Drug – bio-affecting and body treating compositions – Designated organic nonactive ingredient containing other... – Solid synthetic organic polymer
Reexamination Certificate
2001-11-08
2003-09-23
Spear, James M. (Department: 1615)
Drug, bio-affecting and body treating compositions
Designated organic nonactive ingredient containing other...
Solid synthetic organic polymer
C514S050000, C514S046000, C514S047000, C514S048000, C514S049000, C514S045000, C514S912000, C424S078040
Reexamination Certificate
active
06624203
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to ophthalmic solutions used to treat eyes, to deliver active pharmaceutical agents to eyes and to treat ophthalmic devices that in use directly contact corneal tissues. Ophthalmic solutions are used to regularly treat and condition eyes and articles and devices that are regularly used in eyes, such as contact lenses. Because of the intimate contact that such solutions have with corneal tissue, several problems or concerns are regularly presented. For instance, for solutions directly in contact with corneal tissue the compatibility of the solution with the tissue, its ability to not damage or irritate, is important. This compatibility issue is also important for solutions used to treat devices that contact corneal tissue, such as contact lenses and the like. Furthermore, prolonged contact with corneal tissue can lead to the accumulation of material on corneal tissue, or on devices in contact with the solution that then leads to adverse reactions.
Preservative efficacy is measured by the amount that a solution decreases the viability of bacterial or fungal populations. In general, there is an expected trade-off between preservative efficacy and corneal tissue compatibility, as well as “comfort.” Furthermore, the field of the invention relates to preservative systems that are broad ranged, and effective against not only bacterial, but also fungal sources of infection.
International Patent Publication No. WO 91/01763 discloses that solutions having very low concentrations of peroxide, i.e., from 0.01 to 0.5 percent more preferably 0.05 to 0.2 percent can provide disinfection without requiring neutralization. Use of the present invention greatly enhances the microbicidal efficacy of peroxide in such low concentrations.
U.S. Pat. No. 4,758,595 (Ogunbiyi, et al.) discloses that polyhexamethylene biguanide (PHMB) and its water-soluble salts can fulfill minimal disinfection and be harmless to the eye and the lens, if used with a specific buffer, a surfactant, and in specific concentrations.
U.S. Pat. No. 5,869,468 teaches methods for treatment of conditions of abnormally increased intraocular pressure, particularly those caused by glaucoma, by administration of phosphonylmethoxyalkyl nucleoside analogs are provided. The compositions formulated and packaged for intraocular administration for use in the methods are also provided. Administration of the compound may be by intravitreal injection, aqueous humor injection, injection into the external layers of the eye, such as subconjunctival injection or subtenon injection, or may be, when penetrating derivatives are used, by topical application to the eye. The degree of reduction in pressure is dosage-dependent, and significant reduction in pressure is obtained. A single injection can produce prolonged, and perhaps permanent, lowering of the intraocular pressure. Typical formulations have between about 0.50 ml and 0.150 ml and comprises a concentration of the compound of about 10 mu g/0.100 ml up to about 100 mu g/0.100 ml
U.S. Pat. No. 5,770,582 relates to compositions comprising 2′-deoxyribonucleosides. The invention also relates to methods of accelerating the healing of wounds, abrasions, cuts, incisions, and superficial burns induced by heat, sunlight, chemical agents, or infections, and methods for ameliorating the effects of aging of the epidermal tissues comprising administering the compositions of the present invention to an animal. More particularly, it has been found that the combination of 2′-deoxyribonucleosides, 2′-deoxycytidine and 2′-deoxyguanosine, produces a substantial increase in the rate of healing of experimental wounds compared to controls and other two-way combinations. The compositions may contain (a) a major amount of 2′-deoxycytidine and an effective amount of 2′-deoxyguanosine, or, (b) a major amount of 2′-deoxyguanosine and an effective amount of 2′-deoxycytidine. Desirably the binary composition contains from 10% to 90% (by mole) 2′-deoxycytidine and 90% to 10% 2′-deoxyguanosine. Preferred compositions contain from 25% to 75% of the two components. This method teaches very concentrated forms of specific nucleosides in topical form, and does not suggest any antimicrobial function.
U.S. Pat. No. 4,136,175 provides that nucleotide derivatives of certain 2,6 substituted purines have been discovered to have anti-viral activity. Novel compounds and their pharmaceutically acceptable salts, pharmaceutical formulations containing the compounds of this invention, and the treatment of viral infections with these formulations are all disclosed. 2,6 Diamino-9-(beta-D arabinofuranosyl)-purine-5′-phosphate is an example of a more active compound of this invention. There is no suggestion that un-modified nucleotides have the same anti-viral properties.
SUMMARY OF THE INVENTION
The present invention relates to ophthalmic solutions that are broad ranged and effective in low concentrations relative to state of the art systems. In particular it has been found that ophthalmic solutions comprising 0.00001 to about 1.0 percent buy weight of a nucleotide, a nucleoside or a purine or pyrimidine base; 0.00001 to about 0.05 percent by weight a cationic, polymeric preservative display an effective preservative capacity, and an increased capacity over state-of-the-art preservative systems.
The invention also relates to articles of manufacture that employ the solution in their operation. For instance, vials employed to store contact lenses for sale may be filled using the solution
DETAILED DESCRIPTION OF THE INVENTION
The present invention relates to ophthalmic solutions that are broad ranged and effective in low concentrations relative to state of the art systems. In particular it has been found that ophthalmic solutions comprising 0.00001 to about 1.0 percent buy weight of a nucleotide, a nucleoside or a purine or pyrimidine base and 0.00001 to about 0.05 percent by weight a cationic, polymeric preservative display an effective preservative capacity, and an increased capacity over state-of-the-art preservative systems.
The purine and pyrimidine bases used in the present invention (e.g. adenine, guanine, uracil, cytosine and thymine) are well known building blocks of nucleic acid chemistry. As are the nucleosides which consist of a purine or pyrimidine base linked to a pentose (e.g. Ribonucleoside—adenosine, guanosine, uridine, cytidine and Deoxyribonucleoside—deoxyadenosine, deoxyguanosine, deoxythymidine, deoxycytidine). The nucleotides, of course, are the phosphate esters of the nucleosides (Ribonucleotide—adenylate (AMP, ADP, ATP), guanylate (GMP, GDP, GTP), uridylate (UMP, UDP, UTP), cytidylate (CMP, CDP, CTP), Deoxyadenylate (dAMP, dADP, dATP), deoxyguanylate (dGMP, dGDP, dGTP), deoxythymidylate (dUMP, dUDP, dUTP), deoxycytidylate (dCMP, dCDP, dCTP). Collectively, these are termed nucleic acid bases.
The cationic polymeric preservative includes polymeric biguanides such as polymeric hexamethylene biguanides (PHMB), and combinations thereof. Such cationic polymeric biguanides, and water-soluble salts thereof, having the following formula:
wherein Z is an organic divalent bridging group which may be the same or different throughout the polymer, n is on average at least 3, preferably on average 5 to 20, and X
1
and X
2
are
One preferred group of water-soluble polymeric biguanides will have number average molecular weights of at least 1,000 and more preferably will have number average molecular weights from 1,000 to 50,000. Suitable water-soluble salts of the free bases include, but are not limited to hydrochloride, borate, acetate, gluconate, sulfonate, tartrate and citrate salts.
The above-disclosed biguanides and methods of preparation are described in the literature. For example, U.S. Pat. No. 3,428,576 describes the preparation of polymeric biguanides from a diamine and salts thereof and a diamine salt of dicyanimide.
Most preferred are the polymeric hexamethylene biguanides, commercially available, for example, as th
Fubara Blessing
Jaeckle Flesichmann & Mugel, LLP
Spear James M.
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