Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1998-07-17
2000-03-21
Lee, Howard C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514552, 514912, 560205, 560225, A61K 3122, A61K 3123
Patent
active
060403438
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a therapeutic agent for keratoconjunctiva diseases containing gefarnate as an active ingredient.
BACKGROUND ART
In general, organisms directly contact the outside demarcated by mucous surface of digestive tracts, respiratory organs, etc. and are always exposed to the danger of invasion of microbes and foreign substances from outside. Therefore, organisms are equipped with a defense mechanism for protecting the mucous membrane. That is to say, although mucous membrane is covered with only a single layer of mucoepithelium, the epithelial cells are always covered with a viscous exocrine liquid containing mucin secreted from exocrine gland and the exocrine liquid prevents microbes and foreign substances from contacting the epithelial cells directly. In eyes, tear plays such a role and wets the surface of the eye balls.
Tear layer consists of three layers, that are oily layer, aqueous layer and mucus layer, and keratoconjunctiva epithelial cells are adjacent to the mucus layer. Mucin, which constitutes the mucus layer, is a glycoprotein mainly secreted from goblet cells of conjunctiva. It was known that mucin layer covers the surface of the hydrophobic keratoconjunctiva epithelial cells and change the property to hydrophilic ones to assist the maintenance and expansion of aqueous layer in tear whereby it plays an important role in keeping the normal structure of tear (Journal of the Eye, 8, 1037-1042(1991)).
Accordingly, if there is any substance having an action of promoting the secretion of mucin into tear fluid, it is expected that such a substance is useful to keratoconjunctiva diseases having a trouble on keratoconjunctiva epithelium such as dry eye, keratitis, conjunctivitis, corneal erosion and corneal ulcer.
Studies were made recently on the relation between drugs and production and secretion of mucin and it was reported that ebrotidine, which is a therapeutic agent for ulcer, promotes the production and secretion of rat gastric mucin (Gen. Pharmac., 24, 611-617(1993)) and that participation of mucin is presumed in an antiulcerative action of methylmethionine sulfonium chloride (Jpn. Pharmacol. Ther., 22, 4355-4361(1994)).
It was disclosed that gefarnate is a substance showing a strong antiulcerative action and is useful for therapy of peptic ulcers such as gastric ulcer and duodenal ulcer (Japanese Examined Patent Publication 28,230/1964). With regard to its function, it was reported that gefarnate promotes the deposition of acidic mucopolysaccharides on surface of a wound, to increase the amount of mucus such as hexosamine in gastric mucosa and is expected to protect the mucous membrane, etc. and to increase endogenous prostaglandins (Pharma Med., 4, 45-48(1986)).
However, there has been no report on study in ophthalmologic field.
Although various studies have been made already for therapeutic agents for keratoconjunctiva diseases including dry eye, it is a very interesting theme to find new substances which promote the production and secretion of mucin in ophthalmic tissues.
DISCLOSURE OF THE INVENTION
The present inventors paid their attention to known drugs which have been used as therapeutic agents for ulcer from the viewpoint of protection of mucous membrane, studied their influence on production and secretion of mucin in ophthalmic tissues and observed that gefarnate promotes the production and secretion of mucin in keratoconjunctiva whereupon they have found that gefarnate is useful as a therapeutic agent for keratoconjunctiva diseases such as dry eye, keratitis, conjunctivitis, corneal erosion and corneal ulcer.
Although the details of influence of gefarnate on production and secretion of mucin in ophthalmic tissues will be mentioned under the paragraph of Pharmacological Tests, it has been found that gefarnate promotes the secretion of protein containing mucin by the study using sulfate ion which was labeled with radioisotope existing in corneal epithelium (hereinafter, the above-mentioned protein will be referred to as "mucin-containing
REFERENCES:
Fukada et al, "Dry Eye and Corneal and Conjunctival Epithelium", Journal of the Eye, 8, pp. 1037-1042 (1991) and partial English language translation.
Slomiany et al, "Effect of Ebrotidine on the Synthesis and Secretion of Gastric Sulfomucin", Gen. Pharmac., 24, pp. 611-617 (1993).
Watanabe, "Effect Of Methylmethionine Sulfonium Chloride (MMSC) On Gastric Mucin In Relation With Ethanol-Induced Injury in Rats", Jpn. Pharmacol. Ther., 22, pp. 4355-4361 (1994) and partial English language translation.
Shigemoto et al, "Mucosal Protective Drug", Pharma Medica, 4, pp. 45-48 (1986) and partial English language translation.
J. Bilski et al, "Enhancement of the Lipid Content and Physical Properties of Gastric Mucus by Geranylgeranyllacetone", Biochemical Pharmacology, vol. 36, No. 23, pp. 4059-4065, 1987.
Hamano Takashi
Nakamura Masatsugu
Nakata Katsuhiko
Lee Howard C.
Santen Pharmaceutical Co. Ltd.
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