Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
1993-07-16
2001-07-03
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C514S912000
Reexamination Certificate
active
06255299
ABSTRACT:
The present invention relates to an ophthalmic gel composition for human and veterinary use comprising an ophthalmic drug and a vehicle based on a polyanionic polymer.
One of the major problems of topical ophthalmic therapy is to maintain an adequate concentration of the ophthalmic drug at the desired site of action for a prolonged period of time. Thus, only a small volume of preparation can be contained in the fornix inferior and the preparation applied tends to be diluted by the tears and to be drained through the nasolacrimal duct.
It is well known that the duration of action of cationic ophthalmic drugs may be increased by incorporating such drugs into gels based on polyanionic polymers, cf. DE-OS 29 02 863, R. D. Schoenwald et al: Influence of high-viscosity vehicles on miotic effect of pilocarpine, Jour. of Pharm. Sciences, Vol. 67, No. 9, September 1978, 1280-1283, F. Bottari et al: Semisolid ophthalmic vehicles II: Evaluation in albino rabbits of aqueous gel-type vehicles containing lidocaine and benzocaine, Can. J. of Pharm. Sci., vol. 14, No. 2 1979, 39-43, and Engelbert Graf et al: Interaction of Carbopol® 934, with diphenhydramine and dexchlorpheniramine, Acta Pharmaceutica Technologica, 29 (3), 1983, 209-215.
These gel compositions exhibit a duration of action which is about twice that of a conventional ophthalmic drug preparation.
Surprisingly, it has now been found that eye infections can be combatted very effectively with a composition comprising fusidic acid suspended in a gel of the above mentioned type.
The composition of the invention comprises from 0.1 to 4% w/v of fusidic acid suspended in an aqueous vehicle containing from 0.2 to 2% w/v of polyanionic polymer.
The surprising efficiency of the composition of the invention is evidenced by the fact that the duration of action is about 10 times that of a preparation based on fusidic acid and a conventional gelling agent, cf. the example below.
The very substantial prolongment of the action of fusidic acid is particularly surprising, since hitherto it was believed that the prolonged action of the prior art compositions is based on an interaction of a positively charged drug with the negatively charged polymer. Thus, it might be expected that a drug, such as fusidic acid, which is negatively charged at the pH value of the eye, i.e. about 7.4, would be unable to interact with the polyanionic polymer and to provide a prolonged action.
The composition of the invention is particularly useful for the local treatment of eye infections. Thus, whereas conventional ophthalmic preparations, such as chloroamphenicol eye drops, have to be applied 5-6 times daily or even more, it is sufficient to apply preparations based on the composition of the invention 1-2 times daily.
The composition of the invention preferably contains about 1% w/v of fusidic acid in the form of particles having a particle size not exceeding 10 &mgr;m and preferably between 2 and 5 &mgr;m.
A polyanionic polymer is preferably a carboxyvinyl polymer having a molecular weight of from about 400.000 to about 6 million. The viscous solutions which are formed during the preparation of the ophthalmic polymer suspension have a viscosity of from 10 to about 20.000 cps at 25° C. measured on a RVT Brookfield Viscosimeter.
The polyanionic polymer is preferably of the type which is commercially available under the trade name “Carbopol” (B.F. Goodrich Company). A particularly preferred polyanionic polymer is “Carbopol 934”. The “Carbopol” polymers do not blur the normal vision because the gel structure breaks down shortly after application to the eye under the influence of ions contained in the lacrimal fluid.
The pH value of the composition of the invention is preferably from 5.0 to 6.5 and more preferably about 5.8.
The adjustment of the pH value is preferably effected with a pharmaceutically and physiologically acceptable base, such as sodium hydroxide.
A preparation based on the composition of the invention may contain auxiliary agents, such as preservatives, stabilizing agents and bacteriostatic agents.
Preparations based on the composition of the invention are preferably used in dosages of from 5 to 100 mg and more preferably from 20 to 50 mg when the preparation is applied into the fornix inferior of an infected eye.
The frequency of dosing varies dependant upon the severity of the infection. However, as mentioned above an application twice a day ordinarily suffices.
The invention also relates to a method of treating eye infections, said method comprising applying an effective amount of a preparation based on the composition of the invention into the fornix inferior of the infected eye.
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Chem. Abst. 104: 199554(c) (1986)-Hansen*
Hansen, S. “Intraocular penetration of fusidic acid with topical Fucithalmic ®,” European Journal of Drug Metabolism and Pharmaco-kinetics, 1985, vol. 10, No. 4, pp. 329-31.*
Medline abstract AN 86164451 of Hansen.*
Remington's Pharmaceutical Sciences, 1975, pp. 1537-38.
Rote Liste 1977/78.
Chadwick et al,Brit. J. Ophthal.,53(1):26-29 (1968).
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Graf et al,Acta Pharm. Tech.,29(3):209-15 (1983).
Saettone et al,Comm. J. Pharm. Pharmacol.,32:519-521 (1980).
Bottari et al,Can. J. Pharm. Sci.,14(2):39-43 (1979).
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Baun et al,Pharm. Acta Helv.,46:94-113 (1971).
International Publication No. WO84/04080 (Dec. 6, 1984).
International Publication No. WO84/04681 (Dec. 6, 1984).
Remington's Pharmaceutical Sciences, 1975, pp. 1537-38.
Rote Liste 1977/78.
Chadwick et al, Brit. J. Ophtal., 53(1):26-29 (1968).
Schoenwald et al, J. Phar. Sc., 67(9):1280-83 (19778).
Graf et al, Acta Pharm. Tech., 29(3):209-15 (1983).
Saettone et al, Comm. J. Pharm. Pharmacol., 32:519-521 (1980).
Chemical Abstract 104:199554(c) (1986) (Hansan).
Bottari et al, Can. J. Pharm. Sci., 14(2):39-43 (1979).
ABD-Elbary et al, Pharmazie, 36:356-358 (1981).
Baun et al, Pharm. Acta Helv., 46:94-113 (1971).
International Publication No. WO 84/04080 (Dec. 6, 1984).
International Publication No. WO 84/04681 (Dec. 6, 1984).
Fay Zohreh
Leo Pharmaceutical Products Ltd.
Pillsbury & Winthrop LLP
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