Liquid pharmaceutical formulation containing zotepine

Details Liquid pharmaceutical formulation containing zotepine Liquid pharmaceutical formulation containing zotepine

2000-07-25

2001-05-29

Reamer, James H. (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

Reexamination Certificate

active

06239165

ABSTRACT:

This invention relates to a liquid pharmaceutical formulation containing Zotepine.
Zotepine is 2-[(8-chlorodibenzo[b,f]thiepin-10-yl)oxy]-N,N-dimethylethylamine as shown in formula I.
The preparation and the psychotropic and neurotropic activity of Zotepine are described in British Patent Specification 1247067 (Fujisawa). The use of Zotepine in the treatment of gout is described in U.S. Pat. No. 4,443,469 (Fujisawa). The use of Zotepine for preventing relapse in chronic schizophrenic patients is described in British patent application 9526264.8 (Knoll AG). 2-[(8-Chlorodibenzo[b,f]-thiepin-10-yl)oxy]-N,N-dimethylethylamine has been available on prescription for the treatment of schizophrenia in Japan since 1982 under the tradename “Lodopin®”, and in Germany since 1990 under the tradename “Nipolept®”. Zotepine is also known under the tradename “Zoleptil®”.
Zotepine is currently only available in tablet form. However, patient compliance is a well-known problem with anti-psychotic drugs. It would be advantageous to provide Zotepine in a liquid formulation which might be added as drops to food or administered in a drink. However, Zotepine has a low solubility in solvents which would commonly be used in the pharmaceutical industry to prepare oral liquid formulations.
Solubility of Zotepine may be improved by converting it into an acid addition salt, but solutions of acid addition salts are unstable on storage due to acid hydrolysis which produces 8-chlorodibenzo[b,f]thiepine-10(11H)-one. In addition Zotepine in solution may undergo oxidation to give the N-oxide over time. Surprisingly a formulation has now been found which provides Zotepine in a liquid formulation which is stable to storage.


REFERENCES:
patent: 4443469 (1984-04-01), Nishizono
patent: 733 368 A1 (1996-09-01), None
patent: 1 247 067 (1971-09-01), None
patent: WO 97/23477 (1997-07-01), None

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