Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-06-08
2000-07-18
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 3144
Patent
active
060908270
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to an oral pharmaceutical formulation comprising the acid labile H.sup.+, K.sup.+ -ATPase inhibitor omeprazole. The formulation is in the form of a multiple unit dosage form comprising enteric coating layered units of omeprazole. More specifically, the units comprise a core material of omeprazole and optionally an alkaline reacting substance, in admixture with one or more pharmaceutically acceptable excipients such as a binding, filling and/or disintegrating agent. Furthermore, each unit comprises a separating layer to separate the enteric coating layer from the core material. The separating layer and/or the optional binding agent consists of a specific quality of hydroxypropyl methylcellulose (HPMC), and optionally pharmaceutical excipients. More specifically, the HPMC quality has a specific cloud point.
Furthermore, the present invention refers to the use of a specific quality of HPMC in the manufacture of a pharmaceutical formulation comprising omeprazole, and the use of such a pharmaceutical formulation in medicine.
BACKGROUND OF THE INVENTION
Omeprazole, an alkaline salt thereof, the (-)-enantiomer of omeprazole and an alkaline salt of the (-)-enantiomer of omeprazole, all compounds hereinafter referred to as omeprazole, are used in the treatment of gastric acid related diseases. Omeprazole and pharmaceutically acceptable salts thereof are described in EP 5129, and some specific alkaline salts of omeprazole are described in EP 124 495 and WO95/01977. Certain salts of the single enantiomers of omeprazole and their preparation are described in WO94/27988.
Omeprazole is generally known to be useful for inhibiting gastric acid secretion in mammals and man by controlling gastric acid secretion at the final step of the acid secretory pathway. Thus, in a more general sense, it may be used for prevention and treatment of gastric-acid related diseases in mammals and man, including e.g. reflux oesophagitis, gastritis, duodenitis, gastric ulcers and duodenal ulcers. Furthermore, it 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-oesophageal reflux disease, and in patients with gastrinomas. It may also be used in patients in intensive care situations, in patients with acute upper gastrointestinal bleeding, pre-and postoperatively to prevent aspiration of gastric acid and to prevent and treat stress ulceration. Further, it may be useful in the treatment of psoriasis as well as in the treatment of Helicobacter infections and diseases related to these, as well as in the treatment or prophylaxis of inflammatory conditions in mammals, including man.
Omeprazole is, however, susceptible to degradation or transformation in acidic and neutral media. The degradation 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.
With respect to the stability properties of omeprazole, it is obvious that an oral solid dosage form must be protected from contact with the acidic gastric juice and that omeprazole must be transferred in intact form to that part of the gastrointestinal tract where pH is near neutral and where rapid absorption can occur.
A pharmaceutical oral dosage form of omeprazole is best protected from contact with acidic gastric juice by an enteric coating layer. In EP 247 983 such an enteric coated formulation of omeprazole is described. The formulation contains omeprazole in the form of a core unit containing omeprazole together with an alkaline salt or containing an alkaline salt of omeprazole optionally together with an alkaline salt, the core unit is layered with a separating layer and an enteric coating layer. In WO 96/01623 a multiple unit tableted dosage formulation of omeprazole is described.
The oral formulations described in EP 247 983 and t
REFERENCES:
patent: 4786505 (1988-11-01), Lovgren et al.
patent: 5372998 (1994-12-01), Kokubo et al.
Pilbrant, A. et al., "Development of an oral formulation of omeprazole", Scand. J. Gastroenterol, 1985; 20 (suppl): 113-120.
Erickson Magnus
Josefsson Lars
Astrazeneca AB
Henley III Raymond
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