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Carbazochrome sodium sulfonate pharmaceutical composition with good stability and high safety as well as preparation method and application thereof

The technology of sodium carboxylate and composition is applied in the field of sodium carboxylate pharmaceutical composition and preparation thereof, which can solve the problems of intramuscular injection and the like, and achieve the effect of high stability

Active Publication Date: 2018-12-07
CHENGDU TIANXIN PHARMA HEALTH CARE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The adrenochrome monosemicarbazone (Adrenochrome monosemicarbazone, Adrenoxyl, Carbazochrome, carbacol, adrenochrome semicarbazone) modified by the chemical structure of adrenaline has been commercialized due to its improved stability, and is suitable for patients with capillary damage and increased permeability. Hemorrhage caused by epistaxis, retinal hemorrhage, hemoptysis, gastrointestinal bleeding, hematuria, hemorrhoids and uterine bleeding, etc., also used for thrombocytopenic purpura, can be taken orally and injected, but only intramuscular injection can be used for injection

Method used

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  • Carbazochrome sodium sulfonate pharmaceutical composition with good stability and high safety as well as preparation method and application thereof
  • Carbazochrome sodium sulfonate pharmaceutical composition with good stability and high safety as well as preparation method and application thereof
  • Carbazochrome sodium sulfonate pharmaceutical composition with good stability and high safety as well as preparation method and application thereof

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Experimental program
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preparation example Construction

[0059] The preparation of embodiment 1 formula III compound

[0060] Take 10g of sodium carbosulfonate, add 500ml of 50% ethanol aqueous solution, heat and stir to dissolve, add 10ml of triethylamine, reflux in water bath for 60 minutes, and use preparative high-efficiency liquid phase separation for the reflux liquid, and the mobile phase is acetonitrile-ammonium dihydrogen phosphate buffer Liquid, receive product fraction, promptly obtain 0.1g formula III compound. HPLC peak area normalization method, the measured content is not less than 98%. MS (high resolution mass spectrum) is 271.9961 ([M+Na] + ).

[0061] Table 1 HPLC determination result table

[0062] Retention time (minutes)

Peak area

Peak area(%)

8.280

1109907760

98.61

12.533

15674886

1.39

total

1125582646

100.00

[0063] Table 2 1 H NMR and 1 H- 1 H COZY measurement analysis table

[0064]

[0065] The preparation of embodiment 2 f...

Embodiment 3

[0069] Example 3 Toxicity study of compound of formula III

[0070]Using L929 cell line (ATCC CCL1 [NCTC clone 929 (mouse fibroblast)]), sodium carbosulfate (provided by Jiangsu Hanstone Pharmaceutical Co., Ltd., refined to a purity of 99.9%, does not contain the compound of formula III ) and the compound of formula III (the present invention, with a purity of 99.9%) were incubated with L929 cells for 24h, 48h, and 72h (final concentrations were respectively 10, 5, 2.5, 1.25, 0.625, 0.3125, 0.15625, and 0.078125mg / ml), using The cell viability of each test product at different time points was measured by MTT Assay, and the IC50 value of the half maximal inhibitory concentration at each time point was calculated by Bliss method. Results: the IC50 value of sodium carbosulfonate was 3.87 mg / ml, and the IC50 value of the compound of formula III was 0.02 mg / ml. Result shows that the IC50 value of carbosulfonate sodium is about 194 times of formula III compound, and the cytotoxic...

Embodiment 4

[0071] Example 4 Toxicity Study of Sodium Carbosulfonate and Its Composition

[0072] Adopt L929 cell line, test drug carbosulfonate (provided by Jiangsu Hanstone Pharmaceutical Co., Ltd., refined into 99.9% purity, does not contain formula III compound) and formula III compound (the present invention, purity 99.9%) Composition groups with weight ratios of 1:0.1%, 1:0.25%, 1:0.5%, 1:0.75%, 1:1%, 1:1.5%, and 1:2% (hereinafter referred to as "compositions") Before administration, the test drug was dissolved in water for injection, and diluted to the required concentration according to the dosage requirements (wherein the final concentration of sodium carbosulfonate was 1mg / ml), and the colorimetric method of tetramethylazozolium salt (MTT) was adopted. Assay) measured the cell viability of each test product at different time points.

[0073] Table 4 Cytotoxic reaction grading judgment table

[0074] level

Relative survival rate (%)

0

≥100

1

...

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Abstract

The invention provides a carbazochrome sodium sulfonate pharmaceutical composition with good stability and highsafety as well as a preparation method and application thereof. The pharmaceutical composition contains carbazochrome sodium sulfonate and a compound represented by a formula III as shown in the specification, wherein the content of the compound is less than 0.5%.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a drug composition of sodium carbosulfonate with good stability and high safety, a preparation method thereof and an application thereof. Background technique [0002] It is known in the prior art that the physiological hemostatic mechanism includes: coagulation factor, platelet factor, vascular factor and fibrinolytic factor, and 4 factors are closely related, and any deficiency of any one of them will cause bleeding. According to the classification of hemostatic drugs commonly used in clinical practice, they can be divided into procoagulant drugs, antifibrinolytic drugs, and drugs acting on blood vessels. [0003] The first category, procoagulant drugs mainly include phensulfame, hemocoagulase, vitamin K1 and so on. The second category, antifibrinolytic drugs, mainly include tranexamic acid, ethylenediamine diacetamidoacetic acid, aminomethylbenzoic acid and aminocaproic ac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/404C07D209/30A61P7/04G01N30/02
CPCA61K31/404A61P7/04C07D209/30G01N30/02
Inventor 张海杨勇徐海英万树伦罗丹谢克梅
Owner CHENGDU TIANXIN PHARMA HEALTH CARE CO LTD
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