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Claims for Patent: 4,402,949

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Claims for Patent: 4,402,949

Title: Stable solutions of hydrogenated ergotalkaloids
Abstract:Stable solutions of (a) hydrogenated ergot alkaloids and (b) heparin as well as the salts thereof in a carrier medium comprising (c) water, (d) a mono- or poly-alcohol, and (e) urea or a pharmaceutically acceptable calcium or magnesium salt or ethylenediaminetetraacetic acid, and combinations thereof.
Inventor(s): Hartmann; Volker (Nuremberg, DE), Otto; Karl-Heinz (Kastl/Opf., DE), Patt; Ludwig (Nuremberg, DE)
Assignee: Sandoz Ltd. (Basel, CH)
Application Number:06/317,660
Patent Claims: 1. A pharmaceutical composition in stable solution form comprising as active ingredient a combination of

(a) a compound of formula I, ##STR2## wherein R is hydrogen or C.sub.1-4 alkyl,

R.sub.1 is methyl, ethyl or isopropyl,

R.sub.2 is isopropyl, sec.-butyl, isobutyl or benzyl, and

X is hydrogen or methoxy,

or a pharmaceutically acceptable acid addition salt thereof; and

(b) heparin or a pharmaceutically acceptable salt thereof, and a carrier medium comprising

(c) water;

(d) a pharmaceutically acceptable mono- or poly-alcohol; and

(e) urea or a pharmaceutically acceptable calcium or magnesium salt of ethylenediaminetetraacetic acid, or combinations thereof.

2. Composition according to claim 1, having a pH of from 4 to 6.

3. Composition according to claim 1, wherein the compound of formula I is dihydroergotamine.

4. Composition according to claim 1, wherein the compound of formula I is dihydroergovaline.

5. Composition according to claim 3, wherein the compound of formula I is in the form of the methane sulphonate.

6. Composition according to claim 4, wherein the compound of formula I is in the form of the methane sulphonate.

7. Composition according to claim 1, wherein the compound of formula I is 6-nor-6-isopropyl-9,10-dihydro-2'.beta.-methyl-5'.alpha.-benzyl-ergopeptin e.

8. Composition according to claim 7, wherein the compound of formula I is in the form of the maleate.

9. Composition according to claim 1, wherein the heparin is in the form of the sodium salt.

10. Composition according to claim 1, wherein the compound of formula I and heparin are present in a ratio of 1 mg:500 to 70,000 I.U.

11. Composition according to claim 10, wherein the ratio is 1 mg:2,000 to 20,000 I.U.

12. Composition according to claim 1, wherein component (c) is present in an amount of from 45 to 72% based on the total volume of the composition.

13. Composition according to claim 1, wherein component (d) is present in an amount of from 28 to 55% based on the total volume of the composition.

14. Composition according to claim 1, wherein component (d) is selected from the group consisting of ethanol, propylene glycol, polyethylene glycol, diethyleneglycol, triethylene glycol, glycerol and mixtures thereof.

15. Composition according to claim 14, wherein component (d) comprises (i) ethanol and (ii) triethylene glycol or (iii) glycerol and (iv) propylene glycol.

16. Composition according to claim 15, wherein (i) and (ii) are present in a ratio of from 1:6 to 10 parts by weight or (iii) and (iv) are present in a ratio of from 1:8 to 12 parts by weight.

17. Composition according to claim 16, wherein (i) and (ii) are present in a ratio of from 1:8 parts by weight or (iii) and (iv) are present in a ratio of from 1:10 parts by weight.

18. Composition according to claim 1, wherein component (e) comprises a pharmaceutically acceptable calcium or magnesium salt of ethylenediamine tetraacetic acid.

19. Composition according to claim 18, wherein the salt is a polymetal salt incorporating calcium or magnesium together with monovalent metal ions.

20. Composition according to claim 19, wherein the salt is CaNa.sub.2 EDTA.

21. Composition according to claim 1, wherein component (e) is present in an amount of about 2 to about 20 mg based on an amount of 5,000 I.U. heparin.

22. Composition according to claim 21, in unit dosage form, wherein component (e) is present in an amount of from about 2 to about 5 mg based on an amount of 5,000 I.U. heparin.

23. Composition according to claim 1, containing as an additional component (f), a physiologically acceptable anaesthetic.

24. Composition according to claim 23, wherein component (f) is an acetanilide anaesthetic or a pharmaceutically acceptable acid addition salt thereof.

25. Composition according to claim 24, wherein the acetanilide anaesthetic is selected from the group consisting of lidocain, Hostacain and Baycain.

26. Composition according to claim 23, wherein anaesthetic is present in an amount of from 1 to 2% based on the total weight of the composition.

27. Composition according to claim 1 in unit dosage form.

28. Composition according to claim 1 in ampoule form for injection.

29. Composition according to claim 25, containing 0.5 mg of compound of formula I and 2,500 or 5,000 I.U. heparin.

30. Process for the preparation of a pharmaceutical composition according to claim 1, which process comprises the individual steps of:

(1) preparing a solution of an active ingredient (a) in a solvent medium comprising components (d) and, when required, (f);

(2) preparing a solution of an active ingredient (b) in a solvent medium comprising components (c) and (e);

(3) combining the solutions obtained via steps (1) and (2);

(4) optionally adding additional component (c) and/or (d).

31. Process according to claim 30, conducted with protective gassing during solution.

32. Process according to claim 30, wherein the obtained solution is adjusted to pH 4 to 6.

33. A composition according to claim 1, wherein lettered component

(a) represents dihydroergotamine or a pharmaceutically acceptable salt thereof,

(d) represents (i) ethanol and (ii) triethylene glycol or (iii) glycerol and (iv) propylene glycol wherein (i) and (ii) are present in a ratio of from 1:6 to 10 parts by weight or (iii) and (iv) are present in a ratio of from 1:8 to 12 parts by weight, and

(e) represents a pharmaceutically acceptable calcium or magnesium salt of ethylenediaminetetraacetic acid (EDTA), or combinations thereof.

34. A composition according to claim 1, wherein lettered component

(a) represents dihydroergotamine methanesulfonate,

(b) represents heparin-sodium salt,

(d) represents a 1:10 mixture of glycerol and propylene glycol, and

(e) represents CaNa.sub.2 EDTA.

35. A composition according to claim 34 wherein components a:b in non-salt forms, are present in a ratio of 1:2,000 to 20,000 I.U., components (c) and (d) are present in an amount of 45-72% and 28-55% volume percent, respectively, and component (e) is present in an amount corresponding to 2-5 mg. per 5,000 I.U. of component (b).

36. A composition according to claim 35 containing 0.5 mg. of (a) and 2500-5000 I.U. heparin.

37. A composition according to claim 34 containing, as an additional component (f), an acetanilide anaesthetic or a pharmaceutically acceptable acid addition salt thereof.

38. A composition according to claim 35 containing, as an additional component (f), an acetanilide anaesthetic selected from the group consisting of lidocain, Hostocain and Baycain.

39. A composition according to claim 11 wherein component (a) is DHE or a pharmaceutically acceptable acid addition salt thereof, component (c) and (d) are present in an amount, based on the total weight of the composition, of from 45-72% and 28-55%, respectively, and component (e) is present in an amount of from about 2 to about 5 mg. based on an amount of 5,000 I.U. heparin present.
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