Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Liposomes
Patent
1997-05-15
1999-08-31
Kishore, Gollamudi S.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Liposomes
424427, A61K 9127
Patent
active
059451211
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to liposome eye drops useful for treating dry eye or mitigating its symptoms.
BACKGROUND ART
Dry eye (dried state of eyes, reduction of tear fluid) causes discomfort (e.g. dry feeling, hot feeling, eye strain, etc.), corneal injury, corneal damage and the like. In the past, dry eye has been treated by using artificial tear fluids containing boric acid, sodium chloride, potassium chloride, calcium chloride and the like. In addition, there is a proposal for the use of a liposome composition containing a quaternary benzylamine (Japanese Patent Kohyo 2-501730).
However, such prior art has an insufficient effect on mitigating or treating symptoms caused by dry eye.
An object of the present invention is to provide eye drops which have excellent mitigating or treating effects on symptoms caused by dry eye.
DISCLOSURE OF THE INVENTION
As a result of extensive research, the present inventors have found that eye drops comprising a specific composition can achieve the above-problems, and whereby the present invention has been accomplished.
That is, the present invention relates to liposome eye drops comprising taurine, glucose and inorganic salts.
In the present invention, the inorganic salts mean a mixture containing sodium chloride and potassium chloride, and if desired, one or two members selected from the group consisting of calcium chloride, magnesium sulfate and sodium bicarbonate.
The amount of taurine is preferably from 0.5 to 3% by weight. In case where the amount of taurine is less than 0.5% by weight, the treating effect on dry eye is weak, and in case where it is more than 3% by weight, irritation to eye occurs due to hypertonia. The amount of glucose is preferably from 0.01 to 1% by weight, more preferably from 0.03 to 0.2% by weight. In case where the amount of glucose is less than 0.01% by weight, the treating effect on dry eye is weak, and in case where it is more than 1% by weight, the eye drops give discomfort to eye when applied.
In order to enhance the effect of the present invention, the components are preferably combined in such an amount rate that the liposome eye drops prepared finally show a pH of 5.5 to 8.0 and an osmotic pressure of 250 to 450 mOsm. Furthermore, the liposome eye drops contain preferably an aspartate (e.g. magnesium L-aspartate, potassium L-aspartate, magnesium potassium L-aspartate, etc.) as a component. In this case, the amount of the aspartate is preferably 0.01 to 0.5% by weight, and more preferably 0.03 to 0.2% by weight.
A lecithin for composing liposome may be contained in such an amount that the eye drops have an enhanced retentivity on the corneal surface when applied, and that the eye drops do not aggregate when stored, and are stable in galenical pharmacy. That is, the amount of the lecithin is preferably 0.03 to 0.8% by weight, and more preferably 0.05 to 0.5% by weight.
The liposome eye drops of the present invention can be easily prepared by using an ordinary method used for the preparation of a liposome aqueous suspension, for example, a method described in Japanese Patent Kokai 5-4037 or a method described in Japanese Patent Kokai 2-167218 which comprises dispersing an easily hydrolyzable lecithin with other components in water and sizing.
According to the present invention, besides the above-mentioned essential components, if desired, it is possible to contain further components or other active ingredients usable for the preparation of ordinary eye drops, as long as the effects of the present invention are not degraded, for example, neostigmine methyl sulfate, anti-inflammatory agents (e.g. dipotassium glycyrrhizinate, .epsilon.-aminocaproic acid, allantoin, berberine chloride, berberine sulfate, sodium azulene sulfonate, zinc sulfate, zinc lactate, lysozyme chloride, etc.), antihistaminic agents (e.g. diphenhydramine hydrochloride, chlorpheniramine maleate, etc.), hyperemia-releasing agents (e.g. naphazoline hydrochloride, tetrahydrozoline hydrochloride, phenylephrine hydrochloride, etc.), sodium), vitami
REFERENCES:
patent: 4818537 (1989-04-01), Guo
patent: 5389383 (1995-02-01), Huth
patent: 5565213 (1996-10-01), Nakamari
International Search Report.
Egami Fuminobu
Kato Muneyoshi
Ohtsuki Tomohiro
Tsunoda Kenji
Kishore Gollamudi S.
Taisho Pharmaceutical Co. Ltd.
LandOfFree
Liposome eye drops does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Liposome eye drops, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Liposome eye drops will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2425945