Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-03-15
1998-08-18
Fay, Zohreh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514912, A61K 3135
Patent
active
057959137
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
The present invention relates to an ophthalmic composition in the form of a topical aqueous solution for human and veterinary use, as well as the use of the solution, especially for the treatment of glaucoma and ocular hypertension.
It is well known to use polymers alone or in combination with other polymers for the preparation of ophthalmic pharmaceuticals and artificial tear compositions. The inclusion of the polymer aims at increasing the viscosity of the composition so as to provide for a longer contact time with the cornea of the eye, and, for example, in connection with ophthalmic drugs, to provide for a sustained release of the drug into the eye.
For example, the U.S. Pat. Nos. 5,075,104 and 5,209,927 relate to an ophthalmic gel composition and an ophthalmic liquid composition, respectively. The first mentioned composition includes 0.25 to 8% by weight of a carboxy vinyl polymer (polymer of carbomer type), the latter 0.05 to 0.25% by weight, resulting in viscosities of the compositions ranging from 15000 to 300000, or 10 to 20000, respectively.
In the publication WO 93/17664 high viscosity, polymer containing ophthalmic compositions are disclosed containing, in combination, carboxy vinyl polymers of the carbomer type, and cellulosic polymers. According to this disclosure lower polymer concentrations can be used while still achieving the desired higher viscosity. A wide range for the concentration of polymers is given, the broadest range indicated being 0.05 to 3% by weight of carbomer, and 0.05 to 5.0% by weight of cellulose polymer. A similar two-polymer system is described in the WO-publication WO 91/19481, the system being such which gels when exposed to the pH and temperature conditions of the eye surface. In the said publication, an inclusion of up to 0.9% of salt is contemplated for the adjustment of the viscosity.
There is also a number of publications relating to pharmaceutically active ophthalmic compositions containing various polymers, i.a. carboxy vinyl polymers, at various concentrations. As tonicity regulating agents, usually non-ionic polyols are suggested so as not to interfere with the gel structure (WO 93/00887, WO 90/13284). In the publication Int. J. Pharm. 81 (1992) 59-65, aqueous compositions containing timolol maleate and 0.6% polyacrylic acid (MW 250,000), as well as the salt of timolol base with 0.6% polyacrylic acid are described, containing mannitol as tonicity regulator. The viscosity measured at low shear rates is indicated as being 45 centipoise.
In the DE-patent specification 28 39 752 ophthalmic gel compositions are described containing carboxy vinyl polymers in an amount of 0.05 to 5.0% by weight and exhibiting viscosities of 1000 to 100,000 centipoise. According to this disclosure, a small amount of sodium chloride from 0.001 to 0.5% by weight is added in order to prevent the gel from breaking down on the surface of the eye (see column 4, lines 41 ff).
SUMMARY OF THE INVENTION
The present invention is based on the discovery that the beneficial effect of ophthalmic compositions of the above type containing viscosity enhancing agents, is due to the concentration of the polymer present in the composition, rather than on the viscosity thereof. Thus one object of the invention is to provide an ophthalmic composition with a sufficiently high concentration of polymer to control the formation of the polymer film on the cornea of the eye, but which composition is still fluid enough for ocular topical application. A further object of the invention is to provide an easy-to-use eye drop formulation with improved patient compliance.
According to the invention it has now been shown that by raising the concentration of the polymer over a value where the composition normally is a gel rather than a liquid and by simultaneously lowering the viscosity thereof, it is possible to obtain a desired beneficial effect of the active agent in the eye, while simultaneously reducing any discomfort in the patient's eye, as compared to the administration of a compo
REFERENCES:
Florence Thermes et al., "Bioadhesion: The Effect of Polyacrylic Acid on the Ocular Bioavailability of Timolol", 1992, vol. 81, pp. 54-65, International Journal of Pharmaceutica.
Alaranta Sakari
Lehmussaari Kari
Oksala Olli
Pohjala Esko
Reunamaki Timo
Fay Zohreh
Santen Oy
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