Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-10-30
1997-07-01
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514813, A61K 3155
Patent
active
056439059
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP94/00055 filed Jan. 10, 1994.
DESCRIPTION
The present invention relates to pharmaceutical formulations for the treatment of nicotine dependence.
The present invention is particularly directed to pharmaceutical formulations and devices by which galanthamine or one of its pharmaceutically acceptable acid addition salts is released in a controlled, for instance continuous manner to treat nicotine dependence.
The dependence on nicotine complies with all criteria of drug addiction defined by the WHO:
Accordingly, smoking is not a "bad habit" and cannot be suppressed by will alone in all cases. Pharmacologists discovered nicotine receptors in the brain which are the biological explanation for the fact that so many smokers, despite their high motivation and good psychological support, backslide again and again.
In 1975, this finding resulted in a completely new therapeutic approach, the nicotine supply via chewing gum. Although welcomed enthusiastically at first, the system soon showed drawbacks. The bitter taste and the poor social acceptance of the chewing gums were some of the objections. In addition, abuse by overdosage also occured with these systems.
All these drawbacks led to the development of transdermal therapeutic systems which comprise nicotine, e.g., described in German patent DE 36 29 304 and U.S. Pat. No. 4,597,961.
When nicotine is administered transdermally, taste is of no importance, the application is invisible, the substance is delivered without oral substitutive gratification, and plasma peaks are avoided.
Observed side effects are skin irritations at the site of application, i.e. reddenings, slight swellings and itching, which in some cases caused the stop of the therapy.
In addition, another disadvantage of this nicotine therapy is the fact that this form of treatment does not take into account the extreme toxicity of nicotine.
Accordingly, there is a demand for drugs which reliably suppress the symptoms of nicotine dependence; however, the therapeutic doses of the active substance may not have a toxicity comparable to that of nicotine.
Until today, substances from the following groups have been used to treat nicotine dependence: acetic acid, camphor, glucose, vitamins, terpenes, and others
The diversity of therapy principles alone reveals that an efficacious drug for the treatment of nicotine dependence which is not as toxic as nicotine has not yet been found.
Accordingly, it is the object of the present invention to provide a drug in an oral, transdermal, or otherwise parenteral formulation which allows a controlled release of the drug to the greatest possible extent and ensures a reduction in the desire for nicotine. The term parenteral is used to include all forms of application, except for the oral form, such as the rectal, intravenous, intramuscular, intraperitoneal and nasal form of administration.
According to the present invention this object is surprisingly achieved by a formulation for the treatment of nicotine dependence, which is characterized in that it comprises an effective amount of the active substance galanthamine (4a,5,9,11,12-hexahydro-3-methoxy-11-methyl-6H-benzofuro [3a, 3, 2-ef] [2] benzazepine-6-ol) or one of the pharmaceutically acceptable acid addition salts thereof. ##STR1##
This solution is surprising all the more since, although galanthamine has been examined in great detail and the pharmacological effects thereof have been studied thoroughly, the application of a galanthamine-containing formulation to treat nicotine dependence according to the present invention has not been described until today.
Owing to its pharmacological properties galanthamine belongs to the group of reversibly acting cholinesterase inhibitors, its effects are similar to those of physostigmine and neostigmine, however, it stands out for particular specific properties. The therapeutic range of galanthamine is three to six times broader since it is not as toxic as physostigmine or neostigmine.
This advantage compensates for its slightly lower cholineste
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Arzneimittelforschung GmbH & Co. KG
Henley III Raymond
Therapie-System GmbH & Co., KG
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