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|||||I||||IIII US00536466A United States Patent 19 11 Patent Number: 5,364,616 Singer Et Al |||||I||||IIII US00536466A United States Patent 19 11 Patent Number: 5,364,616 Singer et al. (45) Date of Patent: Nov. 15, 1994 (54) USE OF H-2 ANTAGONSTS FOR 89/04178 5/1989 WIPO .......................... A61K 45/06 TREATMENT OF GNGVTS OTHER PUBLICATIONS 75 Inventors: Robert E. Singer, Fairfield; James P. Ash, A. S. F. & H. O. Schild, "Receptors Mediating Ebel, Cincinnati, both of Ohio Some Actions of Histamine', Brit. J. Pharmacol. 73 Assignee: The Procter & Gamble Company, Chemother, vol. 27 (1966), pp. 427-439. Cincinnati, Ohio Black, J. W., W. A. M. Duncan, C. J. Durant, C. R. Ganellin & E. M. Parsons, "Definition and Antagonism 21) Appl. No.: 171,494 of Histamine H2-Receptors', Nature, vol. 236 (Apr. 21, 22 Filed: Dec. 22, 1993 1972), pp. 385-390. Dews, P. B. & J. D. P. Graham, "The Antihistamine Related U.S. Application Data Substance 2786 R.P.', Brit. J. Pharmacol, vol. 1 (1946), p. 278. 60 Division of Ser. No. 19,782, Mar. 5, 1993, Pat. No. Loew, E. R. & O. Chickering, "Gastric Secretion in 5,294,433, which is a continuation-in-part of Ser. No. Dogs Treated with Histamine Antagonist, Thymoxye 868,805, Apr. 15, 1992, abandoned. thyldiethylamine', Proc. Soc. Exp. Biol. and Med., vol. (51) Int. Cl. ......................... A61K 7/16; A61K 7/18; 48 (1941), pp. 65-68. A61K 7/22 Lantz, Michael D. and T. J. Wozniak, "Stability of (52) U.S.C. ........................................ 424/52; 424/49; Nizatidine in Extemporaneous Oral Liquid Prepara 424/54; 514/399; 514/406; 514/900; 514/902 tions', American Journal of Hospital Pharmacy, vol. 47 (58. Field of Search .................................... 424/49-58; (Dec. 1990), pp. 2716–2719. 514/900-902 Nakamoto, T., M. McCroskey & H. M. Mallek, “The Role of Ascorbic Acid Deficiency in Human Gin (56) References Cited givitis-A New Hypothesis', J. Theor. Biol, vol. 108 U.S. PATENT DOCUMENTS (1984), pp. 163-171. 3,574,859 4/1971 Kosti ................................... 424/330 Pernsteiner, C. L. & M. M. Ash, “Effect of Topical 3,822,349 7/1974 Kosti.... ... 424/54 Application of Phenylephrine Hydrochloride on Hy 3,832,460 8/1974 Kosti.... ... 424/54 perplastic Gingivitis', J. Periodontol, vol. 48 (1977), pp. 3,839,522 10/1974 Kosti..................................... 424/54 473–477. 3,950,333 4/1976. Durant et al. .. 260/250 A Trendelenburg, U., “The Action of Histamine and 4,128,658 12/1978 Price et al. .......................... 424/285 5-Hydroxytryptamine on Isolated Mammalian Atria', 4,256,743 3/1981 Goldhaber ...... ... 424/247 J. Pharmacol. & Exp. Ther, vol. 130 (1960), pp. 450-460. 4,283,408 8/1981 Hirata et al. ........................ 424/270 4,293,557 10/1981 Shibata et al. ...................... 424/267 Primary Examiner-Shep K. Rose 4,375,547 3/1983 Pioch ................................... 548/205 Attorney, Agent, or Firm-J. R. Crosmun; M. B. Graff; 4,386,099 5/1983 Cereda et al. ... 424/273 R D. L. Suter 4,569,837 2/1986 Suzuki et al. ......................... 424/28 4,585,790 4/1986 Padfield et al. ..................... 514/471 57) ABSTRACT 4,933,182 6/1990 Higashi et al....................... 424/435 The subject invention relates to methods for prevention FOREIGN PATENT DOCUMENTS or treatment of gingivitis or periodontitis comprising topical administration, to gingival tissues of the oral 95.0833 7/1974 Canada . 0241179 10/1987 European Pat. Off. ....... A61K9/70 cavity, of a composition comprising a safe and effective 0256566 2/1988 European Pat. Off........ A61K 7/26 amount of a selective histamine-2 receptor antagonist 0349657 1/1990 European Pat. Off...... A6K 3/55 compound, and oral care compositions used therefore. 4-89428 3/1992 Japan ........................... A61K 31/13 1045031 10/1966 United Kingdom .......... A61K 7/16 27 Claims, No Drawings 5,364,616 1. 2 Pharmaceutical Company, published Oct. 14, 1987; USE OFH-2 ANTAGONSTS FORTREATMENT OF European Patent Application No. 0,256,566 of ISCO GNGVTS FAR, published Feb. 24, 1988; European Patent Appli cation No. 0,349,657 of Thornfeldt & Thornfeldt, pub This is a division of application Ser. No. 08/019,782, lished Jan. 10, 1990; British Patent Specification No. filed on Mar. 5, 1993, now U.S. Pat. No. 5,294,433, 1,045,031 of Kawakami, published Oct. 5, 1966; Cana which is a continuation-in-part of application Ser. No. dian Patent No. 950,833 of Kosti, issued Jul. 9, 1974; 07/868,805, filed on Apr. 15, 1992, now abandoned. Nakamoto, T., M. McCroskey & H. M. Malek, “The TECHNICAL FIELD Role of Ascorbic Acid Deficiency in Human Gin 10 givitis-A New Hypothesis', J. Theor. Biol, Vol. 108 The subject invention relates to methods and compo (1984), pp. 163-171; and Pernsteiner, C. L. & M. M. sitions for the prevention and treatment of gingivitis and Ash, "Effect of Topical Application of Phenylephrine soft tissue aspects of periodontitis. Hydrochloride on Hyperplastic Gingivitis”, J. Peri BACKGROUND OF THE INVENTION odontol, Vol. 48 (1977), pp. 473–477. 15 H-2 antagonists have not generally been found useful 'Gingivitis', as used herein, means inflammation of for treatment of inflammatory conditions. Instead, they the gingiva (gums); it is often due to infection. Gingivi are extensively used as drugs for preventing release of tis is usually caused by the build-up of plaque, a sticky acid in the stomach to promote the healing of peptic deposit of bacteria, mucous, food particles and other ulcers and to relieve symptoms of esophagitis. Exam irritants, around the base of the teeth. It is believed that ples of well-known H-2 antagonist drugs include cimeti toxins produced by bacteria within the plaque irritate dine, ranitidine and famotidine. the gums, causing the gums to become infected, tender, PCT Patent Application No. WO 89/04178 of Ak and swollen. Gingivitis can also result from injury to tiebolaget Hassle, published May 18, 1989, discloses the the gums, usually from over vigorous tooth brushing or use of H-2 antagonists for treatment of bone diseases, careless flossing. 25 including the bone loss resulting from periodontal dis Periodontitis', as used herein, means inflammation of ease. The disclosed utility is achieved through systemic the periodontium (the tissues that support the teeth). dosing of the H-2 antagonists. It is an object of the Chronic periodontitis is a complication of untreated subject invention to provide a topical, oral treatment for gingivitis. If gingivitis is neglected, inflamed gum tissue gingivitis and soft tissue aspects of periodontitis. at the base of the teeth becomes damaged and pockets 30 form between the gums and the teeth. Plaque then col SUMMARY OF THE INVENTION lects in these pockets. The bacteria in the plaque attack The subject invention relates to methods for preven the periodontal tissues, causing them to become in tion or treatment of gingivitis or periodontitis compris flamed and detached from the teeth. In advanced stages, ing topical administration, to gingival tissues of the oral the bacteria eventually erode the bones surrounding the 35 cavity, of a composition comprising a safe and effective teeth. However, as used herein, periodontitis is limited amount of a selective histamine-2 receptor antagonist to the soft tissue (non-bone) aspects of the disease. compound. Histamine is a chemical present in cells throughout the body that is released during an allergic reaction and DETALED DESCRIPTION OF THE in instances of chronic inflammation. Histamine is one W INVENTION of the substances responsible for the symptoms of in The subject invention involves a novel use of hista flammation. It also stimulates production of acid by the mine-2 (H-2 or H2) receptor antagonist compounds stomach and narrows the bronchi (airways) in the lungs. (H-2 antagonists). As used herein, selective H-2 antago The effects of histamine can be counteracted by anti nists are compounds which block H-2 receptors, but do histaminic drugs, of which there are two well-known 45 not have meaningful activity in blocking histamine-1 classes: histamine-1 receptor antagonists (H-1 antago (H-1 or H1) receptors. nists) and histamine-2 receptor antagonists (H-2 antago nists). H-1 antagonists drugs are commonly used for Selective H-2 Antagonists treatment of a number of inflammatory conditions in Histamine stimulates the contraction of smooth mus cluding hives and other rashes to relieve itching, swell 50 cle from various organs, such as the gut and bronchi, ing and redness, allergic rhinitis to relieve sneezing and and this effect can be suppressed by low concentrations runny nose, colds to dry up nasal secretions, and cough. of mepyramine-a typical antihistaminic drug. The Common H-1 antagonist drugs include chlorphenira pharmacological receptors involved in these mepyra mine, diphenhydramine, promethazine, terphenadine, mine-sensitive histamine responses have been defined as trimeprazine and triprolidine. 55 H-1 receptors (Ash, A. S. F. & H. O. Schild, Brit. J. References which disclose the use of various H-1 Pharmacol Chemother, Vol. 27 (1966), p. 427, incorpo antagonists in oral care products or for treatment of rated herein by reference). Histamine also stimulates the various oral conditions are disclosed in the following secretion of acid by the stomach (Loew, E. R. & O. references: U.S. Pat. No. 3,574,859 issued to Kosti on Chickering, Proc. Soc. Exp. Biol. Med., Vol. 48 (1941), p. Apr. 13, 1971; U.S. Pat. No. 3,822,349 issued to Kostion 60 65, incorporated herein by reference), increases the Jul. 2, 1974; U.S. Pat. No. 3,832,460 issued to Kosti on head rate (Trendelenburg, U., J. Pharmacol, Vol. 130 Aug. 27, 1974; U.S. Pat. No. 3,839,522 issued to Kosti (1960), p. 450, incorporated herein by reference), and on Oct. 1, 1974; U.S. Pat. No. 4,256,743 issued to Gold inhibits contractions in the ratuterus (Dews, P.
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