US4138565A
Expired / Lapsed
US
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Stable solutions and processes for their preparation
Assignee: Sandoz AG
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Filing: 1977-09-15
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Granted: 1979-02-06
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Expires: 1997-09-15
Abstract
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.
Inventors
- 👤 Lothar Ehrhardt
- 👤 Ludwig Patt
- 👤 Volker Hartmann
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 15:58
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/48; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K9/00; A61K9/0012; A61K9/0019; Y; Y10; Y10S; Y10S215/00; Y10S215/03
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
61 words
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.
Claim 2
Dependent Claim
61 words
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.
Claim 3
Dependent Claim
99 words
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 1 is methyl, ethyl or isopropyl, R 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.
Claim 4
Dependent Claim
14 words
A solution according to claim 2 having a dielectric constant between 30 and 46.
Claim 5
Dependent Claim
14 words
A solution according to claim 3 having a dielectric constant between 34 and 46.
Claim 6
Dependent Claim
47 words
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 1 is isopropyl or methyl, provided that R 1 is methyl only when R 2 is benzyl.
Claim 7
Dependent Claim
13 words
A solution according to claim 2 in which component (b) is propylene glycol.
Claim 8
Dependent Claim
20 words
A solution according to claim 2 in which the proportion of component (c) is from 15 to 40% by weight.
Claim 9
Dependent Claim
82 words
A solution according to claim 2 in which component (b) is a mixture of (b 1 ) a pharmacologically acceptable monofunctional alcohol having up to 18 carbon atoms, or mixtures thereof, and (b 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 1 ) to component (b 2 ) being 1:0.1 to 1:100.
Claim 10
Dependent Claim
59 words
A solution according to claim 8 in which the concentration of component (a) is from 0.01 to 1% by weight, component (b 1 ) has up to 10 carbon atoms, the ratio of component (b 1 ) to component (b 2 ) is 1:1 to 1:10, and the proportion of component (c) is from 15 to 40% by weight.
Claim 11
Dependent Claim
52 words
A solution according to claim 9 in which component (b 1 ) has up to 3 carbon atoms and component (b 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.
Claim 12
Dependent Claim
24 words
A solution according to claim 10 in which the ratio of component (b 1 ) to component (b 2 ) is 1:1 to 1:2.
Claim 13
Dependent Claim
27 words
A solution according to claim 10 in which component (b 1 ) is ethanol and component (b 2 ) is propylene glycol or glycerol or mixtures thereof.
Claim 14
Dependent Claim
12 words
A solution according to claim 10 in which component (a) is dihydroergotamine.
Claim 15
Dependent Claim
12 words
A solution according to claim 10 in which component (a) is dihydroergotoxin.
Claim 16
Dependent Claim
89 words
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° C.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-02-05 | 1982-08-07 | 1983-02-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-02-05 | 1986-08-07 | 1987-02-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-02-05 | 1990-08-07 | 1991-02-06 | $7700.00 | Window Closed / Lapsed |