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Sustained release eyedrops

A technology of eye drops and β-blockers, which is applied in the field of eye drops, can solve the problems that affect the corneal permeability of β-blockers, which have not been seen, so as to reduce the frequency of eye drops, improve retention, and avoid troublesome effect

Inactive Publication Date: 2003-10-22
SENJU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But, there is no report pointing out that eyedrops with unsaturated fatty acids such as described sorbic acid can promote the medicine to migrate in the eye, on the contrary, there are reports pointing out that in in vitro tests, there is no effect on the corneal permeability of the β blocker tirirolol ( "Journal of Pharmacy and Pharmacology" J.Pharm.Pharmacol., Vol. 47, pp. 703-707, 1995)
In addition, have not yet seen the C 3 ~C 7 Prior Art Literature on Fatty Acids Affecting Beta-Blocker Corneal Permeability

Method used

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  • Sustained release eyedrops
  • Sustained release eyedrops
  • Sustained release eyedrops

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1, eye drops

[0038] Prepare the following prescription carteolol hydrochloride eye drops according to conventional methods.

[0039] Carteolol Hydrochloride 2.0g

[0040] Sorbic acid 0.3g

[0041] Sodium dihydrogen phosphate 0.1g

[0042] Sodium chloride 0.7g

[0043] Benzalkonium Chloride 0.005g

[0044] Appropriate amount of sodium hydroxide

[0045] Sterilized purified water to a total of 100ml

[0046] pH 7.0

Embodiment 2

[0048] Prepare the following prescription carteolol hydrochloride eye drops according to conventional methods.

[0049] Carteolol Hydrochloride 2.0g

[0050] Sorbic acid 0.3g

[0051] Sodium dihydrogen phosphate 0.1g

[0052] Sodium chloride 0.43g

[0053] Benzalkonium Chloride 0.005g

[0054] Appropriate amount of sodium hydroxide

[0055] Sterilized purified water to a total of 100ml

[0056] pH 7.0

Embodiment 3

[0058] Prepare the following prescription carteolol hydrochloride eye drops according to conventional methods.

[0059] Carteolol Hydrochloride 1.0g

[0060] Sorbic acid 0.3g

[0061] Sodium dihydrogen phosphate 0.1g

[0062] Sodium chloride 0.53g

[0063] Benzalkonium Chloride 0.005g

[0064] Appropriate amount of sodium hydroxide

[0065] Sterilized purified water to a total of 100ml

[0066] pH 6.5

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Abstract

Eye drops containing a beta-blocker such as cartelol hydrochloride are improved in the penetration of the beta-blocker into the eye and the retention thereof in the eye tissues by the incorporation of a C3-7 fatty acid such as sorbic acid to the eye preparations.

Description

technical field [0001] The present invention relates to beta-blockers and C 3 ~C 7 Eye drops of fatty acids or salts thereof. In addition, it also involves adding C to eye drops containing beta blockers 3 ~C 7 Fatty acids or their salts promote the migration of β-blockers into the eye and increase the retention of β-blockers in intraocular tissues. Background technique [0002] β-blockers such as carteolol hydrochloride, timolol maleate, and betaxolol hydrochloride are used as eye drops and are currently used as therapeutic drugs for glaucoma. However, most of the main ingredients of these eye drops (such as carteolol hydrochloride, etc.) are very water-soluble, and in this case, the highly hydrophobic corneal epithelium will become a barrier when migrating into the eye. In order to show the intraocular pressure lowering effect, it is necessary to instill eye drops with high dosage, or to instill eye drops several times. However, in order to separate from the systemic ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/08A61K47/12
CPCA61K9/0048A61K9/08A61K47/12
Inventor 东山昌代大鸟聪
Owner SENJU PHARMA CO LTD
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