JP2019011264A - Oily eye drop - Google Patents

Abstract

To provide an oily eye drop having reduced viscosity while containing castor oil.SOLUTION: An oily eye drop contains castor oil, l-menthol, and water 0-8 mass%.SELECTED DRAWING: None

Description

  The present invention relates to an oily eye drop.

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

  However, eye drops containing a large amount of castor oil have the problem that due to the viscosity of castor oil, the amount of one drop is too large when dropped from a container, overflowing the eyes during use and reducing the feeling of use. .

JP 2000-273061 A

  This problem has been found for the first time by the present inventor, and an object of the present invention is to provide an oily eye drop having a reduced viscosity while containing castor oil.

  As a result of intensive studies by the present inventors in view of the above problems, it has been found that the viscosity of oily eye drops 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 this finding, and is as follows.

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

    Item 2. Item 4. The oily eye drop according to Item 1, wherein the castor oil content is 10% by mass or more.

    Item 3. Item 3. The oily 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 oily eye drop containing castor oil can be reduced by combining castor oil and l-menthol. Thereby, the amount of one drop of oily eye drops can be reduced.

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

  The present invention relates to an oily 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 bean (Ricinus communis) and is a conventionally known oil. Castor oil is not limited as long as it is pharmaceutically or cosmetically acceptable.

  The content of castor oil is not limited, but 10% by mass or more is exemplified in the oily eye drop, preferably 20 to 99.99% by mass, more preferably 30 to 99.99% by mass, and further preferably 40 to 99%. Examples are 9.99% by mass, even more preferably 50 to 99.99% by mass, particularly preferably 60 to 99.99% by mass, and particularly preferably 70 to 99.99% by mass. In the oily eye drop of the present invention, the castor oil content is not limited as long as it is, but more preferably 80 to 99.99% by mass, still more preferably 90 to 99.99% by mass, and still more preferably 95 to 99. And 9.99% by mass, particularly preferably 98 to 99.99% by mass, and particularly preferably 99 to 99.99% by mass.

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

  The content of 1-menthol is not limited, but is preferably 0.005 to 1% by mass, more preferably 0.01 to 0.5% by mass, and still more preferably 0.02 to 0.5% by mass in the oily eye drop. %, Still more preferably 0.05 to 0.5% by weight, particularly preferably 0.08 to 0.5% by weight, particularly preferably 0.1 to 0.5% by weight, still more preferably 0.2%. -0.5 mass% is illustrated.

  The oily eye drop of the present invention may or may not contain water, but when it contains water, its content is 8% by mass or less. From this, the content of water in the oily eye drop 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, Still more preferably, 0 to 1% by mass, particularly preferably 0 to 0.5% by mass, particularly more preferably 0 to 0.3% by mass, and still more preferably 0% by mass.

  The oily eye drop of the present invention may optionally contain an oil component other than castor oil (hereinafter, “oil component” means “oil component other than castor oil”). The oil component is not limited as long as it is pharmaceutically or cosmetically acceptable, but fennel oil, mint oil, bergamot oil, eucalyptus oil, sesame oil, soybean oil, rapeseed oil, corn oil, camellia oil, peanut oil, almond Examples thereof include animal and vegetable oils and fats such as oil, wheat germ oil, sunflower oil, cottonseed oil, olive oil, rose oil and safflower oil, liquid paraffin, petrolatum, macrogol 4000, and macrogol 6000. Preferable examples of the oil component include fennel oil, peppermint oil, bergamot oil, eucalyptus oil, liquid paraffin, petroleum jelly, 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 not limited, but when the oily eye drop of the present invention contains an oily component, the oily eye drop contains 0.0001 to 50% by mass, preferably 0.0001 to 40% by mass, more preferably 0.0001-30% by mass, more preferably 0.0001-20% by mass, still more preferably 0.0001-10% by mass, particularly preferably 0.0001-8% by mass, particularly more preferably 0.0001- Examples are 5% by mass, more particularly 0.0001 to 3% by mass.

  The oily eye drop of the present invention may further contain other optional components that are pharmaceutically or cosmetically acceptable in addition to the above components. Optional ingredients include surfactants, pH adjusters, buffers, solubilizers, preservatives, thickeners, stabilizers, thickeners, antioxidants, dispersants, isotonic agents, chelates Agents, refreshing agents (other than l-menthol), coloring agents, fragrances, various useful ingredients (antiallergic agents, antihistamines, focus control function improving agents, anti-inflammatory agents, astringents, antibacterial agents, corneal protective agents, decongestants, Amino acids, vitamins, etc.). These may be used individually by 1 type, may be used in combination of 2 or more type, and the content should just set suitably according to the objective etc.

  The oily eye drop of the present invention can be produced by mixing castor oil, 1-menthol, and water, an oily component, and optional components as necessary.

  The form of the oily eye drop of the present invention is not limited, and examples thereof include liquid, emulsion and gel at room temperature (24 ° C.), preferably liquid and emulsion, and more preferably liquid.

  Further, the oily eye drop of the present invention is clear, and any color or colorless may be used as long as it is limited.

  The viscosity of the oily 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 still more preferably 300 to 650 cp. . The viscosity was measured using a spindle F in a Brookfield viscometer (LVDV-II +) (manufactured by Brookfield Engineering Labs) and a screw tube No. 7 (35 × 78, manufactured by Maruel Co., Ltd.) is filled with 50 g of an oily eye drop, and the viscosity is 5 minutes after the start of measurement at a rotational speed of 4 rpm and 24 ° C.

  The pH of the oily eye drop of the present invention is not limited as long as it can be used as an eye drop, and examples thereof include pH 5.5 to 8, preferably pH 6 to 7.5 at 24 ° C. 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 fatigue eyes, blurred eyes, itchy eyes, redness, dry eyes, ophthalmitis due to ultraviolet rays (snow eyes, etc.), eye discomfort, conjunctivitis, stylus, sleek eyes, foreign body feeling It can be used for the purpose of prevention and improvement, and for the purpose of corneal protection, corneal repair, antiallergy, antibacterial, UV care, eye disease prevention, dry eye countermeasure, eyelid friction lubrication, tear oil layer supplementation, and the like.

  The oily eye drop of the present invention can be filled in a container used in a conventional eye drop, and is usually used by directly dropping it into the eye from such an eye drop container. The material of the container is not limited, and is made of polypropylene (PP), polyethylene terephthalate (PET), polyacrylate, polyethylene (PE), low density polyethylene (LDPE), polycarbonate, plastic, glass, etc. A conventionally well-known thing is illustrated and it is preferably made of plastic.

  Moreover, the container should just have transparency of the grade which does not interfere with the observation of a foreign material, and may be colored or colorless.

  Moreover, although the capacity | capacitance of a container is not restrict | limited, Preferably 3-20 mL is illustrated, More preferably, 5-15 mL is illustrated.

  In the present invention, the container may be any container as long as it conforms to the description of the ophthalmic preparation in the General Rules for Preparations in the 16th revised Japanese Pharmacopoeia Manual.

  The frequency of use and the amount of dripping of the oily 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, and usually Examples are 1 to several drops per time, preferably 1 to 3 drops per time, and more preferably 1 to 2 drops per time. In addition, the oily eye drop of the present invention is not limited as long as it is dropped into the eyes, but it is preferable that eyes are closed preferably for 10 to 60 seconds, more preferably for 40 to 60 seconds after dropping. As mentioned.

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

  Therefore, according to the present invention, it is possible to reduce the amount of one drop of the oily eye drop, and it is possible to suppress the problem that excessive eye drop overflows from the eye during use and the feeling of use decreases. In addition, from this, according to the present invention, it is possible to suppress the adhesion of the oily eye drops to the wall surface in the container, and in particular, the oily eye drops are used in the container at a later stage of use when the remaining amount in the container is reduced. It is possible to reduce a user's stress that the oily eye drops are difficult to be dropped or cannot be dropped on the wall surface.

  Further, the present inventor has found that it is difficult to understand that oil drops have entered the eye when castor oil alone is applied, and there is a problem that the eye drops are excessively applied and overflow from the eyes. According to the present invention, when l-menthol is used in combination, it is easy to understand that the castor oil has been instilled due to its refreshing feeling, and the feeling of use can be improved.

  Therefore, it can be said that the present invention also provides a method for reducing the viscosity of the oily eye drop, characterized by combining l-menthol in an oily eye drop containing castor oil. The castor oil, oily eye drops, 1-menthol and the like used in the method, the components usable in the oily eye drops, the content of each component, and the like are described in the same manner as described above.

  EXAMPLES Hereinafter, although an Example is shown and this invention is demonstrated in detail, this invention is not limited to these.

Test example 1
According to the following Table 1, castor oil and l-menthol were mixed to prepare an oily eye drop (Example 1). About the obtained oil-based eye drop, the viscosity was measured according to the following procedures.

  Using a spindle F in a Brookfield viscometer (LVDV-II +) (manufactured by Brookfield Engineering Labs), a screw tube No. 7 (35 × 78, manufactured by Maruel) was filled with 50 g of the obtained oily eye drop, and the viscosity after 5 minutes from the start of measurement was measured. 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, compared with castor oil alone (Comparative Example 1), the oily eye drop mixed with castor oil and l-menthol (Example 1) can significantly reduce the viscosity. did it. From this, it was found that the viscosity of the obtained oily eye drop can be reduced by using l-menthol together.

Test example 2
According to the following Table 2, each component was mixed and the oil-based eye drop containing castor oil and 1-menthol was prepared (Examples 1-5). Moreover, each component was mixed according to Table 2, and it replaced with castor oil and the oil-based eyedrops containing d-borneol or dl-camphor instead of 1-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 oily eye drop was filled into a TSE-5 mL (polypropylene) eye drop container, the oil eye drop was dropped from the container, and the weight of one drop with an electronic balance. Was measured and the average value of three times was obtained.

  The results are shown in Table 2 and FIG.

  As apparent from Table 2 and FIG. 1, in Example 1, the weight of one drop was 0.022 mg. Moreover, also in Examples 2-5, the weight of 1 drop was 0.018-0.023 mg, and became the same weight as Example 1.

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

  Thus, from the results of Test Example 1 and the present Test Example, compared with Comparative Example 1 containing only castor oil, Examples 1 to 5 containing 1-menthol had a lower viscosity and one drop was dropped. It turned out that the amount can be reduced.

  Furthermore, surprisingly, in Comparative Example 2 or 3 containing d-borneol or dl-camphor instead of l-menthol, the weight of one drop was 0.029 mg and 0.031 mg, respectively. It was the same as 1 or a value exceeding Comparative Example 1. l-Menthol, d-borneol, and dl-camphor are all classified as monoterpenes, and these are common components in that they are used as cooling agents, but castor oil is combined with d-borneol and dl-camphor. However, no decrease in the dripping amount was observed.

  From this, it was found that by combining castor oil and l-menthol, the viscosity of the oily eye drop can be reduced and the amount of one drop dropped 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 dropped compared to castor oil alone, but one drop when castor oil and dl-camphor were combined with l-menthol. The amount of dripping was reduced. From this, it was found that by combining l-menthol in eye drops, the viscosity of oily eye drops containing castor oil can be relatively lowered and the amount of one drop can be reduced.

Test example 3
The oily eye drops prepared in Test Example 1 (Example 1 and Comparative Example 1) were evaluated for feeling during use. The evaluation is “O” when 10 people who use eye drops on a daily basis notice that oil-based eye drops were dropped on the eyes, and when they did not notice that they were dropped on the eyes. The method was asked to determine that “x”.

  As is apparent from Table 3, in Example 1 containing castor oil and l-menthol, 10 out of 10 people judged “◯” and all the subjects noticed that the oily eye drops were dropped. On the other hand, in Comparative Example 1 with only castor oil, not many of the subjects noticed that 8 of 10 subjects were determined to be “x”, and thus Comparative Example 1 was dropped. It was hard to notice.

  For this reason, the problem of not being instilled when dropping castor oil alone, or being overfilled and overflowing from the eyes, can be solved by using castor oil and l-menthol in combination. It was found that the feeling of use can be improved.

Formulation Example Oily eye drops were prepared according to the formulation shown in Table 4. Formulation Examples 1 to 13 were prepared by mixing the component (A) and the component (B). Formulation Examples 14-16 add the liquid mixture obtained by mixing (A) component to this little by little, heating the liquid mixture obtained by mixing (B) component to 80 degreeC, and stirring. It was prepared by. These are low-viscosity oil-based eye drops that have a low viscosity and are appropriately controlled in the same manner as in the above test examples.

Claims (3)

An oily eye drop containing castor oil, l-menthol, and 0 to 8% by mass of water. The oily eye drop according to claim 1, wherein the content of castor oil is 10% by mass or more. The oily eye drop according to claim 1 or 2, wherein the content of l-menthol is 0.005 to 1% by mass.