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High-safety medicinal composition of cinepazide, and preparation method and application thereof

A technology of cinepazide and composition, which is applied in the field of cinepazide medicinal composition and its preparation, and can solve problems such as ineffective reduction

Active Publication Date: 2012-01-11
BEIJING SIHUAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] 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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  • High-safety medicinal composition of cinepazide, and preparation method and application thereof
  • High-safety medicinal composition of cinepazide, and preparation method and application thereof
  • High-safety medicinal composition of cinepazide, and preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0067] The preparation of embodiment 1 cinepazide nitrogen oxide

[0068] 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%.

[0069] 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

[0070] The preparation of embodiment 2 cinepazide nitrogen oxides

[0071]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%.

[0072] 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

[0073] The preparation of embodiment 3 cinepazide nitrogen oxides

[0074] 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%.

[0075] MS (LC-MS) = 434.2 (M+H + ), 867.5 (2M+H + ).

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Abstract

The invention relates to a high-safety medicinal composition of cinepazide, and a preparation method and application thereof. The medicinal composition comprises cinepazide or pharmaceutically acceptable salt thereof and compounds, of which the content is less than 0.5 and which have the structure shown in the formula III. The medicinal composition of cinepazide and the preparations thereof have higher safety, effectiveness and stability and can effectively reduce or avoid adverse reactions, such as decreasing hemogram, of patients caused by the cinepazide. Moreover, the invention also separates, purifies and characterizes new nitrogen oxides of cinepazide. Complete research on the new nitrogen oxides of cinepazide shows that the toxicity of nitrogen oxides of cinepazide is far higher than that of the cinepazide, and the nitrogen oxides of cinepazide have the insecticidal activity different from that of the cinepazide; moreover, the research shows that the nitrogen oxides of cinepazide can cause the reduction of leukocytes of animals, even affect the formation and the differentiation of granulocytes, which are possibly the main reason for the cinepazide causing adverse reactions such as the decreasing hemogram of patients.

Description

[0001] This application is a divisional application of CN200910180174.X, a highly safe cinepazide pharmaceutical composition, its preparation method and its application, submitted on November 13, 2009. technical field [0002] 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 [0003] 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. [0004] 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 (...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61K9/08A61P9/00A61P9/08C07D295/185
Inventor 车冯升林善良范扶民霍彩霞
Owner BEIJING SIHUAN PHARMA