Method and composition for preventing or treating myopia by vinpocetine

Abstract

The invention relates to the technical field of treatment of myopia, and discloses a method and a composition for preventing or treating myopia by adopting vinpocetine, the method comprises vinpocetine, or tropicamide, or phenylephrine hydrochloride, or a combination of these substances as a sole active ingredient for inhibiting or controlling the progression of myopia; the methods in the present application can reduce the dependency of subjects with such visual impairments on corrective lenses. For example, the methods described herein may result in improved vision, including improved visual acuity. Abnormal axial elongation of eyeballs can be avoided, and therefore complications, especially serious retina diseases threatening vision, can be avoided.

Description

Technical Field

[0001] The invention relates to the technical field of treating myopia, and in particular to a method and a composition for preventing or treating myopia by using vinpocetine. Background Art

[0002] Myopia, also known as short-sightedness, is a common vision problem. It is characterized by the fact that when the eyes are relaxed, parallel light rays pass through the eye's refractive system and focus in front of the retina, causing distant objects to be blurred, while nearby objects are relatively clear. The causes of myopia are complex, mainly including genetic factors, bad eye habits, environmental factors, and developmental factors. Long-term close-range eye use, insufficient outdoor activity time, and insufficient lighting in the reading environment may increase the risk of myopia. In addition, high myopia also has a certain genetic tendency. Myopia treatment mainly includes general treatment, drug treatment, and surgical treatment. Drug treatment should select the most appropriate drug under the guidance of a doctor, and myopia cannot be completely cured.

[0003] The increasing popularity of electronic products such as computers and mobile phones is one of the main reasons for the younger and more severe myopia. High myopia will significantly increase the incidence of ophthalmic diseases. Therefore, it is urgent to find a new method for treating myopia. The present invention will propose a new method for treating myopia. Summary of the invention

[0004] 1. Technical issues to be solved

[0005] In view of the deficiencies of the prior art, the present invention provides a method and composition for preventing or treating myopia using vinpocetine, which has the advantages of promoting blood flow in the eye and facilitating surgical treatment, thereby solving the problem of poor treatment effect.

[0006] (II) Technical solution

[0007] To achieve the above-mentioned object, the present invention provides the following technical solution: a method for preventing or treating myopia using vinpocetine, the method comprising vinpocetine, or tropicamide, or phenylephrine hydrochloride, or a combination of these substances as the sole active ingredient, for inhibiting or controlling the progression of myopia.

[0008] In some embodiments, the myopia is simple myopia selected from the group consisting of myopia, pseudomyopia, hyperopia, and exophoria.

[0009] In some embodiments, the tropicamide, hydrochloric acid is administered to the eye as a topical ophthalmic formulation.

[0010] In some embodiments, the tropicamide hydrochloride is administered to the eye as eye drops.

[0011] In some embodiments, the tropicamide, HCl is administered to the eye by topical application to the periorbital skin.

[0012] In some embodiments, the concentration of vinpocetine, tropicamide, phenylephrine hydrochloride, or a combination of these substances in the medicament, preparation, composition or device is 0.01 μM to 1000 μM.

[0013] In some embodiments, the phenylephrine hydrochloride is selected from the group consisting of albuterol, formoterol, salmeterol, vilanterol, indacaterol, arformoterol, olodaterol, and combinations thereof.

[0014] In some embodiments, the method further comprises administering a muscarinic antagonist to an eye of the subject.

[0015] In some embodiments, the muscarinic antagonist is selected from the group consisting of atropine, scopolamine, hydroxyzine, ipratropium, tropicamide, pirenzepine, diphenhydramine, doxylamine, dimenhydrinate, dicyclomine, flavoxate, oxybutynin, cyclopentolate, metronidazole, trihexyphenidyl, tolterodine, solifenacin, darifenacin, benztropine, mebeverine, procyclidine, and combinations thereof.

[0016] (III) Beneficial effects

[0017] Compared with the prior art, the present invention provides a method and composition for preventing or treating myopia using vinpocetine, which has the following beneficial effects:

[0018] 1. The methods of the present application can reduce the dependence of subjects with such visual impairment on corrective lenses. For example, the methods described herein can lead to improved vision, including improved visual acuity. Abnormal axial elongation of the eyeball can be avoided, thereby also avoiding complications, especially serious, vision-threatening retinal diseases.

[0019] 2. The methods described in this application can reduce or even eliminate the use or dependence on treatments that may have more serious side effects. For example, the commonly used muscarinic agent atropine may produce ocular side effects such as dry eyes, mydriasis, and photophobia. Atropine may cause cardiac arrest when absorbed into the bloodstream due to sympathetic nerve stimulation of the heart rate; this may be caused by reducing or preventing the parasympathetic neuron input that usually negatively regulates the heart rate. Atropine is a derivative of Atropo Belladonna, which is one of the most toxic plants known (e.g., belladonna poisoning). Unrestricted use of atropine in young children may be fatal. The methods described herein can use reduced doses of atropine or other muscarinic antagonists to provide safe and effective alternative treatments for visual impairment. As described herein, the method can provide safe, effective and optimized treatment for visual impairment without the use of atropine.

[0020] 3. The method described in this application can be used before myopia surgery. After the pupil is enlarged, the doctor can more clearly observe the structures inside the eye, such as the retina and vitreous body. In eye surgeries such as refractive surgery, moderate dilation of the pupil can reduce discomfort during the operation and help the doctor to position and operate more accurately. DETAILED DESCRIPTION

[0021] The following will exemplarily show the embodiments of the present application. Although the present application has been described in conjunction with these specific embodiments, it should be understood that the present application is not intended to be limited to such specific embodiments. On the contrary, the present application is intended to cover such alternatives, modifications, substitutions, variations and equivalents that may be included in the spirit and scope of the present application as defined by the appended claims.

[0022] The present application further provides a drug for the treatment of myopia and the control of myopia progression, which is topically applied to the eye and uses vinpocetine as the only or main active ingredient. In the prior art, vinpocetine is mainly tablets and injections, and is administered systemically. When vinpocetine is used to treat myopia, if systemic administration is performed, it will be affected by the first-pass effect of the drug, the blood-retinal barrier (BRB), etc., and a large dose of the drug needs to be given to ensure that the vinpocetine or its metabolites entering the eye reach the therapeutic concentration threshold. Such a treatment strategy has a potential risk of systemic adverse reactions, especially for young people and requires long-term continuous administration. At the same time, systemic administration is affected by more individual differences, which increases the uncertainty of the efficacy of vinpocetine in preventing and controlling myopia. Therefore, the present application has developed a vinpocetine drug with better effectiveness and safety, which is topically applied to the eye. This drug development strategy targets the use of vinpocetine and its related compounds (such as fluorinated compounds) in the prevention and control of myopia in children and adolescents. Its advantages are that it is convenient for patients to use the medicine and has a high degree of compliance. It can be given for a long time (such as one month, half a year, one year, three years, five years, or ten years), the growth and development of young individuals are less affected, and the ophthalmic dosage form is safe and reliable.

[0023] Current drug therapies for alleviating myopia involve reducing parasympathetic neuron tone to relax the ciliary muscles. This is usually achieved by using muscarinic receptor antagonists (almost always atropine). Atropine can cause dry eyes, mydriasis, and photophobia, and can have serious cardiac side effects when absorbed into the bloodstream. In some cases, the effect on heart rate can be fatal. Atropine may also become less effective over time. These characteristics make atropine particularly unpopular and even potentially dangerous in pediatric patients (i.e., the population that should use corrective treatment).

[0024] While the parasympathetic nerves primarily control the effects on ciliary muscle tone, the sympathetic nerves provide the opposite regulatory input. Sympathetic neuronal input relaxes the ciliary muscle, which opposes the contractile activity of the parasympathetic nerves. LABAs can provide a means of stabilizing control of ciliary muscle tone, which can be used in combination with or in place of atropine therapy.

[0025] A method for preventing or treating myopia using vinpocetine, the method comprising vinpocetine, or tropicamide, or phenylephrine hydrochloride, or a combination of these substances as the sole active ingredient, for inhibiting or controlling the progression of myopia.

[0026] In some embodiments, the myopia is simple myopia selected from the group consisting of myopia, pseudomyopia, hyperopia, and exophoria.

[0027] In some embodiments, the tropicamide, hydrochloric acid is administered to the eye as a topical ophthalmic formulation.

[0028] In some embodiments, the tropicamide hydrochloride is administered to the eye as eye drops.

[0029] In some embodiments, the tropicamide, HCl is administered to the eye by topical application to the periorbital skin.

[0030] In some embodiments, the concentration of vinpocetine, tropicamide, phenylephrine hydrochloride, or a combination of these substances in the medicament, preparation, composition or device is 0.01 μM to 1000 μM.

[0031] In some embodiments, the phenylephrine hydrochloride is selected from the group consisting of albuterol, formoterol, salmeterol, vilanterol, indacaterol, arformoterol, olodaterol, and combinations thereof.

[0032] In some embodiments, the method further comprises administering a muscarinic antagonist to an eye of the subject.

[0033] In some embodiments, the muscarinic antagonist is selected from the group consisting of atropine, scopolamine, hydroxyzine, ipratropium, tropicamide, pirenzepine, diphenhydramine, doxylamine, dimenhydrinate, dicyclomine, flavoxate, oxybutynin, cyclopentolate, metronidazole, trihexyphenidyl, tolterodine, solifenacin, darifenacin, benztropine, mebeverine, procyclidine, and combinations thereof.

[0034] In the description of this specification, the description with reference to the terms "one embodiment", "some embodiments", "example", "specific example", "some examples", etc. means that the specific features, structures, materials or characteristics described in conjunction with the embodiment or example are included in at least one embodiment or example of the present application. In this specification, the schematic representations of the above terms do not necessarily refer to the same embodiment or example. Moreover, the specific features, structures, materials or characteristics described may be combined in any one or more embodiments or examples in a suitable manner. In addition, those skilled in the art may combine and combine the different embodiments or examples described in this specification.

[0035] In addition, the technical solutions between the various embodiments can be combined with each other, but they must be based on the fact that they can be implemented by ordinary technicians in this field. When the combination of technical solutions is contradictory or cannot be implemented, it should be deemed that such combination of technical solutions does not exist and is not within the scope of protection required by this application.

[0036] Although embodiments of the present invention have been shown and described, it will be appreciated by those skilled in the art that various changes, modifications, substitutions and variations may be made to the embodiments without departing from the principles and spirit of the present invention, and that the scope of the present invention is defined by the appended claims and their equivalents.

Claims

1. A method for preventing or treating myopia using vinpocetine, characterized in that: The method comprises vinpocetine, tropicamide, phenylephrine hydrochloride, or a combination of these substances as the sole active ingredient, and is used for inhibiting or controlling the progression of myopia.

2. A method for preventing or treating myopia using vinpocetine according to claim 1, characterized in that: The myopia is simple myopia, and the simple myopia is selected from the group consisting of myopia, pseudomyopia, hyperopia and exophoria.

3. A method for preventing or treating myopia using vinpocetine according to claim 2, characterized in that: The tropicamide, hydrochloric acid is administered to the eye as a topical ophthalmic preparation.

4. A method for preventing or treating myopia using vinpocetine according to claim 2, characterized in that: The tropicamide and hydrochloric acid are applied to eyes as eye drops.

5. A method for preventing or treating myopia using vinpocetine according to claim 2, characterized in that: The tropicamide hydrochloride is administered to the eye by topical application to the periorbital skin.

6. A method for preventing or treating myopia using vinpocetine according to claim 1, characterized in that: The concentration of vinpocetine, tropicamide, phenylephrine hydrochloride, or a combination of these substances in the medicine, preparation, composition or device is 0.01 μM to 1000 μM.

7. A method for preventing or treating myopia using vinpocetine according to any one of claims 1 to 5, characterized in that: The phenylephrine hydrochloride is selected from the group consisting of albuterol, formoterol, salmeterol, vilanterol, indacaterol, arformoterol, olodaterol, and combinations thereof.

8. A method for preventing or treating myopia using vinpocetine according to any one of claims 1 to 5, characterized in that: The method further comprises administering a muscarinic antagonist to an eye of the subject.

9. A method for preventing or treating myopia using vinpocetine according to any one of claim 8, characterized in that: The muscarinic antagonist is selected from the group consisting of atropine, scopolamine, hydroxyzine, ipratropium, tropicamide, pirenzepine, diphenhydramine, doxylamine, dimenhydrinate, dicyclomine, flavoxate, oxybutynin, cyclopentolate, metronidazole, trihexyphenidyl, tolterodine, solifenacin, darifenacin, benztropine, mebeverine, procyclidine, and combinations thereof.