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Prophylactic or therapeutic agent for axial myopia

A therapeutic agent and technology for myopia, applied in the direction of organic active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the unrevealed ocular axial length, can not predict the effectiveness of Rho kinase inhibitors in the prevention or treatment of axial myopia and other problems, to achieve the effective effect of prevention or treatment

Inactive Publication Date: 2011-06-22
OSAKA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, the effects of lowering intraocular pressure, improving optic nerve head blood flow, promoting aqueous humor outflow, and inhibiting ciliary muscle contraction did not reveal that they can inhibit the extension of eye axial length, and cannot predict the effect of Rho kinase inhibitors on axial myopia. effective prevention or treatment of

Method used

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  • Prophylactic or therapeutic agent for axial myopia
  • Prophylactic or therapeutic agent for axial myopia
  • Prophylactic or therapeutic agent for axial myopia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] (Embodiment 1: Utilize the eye axis length suppression test (I) of chicken myopia model)

[0053] (1) Chicken Vision Blocking Myopia Model

[0054] A 6-day-old chick (white Leghorn) was taken out, and one eye was covered with a hood made of polyvinyl chloride tape. The right eye is usually covered and the left eye serves as a control. Chicks were reared under normal rearing conditions.

[0055] (2) Rho kinase inhibitors

[0056] As the Rho kinase inhibitor, Y27632 dihydrochloride (manufactured by Wako Pure Chemical Industries, refer to the above formula (I), hereinafter abbreviated as "Y27632") and hydroxyfasudil hydrochloride (manufactured by SIGMA, refer to the above formula (III), hereinafter referred to as "hydroxyfasudil"). Y27632 was formulated to 50 μM in saline. Hydroxyfasudil was prepared at 1 mM in saline. The control group used normal saline.

[0057] (3) Administration method

[0058] For the chicks undergoing myopia induction by occlusion, Y27632 or...

Embodiment 2

[0073] (Embodiment 2: Utilize the axial length inhibition test (II) of chicken myopia model)

[0074] (1) Chicken Vision Blocking Myopia Model

[0075] A chicken vision blocking myopia model was produced in the same manner as in Example 1. That is, a 6-day-old chick (white Leghorn) was taken out, and one eye was covered with a cover made of polyvinyl chloride tape. The right eye is usually covered and the left eye serves as a control. Chicks were reared under normal rearing conditions.

[0076] (2) Rho kinase inhibitors

[0077] As the Rho kinase inhibitor, hydroxyfasudil hydrochloride (manufactured by SIGMA, see the above formula (III), hereinafter abbreviated as "hydroxyfasudil") was used. 50 μl of hydroxyfasudil (concentration: 10 mM) dissolved in BSSPLUS (registered trademark, manufactured by Alcon Co.) was diluted to 1000 μl with physiological saline to prepare 500 nmol / 1000 μl of hydroxyfasudil for use.

[0078] (3) Administration method

[0079] For chicks undergo...

Embodiment 3

[0088] (Example 3: Production example)

[0089] Prescription 1: Eye Drops

[0090] Dissolve Y27632 dihydrochloride ((R)-(+)-trans-N-(4-Pyridyl)-4-(1-aminoethyl)-cyclohexanecarboxamide 2HCl), sodium dihydrogen phosphate dihydrate and Sodium chloride, pH was adjusted to 7 with sodium hydroxide, after that, the total amount was made to 100 ml with sterile purified water, and eye drops of the following prescription were prepared.

[0091] 100ml

[0092] · Y27632 dihydrochloride 0.01g

[0093] ·Sodium dihydrogen phosphate dihydrate 0.1g

[0094] ·Sodium chloride 0.9g

[0095] ·Sodium hydroxide amount

[0096] ·Appropriate amount of sterile purified water

[0097] In addition, eye drops containing 0.1 g and 0.001 g of Y27632 dihydrochloride in 100 ml can be prepared in the same manner as in Prescription Example 1 above.

[0098] Prescription 2: Eye Drops

[0099] Dissolve hydroxyfasudil hydrochloride (1-(1-Hydroxy-5-isoquinoline sulfonyl)homopiperazine HCl), sodium dihydroge...

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Abstract

High myopia increases the risk of retinal detachment, myopic chorioretinal atrophy, myopic choroidal neovascularization, glaucoma and cataract. Therefore, it is expected to establish a method for preventing the progression of myopia. For axial myopia which is believed to cause high myopia, however, there is no effective prophylactic or therapeutic method at present. It is now found that a Rho kinase inhibitor has an activity to inhibit the elongation of a visual axis. Thus, disclosed is a pharmaceutical agent having an excellent prophylactic or therapeutic effect on axial myopia, which comprises a Rho kinase inhibitor as an active ingredient.

Description

technical field [0001] The present invention relates to a preventive or therapeutic agent for axial myopia. More specifically, the present invention relates to a preventive or therapeutic agent for axial myopia comprising a Rho kinase inhibitor as an active ingredient. Background technique [0002] Myopia refers to a state in which an image cannot be accurately captured because light transmitted through the cornea is not imaged on the retina but is imaged in front of the retina. Myopia is roughly divided into two types: accommodation myopia and axial myopia. Accommodative myopia refers to accommodation due to long-term close work, that is, an increase in the diopter of the lens due to hypercontraction of the ciliary muscle. Under normal circumstances, as long as the short-distance work is stopped, the ciliary muscle can be relaxed and the accommodation can be eliminated. The state in which the contraction state is fixed under long-term short-distance work and induces myopi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/4409A61K31/4439A61K31/551A61P27/10A61P43/00C07D213/75C07D401/04C07D401/12
CPCA61K9/0048A61K31/4439C07D213/75A61K31/551A61K31/00A61K9/0051A61K31/4409A61P27/02A61P27/10A61P43/00
Inventor 田野保雄生野恭司
Owner OSAKA UNIV
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