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Claims for Patent: 4,861,786

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Claims for Patent: 4,861,786

Title: Composition for a stable vein compatible injectable solution of torasemide process for the preparation and method of use
Abstract:The present invention provides an aqueous, alkaline injection solution of torasemide ready for injection, which contains a physiologically compatible alkaline buffer with a pH value of from 9.3 to 9.9 and with a buffer capacity of up to 0.1 val/liter together with an organic solvent in an amount of from 5 to 20% by weight selected from the group of polyethylene glycols with a molecular weight of from 100 to 1500, polypropylene glycols with a molecular weight of from 50 to 1000, glycerol, propylene glycol, ethanol and propanol, the torasemide being present in a concentration of from 2 to 40 mg/ml. Torasemide solutions are useful to inhibit inflammation or promote diuresis. The present invention also provides a process for the preparation of this solution, wherein torasemide is suspended in the above organic solvent brought into solution by the addition of aqueous alkali, adding the buffer and other adjuvants and adjusting the pH value to 9.3 to 9.9.
Inventor(s): Demmer; Fritz (Hirschberg-Leutershausen, DE), Gruber; Werner (Birkenau, DE), Woog; Heinrich (Laudenbach, DE)
Assignee: Boehringer Mannheim GmbH (Mannheim, DE)
Application Number:07/071,201
Patent Claims: 1. A composition for an aqueous, sterile, alkaline pharmaceutically active and vein-compatible solution of torasemide for injection in mammals for inhibition of inflammation or promotion of diuresis, comprising 2-40 mg/ml torasemide or a physiologically acceptable salt thereof in a physiologically compatible alkaline buffer of pH 9.3-9.9 and with a buffer capacity of up to 0.1 val/liter, together with an organic solvent substantially free of aldehyde or ketone wherein the organic solvent contains less than 30 ppm aldehyde in an amount of from 5 to 20% by weight selected from the group consisting of at least one of polyethylene glycol in a 100-1500 molecular weight range, polypropylene glycol in a 150-1000 molecular weight range, glycerol, propylene glycol, ethanol and propanol wherein the composition is stored in an oxygen-free atmosphere or in the presence of a physiologically compatible reducing agent.

2. The composition of claim 1 wherein the organic solvent is polyethylene glycol of 200-600 molecular weight.

3. The composition of claim 1 wherein the organic solvent is polyethylene glycol of 400 molecular weight.

4. The composition of claim wherein the organic solvent is about 10% by weight.

5. The composition of claim 1 wherein the torasemide is present in a concentration of 0.01 to 0.2 mole/liter.

6. The composition of claim 1 wherein the torasemide used has a particle size of less than 10 micrometer.

7. The composition of claim 1 wherein the torasamide used has a particle size of less than 2 micrometer.

8. The solution for injection of claim 1, wherein the organic solvent contains less than 10 ppm aldehyde.

9. The torasemide solution for injection of claim wherein the buffer is a sodium, potassium or ammonium salt of a weak acid, a tris-(hydroxymethyl)-aminomethane, or a further physiologically active material acting as a buffer.

10. The torasemide solution of claim 9 wherein the weak acid is a phosphate, carbonate, glycinate, arginate, N-methyl glucosaminate or other amino acid.

11. The torasemide solution of claim 9 wherein the further active material is a diuretic.

12. The torasemide solution of claim 11 wherein the diuretic is canrenoate and/or furosemide.

13. The torasemide solution of claim 9 wherein the further active material is present in an amount of up to 100 mg/ml.

14. The torasemide solution of claim 1 further comprising an agent for the maintenance of the iostonic state.

15. The torasemide solution of claim 14 wherein the agent comprises sodium chloride, fructose, lactose or glucose.

16. The composition of claim 1 further comprising adjuvants and additives from the group of tenside, mineral and vitamin.

17. A kit for the preparation of an injectable solution of torasemide comprising torasemide, a buffer from the group of a sodium, potassium or ammonium salt of a weak acid or tris-(hydroxymethyl)-aminomethane or a further active material acting as an alkaline buffer with a pH of 9.3-9.9, an organic solvent substantially free of aldehyde or ketone wherein the organic solvent contains less than 30 ppm aldehyde selected from the group consisting of at least one polyethylene glycol in a 100-1500 molecular weight range, polypropylene glycol in a 150-1000 molecular weight range, propylene glycol, ethanol and propanol, an agent to maintain isotonicity and a reducing agent.

18. The solution of torasemide for injection of claim 1 prepared by a process of which comprises:

suspending torasemide in an organic solvent substantially free of aldehyde and ketone wherein the solvent is from the group of polyethylene glycol, polypropylene glycol, glycerol, propylene glycol, ethanol and propanol;

bringing the torasemide into solution by the addition of an aqueous alkali to a pH value adjusted to 9.3 to 9.9 by the addition of acid or alkali;

filtering off undissolved particles from the solution, and sterilizing the solution.

19. A method for inhibiting inflammation and promoting diuresis in mammals which comprises injecting the solution of torasemide of claim 1 in a pharmaceutically active amount of mammals in need of such treatment.
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