Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1995-06-20
1998-10-06
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424465, 424467, 424469, 424490, 424475, 514925, A61K 922, A61K 930
Patent
active
058173382
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/SE95/00677 filed Jun. 7, 1995.
FIELD OF THE INVENTION
The present invention is related to new pharmaceutical preparations in the form of a multiple unit tableted dosage form comprising omeprazole or one of its single enantiomers or an alkaline salt of omeprazole or one of its single enantiomers. The novel tableted dosage form is intended for oral use. Furthermore, the present invention refers to a method for the manufacture of such preparations and, to the use of such preparations in medicine.
BACKGROUND OF THE INVENTION
The compound known under the generic name omeprazole, midazole, is disclosed i.a. in EP-A1-0 005 129. Certain salts of omeprazole including alkaline salts of omeprazole are described in EP-A1- 0 124 495 and in WO 95/01977. Novel salts of the single enantiomers of omeprazole are described in WO 94/27988.
Omeprazole or one of its single enantiomers or alkaline salts thereof, in the following stated shortly as omeprazole, are useful for inhibiting gastric acid secretion in mammals and man. In a more general sense, said substances may be used for prevention and treatment of gastric acid related diseases in mammals and man, including e.g. reflux esophagitis, gastritis, duodenitis, gastric ulcer and duodenal ulcer. Furthermore, omeprazole may be used for treatment of other gastrointestinal disorders where gastric acid inhibitory effect is desirable e.g. in patients on NSAID therapy, in patients with Non Ulcer Dyspepsia, in patients with symptomatic gastro-esophageal reflux disease, and in patients with gastrinomas. Omeprazole may also be used in patients in intensive care situations, in patients with acute upper gastrointestinal bleeding, pre- and postoperatively to prevent acid aspiration of gastric acid and to prevent and treat stress ulceration. Further, omeprazole may be useful in the treatment of psoriasis as well as in the treatment of Helicobacter infections and diseases related to these.
Omeprazole is, however, susceptible to degradation/transformation in acidic and neutral media. The half-life of degradation of omeprazole in water solutions at pH-values less than three is shorter than ten minutes. The degradation of omeprazole is catalyzed by acidic compounds and is stabilized in mixtures with alkaline compounds. The stability of omeprazole is also affected by moisture, heat, organic solvents and to some degree by light.
In respect to the stability properties of omeprazole, it is obvious that omeprazole in an oral solid dosage form must be protected from contact with the acidic gastric juice and the active substance must be transferred in intact form to that part of the gastrointestinal tract where pH is near neutral and where rapid absorption of omeprazole can occur.
A pharmaceutical oral dosage form of omeprazole is best protected from contact with acidic gastric juice by an enteric coating layer. In U.S. Pat. No. 4,786,505 such an enteric coated omeprazole preparation is described. Said omeprazole preparation contains an alkaline core comprising omeprazole, a separating layer and an enteric coating layer. In order to further enhance the stability during storage the prepared formulation may optionally be packed with a desiccant.
The hard gelatine capsules containing an enteric coated pellet formulation of omeprazole marketed by the Applicant today, are not suitable for press-through blister packages. Thus, there has been a demand for development of new enteric coating layered multiple unit preparations of omeprazole with good chemical stability as well as improved mechanical stability making it possible to produce well functioning and patient-friendly packages. Furthermore, there is a demand for omeprazole formulations having improved patient acceptance, such as divisible and/or dispersible tablets.
An improved mechanical stability can be obtained with an enteric coating layered tablet for example as described in WO 95/01783. However, only an enteric coating layered multiple units tablet can be made divisible and dispersible. A further advantage
REFERENCES:
patent: 4786505 (1988-11-01), Lovgren et al.
patent: 4853230 (1989-08-01), Lovgren et al.
patent: 4927640 (1990-05-01), Dahlinder et al.
Pharmaceutical Research, vol. 10 (1993), p. S-274.
Drugs Made in Germany, 37, No. 2 (1994), pp.53-60.
Aulton M.E. (Churchill Livingston) Pharmaceutics: The Science of Dosage Form Design (1988), pp. 316-321.
Bergstrand Pontus John Arvid
Lovgren Kurt Ingmar
Astra Aktiebolag
Page Thurman K.
Spear James M.
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