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Composition promoting lacrimal secretion

a technology of lacrimal secretion and composition, applied in the direction of prosthesis, instruments, spectales/goggles, etc., can solve the problems of dry eye symptoms, lack of effect, paropsia and asthenopia, etc., and achieve the effect of promoting lacrimal secretion

Inactive Publication Date: 2003-10-30
FUSO PHARMA INDS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0014] The present invention was done in light of the above prior art, and an object of the present invention is to provide a safe and effective composition for promoting lacrimal secretion. That is, the object of the present invention is to provide a composition possessing the novel lacrimal secretion promoting action, which can solve a problem of side effects caused by conventional artificial lacrimal fluid-type eye drops aiming at supplement of lacrimal fluid components, and lacrimal secretory stimulating agents such as muscarinic drugs or the like.

Problems solved by technology

In addition, it is said that when dry eye becomes severe, it also causes paropsia and asthenopia.
Accordingly, when the production of the oily layer is reduced due to meibomitis, the aqueous layer becomes apt to evaporate and, thereby, symptom of dry eye is exhibited.
However, many of them are a preparation comprising inorganic salts and / or metal chelating agents for the purpose of supplementing the lacrimal fluid and, therefore, although they are temporarily effective to solve the dry feeling of eye followed by a lowered lacrimal secretion, the effect is not sustained because they do not affect the lacrimal secretion itself.
In addition, it is difficult to persistently remove unpleasantnesses such as foreign body feeling and itching upon wearing the contact lens, burning feeling of eye and the like due to dry eye.
Although there is, as the known lacrimal secretion promoting therapy, a method, in which muscarinic drug such as pilocarpine as a lacrimal secretion stimulating agent, it has not been a satisfactory preparation yet because of the problems of side effects and the like.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 2

An Animal Which was Used in Experiments

[0195] Male Wistar-line rat at 6 weeks of age was used in experiments. Each animal was housed for one week under the environment of room temperature of 23.+-.2.degree. C., a humidity of 50.+-.5% and a 12 hours light / dark cycle (light: 07:00-19:00) and, thereafter, it was subjected to experiments. During the housing and experiment period, the animal was fed a solid chaw and water ad lib.

[0196] Four animals were used in Examples 3-4, and the results thereof are shown in the mean.+-.S.E.M. The test of significance was performed according to a Tukey's multiple comparison test.

example 3

[0197] The effect of PAR-2 agonist peptide on a rat lacrimal secretion in vivo was investigated (FIG. 1).

[0198] An amount of rat lacrimal fluid was measured according to the method of Iga et al. (Iga, Y et al., Jpn. J. Pharmacol., 78, 373-80, 1998). That is, the rat was anesthetized with pentobarbital (50 mg / kg, intraabdominal administration), and a paper with 2 mm width for testing human lacrimal secretion function, the Schirmer test paper (Showa Yakuhin Kako Co., Ltd.) was inserted into a lower eyelid of the rat After the period of time fixed has passed, the test paper was removed, and a length of a wetted portion of the test paper was measured using a caliper square. An amount of lacrimal fluid was measured at 1, 2, 4, 6, 8 and 10 minutes after intravenous administration of a solvent or PAR-associated peptides.

[0199] When 5 .mu.mol / kg of a PAR-2 agonist peptide, SLp-NH.sub.2 was administered to the rat intravenously, significant promotion of lacrimal secretion was observed with a...

example 4

[0200] Dose-dependency in the promoting action of rat lacrimal secretion by the PAR-2 agonist peptide in vivo was investigated (FIG. 2).

[0201] An amount of lacrimal fluid was measured as described in Example 3.

[0202] The SLp-NH.sub.2 promoted the rat lacrimal secretion in doses of ranging from 1 to 5 .mu.mol / kg in a dose-dependent manner. On the other hand, a control peptide, LRp-NH.sub.2 had no effect on the rat lacrimal secretion even at 5.mu.mol / kg, and resulted in an amount of lacrimal secretion similar to that of a solvent-administrated group.

[0203] The formulations of the compositions of the present invention manufactured according to the conventional method are shown in each table in the following Examples.

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Abstract

A composition for promoting lacrimal secretion which can be used safely and effectively in the lacrimal secretion promoting therapy, not in the conventional supplemental therapy of lacrimal fluid components is provided. The composition comprises a component which activates PAR-2. Also, a contact lens which retains and / or contains said composition for promoting lacrimal secretion is provided.

Description

[0001] The present invention relates to a composition for promoting lacrimal secretion for. treating and / or preventing an ocular disease followed by lowered lacrimal secretion, that are, dry eye, ectocorneal desquamation, corneitis, corneal ulcer, conjunctivitis and the like. Furthermore, the present invention relates to a DDS (drug delivery system) preparation, a percutaneously absorbing preparation, a topical ophthalmic agent (such as eye drops, ophthalmic ointments and the like) and a composition for a contact lens which contain the composition for promoting lacrimal secretion.[0002] In recent years, dry eye patients have been increased with spread of a contact lens and increase in a VDT-operation. Dry eye is a disease exhibiting symptoms such as xerophthalmia, corneal afflux, foreign body feeling, itching feeling and the like, which results in corneal disorders, in principal, due to a lowered lacrimal secretion. In addition, it is said that when dry eye becomes severe, it also c...

Claims

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Application Information

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IPC IPC(8): G02C7/04A61F9/00A61K9/06A61K9/08A61K9/10A61K38/00A61K38/08A61K38/17A61K38/48A61K45/00A61K45/06A61L27/22A61P27/02A61P43/00C07K7/06C12N9/76C12N9/99G02B1/04G02C13/00
CPCA61K38/177A61K38/482A61K38/4826A61K38/08G02B1/043A61K38/06A61L27/227A61P27/02A61P43/00
Inventor ARAKI, HIROMASAKAWABATA, ATSUFUMITANAKA, SHUICHIKAWAI, KENZONISHIMURA, SACHIYONISHIKAWA, HIROYUKI
Owner FUSO PHARMA INDS
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