Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1998-12-22
2000-04-18
O'Sullivan, Peter
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
424 7804, 514912, 564291, 564292, 528397, A61K 3114
Patent
active
060516119
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
The present invention relates generally to a class of antimicrobials useful in pharmaceutical and cosmetic products. In particular, the present invention relates to polymeric quaternary ammonium compounds which are useful as disinfectants and preservatives for ophthalmic, pharmaceutical and contact lens care products.
Polymeric quaternary ammonium compounds as a class have been known for many years. British Patent No. 536,017 (Aug. 30, 1941), assigned to E. I. DuPont de Nemours (the "DuPont Patent"), discloses linear polymeric quaternary ammonium compounds and methods for their preparation. The method of the DuPont Patent may be generically described as a condensation reaction between a lower alkyl dihalide and a difunctional ditertiary amine. Contemplated uses for the compounds of the DuPont Patent include their use in photographic precessing, to treat leather, as mold inhibitors and pesticides, and as modifying agents. There is no mention of use of these compounds as disinfectants or preservatives in pharmaceutical products.
U.S. Pat. Nos. 3,931,319 (Jan. 6, 1976), 4,001,432 (Jan. 4, 1977) and 4,012,446 (Mar. 15, 1977), all issued to Green, et al., disclose a group of high molecular weight "capped" linear polymeric quaternary ammonium compounds found to be effective microbiocides (antimicrobials). The Green, et al. compounds are "capped" in the sense that both ends of the chains terminate in quaternary ammonium moieties. In a continuation-in-part application, now U.S. Pat. No. 4,027,020 (May 31, 1977), Green, et al. disclose a process for making randomly capped linear polymeric quaternary ammonium compounds; that is, the polymers produced by the improved process include those with very short chain lengths as well as those having relatively long chain lengths. These compounds were also found to have antimicrobial activity.
U.S. Pat. Nos. 4,407,791 (Oct. 4, 1983) and 4,525,346 (Jun. 25, 1985), both issued to Stark, disclose improved disinfecting solutions for contact lenses, wherein the aqueous solutions contain the Green, et al. polymers including the commercially known Onamer M.RTM.. In addition, U.S. Pat. No. 5,037,647 (Aug. 6, 1991), issued to Chowhan et al., disclose aqueous antimicrobials ophthamic solutions containing Onamer M.RTM. in combination with an anionic complexing agent to prevent or to reduce binding of the polymer to contact lenses.
SUMMARY OF THE INVENTION
For purposes of this specification, disinfectants and/or preservatives shall be collectively referred to as "antimicrobials" and compounds having disinfecting and/or preserving efficacy shall be referred to as compounds having "antimicrobial activity." In addition, the terms "polymeric quaternary ammonium compounds" or "polymers" shall hereinafter refer to polymeric quaternary ammonium compounds and their pharmaceutically acceptable salts, and the terms shall be used interchangeably throughout this specification.
It has now been found that certain polymeric quaternary ammonium compounds, of generic relationship to those disclosed in the DuPont Pat. and the Green, et al. patents, are particularly suitable for use in ophthalmic compositions as antimicrobials. However, the polymers of the present invention are unique in at least two respects: 1) it has been discovered that optimum performance for the indicated utility is achieved only for a narrow range of molecular size, i.e., length of the polymer, and 2) the polymers of the present invention are characterized by a terminal end group R, which is --N(CH.sub.3).sub.2. While applicants are bound by no theory, it appears that the polymer length and end capping function of the polymers of the present invention limit cornmeal toxicity, absorption and adsorption to contact lenses and maximize biocidal activity under the product designs and uses disclosed herein.
The ophthalmic compositions of the present invention comprise the polymers of the present invention. These compositions include: contact lens care products, such as chemical disinfecting and storage solu
REFERENCES:
patent: 3874870 (1975-04-01), Green et al.
patent: 3931319 (1976-01-01), Green et al.
patent: 4001432 (1977-01-01), Green et al.
patent: 4012446 (1977-03-01), Green et al.
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patent: 4027020 (1977-05-01), Green et al.
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patent: 4407791 (1983-10-01), Stark
patent: 4444750 (1984-04-01), Green et al.
patent: 4525346 (1985-06-01), Stark
patent: 5037647 (1991-08-01), Chowhan
patent: 5512597 (1996-04-01), Kyba et al.
Kyba Evan P.
Park Joonsup
Alcon Laboratories Inc.
O'Sullivan Peter
Yeager Sally
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