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Cinepazide medicinal composition with high safety, preparation method and application thereof

A technology of cinepazide and composition, which is applied in the field of cinepazide pharmaceutical composition and its preparation, and can solve problems such as not effectively reducing

Active Publication Date: 2010-05-19
BEIJING SIHUAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, the above-mentioned quality control measures have not effectively reduced or avoided the decline in blood images of patients caused by cinepazide.

Method used

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  • Cinepazide medicinal composition with high safety, preparation method and application thereof
  • Cinepazide medicinal composition with high safety, preparation method and application thereof
  • Cinepazide medicinal composition with high safety, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Example 1 Preparation of cinepazide nitrogen oxide

[0067] Dissolve 2 grams of cinepazide in 100 ml of dichloromethane, add 10 grams of peracetic acid, stir until the reaction is complete, filter, spin the filtrate, recrystallize with ethanol, and then freeze-dry to obtain 0.52 g of cinepazide special nitrogen oxides. HPLC peak area normalization method, the measured content is not less than 98%.

[0068] 1 H NMR (300MHz, CDCl 3 )δ (ppm): 7.615 (d, 1H) 6.731 (d, 1H) 6.610 (s, 2H) 3.801 (m, 1H), 4.012 (m, 2H), 4.131 (m, 1H) 4.674 (d, 1H) , 4.278(d,1H)3.907(s,6H)3.882(s,3H)3.251(d,2H),3.589(d,2H)3.504(t,2H)4.137(t,2H)1.914(m,2H) , 2.015(m, 2H)

Embodiment 2

[0069] Example 2 Preparation of cinepazide nitrogen oxide

[0070]Dissolve 2 grams of cinepazide in 100ml of methanol, add 5 grams of peroxybenzoic acid, stir until the reaction is complete, filter, spin the filtrate, and use preparative high-efficiency liquid phase separation, mobile phase is methanol-water, gradient wash Take off and receive the product fraction to obtain 0.3 g of cinepazide nitrogen oxide. HPLC peak area normalization method, the measured content is not less than 99%.

[0071] 1H NMR (600MHz, DMSO) δ (ppm): 7.492 (d, 1H) 7.238 (d, 1H) 7.060 (s, 2H) 4.306 (dd, 2H), 4.090 (s, 2H), 3.913 (m, 1H) 3.835(s, 6H), 3.723(m, 1H) 3.689(s, 3H) 3.641(m, 3H), 3.489(s, 1H) 3.311(t, 2H) 3.186(m, 2H) 1.853(m, 2H) , 1.776(m, 2H)

Embodiment 3

[0072] Example 3 Preparation of cinepazide nitrogen oxide

[0073] Dissolve 5 g of cinepazide maleate in 25 ml of water, add 25 ml of 25% hydrogen peroxide, stir and react at room temperature for 5 days, use preparative high-efficiency liquid phase separation, mobile phase is acetonitrile-water, gradient elution, receive The fraction of the product obtained 500 mg of cinepazide nitrogen oxide. HPLC peak area normalization method, the measured content is not less than 99%.

[0074] MS (LC-MS) = 434.2 (M+H + ), 867.5 (2M+H + ).

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Abstract

The invention relates to a medicine composition with high safety, a preparation method and an application thereof. The medicine composition contains cinepazide or salt thereof which is acceptable in pharmacy and a structural compound which has the content not higher than 0.5% and is shown in the formula (III). The cinepazide medicine composition and a preparation thereof have better safety, effectiveness and stability and can effectively lower or avoid the adverse reactions of hemogram lowering and the like of a patient caused by the cinepazide. Furthermore, the invention also separates, purifies and characterizes a novel cinepazide nitrogen oxide, researches the novel cinepazide nitrogen oxide fully and discovers that the toxicity of the compound is far greater than that of the cinepazide and the compound has an insecticidal activity which is different from that of the cinepazide. Meanwhile, the research discovers that the cinepazide nitrogen oxide can cause the leukopenia of animals, even influences the formation and the differentiation of granular cells and is possibly a main reason of the adverse reactions of the hemogram lowering and the like of the patient caused by the cinepazide.

Description

technical field [0001] The invention belongs to cardiovascular and cerebrovascular expansion drugs, and in particular relates to a high-safety cinepazide medicinal composition, a preparation method thereof and an application thereof. Background technique [0002] Cardiovascular and cerebrovascular diseases, like cancer, have become common and frequently-occurring diseases that seriously threaten people's health. Therefore, the preparation and selection of safer and more effective cardiovascular and cerebrovascular drugs has become an important research topic in the field of medicine. [0003] Cinepazide is a cardiovascular and cerebrovascular dilating drug. It has been widely used in countries all over the world because of its definite curative effect. Its chemical name is (E)-1-{4-[(3′,4′,5′- Trimethoxycinnamoyl)]-1-piperazine}acetylpyrrolidine, having the following structure: [0004] Formula (I). [0005] Cinepazide is mainly used in the prevention and treatment of t...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K9/08A61P9/00A61P9/08
Inventor 车冯升林善良范扶民霍彩霞
Owner BEIJING SIHUAN PHARMA
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