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Cinepazide acid addition salt and preparation method thereof

A technology of cinepazide and cinepazide, which is applied in the field of medicine, can solve the problems of poor photostability, inconvenient drug production, storage, transportation and use, hidden dangers of clinical safety medication and the like

Active Publication Date: 2011-05-18
北京亿灵医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Because cinepazide maleate raw materials and injections are extremely sensitive to light and have poor photostability, they need to be stored away from light and kept in airtight storage, which brings great inconvenience to the production, storage, transportation and use of medicines, and also Bring hidden dangers to clinical safety drug use

Method used

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  • Cinepazide acid addition salt and preparation method thereof
  • Cinepazide acid addition salt and preparation method thereof
  • Cinepazide acid addition salt and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] The preparation of embodiment 1 gluconate

[0083] Dissolve 20 g of cinepazide in 100 ml of ethanol, add 30% gluconic acid ethanol solution dropwise under stirring until the pH value is about 3, slowly add petroleum ether dropwise, continue stirring for 1 hour, filter, and wash with ethanol three times, Dry to obtain gluconate 23.9g, yield 82%.

[0084] 1 H-NMR (DMSO) δ: 2.03 (m, 4H), 2.72 (m, 4H), 3.12 (m, 4H), 3.32 (s, 2H), 3.39 (m, 3H), 3.51 (m, 4H), 3.69 (m, 2H), 3.74 (s, 3H), 3.78 (s, 6H), 6.29 (s, 2H), 7.09 (d, 1H), 7.26 (d, 1H), 10.38 (brs, 1H).

Embodiment 2

[0085] The preparation method of embodiment 2 malate

[0086] Dissolve 20 g of cinepazide in 100 ml of ethanol, add 30% malic acid ethanol solution dropwise under stirring until the pH value is about 3, slowly add petroleum ether dropwise, continue stirring for 1 hour, filter, and wash with ethanol three times, Dry to obtain malate 20.8g, yield 79%.

[0087] 1 H NMR (DMSO) δ: 2.01 (m, 4H), 2.04 (t, 1H), 2.09 (d, 2H), 2.68 (m, 4H), 3.09 (m, 4H), 3.25 (s, 1H), 3.30 (s, 2H), 3.49 (m, 4H), 3.69 (s, 3H), 3.79 (s, 6H), 6.27 (s, 2H), 7.03 (d, 1H), 7.25 (d, 1H), 10.35 ( brs, 2H).

Embodiment 3

[0088] The preparation method of embodiment 3 hydroxymethanesulfonate

[0089] Dissolve 20 g of cinepazide in 100 ml of ethanol, add 30% ethanol solution of hydroxymethanesulfonate dropwise under stirring until the pH value is about 2, slowly add petroleum ether dropwise, continue stirring for 1 hour, filter, and wash with ethanol After drying for three times, 18.5 g of hydroxymethanesulfonate was obtained, with a yield of 73%.

[0090] 1 HNMR (DMSO) δ: 2.04 (m, 4H), 2.56 (s, 2H), 2.77 (m, 4H), 3.15 (m, 4H), 3.34 (s, 2H), 3.49 (m, 4H), 3.80 ( s, 3H), 3.81 (s, 6H), 6.32 (s, 2H), 7.16 (d, 1H), 7.30 (d, 1H), 10.69 (brs, 1H).

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Abstract

The invention discloses a cinepazide organic acid medicinal salt and provides a preparation method and medicinal preparation of the cinepazide organic acid medicinal salt, werein,organic acid comprises gluconic acid, hydroxyl methanesulfonic acid, isethionic acid, ethyl sulfonic acid, benzene sulfonic acid, malic acid and oxalic acid,preferably gluconic acid. The cinepazide organic acid medicinalsalt is mainly used for treating and preventing cerebrovascular disease, cardiovascular disease and peripherial ascular disease. The cinepazide organic acid medicinal salt provided by the invention has the characteristics of good stability and good dissolvability, and is especially used for solving the defect of optical unstability of the maleic acid cinepazide.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a medicinal salt of cinepazide and a preparation method, dosage form and application thereof. Background technique [0002] Cardiovascular and cerebrovascular diseases are a general term for cardiovascular diseases and cerebrovascular diseases. Cardiovascular disease is mainly coronary heart disease, which can be manifested in various forms such as recessive heart disease, angina pectoris, myocardial infarction, myocardial sclerosis, and sudden cardiac death; A group of diseases with cerebral hemorrhagic or ischemic injury symptoms as the main clinical manifestations. In severe cases, disturbance of consciousness and limb paralysis may occur. It is the main disease causing death and disability. It is very important to treat cardiovascular and cerebrovascular diseases early and effectively to reduce the mortality and disability rate of patients. Therefore, it is an ...

Claims

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Application Information

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IPC IPC(8): C07D295/185C07C59/105C07C59/245C07C309/08C07C309/04C07C309/29C07C55/07A61K31/496A61P9/00A61P9/08A61P7/02
Inventor 关屹闫冬
Owner 北京亿灵医药科技发展有限公司
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