Aqueous composition for ophthalmic administration

A water-based composition and composition technology, applied in the direction of drug combination, boron compound active ingredients, drug delivery, etc., to improve QOL, reduce the number of administrations, and prevent the effect of curative effect reduction

Inactive Publication Date: 2013-05-01
WAKAMOTO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, nothing is known about the use of boric acid and sugar alcohols other than the enhanced antibacterial effect.

Method used

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  • Aqueous composition for ophthalmic administration
  • Aqueous composition for ophthalmic administration
  • Aqueous composition for ophthalmic administration

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Add 0.68 g of timolol maleate, 1.5 g of mannitol, 0.85 g of boric acid, 1.0 g of sodium citrate, and 0.2 mL of 0.5 w / v% benzalkonium chloride into 70 mL of sterilized purified water and dissolve. 1N sodium hydroxide was added thereto to adjust the pH to 6.9. Next, sterilized purified water was added to make it 100 mL, and it was filtered with a membrane filter. Among them, 5 mL was filled in a plastic eye drop bottle to prepare Example 1.

Embodiment 2

[0070] 2.0 g of carteolol hydrochloride, 2.0 g of mannitol, 0.7 g of boric acid, 1.0 g of sodium citrate, and 0.5 g of hydroxyethylcellulose were added to 70 mL of sterilized purified water and dissolved. 1N sodium hydroxide was added thereto to adjust the pH to 6.9. Next, sterilized purified water was added to make it 100 mL, and it was filtered with a membrane filter. Of these, 5 mL was filled in a plastic eye drop bottle to prepare Example 2.

Embodiment 3

[0072] Add 2.0 g of carteolol hydrochloride, 3.9 g of mannitol, 1.0 g of sodium citrate, 0.5 g of hydroxyethyl cellulose, and 0.2 mL of 0.5 w / v% benzalkonium chloride into 70 mL of sterilized purified water, dissolve . 1N sodium hydroxide was added thereto to adjust the pH to 7.9. Next, sterilized purified water was added to make it 100 mL, and it was filtered with a membrane filter. 5 mL of these were filled in a plastic eye dropper to prepare Example 3.

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Abstract

An aqueous composition for ophthalmic administration which contains a ss-blocker typified by, for example, timolol or carteolol and a sugar alcohol typified by mannitol or sorbitol optionally together with boric acid. The aforesaid composition can increase the corneal permeability of a drug. As a result, the drug dosage can be decreased, e.g., a lowering in the frequency of ophthalmic administration. Thus, it is expected that the risk of systemic side effects such as cardio toxicity or respiratory toxicity, which might be induced by the ophthalmic administration of the ss-blocker, can be reduced thereby. It is also expected that a decrease in the frequency of ophthalmic administration would contribute to the improvement in QOL and prevent a decrease in the therapeutic effect caused by missed dose.

Description

technical field [0001] The present invention relates to an aqueous ophthalmic composition having improved intraocular transferability of a drug when a composition containing a drug and sugar alcohol is administered to the eye. Background technique [0002] Currently, timolol maleate, carteolol hydrochloride and nipradilol represent β Eye drops of blocking agents are widely used as glaucoma treatment drugs. However, these drugs are generally highly water-soluble, so the highly hydrophobic corneal epithelium becomes an obstacle when the drug is transferred into the eye. In order to obtain a sufficient amount of drug transferred into the eye to show the effect, it is necessary to give a high dose of the drug by eye drops. β Blocker eye drops, or multiple eye drops. However, according to such an administration method, the drug that is not absorbed in the eye is absorbed systemically, so it is considered that β Side effects of blockers, namely severe cardiotoxicity, increased ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K9/08A61K31/138A61K31/353A61K31/4704A61K31/5377A61K47/10A61K47/26A61P27/06
CPCA61K9/0048A61K47/10A61K33/22A61K47/26A61K31/5377A61K45/06A61K31/4704A61P27/02A61P27/06A61P43/00A61K2300/00
Inventor 高岛光代高田真由美铃木秀一
Owner WAKAMOTO PHARMA
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