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Aqueous ophthalmic composition containing diquafosol or salt thereof, and polyvinylpyrrolidone

A polyvinylpyrrolidone and water-based composition technology, applied in the field of water-based ophthalmic compositions, can solve the problems of inability to obtain expected effects, poor compliance with eye drops, unable to obtain sufficient therapeutic effects, etc., and achieve excellent preservation efficacy and compliance with eye drops. The effect of sexual improvement, strong dry eye treatment effect

Pending Publication Date: 2022-04-05
SANTEN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

DIQUAS (注册商标) The dosage of eye drops is usually 1 drop at a time, 6 times a day (Non-Patent Document 1), but there are also patients with severe dry eye who cannot obtain sufficient therapeutic effect even with the prescribed dosage
In addition, in daily life, there are situations where it is difficult to regularly instill eye drops on a daily basis. Therefore, there are also patients who cannot achieve the desired effect due to poor eye instillation compliance.
In addition, although the frequency is low, there are still due to DIQUAS (注册商标) Patients complaining of side effects such as eye irritation from the use of eye drops (Non-Patent Document 1)

Method used

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  • Aqueous ophthalmic composition containing diquafosol or salt thereof, and polyvinylpyrrolidone
  • Aqueous ophthalmic composition containing diquafosol or salt thereof, and polyvinylpyrrolidone
  • Aqueous ophthalmic composition containing diquafosol or salt thereof, and polyvinylpyrrolidone

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Embodiment

[0151] The results of pharmacological tests and preparation examples are shown below, but these examples are for better understanding of the present invention and do not limit the scope of the present invention.

[0152] [test 1]

[0153] Using normal male white rabbits, the temporal change in the amount of tears after instilling the present composition was evaluated.

[0154] (Sample preparation method)

[0155] Eye drops 1:

[0156] According to the formulation table shown in Table 1, eye drop 1 was prepared. That is, diquafosol sodium (9 g), sodium hydrogen phosphate hydrate (0.6 g), edetate sodium hydrate (0.03 g) and sodium chloride (1.35 g) were dissolved in sterilized purified water to make It was 50 mL, resulting in a 6-fold concentrate. In addition, after mixing 10 mL of the 6-fold concentrated solution with 5 mL of sterilized purified water, a pH regulator was appropriately added to adjust the pH to 7, and 20 mL of sterilized purified water was added to obtain a ...

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Abstract

An aqueous ophthalmic composition containing diquafosol or a salt thereof, and polyvinylpyrrolidone. An aqueous ophthalmic composition for preventing or treating xerophthalmia, which contains diquafosol sodium at a concentration of 3% (w / v), polyvinylpyrrolidone having a K value of 90, and silver nitrate, and which is characterized by being administered to the eye by 1-2 drops at a time and 2-4 drops per day. An aqueous ophthalmic composition for preventing or treating dry eye, which contains diquafosol sodium at a concentration of 3% (w / v), polyvinylpyrrolidone, and silver nitrate, has a viscosity of 3-30 mPa.s at 25 DEG C, and is characterized by being used so as to be administered to the eye 1-2 drops at a time and 2-4 drops per day.

Description

technical field [0001] The present invention relates to an aqueous ophthalmic composition containing diquafosol or a salt thereof, and polyvinylpyrrolidone. Background technique [0002] Diquafosol is also known as P 1 ,P 4 - a purinergic receptor agonist of di(uridine-5') tetraphosphate or Up4U, which has a lacrimal secretion promoting effect, its salt diquafosol sodium as "DIQUAS (注册商标) Eye Drops 3%" (hereinafter, also referred to as "DIQUAS (注册商标) eye drops") for the treatment of dry eye syndrome (Japanese Patent No. 3652707 (Patent Document 1), DIQUAS (注册商标) 3% Drug Instructions for Eye Drops (Non-Patent Document 1)). DIQUAS (注册商标) The dosage of eye drops is usually 1 drop at a time, 6 times a day (Non-Patent Document 1), but there are patients with severe dry eye who cannot obtain sufficient therapeutic effect even with the prescribed dosage. In addition, in daily life, it may be difficult to instill eye drops regularly and frequently every day. Therefore, there a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/7084A61K47/02A61K47/32A61P27/04
CPCA61K31/7084A61K47/32A61K47/02A61P27/04A61K9/08A61K9/0048
Inventor 森岛健司浅田博之桃川雄介神村明日香远藤健一
Owner SANTEN PHARMA CO LTD
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