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`= Patent Translate
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`
`Notice
`This translation is machine-generated. It cannot be guaranteed thatit is intelligible, accurate,
`complete, reliable or fit for specific purposes. Critical decisions, such as commercially relevant or
`financial decisions, should not be based on machine-translation output.
`
`DESCRIPTION JP2007308398
`
`An eye drop having the effect of suppressing increase in myopic power, improving the
`phenomenon of photophobia after instillation, shortening the period of mydriasis, and free of
`systemic side effects, and a method of manufacturing the same. | do. A manufacturing method
`characterized by comprising a step of diluting with an eye drop containing atropine and a liquid
`harmless to the human bodyto adjust the concentration of atropine to 0.1% orless, preferably
`0.05% orless. Preferably, in the method,the liquid is distilled water or saline. [Selection diagram]
`None
`
`Eye drops and manufacturing method thereof
`
`[0001]
`The present invention relates to eye drops, and more particularly to an eye drop containing
`atropine which has an action of suppressing an increase in special myopia and a method for
`producing the same.
`
`[0002]
`
`Myopia is one of the serious diseases of the eye.
`
`In particular, as the diopter value increases in the negative direction, juvenile cataract, glaucoma,
`etc. are morelikely to occur, and retinal detachment, macular bleeding, retinal degeneration,etc.
`may occur, and even severe blindness may occur is there. Prevention of myopia has become very
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`important in Taiwan, as myopia is the second leading causeof blindnessin the elderly.
`
`[0003]
`
`Prevention of myopia must begin as a child. Accordingto statistics, children’s myopia increases
`by an average of 75 to 100 degreesevery yearin Asia, and children’s myopia increases by an
`average of 50 degrees every year in Europe. When a child becomes myopic, myopia increases
`steadily and stops increasing at the end of puberty. When a child becomes myopic, the
`probability of becoming severe myopia after adulthoodis very high. Therefore, how to effectively
`suppressthe increase in the myopic power has become an importantissue.
`
`[0004]
`
`Treatment to improve the increase in myopic power in children and preventive measuresto
`prevent severe myopia are important issues. Conventional research papers indicate that atropine
`is effective for suppressing an increase in myopic power.
`
`[0005]
`According to a research paper (Non-Patent Document 1) by Dr. Yutaka Shiei of Taiwan
`University, etc., it is introduced that 0.5% of atropine is the mosteffective.
`
`[0006]
`
`Currently, many countries use eye drops with an atropine concentration of 1%.
`
`In Taiwan, eye drops with an atropine concentration of 0.5% are used. However, although eye
`drops containing these atropines have a certain degree of effect, they are difficult to use clinically
`continuously. The main reasonis that after instillation, photophobia appears. For this reason, for
`example, elementary school children cannotparticipate in physical education classes. In addition,
`the time of mydriasis occurring afterinstillation is long. Therefore, it becomes impossible to
`adaptto eye drops, and as a result, the rate of abandoning treatment increases. Therefore, there
`is a demand for the developmentof eye dropsthat can efficiently suppress side effects such as
`photophobia or prolonged mydriasis. In 1999, a research paper from Taiwan University (Shih YF,
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`
`Chen CH, Chou AC,etal Ef fects of different
`
`concentrations of atropineoncontrolling
`
`myopiainmyopicchildren. JOcul Pharmacol
`Ther1999;15:85-90.
`)
`
`[0007]
`The present invention provides an eye drop having the effect of suppressing increase in myopic
`power, improving the phenomenon of photophobia after instillation, shortening the time of
`mydriasis, and having no systemic side effects, and a method for producing the same. The taskis
`to provide.
`
`[0008]
`Therefore, the present inventor has conductedintensive studies in view of the drawbacks found
`in the prior art, and as a result, dilute atropine with a liquid harmless to the human body to
`control the content to 0.1% orless, preferably atropine. The present invention was completed
`based on such findings, focusing on the point that the problem can be solved by eye drops
`having a concentration of 0.05% and a method for producing the eye drops.
`
`[0009]
`
`Hereinafter, the present invention will be described specifically.
`
`The eye drop according to claim 1 is an eye drop containing atropine, and the concentration of
`the atropine is adjusted to 0.1% or less.
`
`[0010]
`The eye drop described in claim 2 has the atropine concentration in claim 1 of 0.05%.
`
`[0011]
`An eye drop manufacturing method according to claim 3 is a method for manufacturing an eye
`drop containing atropine, wherein the atropineis diluted to a concentration of 0.1% or less with a
`liquid harmless to the human body.
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`
`
`[0012]
`According to a fourth aspect of the present invention, the harmlessliquid for diluting atropine
`according to the third aspectis distilled water.
`
`[0013]
`In the method for producing a medicine according to claim 5, the harmlessliquid for diluting
`atropine according to claim 3 is a physiological saline.
`
`[0014]
`The present invention has the effect of suppressing an increase in myopic power, improves the
`phenomenonof photophobia afterinstillation, can reduce the time for mydriasis, and
`furthermore does not cause systemic side effects. , And is effective for continuing treatmentfor a
`long period of time.
`
`[0015]
`The presentinvention is to provide an eye drop whichefficiently suppresses increase in myopic
`power, without presenting photophobia, and which reducesthe time required for mydriasis, and
`a method for producing the same. In eye drops containing atropine, the concentration of atropine
`is reduced.
`
`[0016]
`
`The theory that the concentration of atropine in eye dropsis 0.5% is the most effective since the
`publication of the research by Dr. Yutaka Shiei mentioned above has been a generally accepted
`theory.
`
`For this reason, nobody thoughtthat atropine concentration of 0.1% or less would be effective.
`
`However, the inventor has discovered that adjusting the concentration of atropine to 0.1% orless
`can provide a favorable effect.
`
`Thatis, an eye drop containing atropine originally has an effect of efficiently suppressing an
`increase in myopia, but if the concentration of atropine is adjusted to 0.1% orless, a similarly
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`4
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`
`
`favorable effect of suppressing myopia can be obtained. In addition, phenomena such as
`photophobia and mydriasis that occur after instillation can be efficiently suppressed, and
`systemic side effects do not occur.
`
`Thatis, favorable adaptability to the eye dropsof the patient is obtained.
`
`Furthermore, experiments have shown that when the concentration of atropine is set to 0.05%,
`more favorable adaptability can be obtained as comparedwith the concentrations of 0.1% and
`0.25%.
`
`Specific examples will be described below in detail to describe the characteristics of the eye
`drops and the method for producing the eye drops, and are described below.
`
`[0017]
`
`The eye drops according to the present invention are prepared by diluting atropine with a liquid
`harmless to the human bodysuchasdistilled water or physiological saline to adjust the
`concentration to 0.1% or less.
`
`Preferably, the concentration of atropine is 0.05%.
`
`[0018]
`
`An eye drop according to the present invention has an object to suppress an increase in myopic
`power and to improve phenomenasuch as photophobia and mydriasis that occur after
`instillation. That is, the user's adaptability to eye drops is improved.In this regard, as disclosed in
`FIG. 1, according to clinical experiments, even if the concentration of atropine is 0.1%,it still
`exhibits photophobia andits adaptability to eye dropsis not preferable. However, when the
`concentration of atropine is 0.05%, the phenomenon of pupil enlargement and photophobia is
`significantly improved as compared with 0.1%. However, regarding the effect of suppressing the
`increase in the myopic power, the difference is not large even when comparing the case where
`the concentration of atropine is set to 0.1% and the case wherethe concentration of atropine is
`set to 0.25%.
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`
`[0019]
`
`The following Table 1 showsthe results of clinical experiments conducted by Dr. Yutaka Seinaga
`in 1999 on the relationship between the concentration of atropine andthe effect of suppressing
`increase in myopia. In this test, eye drops with atropine concentrations of 0.5%, 0.25%, and 0.1%,
`respectively, were continuously instilled into experimental groups divided into three, and
`separately atropine was added to the control group. An eye drop containing no wasinstilled and
`compared with myopia oneyearlater. As a result, as disclosed in Table 1, when the atropine
`concentration was 0.5%, the most preferable result was obtained.
`
`[0020]
`
`Therefore, the present inventors conducted similar clinical experiments with eye drops having an
`atropine concentration of 0.05, and compared the results with those in Table 1 described above.
`In the clinical experiment, 21 myopic patients aged 6 to 12 years weretreated with an eye drop
`having an atropine concentration of 0.05% twice a day and continued for one year. Similarly, 36
`myopic patients aged 6 to 12 wereinstilled twice a day with eye drops containing no atropine as
`a control group, and this was continued for one year. The average age of the experimental group
`was8.38 years, and the genderratio was 8 boys and 12 girls. The average age of the control
`group was8.11, and the proportion of men and women was 18 women and 18 boys. One year
`later, the results of measuring myopia are disclosed in Table 2.
`
`[0021]
`Comparing the experimental results in Table 1 described above with the experimental results in
`Table 2, it can be seen that even when the atropine concentration is 0.05%, a favorable effect of
`suppressing myopia can be obtained.
`
`[0022]
`In addition, the inventor of the present invention performed experiments on the experimental
`groupsin the experiments in Table 2 described above for three years, and measured the diopter
`increase rate every year.
`
`[0023]
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`
`
`As is clear from Table 3, when the eye drops having an atropine concentration of 0.05% are
`continuously used for a long period of time, a favorable effect of suppressing an increase in
`myopia can be obtained.
`
`[0024]
`
`Also, when looking at an object at a short distance, an adjusting force for adjusting the thickness
`of the crystalline lens is used.
`
`The long-lasting effect of the adjusting force is a factor of deteriorating the myopic power.
`
`For example, when working while looking at an object at a short distance,it is necessary to
`reduce the excessive action of the adjusting force.
`
`[0025]
`
`Then, in orderto clarify the relationship between the atropine concentration and the moderating
`action of the regulating power, the inventorinstilled eye drops twice a day with an atropine
`concentration of 0.05% in the first experimental group using 21 myopic patients. After one year,
`the adjustability was examined.
`
`Nine myopic patients wereinstilled with eye drops having an atropine concentration of 0.1%
`twice a day in a second experimental group, and after one year, the adjusting power was
`examined. Separately, an eye drop containing no atropine wasinstilled twice a day using 6
`myopic patients as a control group, and after one year, the adjusting power was examined. The
`average ageofthe first experimental group was 9.4 years, and the proportion of men and women
`was 12 boys and 10 girls. The average age of the second experimental group was 11 years, and
`the proportion of males and females was 5 boys and 4 girls. The average age of the control group
`was 10 years, and the proportion of males and females was 3 boys and 3 girls. The results are
`disclosed in Table 4. In each test of the adjusting power, the time until 2 hours passed after the
`instillation was defined as the observation time.
`
`[0026]
`
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`7
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`
`
`As can be seen from the results in Table 4, when the atropine concentration was compared with
`the case where the atropine concentration was 0.05% and the case where the atropine
`concentration was 0.1, no clear difference was found, but the control group was subjected to the
`first experiment. P (probability) = 0.001 (P <0.05) for both the group and the second
`experimental group. This is statistically significant, indicating that it has the effect of moderating
`the adjusting power. Therefore, it can be said that eye drops having an atropine concentration of
`0.05% have a favorable effect of relaxing the adjusting power.
`
`[0027]
`
`In the experiments in Table 4, the pupil was examined at the same time as the adjustment power
`was examined, and the relationship between atropine concentration and mydriasis was examined.
`The results are disclosed in Table 5.
`
`[0028]
`As can be seen from Table 5, when the atropine concentration is 0.05%, the effect of the
`mydriasis is statistically lower than that when the atropine concentration is 0.1% (P <0.05).
`
`[0029]
`Further, the inventor conducted a test regarding photophobia for the first experimental group
`and the second experimental group in the experiments in Table 4, and discloses the results in
`Table 6.
`
`[0030]
`
`As can be seen from FIG. 6, it can be said that an eyedrop having an atropine concentration of
`0.1% has a high probability of exhibiting photophobia and has poor adaptability to the eyedrop.
`
`However, eye drops with atropine concentration of 0.05% have a lower probability of exhibiting
`photophobia than those with a concentration of 0.1%.
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`
`
`[0031]
`
`The results of an experiment on the relationship between atropine concentration and mydriasis
`time are listed in the following table.
`
`Whenan eyedrop having an atropine concentration of 1% wasinstilled, the mydriasis time was
`about 7-14 days. Wheneye drops containing cyclopentolate hydrochloride wereinstilled, the
`mydriasis was about 2 days. When eye dropscontaining tropicamide wereinstilled, the mydriasis
`time was 6 hours. Whenthese three drugs were tested as therapeutic agents for myopia, only
`atropine waseffective. As shown in the following table, in the present invention, the
`concentration of atropine is 0.05%. In this case, the mydriasis time is about 12 to 18 hours, and a
`mydriatic effect more preferable than an eyedrop having an atropine concentration of 1% can be
`obtained.
`
`[0032]
`
`As is clear from the above experiments and the results, when the concentration of atropine is
`0.1% or less, the increase in myopia can be suppressedefficiently, and photophobia or mydriasis
`continues for a long time Symptomssuch as doing can be improved. In addition, no systemic side
`effects occurred. Therefore, favorable adaptability to eye drops is obtained, whichis
`advantageous in continuing treatment for a long period of time. The atropine concentration is
`preferably 0.05%.
`
`[0033]
`The eye drops of the present invention preferably have an atropine concentration of 0.05%.
`
`[0034]
`
`The aboveis a preferred embodiment of the present invention, and does not limit the scope of
`the present invention.
`
`Therefore, any modifications or changes that can be madeby thoseskilled in the art, which are
`madein the spirit of the present invention and which have an equivalent effect on the present
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`11-03-2020
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`9
`
`
`
`invention, are all within the scope of the claims of the present invention. | do.
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`11-03-2020
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`Pee as)
`
`= Patent Translate
`eettt
`Powered by EPO and Google
`
`Notice
`This translation is machine-generated. It cannot be guaranteed thatit is intelligible, accurate,
`complete, reliable or fit for specific purposes. Critical decisions, such as commercially relevant or
`financial decisions, should not be based on machine-translation output.
`
`CLAIMS JP2007308398
`
`1.
`
`An eye drop containing atropine, wherein the concentration of the atropine is adjusted to 0.1% or
`less.
`
`2.
`
`The eye drop according to claim 1, wherein the concentration of the atropine is 0.05%.
`
`3.
`
`A method for producing an eye drop containing atropine, comprising the step of diluting the
`atropine to a concentration of 0.1% or less with a liquid harmless to the human body.
`
`4.
`
`The method according to claim 3, wherein the liquid harmless to the human bodyfordiluting the
`atropine is distilled water.
`
`5.
`
`The method according to claim 3, wherein the liquid harmless to the human bodyfordiluting
`atropine is physiological saline.
`
`11-03-2020
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`1
`
`
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