Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Reexamination Certificate
2001-04-25
2004-02-03
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
C424S422000, C514S212010, C514S213010, C514S218000, C514S219000, C514S029000, C514S912000, C514S954000, C514S964000, C514S187000
Reexamination Certificate
active
06685958
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid compounds in a vehicle that permits administration in drop form. The invention also relates to quinolone carboxylic acid compositions and methods of preparing the same.
BACKGROUND OF THE INVENTION
Treatment of ocular and periocular infections can be effected by the application of ointments or the instillation of topical antibiotic suspensions to the eye. Such compositions can employ, for example, one or more of the following antibiotic agents: neomycin, polymixin B, bacitracin, trimethoprim, tobramycin, terramycin, sulfacetamide (e.g., CORTICOSPORIN™, Monarch Pharmaceuticals, Bristol, Tenn.; NEODECADRON™, Merck & Co., West Point, Pa.; POLYSPORIN™, Glaxo Wellcome Inc., Research Triangle Park, N.C.; POLYTRIM™ AND BLEPHAMIDE™, Allergan Inc., Irvine, Calif.; TOBRADEX™, Alcon Laboratories, Fortworth, Tex.; TERA-COTRIL™, Pfizer Inc., New York, N.Y. etc.). Compositions such as: CHIBOXIN™ (Merck and Co., West Point, Pa.), CILOXAN™ (Alcon Laboratories, Fortworth, Tex.) and OCUFLOX™ (Allergan Inc., Irvine, Calif.) employ quinolone antimicrobials in aqueous solution or aqueous suspension.
As in the topical administration of other medicaments to the eye, the delivery of antimicrobial agents is influenced by a variety of factors, among them comfort, consistency and accuracy of dosage, type and time of any vision interference, ease of administration, and timing of delivery. These factors have been discussed, for example, in Davis et al., U.S. Pat. No. 5,192,536.
While the art has produced a variety of compositions for the treatment of ocular and periocular infections, there is still a need for broad-spectrum antimicrobial compositions with the characteristics of high bioavailabity and adsorption. Such compositions would be even more desirable provided they comprise a vehicle that readily permits accurate administration of dosages in a convenient form such as drops. It is also desirable that the composition be non-irritating and soothing to already irritated ocular and periocular tissues. The aforementioned compositions are even more desirable when they also provide sustained release of the antimicrobial compositions and are not subject to rapid dilution or rapid removal of the antibiotics by lacrimation.
There is a need in the art for topically applied anti-microbial agents and compositions useful in their administration.
SUMMARY OF THE INVENTION
The present invention includes and provides a topical ophthalmic composition comprising a quinolone carboxylic acid derivative of formula (I),
wherein R
1
is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in vivo, R
2
is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom, Y is CH
2
, O, S, SO, SO
2
, or N—R
3
, wherein R
3
is a hydrogen atom or a lower alkyl group, and Z is an oxygen atom or two hydrogen atoms.
The present invention includes and provides a method of treating or preventing an infection in the ocular or periocular region comprising: delivering to the ocular or periocular region a composition comprising a quinolone carboxylic acid derivative of formula (I),
wherein R
1
is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in vivo, R
2
is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom, Y is CH
2
, O, S, SO, SO
2
, or N—R
3
, wherein R
3
is a hydrogen atom or a lower alkyl group, and Z is an oxygen atom or two hydrogen atoms.
The present invention includes and provides a method of preparing a sustained release topical ophthalmic delivery system, comprising: preparing an composition comprising a quinolone carboxylic acid derivative of formula (I),
wherein R
1
is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in vivo, R
2
is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom, Y is CH
2
, O, S, SO, SO
2
, or N—R
3
, wherein R
3
is a hydrogen atom or a lower alkyl group, and Z is an oxygen atom or two hydrogen atoms; and, packaging said composition for administration to the eye.
REFERENCES:
patent: 3868445 (1975-02-01), Ryde et al.
patent: 4551456 (1985-11-01), Katz
patent: 4615697 (1986-10-01), Robinson
patent: 4692454 (1987-09-01), Mich et al.
patent: 4851415 (1989-07-01), Mich et al.
patent: 5124154 (1992-06-01), Babcock et al.
patent: 5188826 (1993-02-01), Chandrasekaran et al.
patent: 5192535 (1993-03-01), Davis et al.
patent: 5209926 (1993-05-01), Babcock et al.
patent: 5252319 (1993-10-01), Babcock et al.
patent: 5256408 (1993-10-01), Babcock et al.
patent: 5332582 (1994-07-01), Babcock et al.
patent: 5340572 (1994-08-01), Patel et al.
patent: 5385900 (1995-01-01), Konno et al.
patent: 5430028 (1995-07-01), Kaihoh et al.
patent: 5447926 (1995-09-01), Konno et al.
patent: 5474764 (1995-12-01), Patel et al.
patent: 5538721 (1996-07-01), Babcock et al.
patent: 5767153 (1998-06-01), Bowman et al.
patent: 5814655 (1998-09-01), Patel et al.
patent: 5977171 (1999-11-01), Bowman et al.
patent: 6159458 (2000-12-01), Bowman et al.
patent: 6239113 (2001-05-01), Dawson et al.
patent: 6265444 (2001-07-01), Bowman et al.
patent: 6309630 (2001-10-01), Patel et al.
patent: 6378526 (2002-04-01), Bowman et al.
patent: 6397849 (2002-06-01), Bowman et al.
patent: 0 142 426 (1985-05-01), None
Davies. Biopharmaceutical considerations in topical ocular drug delivery. Clinical and Experimental Pharmacology & Physiolog (2000), 27, 558-562. 2000.*
Ralf Stahimann and Hermut Lode,Safety Overview, Ocular Toxicity, inThe Quinolones, 3rdEdition, pp. 407-408 (Vincent T. Andriole ed., 2000) Academic Press, San Diego.
Asaoka Takemitsu
Bowman Lyle M.
Chandrasekaran Santosh Kumar
Imamori Katsumi
Roy Samir
Arnold & Porter
Channavajjala Lakshmi
InSite Vision Incorporated
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