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Last Updated: April 23, 2024

Details for Patent: 5,877,192


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Title: Method for the treatment of gastric acid-related diseases and production of medication using (-) enantiomer of omeprazole
Abstract:A method for treatment of gastric acid related diseases by inhibition of gastric acid secretion comprising administering to a mammal in need of treatment a therapeutically effective amount of the (-)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benz imidazole or a pharmaceutically acceptable salt thereof, so as to effect decreased interindividual variation in plasma levels upon administration. The use of the (-)-enantiomer of omeprazole to receive increased average plasma levels (AUC) upon administration of the same doses of the (-)-enantiomer of omeprazole compared to those of racemic omeprazole is also claimed, as well as an improved antisecretory effect and a better clinical effect.
Inventor(s): Lindberg; Per (Molndal, SE), Weidolf; Lars (Vastra Frolunda, SE)
Assignee: Astra Aktiebolag (Sodertalje, SE)
Filing Date:Apr 11, 1997
Application Number:08/833,962
Claims:1. A method for treatment of gastric acid related diseases by inhibition of gastric acid secretion comprising administering to a mammal in need of treatment a therapeutically effective amount of a proton pump inhibitor consisting essentially of the (-)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benz imidazole or a pharmaceutically acceptable salt thereof, so as to effect decreased interindividual variation in plasma levels (AUC) during treatment of gastric acid related diseases.

2. A method for treatment of gastric acid related diseases by inhibition of gastric acid secretion comprising administering to a mammal in need of treatment a therapeutically effective amount of a proton pump inhibitor consisting essentially of the (-)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H- benzimidazole or a pharmaceutically acceptable salt thereof, so as to effect an increased average plasma levels (AUC) per dosage unit.

3. The method according to claim 1 or 2 so as to effect a less pronounced increase in gastrin levels in slow metabolisers during treatment of gastric acid related diseases.

4. The method according to claim 1 or 2 so as to effect a decreased CYP1A induction in slow metabolisers during treatment of gastric acid related diseases.

5. The method according to claim 1 or 2 so as to elicit an improved antisecretory effect during the treatment of gastric acid related diseases.

6. The method according to claim 1 or 2 so as to elicit an improved clinical effect comprising accelerated rate of healing and accelerated rate of symptom relief during the treatment of gastric related diseases.

7. The method according to claim 1 or 2, wherein the (-)-enantiomer of omeprazole or a pharmaceutically acceptable salt thereof, is administered orally in the form of a tablet or a capsule.

8. The method according to claim 1 or 2, wherein the (-)-enantiomer of omeprazole or a pharmaceutically acceptable salt thereof, is administered parenterally.

9. The method according to claim 1 or 2, wherein the (-)-enantiomer of omeprazole or a pharmaceutically acceptable salt thereof, is administered by intravenous infusion.

10. The method according to claim 1 or 2, wherein the amount administered is about 5-80 mg total daily dose.

11. The method according to claim 1 or 2, wherein the amount administered is about 20-60 mg total daily dose.

12. A method for the production of a medicament for treating gastric acid related diseases, which comprises: combining a therapeutically effective amount of a proton pump inhibitor consisting essentially of the (-)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzi midazole or a pharmaceutically acceptable salt thereof, with a pharmaceutically acceptable carrier.

13. The method according to claim 12, wherein the medicament causes a decreased interindividual variation in plasma levels (AUC) per unit dosage during the treatment of gastric acid related diseases.

14. The method according to claim 12, wherein the medicament causes an increased average plasma level (AUC) per unit dosage during the treatment of gastric acid related diseases.

15. The method according to claim 12, wherein the medicament causes a less pronounced increase in gastrin levels in slow metabolisers during treatment of gastric acid related diseases.

16. The method according to claim 12, wherein the medicament causes a decreased CYP1A induction in slow metabolisers during treatment of gastric acid related diseases.

17. The method according to claim 12, wherein the medicament causes an improved antisecretory effect during the treatment of gastric acid related diseases.

18. The method according to claim 12, wherein the medicament causes an improved clinical effect comprising accelerated rate of healing and accelerated rate of symptom relief during the treatment of gastric related diseases.

19. The method according to claim 12, wherein the medicament produced for oral administration is in the form of a tablet or capsule.

20. The method according to claim 12, wherein the medicament is administered parentally, by intravenous infusion.

21. The method according to any of claims 12-20, wherein the medicament is administered in the amount of about 5 mg to 80 mg total daily dose.

22. The method according to any of claims 12-20, wherein the medicament is administered in the amount of about 20 mg to 60 mg total daily dose.

23. The method according to claim 1 or 2 wherein the (-)-enantiomer of the proton pump inhibitor is essentially devoid of its (+)-enantiomeric contaminant.

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