GB2033222A - Topical Ophthalmic Composition - Google Patents
Topical Ophthalmic Composition Download PDFInfo
- Publication number
- GB2033222A GB2033222A GB7844165A GB7844165A GB2033222A GB 2033222 A GB2033222 A GB 2033222A GB 7844165 A GB7844165 A GB 7844165A GB 7844165 A GB7844165 A GB 7844165A GB 2033222 A GB2033222 A GB 2033222A
- Authority
- GB
- United Kingdom
- Prior art keywords
- labetalol
- composition
- percent
- group
- phenyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
Abstract
An ophthalmic composition comprises a compound of formula: <IMAGE> where X is selected from the group consisting of -CH2-CH2-, -CH2- and -OCH2- and Y from the phenyl, P-methoxy phenyl and O- methoxy phenyl groups pharmaceutically acceptable salts thereof and a topically administrable ophthalmic pharmaceutical carrier. The composition lowers intraocular pressure in the eye and is used to treat glaucoma.
Description
SPECIFICATION
Topical Ophthalmic Composition and Method of Use
Technical Field
The present invention relates to a topical ophthalmic composition and method for the therapeutic use thereof. More particularly, the present invention relates to a topical, ophthalmic composition useful in temporarily reducing intraocular pressure and alleviating the symptoms of glaucoma.
Background of Prior Art
The active compounds described herein are known in the art, e.g., German Offen. 2,021,445.
Labetalol is the designated name for a compound having the structural formula
with the chemical name 5-[1-hydroxy-2(1-methyl-3-phenylpropyl)aminoethyljsalicylamide. Its method of manufacture is disclosed in German Offen. 2,032,642, the relevant portions of which are hereby incorporated by this reference. Labetalol is known to be a systemic inhibitor of both alpha and beta adrenergic receptors and has been used heretofore in the treatment of systemic hypertension.
Glaucoma is a condition of the eye characterized by increased intraocular pressure. Untreated, the condition eventually leads to irreversible retinal damage and blindness. Conventional therapy for glaucoma is with pilocarpine and/or epinephrine administered topically to the eye several times daily.
Brief Summary of Invention
The present invention relates to a therapeutic composition comprising a topically administrable ophthalmic formulation containing an effective amount of a compound selected from the group consisting of a compound having the structural formula
wherein X is selected from the group consisting of CH2-CH2, Cm, and OCH2; and Y is selected from the group consisting of phenyl, P-methoxy phenyl and O-methoxy phenyl and a pharmaceutically acceptable salt thereof.
The present invention also relates to a method for temporarily reducing intraocular pressure in humans comprising topically administering to the eyes of a human an effective amount of the foregoing composition.
The present invention also relates to a method for temporarily alleviating the symptoms of glaucoma in humans comprising topically administering to the eyes of a human having glaucoma an effective amount of the foregoing composition.
Detailed Description of Invention
Many physiologically and pharmaceutically acceptable salts of the compounds discussed above are known to those skilled in the art and all such salts may be employed in the present invention.
Examples of suitable acids to form salts with Labetalol include fumaric, hydrochloric, nitric, sulfuric and tartaric acids.
The concentration of the active compound which may be used in the present invention ranges from about 0.1 to about 5 percent and preferably from about 0.5 to about 2 percent by weight.
Suitable ophthalmic carriers are known to those skilled in the art and all such conventional carriers may be employed in the present invention. Thus, a particular carrier may take the form of a sterile, ophthalmic ointment, cream, gel, solution, or dispersion. Also including as suitable ophthalmic carriers are slow release polymers, e.g., "Ocusert" polymers, "Hydrogen" polymers, etc. Stabilizers may also be used such as, for example, chelating agents, e.g., EDTA. Antioxidants may also be used, e.g., sodium bisulfite, sodium thiosulfite, 8-hydroxy quinoline or ascorbic acid.Sterility typically will be maintained by conventional ophthalmic preservatives, e.g., chiorbutanol, benzalkonium chloride, cetylpyridium chloride, phenyl mercuric salts, thimerosal, etc., for aqueous formulations, and used in amounts which are non-toxic and which generally vary from about 0.001 to about 0.1% by weight of the aqueous solution. Conventional preservatives for ointments include methyl and propyl parabens.
Typical ointment bases include white petrolatum and mineral oil or liquid petrolatum. However,
preserved aqueous carriers are preferred. Solutions may be manually delivered to the eye in suitable
dosage form, e.g., eye drops, or delivered by suitable microdrop or spray apparatus typically affording a
metered dose of medicament. Examples of suitable ophthalmic carriers include sterile, substantially
isotonic, aqueous solutions containing minor amounts, i.e., less than about 5% by weight
hydroxypropylmethylcellulose, polyvinyl alcohol, carboxymethylcellulose, hydroxyethylcellulose,
glycerin and EDTA. The solutions are preferably maintained at substantially neutral pH and isotonic
with appropriate amounts of conventional buffers, e.g., phosphate, borate, acetate, tris, etc.
A preferred ophthalmic composition is a preserved aqueous solution containing the following
ingredients at the indicated concentration.
Labetalol Wt. percent 1.0
Stabilizer ,, 0.01
Preservative ,, 0.005
Buffer M 0.05
NaCI q.s. ad isotonic.
Water q.s. ad 100 percent.
The amount of the foregoing composition to be used in the therapeutic treatment of glaucoma
will vary with the age of the patient and the severity of the glaucoma. Generally a dose level of one or
two drops of the foregoing aqueous solution 1-4 times daily would be a suitable dosage amount.
Example
The intraocular pressure of six aibino rabbits was measured tonometrically to obtain a baseline. A 1% isotonic, aqueous solution of Labetalol was prepared and 0.05 ml administered to the right eye of
each rabbit. A similar volume of physiologic saline was placed in the left eye. At specified intervals (0,
0.5, 1, 2, 3, 4 and 5 hours after treatment) the intraocular pressure of both eyes of each rabbit was
measured tonometrically. The results are shown in Table I below.
Table I
Intraocular Pressure (mm-Hg)
Rabbit
No. Eye Ohr. 0.5 hr. 1 her. 2 hr. 3hr. 4hr. 5hr.
1 R 24 21 21 19 22 23 24
L 25 24 27 24 24 24 26
2 R 24 17 19 20 21 22 24
L 24 24 25 21 21 25 22
3 R 28 16 18 19 20 21 22
L 27 26 26 24 23 22 23
4 R 26 19 19 21 20 19 23
L 24 22 21 22 20 19 21
5 R 22 18 17 19 24 21 22
L 22 29 22 22 25 21 22
6 R 27 22 23 21 20 21 24
L 26 26 26 23 23 24 24
Mean R 25 19 20 20 21 21 23
L 25 25 25 23 23 23 23
Mean +0.5 -6.0 -5.0 -3.0 -1.5 -1.0 0
diff. (R-L)
Conclusions: Treatment of one eye of each six normal albino rabbits with 0.05 ml of a 1 %
solution of Labetalol resulted in a significant decrease in 1 OP of the treated eye as
compared to the control eye. The peak effect was seen 30 minutes after treatment.
Pressure values returned approximately to pretreatment levels within about five
hours after treatment.
Claims (12)
1. A therapeutic composition for topical ophthalmic use comprising an effective amount of a compound having the structural formula
wherein X is selected from the group consisting of CH2-CH2,CH2and OCH2; and Y is selected from the group consisting of phenyl, P-methoxy phenyl and O-methoxy phenyl and a pharmaceutically acceptable salt thereof and a topically administrable ophthalmic carrier.
2. The composition of Claim 1 wherein the compound is Labetalol.
3. The composition of Claim 2 wherein an effective amount of Labetalol is between about 0.1 and about 5 percent.
4. The composition of Claim 2 wherein an effective amount of Labetalol is between about 0.5 and about 2 percent.
5. A composition comprising the following constituents in approximately the amounts stated:
percent
Labetalol 1.0
Preservative 0.005
NaCI q.s. ad Isotonic
Water q.s. ad 100 percent.
6. A method for temporarily reducing intraocular pressure in humans comprising topically administering to the eye of a human a composition comprising an effective amount of a compound having the structural formula
wherein X is selected from the group consisting of CH2-CH2, Cm, and OCH2; and Y is selected from the group consisting of phenyl, P-methoxy phenyl and O-methoxy phenyl and a pharmaceutically acceptable salt thereof and a suitable ophthalmic carrier.
7. The method of Claim 6 wherein the compound is Labetalol.
8. The method of Claim 7 wherein an effective amount of Labetalol is between about 0.1 and about 5 percent.
9. The method of Claim 7 wherein an effective amount of Labetalol is between about 0.5 and about 2 percent.
10. A method of temporarily alleviating the symptoms of glaucoma in humans comprising administering topically to the eye of a human having glaucoma an effective, therapeutic amount of a compound having the structural formula
wherein X is selected from the group consisting of CH2-CH2, CH2 and OCH2; and Y is selected from the group consisting of phenyl, P-methoxy phenyl and O-methoxy phenyl and a pharmaceutically acceptable salt thereof and a suitable ophthalmic carrier.
11. A composition as claimed in any one of Claims 1 to 5, substantially as hereinbefore described and exemplified.
12. A method as claimed in any one of Claims 6 to 10, substantially as hereinbefore described.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB7844165A GB2033222A (en) | 1978-11-11 | 1978-11-11 | Topical Ophthalmic Composition |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB7844165A GB2033222A (en) | 1978-11-11 | 1978-11-11 | Topical Ophthalmic Composition |
Publications (1)
Publication Number | Publication Date |
---|---|
GB2033222A true GB2033222A (en) | 1980-05-21 |
Family
ID=10500984
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
GB7844165A Withdrawn GB2033222A (en) | 1978-11-11 | 1978-11-11 | Topical Ophthalmic Composition |
Country Status (1)
Country | Link |
---|---|
GB (1) | GB2033222A (en) |
-
1978
- 1978-11-11 GB GB7844165A patent/GB2033222A/en not_active Withdrawn
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
WAP | Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1) |