Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-07-09
1998-12-29
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 31415
Patent
active
058542701
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/1B95/01152 filed Nov. 20, 1995. The present invention relates to a pharmaceutical composition containing, as active ingredient, azol4-one, in particular a liquid composition for oral administration.
In UK Patent No. 2153821B we disclose, inter alia, zol-4-one, now known as ondansetron, which may be represented by the formula (I) ##STR1## and physiologically acceptable salts, solvates and physiologically acceptable equivalents thereof.
In the aforementioned specification the compounds are described as potent and selective antagonists of 5-hydroxytryptamine (5 HT) at 'neuronal' 5 HT receptors of the type located on terminals of primary afferent nerves, and which are also present in the central nervous system. Receptors of this type are now designated 5 HT.sub.3 receptors. The compounds are described as being of use in the treatment of a human or animal subject suffering from a condition caused by a disturbance of neuronal 5 HT function, for example in the treatment of migraine pain or a psychotic disorder such as schizophrenia. It is also stated that the compounds may be useful in the treatment of conditions such as anxiety, obesity and mania.
According to our European Patent Application publication No. 226266, the compounds have also been found to be anti-emetics, and may be used in the treatment or prevention of nausea and vomiting. The use of these compounds for the treatment of emesis is also described in European Patent No. 201165, which additionally refers to the use of the compounds for the treatment of irritable bowel syndrome.
Numerous clinical studies have demonstrated the effectiveness of ondansetron for the treatment of emesis, particularly the nausea and vomiting associated with cancer chemotherapy and radiotherapy and that occurring post-operatively. Hitherto, the drug has always been administered either by injection or orally.
Oral administration in the form of a conventional tablet, pill or capsule constitutes the generally preferred route for administration of pharmaceuticals since this route is generally convenient and acceptable to patients. Unfortunately such compositions may be associated with certain disadvantages, particularly in the treatment of paediatric or geriatric patients, who may dislike or have difficulty in swallowing such compositions, or where administration of a conventional tablet, pill or capsule is not feasible. It is highly desirable, particularly in the treatment of acute conditions, that pharmaceutical compositions have a rapid and consistent onset of action combined with sustained activity and good bioavailability. Rapid absorption can be achieved by parenteral injection but this is unacceptable to some patients, particularly if the drug is to be administered without direct medical supervision, i.e. self-administered.
Alternative routes for administration of ondansetron are proposed in GB 2153821, including liquid formulations for oral administration. GB 2153821 discloses a number of pharmaceutical formulations containing ondansetron, in the form of its hydrochloride dihydrate, and sucrose and sucrose-free syrup formulations for oral administration containing ondansetron hydrochloride dihydrate are specifically disclosed therein.
The present invention provides a particularly advantageous pharmaceutical composition, not hitherto specifically disclosed, which is a liquid composition of ondansetron suitable for oral administration.
The present invention therefore provides in a first aspect a liquid composition for oral administration comprising ondansetron or a pharmaceutically acceptable derivative thereof, a sweetener and one or more pharmaceutically acceptable excipients, characterised in that the sweetener comprises one or more polyhydric alcohols and the pH of the composition lies in the range 2.0 to 5.0.
By pharmaceutically acceptable derivative is meant any pharmaceutically acceptable salt or solvate of ondansetron, or any other compound, which upon administration to the recipient is capable of providing (directly or indirectly)
REFERENCES:
Dittert, Sprowls' American Pharmacy, 7th Edition, pp. 84-85 (1974).
Glaxo Wellcome Inc.
Henley III Raymond
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