JP7009093B2 - Oil-based eye drops - Google Patents

Description

The present invention relates to oil-based eye drops.

Castor oil is known as one of the components that can be blended in eye drops (Patent Document 1).

However, in the case of eye drops containing a large amount of castor oil, there is a problem that the viscosity of the castor oil causes the amount of one drop to be too large when dropped from the container, and the eye drops overflow from the eyes during use to reduce the usability. ..

Japanese Unexamined Patent Publication No. 2000-273061

This problem was first discovered by the present inventor, and an object of the present invention is to provide an oil-based eye drops containing castor oil but having a reduced viscosity.

As a result of diligent studies in view of the above problems, the present inventor has found that the viscosity of an oil-based eye drop containing castor oil can be reduced by combining castor oil and l-menthol. The present invention has been completed as a result of further studies based on the findings, and is as follows.

Item 1. An oil-based eye drop containing castor oil, l-menthol, and 0 to 8% by mass of water.

Item 2. Item 2. The oil-based eye drop according to Item 1, wherein the content of castor oil is 10% by mass or more.

Item 3. Item 2. The oil-based eye drop according to Item 1 or 2, wherein the content of l-menthol is 0.005 to 1% by mass.

According to the present invention, the viscosity of an oil-based eye drop containing castor oil can be reduced by combining castor oil and l-menthol. This makes it possible to reduce the amount of one drop of oil-based eye drops.

FIG. 1 shows the weight of one drop of an oil-based eye drop containing only castor oil, and the weight of one drop of an oil-based eye drop containing castor oil and l-menthol, dl-camphor or d-borneol. Is shown.

The present invention relates to an oil-based eye drop containing castor oil, l-menthol, and 0 to 8% by mass of water.

Castor oil is a fatty oil obtained from the seeds of castor oil (Ricinus communis) and is a conventionally known oil. Castor oil is not limited as far as pharmaceutically or cosmetically acceptable.

The content of castor oil is not limited, but 10% by mass or more is exemplified in the oil-based eye drops, preferably 20 to 99.99% by mass, more preferably 30 to 99.99% by mass, and further preferably 40 to 99. An example is .99% by mass, more preferably 50 to 99.99% by mass, particularly preferably 60 to 99.99% by mass, and particularly more preferably 70 to 99.99% by mass. In the oil-based eye drops of the present invention, the content of castor oil is not limited to this extent, but is more preferably 80 to 99.99% by mass, still more preferably 90 to 99.99% by mass, and even more preferably 95 to 99. An example is .99% by mass, particularly preferably 98 to 99.99% by mass, and particularly more preferably 99 to 99.99% by mass.

l-Menthol is conventionally known and is not limited as far as pharmaceutically or cosmetically acceptable.

The content of l-menthol is not limited, but is preferably 0.005 to 1% by mass, more preferably 0.01 to 0.5% by mass, still more preferably 0.02 to 0.5% by mass in the oil-based eye drops. %, More preferably 0.05 to 0.5% by mass, particularly preferably 0.08 to 0.5% by mass, particularly more preferably 0.1 to 0.5% by mass, still more preferably 0.2. Up to 0.5% by mass is exemplified.

The oil-based eye drops of the present invention may or may not contain water, but when water is contained, the content thereof is 8% by mass or less. From this, the content of water in the oil-based eye drops of the present invention is 0 to 8% by mass, preferably 0 to 5% by mass, more preferably 0 to 3% by mass, still more preferably 0 to 2% by mass. Further preferably, 0 to 1% by mass, particularly preferably 0 to 0.5% by mass, particularly more preferably 0 to 0.3% by mass, still particularly preferably 0% by mass is exemplified.

The oil-based eye drops of the present invention may optionally contain an oil-based component other than castor oil (hereinafter, "oil-based component" means "oil-based component other than castor oil" in the present specification). The oily ingredients are not limited as far as pharmaceutically or cosmetically acceptable, but uikyo oil, peppermint oil, bergamot oil, eucalyptus oil, sesame oil, soybean oil, rapeseed oil, corn oil, camellia oil, lacquer oil, almond. Examples thereof include animal and vegetable fats and oils such as oil, wheat germ oil, sunflower oil, cottonseed oil, olive oil, rose oil, and Benibana oil, liquid paraffin, vaseline, macrogol 4000, and macrogol 6000. Preferred oily components include fennel oil, peppermint oil, bergamot oil, eucalyptus oil, liquid paraffin, petrolatum, macrogol 4000, macrogol 6000 and the like. These may be used alone or in combination of two or more.

The content of the oily component is also not limited, but when the oily eye drops of the present invention contain the oily components, 0.0001 to 50% by mass, preferably 0.0001 to 40% by mass, more preferably 0.0001 to 40% by mass in the oily eye drops. 0.0001 to 30% by mass, still more preferably 0.0001 to 20% by mass, even more preferably 0.0001 to 10% by mass, particularly preferably 0.0001 to 8% by mass, and particularly more preferably 0.0001 to 0.0001. 5% by mass, more particularly 0.0001 to 3% by mass is exemplified.

In addition to the above-mentioned components, the oil-based eye drops of the present invention may further contain any other pharmaceutically or cosmetically acceptable component. Optional ingredients include surfactants, pH regulators, buffers, solubilizers, preservatives, thickeners, stabilizers, thickeners, antioxidants, dispersants, isotonic agents, chelates. Agents, refreshing agents (other than l-menthol), coloring agents, fragrances, various useful ingredients (anti-allergic agents, antihistamines, focus control function improving agents, anti-inflammatory agents, astringent agents, antibacterial agents, corneal protective agents, decongestants, Amino acids, vitamins, etc.) are exemplified. These may be used alone or in combination of two or more, and the content thereof may be appropriately set according to the purpose and the like.

The oily eye drops of the present invention can be produced by mixing castor oil, l-menthol, water if necessary, an oily component, and any component.

The form of the oil-based eye drop of the present invention is not limited, and liquid, milky liquid, gel-like, etc. are exemplified at room temperature (24 ° C.), preferably liquid, milky liquid, and more preferably liquid.

Further, the oil-based eye drop of the present invention is clear and may be colored or colorless as long as it is used.

The viscosity of the oil-based eye drop of the present invention is not limited as long as it can be used as an eye drop, but is preferably 50 to 800 cp at 24 ° C., more preferably 200 to 700 cp, and further preferably 300 to 650 cp. .. For the viscosity, a spindle F was used in a Brookfield viscometer (LVDV-II +) (manufactured by Brookfield Engineering Labs), and the screw tube No. 7 (35 × 78, manufactured by Maruel Co., Ltd.) is filled with 50 g of oil-based eye drops, and the viscosity is 5 minutes after the start of measurement at a rotation speed of 4 rpm and 24 ° C.

The pH of the oil-based eye drop of the present invention is also not limited as long as it can be used as an eye drop, but pH 5.5 to 8, preferably pH 6 to 7.5 at 24 ° C. is exemplified. The pH is measured with a desktop pH meter F-52 (manufactured by HORIBA, Ltd.).

The oily eye drops of the present invention are used for tired eyes, blurred eyes, itchy eyes, congestion, dry eyes, eye inflammation (snow eyes, etc.) due to ultraviolet rays, eye discomfort, conjunctivitis, lumps, swelling eyes, foreign body feeling, etc. It can be used for the purpose of prevention and improvement, and also for the purpose of corneal protection, corneal repair, antiallergic, antibacterial, ultraviolet care, eye disease prevention, dry eye countermeasures, eyelid friction lubrication, tear oil layer replenishment, and the like.

The oil-based eye drop of the present invention can be filled in a container used for conventional eye drops, and is usually used by dropping directly into the eye from such a container for eye drops. The material of the container is not limited, and it is made of polypropylene (PP), polyethylene terephthalate (PET), polyacrylate, polyethylene (PE), low density polyethylene (LDPE), plastic such as polycarbonate, glass, etc. Conventionally known ones are exemplified, preferably made of plastic.

Further, the container may be colored or colorless as long as it has transparency to such an extent that there is no problem in observing foreign substances.

Further, the capacity of the container is not limited, but preferably 3 to 20 mL is exemplified, and more preferably 5 to 15 mL is exemplified.

In the present invention, the container is preferably one that follows the description of the eye drops in the general formulation rules of the 16th revised Japanese Pharmacopoeia.

The number of times and the amount of the oil-based eye drop of the present invention are not limited, and usually 1 to several times a day, preferably 3 to 6 times a day, more preferably 3 to 4 times a day are exemplified, and usually. An example is 1 to several drops at a time, preferably 1 to 3 drops at a time, and more preferably 1 to 2 drops at a time. Further, the oil-based eye drop of the present invention is not limited as long as it is used by dropping it into the eyes, but it is preferable to keep the eyes closed for 10 to 60 seconds, more preferably 40 to 60 seconds after the dropping. Is mentioned as.

According to the present invention, by using castor oil and l-menthol in combination, even when castor oil is contained, particularly even when castor oil is contained in a high content. , The viscosity of oil-based eye drops can be reduced.

From this, according to the present invention, it is possible to reduce the amount of one drop of the oil-based eye drop, and it is possible to suppress the problem that excess eye drop overflows from the eye during use and the feeling of use is deteriorated. Further, according to the present invention, according to the present invention, it is possible to suppress the adhesion of the oil-based eye drops to the wall surface inside the container, and in particular, the oil-based eye drops are contained in the container in the late stage of use when the remaining amount in the container is low. It is possible to reduce the stress of the user, such as the oil-based eye drops that adhere to the wall surface and are difficult or impossible to drip.

In addition, the present inventor has noticed that it is difficult to tell that oil droplets have entered the eyes even when castor oil alone is instilled, and there is a problem that the oil droplets are instilled too much and overflow from the eyes. According to the present invention, by using l-menthol in combination, it becomes easy to understand that castor oil is instilled due to the refreshing feeling, and the feeling of use can be improved.

From this, it can be said that the present invention also provides a method for reducing the viscosity of an oil-based eye drop containing castor oil, which is characterized by combining l-menthol. Castor oil, oil-based eye drops, l-menthol and the like used in the method, components that can be used in the oil-based eye drops, the content of each component and the like will be described in the same manner as described above.

Hereinafter, the present invention will be described in more detail with reference to examples, but the present invention is not limited thereto.

Test Example 1
According to Table 1 below, castor oil and l-menthol were mixed to prepare an oil-based eye drop (Example 1). The viscosity of the obtained oil-based eye drops was measured according to the following procedure.

Spindle F was used in the Brookfield Viscometer (LVDV-II +) (manufactured by Brookfield Engineering Labs), and the screw tube No. 7 (35 × 78, manufactured by Maruel Co., Ltd.) was filled with 50 g of the obtained oil-based eye drops, and the viscosity was measured 5 minutes after the start of measurement. The measurement was performed at a rotation speed of 4 rpm and room temperature (24 ° C.). As Comparative Example 1, the viscosity of castor oil was measured in the same manner (Comparative Example 1).

The results are shown in Table 1.

As is clear from Table 1, the viscosity of the oil-based eye drops in which castor oil and l-menthol are mixed (Example 1) can be significantly reduced as compared with castor oil alone (Comparative Example 1). did it. From this, it was found that the viscosity of the obtained oil-based eye drops can be reduced by using l-menthol in combination.

Test Example 2
According to Table 2 below, each component was mixed to prepare an oil-based eye drop containing castor oil and l-menthol (Examples 1 to 5). In addition, each component was mixed according to Table 2 to prepare castor oil and an oil-based eye drop containing d-borneol or dl-camphor instead of l-menthol (Comparative Examples 2 and 3). In Table 2, Example 1 and Comparative Example 1 are the same as those prepared in Test Example 1.

3 mL of the obtained oil-based eye drops is filled in a container for eye drops of TSE-5 mL (made of polypropylene) (manufactured by Taisei Kako Co., Ltd.), the oil-based eye drops are dropped from the container, and the weight of one drop is on an electronic balance. Was measured, and the average value of 3 times was obtained.

The results are shown in Table 2 and FIG.

As is clear from Table 2 and FIG. 1, the weight of one drop in Example 1 was 0.022 mg. Further, in Examples 2 to 5, the weight of one drop was 0.018 to 0.023 mg, which was about the same as that in Example 1.

On the other hand, in Comparative Example 1, the weight of one drop was 0.029 mg, which was heavier than in Examples 1 to 5, and it was found that the amount of one drop was large.

As described above, from the results of Test Example 1 and this Test Example, the viscosity is lower in Examples 1 to 5 containing l-menthol as compared with Comparative Example 1 containing only castor oil, and one drop is dropped. It turned out that the amount could be reduced.

Furthermore, surprisingly, in Comparative Example 2 or 3 containing d-bornol or dl-camphor instead of l-menthol, one drop weighs 0.029 mg and 0.031 mg, respectively, which is a comparative example. It was the same as 1 or higher than Comparative Example 1. l-menthol, d-borneol, and dl-camphor are all classified as monoterpenes, and these are common ingredients in that they are also used as a cooling agent, but castor oil is combined with d-borneol and dl-camphor. However, no decrease in the amount of dripping was observed.

From this, it was found that by combining castor oil and l-menthol, the viscosity of the oil-based eye drops can be lowered and the amount of one drop can be reduced.

In addition, when castor oil and dl-camphor were used in combination as in Comparative Example 3, the amount of one drop was increased as compared with castor oil alone, but when castor oil and dl-camphor were combined with l-menthol, one drop was added. The amount of dripping has decreased. From this, it was found that by combining l-menthol in the eye drops, the viscosity of the oil-based eye drops containing castor oil can be relatively lowered, and the amount of one drop can be reduced.

Test Example 3
The oil-based eye drops prepared in Test Example 1 (Example 1 and Comparative Example 1) were evaluated for their usability at the time of instillation. The evaluation was "○" for 10 people who use eye drops on a daily basis, when they noticed that the oil-based eye drops were dropped on their eyes, and when they did not notice that they were dropped on their eyes. Was judged as "x".

As is clear from Table 3, in Example 1 containing castor oil and l-menthol, 10 out of 10 subjects were judged to be "○", and all the subjects noticed that the oil-based eye drops were dropped. On the other hand, in Comparative Example 1 containing only castor oil, many of the subjects did not notice that the oil was dropped, and 8 out of 10 subjects judged it as "x", and in this way, Comparative Example 1 was dropped. It was hard to notice.

From this, the problem of not being aware of the instillation that occurs when castor oil alone is dropped, and the problem of excessive instillation and overflowing from the eyes can be solved by using castor oil and l-menthol in combination. It was found that it was possible to improve the usability.

Prescription Example An oil-based eye drop was prepared according to the prescription shown in Table 4. Formulation Examples 1 to 13 were prepared by mixing the component (A) and the component (B). In Formulation Examples 14 to 16, the mixed solution obtained by mixing the component (B) is warmed to 80 ° C., and the mixed solution obtained by separately mixing the component (A) is added little by little to the mixture while stirring. Prepared by These are oil-based eye drops having a low viscosity and an appropriate amount of appropriately controlled oil-based eye drops with a good usability, as in the case of the above test example.

Claims (1)

An oil-based eye drop containing 98 to 99.99 % by mass of castor oil, 0.01 to 0.5 % by mass of l-menthol, and 0 to 2 % by mass of water.

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