Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-12-07
2001-03-13
Henley, III, Raymond (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S627000
Reexamination Certificate
active
06201014
ABSTRACT:
The present invention relates to compositions for the treatment of irritable bowel syndrome (IBS) and more particularly to locally acting compositions which are active in the post-stomach region of the gastro-intestinal (GI) tract.
BACKGROUND OF THE INVENTION
Irritable Bowel Syndrome (IBS) is part of a spectrum of diseases known generally as Functional Gastrointestinal Disorders which include diseases such as non-cardiac chest pain, non-ulcer dyspepsia, and chronic constipation or diarrhoea. These diseases are all characterised by chronic or recurrent gastrointestinal symptoms for which no structural or biochemical cause can be found. Irritable bowel syndrome in the UK alone is responsible for 30-50% of all gastroenterology referrals to secondary care.
IBS is believed to be due to a number of factors such as physiological, emotional, cognitive and behavioural factors and is frequently encountered during periods of stress. Diagnosis of IBS is one of exclusion and is based on the observed symptoms in any given case. Commonly accepted criteria for IBS, known as the “Rome” criteria, include at least 3 months of continuous or recurrent symptoms of:
1. abdominal pain or discomfort that is relieved with defecation, and/or associated with a change in the frequency of stools, and/or associated with a change in the consistency of stool; and
2. two or more of the following on at least a quarter of occasions: altered stool frequency, altered stool form, altered stool passage, passage of mucus, and/or bloating or feeling of abdominal distension.
Conventional treatments of IBS are based on the severity and the nature of each person's symptoms and whether or not any psychological factors are involved. Treatment of IBS may include one or more of the following: lifestyle changes, pharmacological treatment and psychological treatment. However, there is no general treatment which is applicable to all cases of IBS.
In certain cases, the exclusion of foods which aggravate IBS symptoms is recommended. However, this type of treatment is only effective when the underlying cause of IBS is related to diet.
Pharmacologically active agents are often used to treat IBS. Anti-diarrhoeals (for example, loperamide), smooth muscle relaxants (for example, mebeverine hydrochloride or alverine citrate), or antidepressants may be effective in treating IBS. However, there is no single pharmacologically active agent which is completely effective in alleviating the symptoms or curing TBS.
Psychological factors may be used in the treatment of IBS. Again, however, this treatment does not provide a universal cure for the symptoms of IBS since not all cases of IBS are due to psychological factors.
One method of treating pathological conditions of the small and large intestines is disclosed in U.S. Pat. No. 5,431,914. This patent discloses that the external application of capsaicin to the skin in specific regions affects certain nerves in the skin which lead to spinal cord segments. Thus, it is suggested that topical application of a dose of 0.03 mg capsaicin to the anterior and posterior divisions of spinal nerves T12 to S3 can be used to treat IBS. However, a clear mechanism of the mode of operation of this invention is not known.
Such a regime of self-administration is unlikely to be effective because the composition must be applied to a specific site which is not necessarily readily apparent to the patient. In addition, it is likely to be difficult to control the dosage when applying the composition of U.S. Pat. No. 5,431,914 since it is in the form of a topical cream.
A need therefore exists for a composition which is able to relieve the symptoms of irritable bowel syndrome which ideally is in a form which is easily handled, may be administered in a unit dosage form and which is capable of being self administered by patients.
SUMMARY OF THE INVENTION
To alleviate the problems of IBS, according to a first aspect to the present invention, there is provided a pharmaceutical composition for use in the treatment of irritable bowel syndrome, diarrhoea, constipation, abdominal pain and/or bloating or abdominal distension in a mammal, preferably a human patient, the composition comprising:
i) one or more vanilloid compounds, pharmaceutically acceptable salts, analogues and/or derivatives thereof, (component a); and
ii) a pharmaceutically acceptable vehicle (component b),
wherein component b) is selected to enable component a) to be released in the gastrointestinal tract between the stomach and the rectum of the mammal.
Preferably component a) is present in a IBS symptom alleviating amount.
Preferably the composition according to the invention contains from 0.001 to 30% of component a), more preferably from 0.01 to 20%, most preferably from 0.1 to 10% by weight of the pharmaceutical composition.
Preferably the composition according to the invention contains from 70 to 99.999% component b), more preferably from 80 to 99.99%, most preferably from 90 to 99.9% by weight of the composition.
According to a second aspect of the invention, there is provided a pharmaceutical composition as described above with respect to the first aspect of the invention, but which further includes an enteric coating (component c) encasing components (a) and (b).
According to a third aspect of the invention, there is provided a process for the alleviation of symptoms associated with Irritable Bowel Syndrome (IBS) in a mammalian patient, preferably a human patient, afflicted with said symptoms, which process comprises the step of:
administering, preferably orally administrating, a therapeutically effective amount of the pharmaceutical composition according to either the first, or second aspects of the invention as described above, in order to alleviate said symptoms associated with Irritable Bowel Syndrome (IBS).
According to a fourth aspect of the invention, there is provided the process according to the third aspect of the invention as described above, wherein the pharmaceutical composition is in a sustained release form, which form is substantially released (i.e., at least 75% of component (a) in the pharmaceutical composition) in the gastrointestinal region after the stomach and before the rectum of the patient being treated.
DETAILED DISCLOSURE
In the context of the present invention, component a) should be understood to be a compound or a mixture of compounds having a biologically active vanillyl group. Component a) therefore includes both naturally occurring and synthetic vanilloids, pharmaceutically acceptable salts of the vanilloid compound (whether natural or synthetic) as well as pharmaceutically acceptable derivatives and/or analogues thereof (whether natural or synthetic).
Included in the ambit of the naturally occurring vanilloid compounds are both crude extracts and purified extracts of active vanilloid compounds.
Examples of natural vanilloid compounds suitable for use in the present invention therefore include both the crude extracts and the purified extracts of active vanilloid compounds from: capsicum, cayenne pepper, black pepper, paprika, cinnamon, clove, mace, mustard, ginger, turmeric, papaya seed and the cactus-like plant
Euphorbia resinifera.
Synthetic vanilloid compounds such as synthetic capsaicin as defined in WO 96/40079 are also envisaged to be included in or comprise component a) in the compositions of the present invention and the disclosure of such compounds as exemplified in WO 96/40079 is incorporated herein by reference.
The composition of the present invention may therefore include both a crude vanilloid compound-containing extract (obtained by extracting the natural product) and/or a pure vanilloid compound itself (obtained either by synthesis or by refining a crude extract). Thus, in the case of capsaicin, for example, one might also find dihydrocapsaicin present in the crude extract.
In so far as the pharmaceutically acceptable salts of component a) are concerned, the therapeutic activity resides in the moiety derived from the vanilloid, and identity of any salt portion when present is of minor importance
Fish & Richardson P.C.
Henley III Raymond
Reckitt & Colman Products Limited
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