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Claims for Patent: 4,138,565

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Claims for Patent: 4,138,565

Title: Stable solutions and processes for their preparation
Abstract:Solutions of certain hydrogenated ergopeptide alkaloids in mixtures of pharmacologically acceptable alcohols and water have improved stability. Preferred solvents are mixtures of ethanol, propylene glycol and glycerol containing from 15-40% wt. of water and having dielectric constants between 34 and 46. With these solutions it is not essential to carry out the filing operation under an inert atmosphere.
Inventor(s): Ehrhardt; Lothar (Nuremberg, DE), Patt; Ludwig (Nuremberg, DE), Hartmann; Volker (Nuremberg, DE)
Assignee: Sandoz Ltd. (Basel, CH)
Application Number:05/833,784
Patent Claims: 1. A hydrogenated ergopeptide alkaloid solution which is stable against decomposition on storage consisting essentially of

(a) a hydrogenated ergopeptide alkaloid or a pharmacologically acceptable acid addition salt thereof, or a mixture thereof

(b) a pharmacologically acceptable alcohol or mixture thereof, and

(c) up to 40% by weight of the solution of water, and having a dielectric constant of 50 or less.

2. A stable solution according to claim 1 consisting essentially of

(a) a hydrogenated ergopeptide alkaloid of formula I, ##STR2## in which R is hydrogen or alkyl having from 1 to 4 carbon atoms, other than t-butyl,

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, or a mixture thereof,

(b) a pharmacologically acceptable alcohol or mixture thereof and

(c) up to 40% by weight of the solution of water, said solution having a dielectric constant of 50 or less.

3. A solution according to claim 2 having a dielectric constant between 30 and 46.

4. A solution according to claim 3 having a dielectric constant between 34 and 46.

5. A solution according to claim 2 in which component (a) is a compound of formula I, stated in claim 2, in which

R is methyl

X is hydrogen and

R.sub.1 is isopropyl or methyl,

provided that R.sub.1 is methyl only when R.sub.2 is benzyl.

6. A solution according to claim 2 in which component (b) is propylene glycol.

7. A solution according to claim 2 in which the proportion of component (c) is from 15 to 40% by weight.

8. A solution according to claim 2 in which component (b) is a mixture of

(b.sub.1) a pharmacologically acceptable monofunctional alcohol having up to 18 carbon atoms, or mixtures thereof, and

(b.sub.2) a polyfunctional alcohol having up to 6 carbon atoms and 6 hydroxy groups or a polymeric polyfunctional alcohol having a molecular weight of from 200 to 20,000, or mixtures thereof,

the weight ratio of component (b.sub.1) to component (b.sub.2) being 1:0.1 to 1:100.

9. A solution according to claim 8 in which the concentration of component (a) is from 0.01 to 1% by weight, component (b.sub.1) has up to 10 carbon atoms, the ratio of component (b.sub.1) to component (b.sub.2) is 1:1 to 1:10, and the proportion of component (c) is from 15 to 40% by weight.

10. A solution according to claim 9 in which component (b.sub.1) has up to 3 carbon atoms and component (b.sub.2) is a polyfunctional alcohol of 2 or 3 carbon atoms and 2 or 3 hydroxy groups or a polymeric polyfunctional alcohol having a molecular weight of 200 to 600.

11. A solution according to claim 10 in which the ratio of component (b.sub.1) to component (b.sub.2) is 1:1 to 1:2.

12. A solution according to claim 10 in which component (b.sub.1) is ethanol and component (b.sub.2) is propylene glycol or glycerol or mixtures thereof.

13. A solution according to claim 10 in which component (a) is dihydroergotamine.

14. A solution according to claim 10 in which component (a) is dihydroergotoxin.

15. A method of preparing a hydrogenated ergopeptide alkaloid solution which is stable to decomposition on storage according to claim 2, consisting essentially of dissolving a compound of formula I, stated in claim 2, or a pharmaceutically acceptable acid addition salt thereof or a mixture thereof in a solvent consisting essentially of:

(a) a pharmacologically acceptable alcohol or a mixture thereof

(b) up to 40% by weight of the solution of water,

said solvent having a dielectric constant of 50 or less, at a temperature of 15 to 25.degree. C.
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