Method of obtaining ergoalkaloids

专利摘要:
The invention relates to a process for the preparation of a solid material composed of ergot peptide alkaloids, their hydrogenated forms or their salts and polyvinylpyrrolidone. The solid material obtained according to the invention can be used for the preparation of pharmaceutical compositions.
公开号:SU1165223A3
申请号:SU762412401
申请日:1976-10-15
公开日:1985-06-30
发明作者:Эрхардт Лотар；Хартманн Фолькер；Патт Людвиг；Отто Карл-Хайнц
申请人:Сандос Аг (Фирма)；
IPC主号:

专利说明:

The invention relates to the pharmaceutical industry and relates to a method for producing galenic preparations comprising ergoalkaloids.
The aim of the invention is to increase the resorption of ergoalkaloids;
Example 1. In a 4-liter flask, 34.6 g of dihydroergotamine methanesulfonate, 195.4 g of polyvinylpyrrolidone (average mol.m. 25000) and 500 ml of methanol are placed. The flask is attached to a rotary evaporator. At a bath temperature of 60 ° C. with a rotating flask, the contents are heated to 60 ° C. This forms a clear solution.
Methanol is distilled off from the solution under reduced pressure (about 250 torr.) And a bath temperature of 60 ° C until the residue reaches a syrupy consistency of 20. This mass is introduced into evaporation plates and incubated for about 2 hours at room temperature. Then drying is carried out in a vacuum oven at 25 ° C and a pressure of 1 torr for about 12 hours, then the mixture is ground and subjected to further drying. The resulting powder is processed into dosage form 30 using conventional excipients used in pharmaceutical practice.
Example 2. 34.6 g of dihydroergotamine ~ ₃₅ methanesulfonate, 193.165 g of polyvinylpyrrolidone (average mol.m. 25000), 2.26 g of polyethylene glycol-1800-stearate and 500 ml of methanol are placed in a 4-liter flask. The flask is attached to a rotary evaporator. At a bath temperature of 60 ° C. with a rotating flask, the contents are heated to approximately 60 ° C. A clear solution is formed.
Methanol is distilled off from the solution under reduced pressure (250 torr) and a bath temperature of 60 ° C until the residue reaches a syrupy consistency. This mass is introduced into the evaporation cups and aged for about 2 hours at room temperature. Then drying is carried out in a vacuum oven at 30 ° C, a pressure of 1 torr for 12 hours, after which the mixture is milled and further dried.
Example 3. . 34.6 g of dihydroergotamine methanesulfonate, 195.4 g of polyvinyl pyrrolidone and mol. weight
25,000 and 500 ml of ethyl alcohol. The flask is attached to a rotary evaporator and at a bath temperature of 35 ° C, the contents are heated while the flask rotates to 30 ° C. After complete dissolution, the temperature of the bath is raised to 70 C, and the pressure in the flask is reduced to about 250 mm Hg. Ethanol is distilled off until the residue in the flask assumes a syrup-like consistency. After that, the mass is shaken in a cup at room temperature for a period. 2 hours. Then carry out the drying in a vacuum oven at 30 C, a pressure of 1 mm RT.article. for 12 hours, after which the mixture is ground and dried. The yield is 96% of the theoretically calculated value.
PRI me R 4. The method is carried out analogously to example 1, using a mixture of dihydroergocristine methanesulfonate, dihydroergocriptine methanesulfonate and dihydroergocornine methanesulfonate in a ratio of 1: 1: 1.
EXAMPLE 5. By using the methodology described in example 1, as well as 0.2 g of dihydroergotamine methanesulfonate and 199.8 g of polyvinylpyrrolidone with a molecular weight of 115,000, a substance is obtained which is processed into preparations with appropriate additives. Yield 94%.
PRI me R 6. By using the methodology described in example 1, as well as 100 g of dihydroergotamine methanesulfonate and 100 g of polyvinylpyrrolidone with a molar weight of 40,000 receive a substance that is processed with the usual additives in the preparations. Yield 95%. .
PRI me R 7. By using the methodology described in example 1, and the indicated ratios of the components are dissolved in ethanol at 30 ° C. The yield of 96%.
Example 8. By using the methodology described in example 2 and the indicated ratios of the components, dissolution in ethanol is carried out at 70 ° C. Yield 94%.

权利要求:
Claims (4)
[1]
1. A METHOD FOR PRODUCING ERGOALKALOIDS, including their mixing with excipients, which is important because, in order to increase resorption, dihydroergotamine methanesulfonate or a mixture of salts of dihydroergocriptine, dihydrohydrinergic dihydroergene are used as ergoalkaloids 1: 1: 1, which is a solvent with excellent salt quality mixed with poly (Y-vinyl) pyrrolidone with a mol.m. 11500-40000 and / or. polyethylene glycol (mol.m. 1600) with stearate at a ratio of active and auxiliary substances (0.1-99.9) (50-50), then the resulting mixture is dissolved by heating in an organic solvent and distilled off.
[2]
2. The method according to claim 1, with the fact that methanesulfonate is used in dihydroergocriptine, dihydroergocornin and dihydroergocristine.
[3]
3. The method according to π. 1, about t and h and a - - - with. The fact that methanol or ethanol is used as an organic solvent.
[4]
4. The method according to π. 1, with the fact that the dissolution of the mixture is carried out at a temperature of 30-70 and.

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引用文献:

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法律状态:

优先权:

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申请号 | 申请日 | 专利标题

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DE2546577A|DE2546577B2|1975-10-17|1975-10-17|Solid substances made from polyvinylpyrrolidone and ergot alkaloids|

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