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Amorphous calcium bucladesine sterile powder

A technology of calcium dibutyryl cyclic adenosine monophosphate and sterile powder, which is applied in the field of preparation of amorphous dibutyryl cyclic adenosine calcium monophosphate sterile powder, can solve problems such as allergic reactions and abnormal vision, and achieve high separation, impurity types and The effect of content reduction, purity and stability improvement

Inactive Publication Date: 2015-01-07
北京赛盟医药科技发展有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, my country has only approved the freeze-dried powder preparation of dibutyryl cycloadenosine calcium produced by Shanghai No. 1 Biochemical for clinical application, but the literature: "A case of allergic reaction induced by dibutyryl cycloadenosine calcium for injection" Zhongnan Pharmaceutical Sciences 2013 November Volum

Method used

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  • Amorphous calcium bucladesine sterile powder
  • Amorphous calcium bucladesine sterile powder
  • Amorphous calcium bucladesine sterile powder

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Preparation of Sterile Powder of Amorphous Calcium Dibutyryl Cycloadenosine Phosphate

[0041] (1) Add triethylamine water (1:5, v / v) solution to 200.0g cyclic adenosine monophosphate, stir at 30-40°C, evaporate to dryness under reduced pressure, add 1000ml pyridine, repeat once, vacuum decompression Dry to obtain intermediate 1, and detect the content of the intermediate.

[0042] (2) Take 250.0 g of the above intermediate 1 and add 10-15 times the volume of pyridine and 5-10 times the volume of n-butyric anhydride for acylation, and stir at 30-35 ° C. Absorb the acid anhydride with an appropriate amount of diethyl ether at low temperature, extract with 2-3 times the volume of water, repeat two to three times, and concentrate the obtained dibutyrylcyclic adenosine triethylamine saline solution under reduced pressure to dryness to obtain intermediate 2;

[0043] (3) The above intermediate 2 was dissolved with 3-5 times (m / v) ethanol solution, and an equivalent amount o...

Embodiment 2

[0049] Example 2 Amorphous calcium dibutyryl cyclic adenosine monophosphate sterile powder preparation

[0050] Dibutyryl cyclic adenosine monophosphate calcium aseptic powder prepared in the above example is divided into vials in a sterile environment, 20 mg / bottle.

[0051] According to the Chinese Pharmacopoeia 2010 edition second appendix I B inspection items for injection of sterile powder inspection items, three consecutive batches of products were inspected. The inspection indicators are visible foreign matter, insoluble particles, sterility test, and bacterial endotoxin, all of which meet the requirements of the Pharmacopoeia.

Embodiment 3

[0052] Example 3 Amorphous calcium dibutyryl cyclic adenosine monophosphate sterile powder preparation

[0053] The amorphous calcium dibutyryl cyclic adenosine monophosphate sterile powder prepared in Example 1 is for subsequent use;

[0054] Glycine refining: first dissolve crude glycine in hot water, add powdered activated carbon for adsorption and decolorization, and then separate the activated carbon by filtration;

[0055] Under a sterile environment, the above solutions are passed through 0.45 μm and 0.22 μm microporous membranes respectively, and the filtrate is heated and concentrated. When the volume of the concentrated solution is 1 / 2 of the original volume, cool to room temperature, and then add 3-4 times the volume of non-toxic Glycine is crystallized and precipitated with bacterial ethanol or methanol, and dried to obtain sterile refined glycine;

[0056] Under a sterile environment, mix amorphous calcium dibutyryl cyclic adenosine monophosphate and glycine ac...

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Abstract

The invention provides calcium bucladesine sterile powder and a preparation thereof. The calcium bucladesine sterile powder is characterized in that the calcium bucladesine sterile powder is in an amorphous form state and has the purity of over 98 percent. Furthermore, the invention also provides amorphous calcium bucladesine sterile powder and a preparation method of a calcium bucladesine sterile powder preparation. The preparation method comprises the following steps: purifying chemically synthetic a crude calcium bucladesine solution through preparative high pressure liquid chromatography, concentrating, filtering, and performing freeze drying, thereby obtaining the sterile powder, wherein the X-ray powder diffraction and infrared absorption spectrum prove that the sterile powder refers to the amorphous calcium bucladesine sterile powder. Compared with a commercially available mixed crystal form calcium bucladesine powder-injection preparation, the amorphous calcium bucladesine sterile powder is high in content and high in stability. The amorphous calcium bucladesine sterile powder and the preparation thereof provided by the invention are used for treating angor pectoris, myocardial infarction, myocarditis, cardiogenic shock, immune genetic diseases such as lupus erythematosus and parapsoriasis guttata as well as other cardiovascular diseases.

Description

technical field [0001] The invention relates to the field of drug synthesis and drug preparations, in particular to the preparation of an amorphous calcium dibutyryl cyclic adenosine monophosphate sterile powder. Background technique [0002] Dibutyryl cyclic adenosine monophosphate calcium is a nucleotide derivative, as a G protein-coupled receptor drug, it can simultaneously activate protein kinase A and protein kinase C. Protein kinase is an allosteric enzyme that is catalyzed by two Subunit and two regulatory subunits, the catalytic subunit can catalyze protein (or enzyme) phosphorylation. Therefore, calcium dibutyryl cyclic adenosine monophosphate can catalyze the most basic biochemical metabolism in the human body - oxidative phosphorylation reaction and tricarboxylic acid cycle, make most proteins and enzymes active, activate various reactions in the human body, and generate a large amount of ATP at the same time, Improve cell and energy metabolism, so as to realize ...

Claims

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Application Information

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IPC IPC(8): C07H19/213C07H1/00A61K9/14A61K9/19A61K31/7076A61P9/10A61P9/02A61P17/06A61P37/02A61P9/00
CPCC07H19/207A61K9/0019A61K9/14A61K9/19C07B2200/13C07H1/00
Inventor 关屹闫冬
Owner 北京赛盟医药科技发展有限公司
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