Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1996-10-22
2000-12-19
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514 30, 514398, 424653, A61K 3170, A61K 31415, A61K 3324
Patent
active
061627925
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a new therapeutic application of spiramycin optionally in combination with metronidazole.
Spiramycin, optionally in combination with metronidazole, may be useful for the preparation of a medicinal product intended for the prevention or treatment of gastrointestinal disorders involving Helicobacter pylori.
Numerous cases of peptic ulcers are identified each year. These ulcers are usually treated with anti-ulcer agents such as anti-H.sub.2, bismuth derivatives or proton pump inhibitors. However, these are long-term treatments which are very expensive, which are not easily accepted by patients and in which numerous relapses are observed.
Helicobacter pylori, which was isolated for the first time from the gastric mucous membrane in 1982, is responsible for gastropathies such as gastritis and peptic ulcers, and is probably also responsible for the appearance of gastric cancers. The eradication of Helicobacter pylori greatly modifies the extent of ulcer diseases. Not only do the ulcers disappear rapidly (about 90%), but cases of relapses are almost completely eliminated.
Treatments for eradicating Helicobacter pilori by means of compositions comprising an antibacterial agent and an anti-ulcer agent are already mentioned in patent applications EP 206 625, EP 282 131 and WO 92/04 898 and WO 93/21 920.
However, numerous publications report manifestations of intolerance which appear in 20 to more than 40% of patients, in most cases consisting of nausea and diarrhea, but also of abdominal pain. These side effects result from the nature of the products currently used in clinical medicine, the high doses which have to be administered and the duration of the treatments.
Furthermore, the majority of effective therapies consist in the administration of 3 medicinal products, which is poorly accepted by patients. Thus, the practitioner is confronted with the difficult choice between the potency of the treatment, the limitation of the side effects and the poor acceptance by the patient for such a medication.
Spiramycin is a well known antibacterial agent isolated from Streptomyces ambofaciens: U.S. Pat. No. 2,943,023, U.S. Pat. No. 2,978,380 and U.S. Pat. No. 3,011,947.
Metronidazole is a nitroimidazole derivative which is also known (U.S. Pat. No. 2,944,061) and which is endowed with a parasiticidal and antibacterial action. The spiramycin/metronidazole combination marketed under the name Rodogyl.RTM. is known for its action on anaerobic microbes of the dentibuccal flora.
However, the activity of spiramycin or of its combinations with metronidazole does not suggest that an action can be observed in clinical medicine on a microbe which is difficult to eradicate, such as Helicobacter pylori for which it is usually necessary to use much more potent antibacterial agents, with the consequences that are known.
It has now been shown that it is possible to obtain the eradication of Helicobacter pylori by the administration of spiramycin or of a spiramycin/metronidazole combination, with a level of side effects which is completely reduced compared with other treatments.
The administration is carried out before, after or at the same time as the administration of an anti-ulcer agent.
The anti-ulcer agents are chosen equally well from the antacids, the anti-H.sub.2 agents and the proton pump inhibitors.
The antacids may be especially bismuth derivatives or combinations of aluminium hydroxide and magnesium hydroxide such as Maalox.RTM..
The anti-H.sub.2 agents may be for example ranitidine, cimetidine, famotidine and the like.
The proton pump inhibitors may be for example omeprazole, lansoprazole, partoprazole and the like.
Among the spiramycin/metronidazole combinations, more particularly preferred is the combination which comprises Rodogyl.RTM. (750,000 I.U. spiramycin base/125 mg metronidazole combination). This pre-existing combination makes it possible, moreover, to administer only one antibacterial proprietary medicinal product during the treatment.
The activity was demonstrated in a 10-day treatme
REFERENCES:
Axon, V. Helicobacter pylori therapy: Effect on peptic ulcer disease, J. Gastroenterol. Hepatol., vol. 6, No. 2, pp. 131-137 (1991).
The Merck Index, 11th Ed., 1989, pp. 8703, 8720, 9130, 9131.
Forfang Erik T.
Larssen Sven-Erik
Aventis Pharma S.A.
Goldberg Jerome D.
Newman Irving
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