Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2000-06-21
2001-10-16
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S772300, C514S912000
Reexamination Certificate
active
06303631
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a water-soluble eye drop. More particularly, it relates to a water-soluble eye drop which has a remarkably long duration time of drug efficacy, and which is superior in an intraocular pressure inhibition action and is effective for treatment of glaucoma.
BACKGROUND ART
It has been well known that a carbostyryl derivative represented by the formula (1):
wherein R represents a tert-butyl group, or an acid addition salt thereof is a compound which is effective as a remedy for glaucoma (U.S. Pat. No. 4,309,432). The compound represented by the above formula (1) is referred to as carteolol.
On the other hand, an eye drop or an ophthalmic ointment is often used as the eye drop.
In case of the eye drop, since a base is usually purified water, it is difficult to adhere the eye drop onto the cornea in the case of dropping it in the eyes. Furthermore, it is impossible to avoid that the eye drop is diluted with lacrimal fluid and falls from the eyes. Accordingly, it was difficult for a conventional eye drop to sufficiently retain a drug in the eye drop in the eyes.
Furthermore, the ophthalmic ointment is prepared by adding liquid paraffin, purified lanolin or the like to petrolatum as a base. Such an ophthalmic ointment is liable to be discharged from the eyes by means of lacrimal fluid because of its poor hydrophilicity. Therefore, there is such a drawback that the opthalimic ointment is not sufficiently adhered onto the cornea and ophthalmic mucosa and, as a result, the amount of the drug in the ophthalmic ointment, which arrives the affected part and is absorbed, is small. The ophthalmic ointment also has a drawback that an unpleasant feel arises in the eyes after applying it because of oiliness of an oily base.
To solve the above drawbacks of the conventional eye drop and ophthalmic ointment, British Patent No. 2,007,091 corresponding to Japanese Patent Laid-Open Publication No. 67021/1979 suggests a gelled eye drop. The gelled eye drop described in said publication is an eye drop prepared by mixing an aqueous crosslinked type polyacrylic acid solution with a water-soluble basic substance and a drug for eye drop, which has the pH of 5 to 8 and the viscosity of 1,000 to 100,000 centipoise at 20° C.
However, such a gelled eye drop is insufficient in duration time of drug efficacy, and is inferior in intraocular pressure inhibition action. Furthermore, the gelled eye drop is also insufficient in ease of handling and affinity to the eyes (feeling in the case of dropping it in the eyes). Accordingly, it is difficult to use such a gelled eye drop as an eye drop which is particularly effective for treatment of glaucoma requiring the control of the intraocular pressure.
SUMMARY OF THE INVENTION
To develop a water-soluble eye drop having no drawbacks described above, the present inventors have intensively studied. As a result, they have found that a water-soluble eye drop comprising the following component (a), component (b) and component (c) can be used as a desired water-soluble eye drop having no drawbacks described above.
That is, the present invention relates to a water-soluble eye drop comprising (a) at least one selected from carteolol and an acid addition salt thereof, (b) at least one acrylic polymer selected from a straight-chain type polyacrylic acid and a pharmaceutically acceptable water-soluble salt thereof, and (c) at least one selected from a water-soluble alkali metal salt and a water-soluble amine.
Although a base is purified water, the eye drop of the present invention is easily applied onto the cornea in the case of dropping it in the eyes and is not likely to fall from the eyes even if the eye drop is diluted with lacrimal fluid. Accordingly, according to the eye drop of the present invention, a drug component in the eye drop in the eye drop can be retained sufficiently in the eyes.
The water-soluble eye drop of the present invention has a remarkably long duration time of drug efficacy, and is superior in intraocular pressure inhibition action. Accordingly, the water-soluble eye drop of the present invention is an eye drop which is particularly effective for treatment of glaucoma requiring the control of the intraocular pressure.
Furthermore, the water-soluble eye drop of the present invention is satisfactory in ease of handling and affinity to the eyes (feeling in the case of dropping it in the eyes).
DETAILED DESCRIPTION OF THE INVENTION
The water-soluble eye drop of the present invention includes embodiments described hereinafter.
1) A water-soluble eye drop comprising (a) at least one selected from carteolol and an acid addition salt thereof, (b) at least one acrylic polymer selected from a straight-chain type polyacrylic acid and a pharmaceutically acceptable water-soluble salt thereof, and (c) at least one selected from a water-soluble alkali metal salt and a water-soluble amine.
2) The water-soluble eye drop according to the above item 1), wherein the component (a) and the component (b) are contained in the amount of about 0.1 to 5% by weight and the amount of about 0.3 to 10% by weight, respectively, and the concentration of the component (c) is from-about 10 to 140 mmol.
3) The water-soluble eye drop according to the above item 2), wherein the pH of the water-soluble eye drop is from about 4 to 10 and the viscosity at 25° C. of the water-soluble eye drop is from about 5 to 100 centipoise and, furthermore, the viscosity-average molecular weight of the acrylic polymer of the component (b) is from about 100,000 to 3,000,000.
4) The water-soluble eye drop according to the above item 3), wherein the pH of the water-soluble eye drop is from about 5 to 9 and the viscosity at 25° C. of the water-soluble eye drop is from about 10 to 70 centipoise and, furthermore, the viscosity-average molecular weight of the acrylic polymer of the component (b) is from about 2,000,000 to 3,000,000.
5) The water-soluble eye drop according to the above item 2), wherein the component (a) and the component (b) are contained in the amount of about 0.5 to 3% by weight and the amount of about 0.3 to 0.5% by weight, respectively, and the concentration of the component (c) is from about 30 to 120 mmol.
6) The water-soluble eye drop according to the above item 5), wherein the pH of the water-soluble eye drop is from about 4 to 10 and the viscosity at 25° C. of the water-soluble eye drop is from about 5 to 100 centipoise and, furthermore, the viscosity-average molecular weight of the acrylic polymer of the component (b) is from about 100,000 to 3,000,000.
7) The water-soluble eye drop according to the above item 5), wherein the pH of the water-soluble eye drop is from about 5 to 9 and the viscosity at 25° C. of the water-soluble eye drop is from about 10 to 70 centipoise and, furthermore, the viscosity-average molecular weight of the acrylic polymer of the component (b) is from about 2,000,000 to 3,000,000 and sodium chloride as the component (c) is contained in the amount of about 0.05 to 0.8% by weight.
8) The water-soluble eye drop according to the above item 1), wherein the pH of the water-soluble eye drop is from about 4 to 10 and the viscosity at 25° C. of the water-soluble eye drop is from about 5 to 100 centipoise and, furthermore, the viscosity-average molecular weight of the acrylic polymer of the component (b) is from about 100,000 to 3,000,000.
9) The water-soluble eye drop according to the above item 8), wherein the. pH of the water-soluble eye drop is from about 5 to 9 and the viscosity at 25° C. of the water-soluble eye drop is from about 10 to 70 centipoise and, furthermore, the viscosity-average molecular weight of the acrylic polymer of the component (b) is from about 2,000,000 to 3,000,000.
10) The water-soluble eye drop according to the above item 1), wherein the component (a) is carteolol hydrochloride.
11) The water-soluble eye drop according to the above item 1), wherein the component (b) is sodium polyacrylate.
12) The water-soluble eye drop according to the above item 1), wherein the component (c) is a water-soluble alkali
Odomi Masaaki
Sakata Kazuya
Sugahara Yuji
Fay Zohreh
Finnegan Henderson Farabow Garrett & Dunner L.L.P.
Otsuka Pharmaceutical Co. Ltd.
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