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Ophthalmic percutaneous absorption type preparation

An absorption-type, ophthalmic technology, applied in medical preparations containing active ingredients, allergic diseases, drug combinations, etc., can solve the problems of adding ophthalmic drugs, not described, etc.

Inactive Publication Date: 2009-09-09
SENJU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the aforementioned references do not describe a method of increasing the amount of ophthalmic drugs transferred to the local area in the eye, especially the anterior segment, by administering an ophthalmic percutaneous absorption preparation containing a vasoconstrictor drug to the eyelid skin surface, and such Ophthalmic Percutaneous Absorption Preparations

Method used

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Embodiment

[0092] Although the present invention can be explained in more detail with reference to the following Experimental Examples and Examples, they should not be construed as limiting the present invention.

[0093] Test Method and Results

[0094]

[0095] Ketotifen fumarate (Sigma Co., Ltd.), phenylephrine hydrochloride (for biochemistry, Wako Pure Chemical Co., Ltd.), hydroxypropyl methylcellulose (Metolose 60SH-4000, Shin-Etsu Chemical Co., Ltd.), phosphoric acid Sodium dihydrogen dihydrate (first-class product, Wako Pure Chemical Co., Ltd.) and sodium hydroxide (Japanese Pharmacopoeia, Nacalai Tesque).

[0096]

Embodiment 1

[0098] Example 1: Gel formulation containing 20% ​​ketotifen fumarate and 2% phenylephrine hydrochloride

Embodiment 2

[0099] Example 2: Gel formulation containing 20% ​​ketotifen fumarate and 4% phenylephrine hydrochloride

[0100] These formulations were prepared according to the formulations in Table 1 and the formulation methods mentioned below.

[0101] Table 1

[0102]

[0103]

[0104] (Unit: w / w%)

[0105]

[0106] Comparative example 1 preparation

[0107] Sodium dihydrogenphosphate dihydrate was added to purified water, and the mixture was stirred until completely dissolved. Heat the solution to about 70°C in a water bath, add hydroxypropyl methylcellulose in small amounts and stir to dissolve. After standing at room temperature for 10 minutes, 1N aqueous sodium hydroxide solution was added. The pH of the mixture was adjusted to 6 to obtain a gel matrix. Ketotifen fumarate and gel matrix were measured on a glass petri dish, and stirred well with a spatel stirrer to obtain a formulation of Comparative Example 1 (gel formulation containing 20% ​​ketotifen fumarate).

[01...

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Abstract

The present invention provides an ophthalmic percutaneous absorption type preparation containing an ophthalmic drug and a vasoconstrictor, which can increase the amount of the ophthalmic drug transferred through the eyelid to a topical area in the eye, particularly the anterior segment of the eye such as conjunctiva, lacrimal fluid, aqueous humor, cornea and the like by administration to the skin surface of an eyelid.

Description

technical field [0001] The present invention relates to an ophthalmic percutaneous absorption type preparation that increases the amount of an ophthalmic drug transferred to a localized area in the eye through the eyelid when the ophthalmic drug is administered to the skin surface of the eyelid, and increases the transfer of the ophthalmic drug to the localized area in the eye through the eyelid method of quantity. Background technique [0002] As a traditional form of ophthalmic medicine to be topically applied to the eye, eye drops are most commonly used. However, eye drops exhibit low local ocular bioavailability due to the effect of tear turnover on the ocular surface, sometimes requiring frequent dosing to maintain a long duration of efficacy. [0003] Recently, a transdermal absorption type preparation having a structure in which an ointment layer containing a therapeutic drug for ophthalmic diseases is formed on a support has been proposed as one of preparations for ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/137A61K31/4535A61K31/55A61P27/02A61K9/00
CPCA61K9/0048A61P9/00A61P27/02A61P27/14A61P37/08A61K9/70A61K31/137
Inventor 礒胁明治中嶋朋子大鸟聪
Owner SENJU PHARMA CO LTD
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