitably used.

The above-mentioned alkylamine compound or a salt thereof exhibits an effective effect when its use concentration is in the range of 0.01 to 1000 ppm, and preferably 0.1 to 2 ppm.
When used in the range of 00 ppm, a particularly effective antiseptic or bactericidal effect is exhibited. If the concentration of the alkylamine compound or a salt thereof is lower than 0.01 ppm, it is difficult to obtain a sufficient antiseptic and bactericidal effect, and if the concentration is as high as 1000 ppm or more, the human body may be damaged. This is because there is a risk of adversely affecting the device.

Further, the pH value suitable for using the contact lens agent according to the present invention is effectively in the range of 5 to 9, preferably 6 to 9. Take it, take p
If the value of H is lower than 5 or higher than 9,
This is because it causes irritation to the eyes and may cause damage.

In order to keep the pH of such a contact lens agent effective and safe for the eyes, at least one kind of buffer is generally added. The agent is appropriately selected from various conventionally known agents and used.
Specific examples include a borate buffer, a phosphate buffer, a Tris buffer, a citrate buffer, and the like, and among them, those used in combination with a borate buffer or a Tris buffer. Preferably, more preferably, it is used in combination with a borate buffer. The mixing ratio of the buffer is generally 0.05 to 3.0 w / v%, preferably 0.1 to 1.5 w / v%. However, if the concentration of the buffer is lower than 0.05 w / v%, it is difficult to keep the pH of the agent for contact lenses constant, and even if the concentration is higher than 3.0 w / v%. , PH
This does not mean that the stability of the is improved.

Further, in the contact lens agent according to the present invention, a predetermined surfactant is advantageously added and contained in order to improve the effect of removing dirt such as eye oils adhered to the contact lens. Becomes As this surfactant, various types of conventionally known anionic, cationic, amphoteric, or nonionic surfactants can be used as long as they have high safety to living bodies and do not affect the material of contact lenses. Any of the agents can be selected.

Further, in the present invention, in order to obtain a higher bactericidal effect, it can be used in combination with another bactericide. Such fungicides that can be used in combination with the alkylamine compound or a salt thereof according to the present invention include:
Specifically, guanidine fungicides that are also cationic surfactants, quaternary ammonium salt fungicides, thiazoline fungicides, glycine-based fungicides that are also amphoteric surfactants, and the like. By being combined, the bactericidal effect of each bactericide is increased additively, and a more excellent bactericidal effect can be obtained than when such an alkylamine compound or a salt thereof is used alone.

In addition, other additives include a chelating agent, a thickening agent, a tonicity agent, a protein removing agent, and the like.
Any known substances can be used as long as they are safe for the living body and do not adversely affect the material of the contact lens. Alternatively, it is also possible to incorporate them in a contact lens agent in combination in a quantitative range that does not inhibit the bactericidal effect of the salts thereof. Specifically, as a chelating agent to be contained, there are sodium edetate, trihydroxymethylaminomethane, and the like, and as a thickener, propylene glycol, hydroxymethylcellulose, polyvinylpyrrolidone, a thickening polysaccharide, and the like. No. Further, the contact lens agent according to the present invention, as a rinsing liquid,
Alternatively, when used as a preservative, it is desirable to use an isotonic agent to reduce irritation to the eyes, in which case the osmotic pressure is generally adjusted to about 150 to 400 mOsm, preferably about 200 to 350 mOsm. You. As such a tonicity agent, sodium chloride, potassium chloride, sodium bicarbonate and the like can be used. Furthermore, when it is desired to have a cleaning effect on protein stains, serine protease, thiol protease,
It can be appropriately selected from among protein removing agents (proteolytic enzymes) such as metal proteases and carboxyl proteases, and can be contained.

By the way, the alkylamine compound or its salt according to the present invention can be supplied in a solid or liquid state, but when supplied as a solid, it may be supplied in preparation for use. As in the case of preparing an ordinary aqueous solution, it may be dissolved using an appropriate diluent. The contact lens agent thus obtained is clear and can be subjected to aseptic filtration or the like, if necessary.

When the contact lens is prepared using the contact lens agent according to the present invention obtained as described above, the contact lens is specifically treated according to the following method. First, a few drops of the contact lens agent according to the present invention are dropped on the contact lens removed from the eye, and then, while holding the contact lens between the thumb and the index finger or on the palm, for several tens of seconds. , Scrub. Next, the contact lens is rinsed with the contact lens agent, and then immersed in a storage case filled with the contact lens agent for 10 minutes to 24 hours, preferably 30 minutes to 4 hours to perform storage disinfection. It is. However, it should be understood that this is merely an example, and the method of caring for a contact lens using the agent of the present invention is not limited to the above.

By such a series of operations, the contact lens can be effectively and simply disinfected without using a special device such as a boiling device as in the related art. At the same time, since the alkylamine compound, which is a bactericidal component, has low toxicity to the eyes and does not affect the physical properties of the contact lens at all, the contact lens is used as the contact lens agent. Even when immersed for a long time, contact lenses can be disinfected safely without causing any damage to the eyes.

[0027]

EXAMPLES In order to clarify the present invention more specifically, some examples of the present invention will be shown below.
It goes without saying that the present invention is not subject to any restrictions by the description of such embodiments. In addition, in addition to the following examples, the present invention, in addition to the above-described specific description, various changes, corrections, and modifications based on the knowledge of those skilled in the art without departing from the spirit of the present invention. It should be understood that improvements can be made.

Example 1 {Test for bactericidal effect: effect of buffer} A borate buffer, a citrate buffer, and a Tris buffer were prepared according to the following formulation. ─Ingredients of borate buffer─ Boric acid 1.16% Borax 0 .11% Sodium chloride 0.31% {Citrate buffer component} Citric acid (anhydrous) 0.019% Sodium citrate 2.91% {Component of Tris buffer} 2-amino-2-hydroxymethyl-1,3-propanediol 0.061% sodium chloride ········· 0.59% hydrochloric acid

As test bacteria, Staphylococcus aureus (St.a.:St.
aphylococcus aureus ATCC 6538) and Candida albicans ATCC 10231 (Ca: Candida albicans ATCC 10231).
What was cultured at 5 ° C for 24 hours, and for Ca,
Cultured in a glucose peptone medium at 23 ° C. for 48 hours, each was suspended in physiological saline, and 10 ⁸ cfu
/ ML of the test bacterial solution.

On the other hand, various contact lens agents of Examples 1 to 3 of the present invention and Comparative Examples 1 to 3 were prepared with the component compositions shown in Table 1 below, and their pH was adjusted to be 7. Next, 10 mL of each of the prepared various contact lens agents was placed in another sterilized test tube, and 0.05 mL of the test bacterial solution was added thereto. Thereafter, the various test liquid mixtures were stored in a constant-temperature bath at 23 ° C.
After 4 and 24 hours, remove a fixed amount of each formulation
Each of the mixed solutions was diluted with sterilized physiological saline, and the number of viable cells was examined by a pour plate method. The culture conditions in this pour plate method were as follows: St.a. was at 35 ° C. × 3 days using soybean casein medium;
About a., it was made into the glucose peptone culture medium at 23 degreeC x 5 days.

According to the above method, the number of viable bacteria immediately after inoculation,
From the viable cell counts at 2, 4, and 24 hours after the preparation of the mixture, the reduction rate of the bacteria at each time point was determined. The results are also shown in Table 1. As the tetradecylamine acetate, "Nissan Cation MA" (manufactured by NOF CORPORATION) was used. Similarly, in the following examples, “Nissan cation M” was used as tetradecylamine acetate.
A "is used.

[0032]

From the above results, there is a bactericidal effect in combination with any of the buffers, especially borate buffers,
In combination with a Tris buffer, a more effective bactericidal effect is exhibited, and the most preferred combination is
Combination with borate buffer.

Example 2 << Test of bactericidal effect: influence of pH >> As a test bacterium, Staphylococcus aureus (St.a.) was used and in the same manner as in Example 1, 10 ⁸ cfu / mL test bacterium was used. While preparing the liquid, various contact lens agents of Examples 4 to 6 of the present invention were prepared in the component compositions shown in Table 2 below, and the pH was adjusted. Next, using the prepared various contact lens agents and the test bacterial solution, a compound solution thereof was prepared in the same manner as in Example 1, and 2, 4, and 24 hours after the preparation of the compound solution. Thereafter, a fixed amount of each compounded solution was taken out, the number of viable bacteria was checked for each compounded solution, the reduction rate at each time point was obtained, and the results were shown in Table 2.
Are also shown.

[0035]

From the above results, it can be concluded that the contact lens agent according to the present invention has a high bactericidal effect over a wide hydrogen concentration range of pH 6.0 to 8.0 which is acceptable in the ophthalmic field. I understand.

Example 3 {Test for bactericidal effect: effect on mold} As a test bacterium, Aspergillus niger (An: Aspergil)
lus niger ATCC 16404) and cultured in glucose peptone medium at 23 ° C. for 7 days.
Was suspended in a physiological saline solution containing 0.05% of spores, and the spore suspension obtained by filtration with sterile polypropylene cotton was adjusted to 10 ⁸ cfu / mL. Liquid.

On the other hand, various agents for contact lenses of Examples 6 and 7 of the present invention and Comparative Example 4 were prepared with the component compositions shown in Table 3 below. Next, 10 mL of each of the prepared various contact lens agents was placed in a separate sterilized test tube, and 0.05 m of the test bacterial solution was placed there.
L was added. Then, mix these various test bacterial liquids with 2
Stored in a thermostat at 3 ° C., and after 2, 4, and 24 hours from the preparation of the formulation, a fixed amount of each formulation was taken out, and for each formulation, sterile saline was used. After dilution, the viable cell count was determined by the pour plate method. For the culture in this pour plate method, a method of culturing using a glucose peptone medium at 23 ° C. for 5 days was employed.

According to the above method, the number of viable bacteria immediately after inoculation,
From the viable cell counts at 2, 4, and 24 hours after the preparation of the mixture, the rate of bacterial reduction at each time point was determined. The results are also shown in Table 3.

[0040]

From the above results, it can be seen that the agent for contact lenses according to the present invention exerts a high bactericidal effect on mold.

Example 4 {Test for bactericidal effect: comparison with current products against molds and yeasts} Aspergillus niger (An) and Candida albicans (Ca) were used as test bacteria. Similarly, with respect to Ca, a test bacterial solution of 10 ⁸ cfu / mL was prepared in the same manner as in Example 1.

Next, the contact lens agent of Example 6 of the present invention used in Example 3 and the chemical disinfectants for soft contact lenses currently on the market as shown in Table 4 below as Comparative Examples 5 to 11 And prepared.

Using each of the contact lens preparations and the test bacterial solution prepared above, a compounded solution thereof was prepared in the same manner as in Example 3 for An and in the same manner as in Example 1 for Ca. And store it in a 23 ° C.
Four hours after the preparation of the liquid mixture, a fixed amount of each test liquid was taken out, the number of viable bacteria was examined, and the respective reduction rates were obtained. The results are shown in Table 4.

[0045]

From the above results, it can be seen that the contact lens agent according to the present invention has a significantly higher bactericidal activity against both mold and yeast compared to products of other companies.

Example 5 {Test for Growth Inhibitory Effect: Effect of Combination with Other Fungicide} In order to examine the growth inhibitory effect on bacteria when an alkylamine compound is combined with another fungicide, the Japanese Society of Chemotherapy was used. According to the MIC measurement method of
The presence or absence of bacterial growth was observed. That is, Pseudomonas aeruginosa (Pa: Pseu
domonas aeruginosa ATCC 9027) and using Staphylococcus aureus (St.a.), respectively, were suspended in physiological saline followed by culturing 35 ° C. × 24 hours Soybean Casein medium, of 10 ⁷ cfu / mL It was prepared to be a test bacterial solution.

Subsequently, the alkylamine salt tetradecylamine acetate was added to the glycine fungicide alkylaminoethyl glycine hydrochloride or 4 so as to obtain the component compositions shown in Tables 5 to 7 below. A test solution combining hexadecyltrimethylammonium salt, which is a quaternary ammonium salt bactericide, was prepared in a Mueller-Hinton medium, and 0.01 mL of the test bacterial solution was added to 1 mL of the test solution, and the solution was added at 35 ° C. After culturing for 24 hours, the presence or absence of bacterial growth was observed. The results are shown in Table 6 for the effect on Pa, and in Tables 5 and 7 for the effect on St.a. The evaluation criteria are as follows. +++: Turbidity due to bacterial growth was remarkably observed. ++: Turbidity due to bacterial growth was observed. +: Slight turbidity due to bacterial growth was observed. -: No bacterial growth was observed.

The tetradecylamine acetate may be Nissan Cation MA (manufactured by NOF Corporation).
"TEGO-51" (manufactured by Nippon Shoji) as alkylaminoethylglycine hydrochloride, and "PB-300" (manufactured by NOF Corporation) as hexadecyltrimethylammonium salt.

[0050]

[0051]

[0052]

As is clear from the above results, it can be confirmed that when the alkylamine compound is combined with another fungicide, the antibacterial effect is further enhanced as compared with the case where each is used alone.

Example 6 {Test of bactericidal effect: effect of addition of washing aid} Staphylococcus aureus (St.a.) and Candida.
Using Albicans (Ca), as in Example 1,
While preparing a 10 ⁸ cfu / mL test bacterial solution, various contact lens agents of Examples 8 to 10 of the present invention were prepared according to Table 8 below.
And the pH of the composition
Was adjusted. Next, using the thus prepared various contact lens agents and the test bacterial solution, a mixture thereof was prepared in the same manner as in Example 1. From the preparation of the mixture, 1 staphylococcus aureus was obtained. After 2, 4, and 24 hours, and 4 and 24 for Candida albicans
After a certain time, a fixed amount of each mixed solution was taken out, the number of viable bacteria was checked for each mixed solution, the reduction rate at each time point was obtained, and the results are shown in Table 8.

Here, "F-127" (polyoxyethylene-polyoxypropylene copolymer; manufactured by BASF) is used as a nonionic surfactant, and "PVPK-90" (polyvinylpyrrolidone) is used as a thickener. ; Wako Pure Chemical Industries, Ltd.) and disodium ethylenediaminetetraacetate as a chelating agent in the proportions shown in Table 8 below.

[0056]

From the above results, it can be seen that the contact lens agent of the present invention does not inhibit the bactericidal effect even if a nonionic surfactant, a thickener and a chelating agent are present as a cleaning aid. Can be confirmed.

Example 7 {Cytotoxicity Test: Influence on Soft Contact Lenses} Using the contact lens agent of the present invention, a cytotoxicity test was performed as follows to evaluate safety.

First, Examples 1 and 2 of the present invention used in Example 1
And the various contact lens agents of Examples 11 and 12 and Comparative Examples 12 and 13 prepared in the component compositions shown in Table 9 below were prepared as test solutions. Note that the buffer used here conforms to the composition in Example 1. Then, in 2.0 mL of each test solution, a water-containing soft contact lens, Menicon Soft MA (manufactured by Menicon Co., Ltd.), a water-containing soft contact lens Menicon Soft 72 (manufactured by Menicon Co., Ltd.), and a hard contact lens were used. Certain Menicon Super EX (manufactured by Menicon) were immersed one by one for 24 hours to prepare them as test lenses.

On the other hand, L-929 cells cultured in a CO ₂ incubator at 37 ° C. for 3 days were peeled off from the flask using a trypsin / EDTA solution, and then washed with a MEM Eagle medium at about 2 × 10 ⁵ cells / mL. A cell suspension was used. This cell suspension is 60 mm x 15 m
4.5 mL each in a Petri dish of m
The cells were cultured in an O ₂ incubator for 48 hours. afterwards,
The old medium was discarded, and 4.5 mL of the agar medium for overlay was poured into the medium. After confirming that the medium had solidified, a neutral red solution was further added, and the mixture was cultured for 1 hour in a CO ₂ incubator at 37 ° C. The red solution was discarded. Then, the test lens was placed thereon, and the cells were cultured as they were in a CO ₂ incubator at 37 ° C. for 48 hours. Then, the size of the bleaching zone due to dead cells was visually observed to evaluate the toxicity. Done. The observation results are shown in Table 9 below.

[0061]

From the above results, in the contact lens agents according to Examples 1, 2, 11 and 12 of the present invention, no fading due to dead cells was observed in any of the contact lenses. About the agent for contact lenses according to the invention examples, no toxicity to cells was observed,
It turns out that it is highly safe for the eyes. On the other hand, conventionally used bactericides, such as chlorhexidine gluconate used in Comparative Example 12, have toxicity to cells and are not necessarily safe for eyes. You can see that there is.

Example 8 << Lipid Removal Effect Test >> With respect to the contact lens agents of Examples 8 and 9 of the present invention in Example 6, a cleaning effect confirmation test was carried out as follows.

First, sorbitan monooleate: 6 w / v for use in such a washing effect confirmation test
%, Castor oil: 16 w / v%, lanolin: 35 w / v
%, Oleic acid: 5 w / v%, sorbitan trioleate: 4 w / v%, cetyl alcohol: 2 w / v
%, Cholesterol: 2 w / v%, and cholesterol acetate: 30 w / v% are dissolved, and 2.5 parts of an artificial lipid solution homogenized by stirring and 97.5 parts of physiological saline are mixed, and artificially mixed. A lipid solution was prepared.

A hard contact lens (Menicon Super EX; manufactured by Menicon Co., Ltd.) was prepared as a test lens, and the artificial lipid solution was uniformly adhered to both surfaces of the lens in an amount of 5 μL each on the surface of the lens. Obtained. Then, the obtained artificial lipid-stained lens is picked up on the palm, and 3 drops (6 drops per one piece) of the test solution are dropped on one side of the contact lens, and the contact lens is cleaned by rubbing with a fingertip for 5 seconds. Processing was performed.

After the washing treatment, the appearance of the contact lens was observed, and it was found that the artificial lipid stain attached to the contact lens was completely removed from each lens. As is clear from these results, the agent for contact lenses according to the present invention has an excellent cleaning effect in addition to its excellent bactericidal effect.

Example 9 << Protein washing effect test >> Each of the following components was dissolved in purified water to make the total volume 1 L.
Further, the obtained aqueous solution was adjusted to pH 7.0 using 1N sodium hydroxide to obtain an artificial tear. Beef albumin 3.88 g γ-globulin 1.61 g egg white lysozyme 1.20 g sodium chloride 9.0 g calcium chloride dihydrate 0.15 g sodium dihydrogen phosphate dihydrate 1.04 g

Next, as a contact lens for testing,
A hard contact lens (Menicon Super EX; manufactured by Menicon Co., Ltd.) was prepared and subjected to a heat treatment at 80 ° C. for 30 minutes while immersing it in the artificial tear.
Rinse with tap water. After repeating this operation five times, it was confirmed that the lens surface was completely clouded, and these artificial clouded lenses were used as test lenses.

On the other hand, various contact lens agents of Examples 13 to 15 of the present invention and Comparative Examples 14 to 20 each containing bioprolase (manufactured by Nagase Seikagaku Corporation) as a proteolytic enzyme were prepared according to the following Tables 11 to 13. And the protein lens was washed by immersing the test lens in 1 mL of each test solution at room temperature for 4 hours. Thereafter, the detergency was evaluated by observing the degree of removal of protein stain by magnifying 20 times using a dark-field stereo microscope (Olympus Optical Co., Ltd.). The results are shown in Tables 11 to 13 below. The evaluation criteria are as follows. ：: Protein stain on the lens surface was completely removed △: Slight protein stain on the lens surface remains ▲: Protein stain on the lens surface remains

[0070]

[0071]

[0072]

From the above results, those containing polyhexamethylene biguanide or chlorhexidine as fungicides inhibit the washing effect by proteolytic enzymes in a concentration-dependent manner. Those containing no inhibition of the washing effect by the protease.

Example 10 {Effect on Water Wettability to Hard Contact Lens} As the test solution, the contact lens agent according to Example 8 of the present invention used in Example 6 and physiological saline were prepared as test solutions. Then, in 2 mL of each test solution, as a test lens,
A hard contact lens having good water wettability (Menicon Super EX; manufactured by Menicon Co., Ltd.) was immersed and left at 35 ° C. for 1 day. Then take out the contact lens,
Their water wettability was observed.

As a result, it was shown that the contact lens immersed in the contact lens agent according to Example 8 of the present invention was uniformly wet on the entire surface and maintained in a good condition. Also, contact lenses immersed in physiological saline
Water was slightly repelled at the peripheral portion, and a slight deterioration in water wettability was observed. Therefore, it can be seen that the contact lens agent according to the present invention has no effect on the water wettability of the contact lens.

[0076]

As is apparent from the above description, according to the agent for contact lenses according to the present invention, since an alkylamine compound or a salt thereof is used as a bactericidal component, it can be used for contact lenses using other bactericides. It can be said that it has an excellent bactericidal effect as compared with the preparation. In addition, in terms of eye safety, it is advantageously superior to those conventionally used, and in addition to physical properties such as water wettability of contact lenses,
It has no effect. Further, such an alkylamine compound or a salt thereof can be combined with another bactericide, and depending on the combination with such another bactericide, the bactericidal effect of each bactericide is synergistically enhanced. It is possible to exhibit a more effective bactericidal effect.

In particular, since the contact lens agent according to the present invention does not inhibit the protein removing effect of the protease, it contains a predetermined protease to disinfect the protein together with the disinfecting treatment. Simultaneously performing the washing process can be advantageously performed,
Furthermore, by including other additional components, each of the agent for contact lens according to the present invention can be advantageously used for cleaning, disinfecting, rinsing, and preserving both soft contact lenses and hard contact lenses. Can be
It is possible to minimize the burden on the wearer in maintaining the contact lenses.

Claims (4)

[Claims] [Claim 1] [Where R ₁ is an alkyl group having 4 to 18 carbon atoms, tallow alkyl, coconut oil alkyl, or R ₄ NHR ₅ −
(Where R ₄ is an alkyl group having 4 to 18 carbon atoms, tallow alkyl or coconut oil alkyl, and R ₅ is an alkylene group having 1 to 3 carbon atoms), and R ₂ and R _2
3 is H or an alkyl group having 1 to 3 carbon atoms], or a salt thereof as a bactericidal active ingredient. 2. The agent for contact lenses according to claim 1, wherein the alkylamine compound or a salt thereof is contained in a range of 0.01 to 1000 ppm. 3. The contact lens agent according to claim 1, further comprising a borate buffer. 4. The contact lens agent according to claim 1, wherein the agent is in a liquid form, the pH being adjusted to a range of 5 to 9.