Percutaneously absorptive ophthalmic preparation comprising epinastine

A technology for transdermal absorption preparations and preparations, which can be applied in directions such as aerosol delivery, sensory diseases, pharmaceutical formulations, etc., and can solve the problems of no disclosure of the application of epinatine, no disclosure of percutaneous absorption preparations, etc.

Inactive Publication Date: 2008-07-09
SENJU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, WO2004 / 064817 does not disclose the application of epinadine to transdermal preparations
In addition, U.S. Patent No. 4,313,931 does not disclose transdermal absorption preparations as epinatine dosage forms

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0099] (Example 1: Adhesive preparation containing epinatine)

[0100] Epinatine Hydrochloride 0.3g

[0101] Isopropyl myristate 1.2g

[0102] Acrylic pressure-sensitive adhesive (PE-300) 1.485g (based on solid content)

[0103] Polyisocyanate compound (CK 101) 0.00675g (based on solid content)

[0104] Proper amount of ethyl acetate

[0105]

[0106] Total 3g

[0107] Epinatidine hydrochloride (SANYO KAGAKU KENKYUSYO CO.LTD.) was mixed with about 2 mL of ethyl acetate. The mixture was then sonicated for 30 seconds in a disposable cup to dissolve or disperse the epinatine hydrochloride and mixed thoroughly with isopropyl myristate. Acrylic pressure-sensitive adhesive 3.7125g (PE-300; acrylic acid copolymer; solid content is 40% by weight (ethyl acetate / toluene mixed solvent): 1.485g; Nippon Carbide Industries Co.Ltd.) and polyisocyanate compound (crosslinked Joint agent) 0.015g (CK 101; metal chelate; solid content is about...

Embodiment 2

[0108] (embodiment 2: ointment)

[0109] Epinatine Hydrochloride 0.3g

[0110] Isopropyl myristate 1.2g

[0111] White Vaseline 1.5g

[0112] Total 3g

Embodiment 3

[0113] (embodiment 3: gel)

[0114] Epinatine Hydrochloride 0.3g

[0115] Isopropyl myristate 1.2g

[0116] 2% carboxyvinyl polymer gel 1.5g

[0117]

[0118] Total 3g

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Abstract

The present invention provides a transdermal absorption preparation for preventing or treating allergic eye diseases, the preparation comprising epinatidine or a salt thereof as an active ingredient. In addition, the present invention provides a method for preventing or treating allergic eye diseases, the method comprising applying a transdermal absorption preparation comprising epinatine or a salt thereof to the skin surface including the eyelid skin surface, whereby a therapeutically effective amount of epinatine Nadine or its salts are transferred from the formulation to the anterior part of the eye through the eyelid skin rather than the systemic blood stream. Compared with conventional preparations such as eye drops, the preparation of the present invention can exhibit long-acting pharmacological effects through a single application.

Description

technical field [0001] The present invention relates to a transdermal absorption preparation for preventing or treating allergic eye diseases, the preparation comprising epinadine or a salt thereof as an active ingredient. Furthermore, the present invention relates to a method for transdermally delivering a therapeutically effective amount of epinatine or a salt thereof to an anterior ocular segment and for preventing or treating allergic eye diseases. Specifically, these methods comprise applying to the skin surface comprising epinatine or its salt transdermal absorption formulation, described skin surface comprises eyelid skin surface, thereby make the therapeutically effective amount of epinatine or its salt from formulation transferred to the front part of the eye. Background technique [0002] U.S. Patent 4,313,931 discloses the therapeutic agent epinadine (3-amino 9,11b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]nitrogen for the treatment of allergic eye disease Miscellane...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K9/107A61K9/06A61P37/08A61P27/14
CPCA61K9/0048A61K9/06A61K9/107A61K9/7023A61P27/14A61P37/08A61K9/08A61K31/55
Inventor 礒脇明治中岛朋子大鸟聪
Owner SENJU PHARMA CO LTD
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