Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1998-06-11
2001-09-11
Travers, Russell (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C424S195110, C424S440000, C426S646000
Reexamination Certificate
active
06288087
ABSTRACT:
This invention is directed to Compositions for use in the control of smoking, and methods which control or reduce the desire to smoke.
Cigarette smoking is recognized world wide as a health risk. Compared to non-smokers, there is a clear increase in morbidity and mortality across all age groups of cigarette smokers. Apart from well described negative effects upon asthma (J. Wakefield, (1988)
Personality and Individual Differences
, 9(2)465-477), clinical contact with smokers provides anecdotal data supporting the notion that smoking is associated with breathlessness, fatigue, or reduced fitness. These deleterious health effects of cigarette smoking have been widely publicized. It is reported that many smokers are convinced that smoking is indeed a health hazard (S. M. Glynn and S. Sussman, (1990)
Hospital and Community Psychiatry
41(9)1027-1028). Despite this conviction, approximately one adult in three continues to smoke (Australian Institute of Health and Welfare, (1992)
The Third Biennial report of the AIHW
, AGPS, Canberra).
Various proposals have been put forward for the control of smoking and for the treatment of withdrawal symptoms associated therewith. One proposal is the use of transdermal (or gum-delivered) nicotine as an anti-smoking therapy. This approach is based on the view that nicotine addiction is the primary chemical reason for smoking (see, for example, Australian Patent No 607214). Outcome studies have cast doubt upon the assumption that nicotine is the reason for smoking. Even when using a concomitant programme to treat the behavioural, aspects of the smoking habit, the success of nicotine-based interventions are little better than placebo or psychological therapy alone (Buchkremer et al, (1991)
Pharmacopsychiatry
24(3):96-102).
Hypnotism, acupuncture and other “natural therapies” have also been used for the control of smoking, again with little success.
There is accordingly a need for alternative treatments for the control of smoking.
In accordance with one aspect of this invention, there is provided a composition for the control of smoking, said composition comprising:
(a) a xanthine oxidase inhibitor;
(b) a cytochrome P450 inducing compound;
(c) a sugar;
(d) a source of phosphate; and, optionally,
(e) one or more pharmaceutically acceptable carriers or excipients.
In accordance with another aspect of this invention, there is provided a method for the control of the desire to smoke, which comprises administering to a subject in need of such treatment a composition which comprises:
(a) a xanthine oxidase inhibitor;
(b) a cytochrome P450 inducing compound;
(c) a sugar;
(d) a source of phosphate; and, optionally,
(e) one or more pharmaceutically acceptable carriers or excipients.
In another aspect this invention relates to the use of a composition comprising:
(a) a xanthine oxidase inhibitor;
(b) a cytochrome P450 inducing compound;
(c) a sugar;
(d) a source of phosphate; and optionally,
(e) one or more pharmaceutically acceptable carriers or excipients. in the manufacture of a medicament for the control of smoking.
In a still further aspect of this invention there is provided agents for the control of smoking, which agent comprises:
(a) a xanthine oxidase inhibitor;
(b) a cytochrome P450 inducing compound;
(c) a sugar;
(d) a source of phosphate; and optionally,
(e) one or more pharmaceutically acceptable carriers or excipients.
The compositions according to this invention have surprisingly been found to control smoking. Reference to the control of smoking includes suppression of the desire or need to smoke, This may in turn result in a substantial reduction in the number of cigarettes smoked by an individual, or may result in a cessation of smoking. The applicants do not wish to place any limitations on the mechanism of action of the compositions of the invention. Clinical results, as described herein, demonstrate that the compositions of the invention suppress the desire or need to smoke.
As mentioned above, the compositions according to this invention comprise:
(a) a xanthine oxidase inhibitor;
(b) a cytochrome P450 inducing compound;
(c) a source of phosphate;
(d) a sugar; and, optionally,
(e) one or more pharmaceutically acceptable carriers or excipients.
The term “xanthine oxidase” as used herein will be understood to include xanthine dehydrogenase and xanthine oxidoreductase.
Xanthine oxidase inhibitors are well known in the art. The inhibitors block xanthine oxidase activity by a variety of mechanisms which include competitive inhibition (where the compounds act as antagonist), binding to xanthine oxidase at or near the active site thereby blocking enzymatic activity, altering the conformation of the xanthine oxidase by binding to xanthine oxidase generally outside of The active site, binding or otherwise inactivating free radical agents produced by xanthine oxidase, or other mechanisms.
A first group of xanthine oxidase inhibitors are the flavonoids which may otherwise be referred to a bioflavonoids (see, for example, Harborne et al, (Eds),
The Flavonoids
, Academic Press, New York, 1975; Harborne et al,
The Flavonoids, Advances in Research Since
1986, 1994; Princemail et al, (1987), ‘Ginkgo Biloba extract inhibits oxygen species production generated by phorbol myristate acetate stimulated human leukocytes’,
Experientia
, Feb 15 43(2), 181-184; Frage et al, (1987), ‘Flavonoids as antioxidants evaluated in vitro and in situ liver chemiluminescence’,
Biochem. Pharmacol
., Mar 1 36(5):717-720; Schmeda-Hirschmann et al (1987). ‘Preliminary pharmacological studies on
Eugenia uniflora
leaves: xanthine oxidase activity’
J. Ethnopharmacol
., Nov 21(2) 183-186; Zeng L. H. and Wu T. W., (1992), ‘Purpurogallin is a more powerful protector of kidney cells than Trolux and allopurinol’,
Biochemistry and Cell Biology,
70:604-709; Siggins F. M., (1888), ‘Analysis of the leaves of
Eupatorium purpurem’, Am. J. of Pharm
., 60:121-122; Manger C. C., (1894), ‘Euparin’,
Am. J. of Pharm
., 66:120-124; Trimble H., (1890) ‘
Eupatorium purpurem’, Am. J. of Pharm
., Feb 62:73-80).
The flavonoids are a large group of secondary plant metabolites derived from flavan. The basic structure of the flavanoids is flavanone (flavan-4-one) from which the flavonoid derivatives flavonol (flavan-3-ol), flavone and flavonol are derived. The anthocyanins and catechols are derived from flavan and are to be regarded for the purposes of this invention as flavonoids (see
Concise Encyclopedia of Chemistry
, de Gruyter, 1994, particularly pages 77, 190 and 411 to 413). Examples of anthocyanins include cyanin, pelargonin, delphin, idaein, malvin, petunin keracyanin, micocyanin, frasarin, paeonin, oenin, and chyrsanthemin, and the like. These compounds may be hydrolyzed by acids and glycosidases to the corresponding aglycons (anthocyanins). Sugar residues may be bound 3- or 5-positions of the anthocyanins, Catechol tannins are a group of tannin in which the monomeric units are flavan-3-ol (catechols) or flavan-3,4-diol. Catechol is a 5,7,3′,4′-tetrahydroxyflavan-3-ol. The above compounds are to be regarded as flavonoids for the purposes of this invention.
The most widely occurring flavanoids are the flavones. Flavones are yellow pigments of the flavonoid group which comprise the flavone, isoflavone or flavanone skeleton. Flavones occur widely in nature, for example, in blossoms, woods and roots, usually as glycosides or esters of tannic acid and can be readily extracted from these natural sources, using long established techniques well known in the art such as those described in
The Flavonoids, Advances in Research Since
1986, Harborne et al , 1994. Examples of flavones include apigenin, chrysin, eupatorin, fisetin, genistein, hesperitin, kaempherol, luteolin, morin, myricetin and quercetin. Flavonoid compounds and other xanthine oxidase inhibitor within the scope of this invention may be extracted from a wide variety of plant species including
Eupatorium purpurem
(otherwise known as Gravel Root, Queen of the Meadow, or Jo Pye Weed),
Eupatorium cannibium
(otherw
Dann Dorfman Herrell & Skillman
Travers Russell
Wang Shengjun
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