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Co-amorphous substance of puerarin nicotinamide

An amorphous, plain nicotinamide technology, applied in the field of medicine, can solve problems such as delayed allergic reactions, frequent, and limited clinical applications

Inactive Publication Date: 2018-05-04
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the only route of administration of puerarin is intravenous injection, but frequent and long-term injection will cause side effects such as delayed hypersensitivity, which greatly limits its clinical application

Method used

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  • Co-amorphous substance of puerarin nicotinamide
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  • Co-amorphous substance of puerarin nicotinamide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Example 1: Preparation of puerarin nicotinamide co-amorphous

[0067] Add 2.00g of puerarin and 0.58g of nicotinamide into 50mL of methanol, and ultrasonically dissolve at room temperature to obtain a clear solution. The clear solution is rotatated to evaporate the solvent under reduced pressure at 35°C, and dried in vacuum at 25°C for 12h to obtain 2.34g of white powder.

Embodiment 2

[0068] Example 2: Preparation of puerarin nicotinamide co-amorphous

[0069] Add 2.00g of puerarin and 0.58g of nicotinamide into 50mL of ethanol, and ultrasonically dissolve at room temperature to obtain a clear solution. The clear solution is evaporated under reduced pressure at 50°C and dried in vacuum at 25°C for 12 hours to obtain 2.28g of white powder.

Embodiment 3

[0070] Example 3: Preparation of puerarin nicotinamide co-amorphous

[0071] Add 2.00g of puerarin and 0.58g of nicotinamide into 50mL of methanol-ethanol (50:50, v / v) mixed solvent, and ultrasonically dissolve at room temperature to obtain a clear solution. °C and vacuum dried for 12 hours to obtain 2.32 g of white powder.

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Abstract

The invention relates to a co-amorphous substance of puerarin nicotinamide, which can significantly improve dissolubility of an insoluble medicine, namely puerarin. The co-amorphous substance is in anamorphous state completely different from that of a puerarin crystal, and a melting point, an X-ray powder diffraction pattern, a DSC (differential scanning calorimetry) spectrogram and an infrared spectrum of the co-amorphous substance are different from those of the puerarin crystal. With the adoption of Cu-k alpha radiation, an X-ray powder diffraction spectrum expressed by 2 theta degree hasno sharp diffraction peak. A glass transition temperature of the substance is approximately 64.1 DEGC. A dissolving experiment result shows that the co-amorphous substance can increase an intrinsic dissolution rate of the puerarin by about 78 times and keep an oversaturation state higher than the dissolvability of the puerarin crystal for 24h.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to co-amorphous puerarin and nicotinamide formed by combining puerarin and nicotinamide at a molar ratio of 1:1 and a preparation method thereof. Background technique [0002] Puerarin, the chemical name is 8-β-D-glucopyranose-4′, 7-dihydroxyisoflavone, and its chemical structure is as follows: [0003] [0004] Puerarin has a wide range of pharmacological effects, such as dilating blood vessels, protecting the heart, protecting nerves, anti-cancer, promoting bone formation and reducing insulin resistance, etc., and can be used to treat cardiovascular and cerebrovascular diseases (such as angina pectoris, coronary heart disease), diabetes and diabetic complications and cancer etc. Puerarin has rich drug sources, good curative effect, wide safety range, and broad development prospects. However, it belongs to Class IV drugs in the biopharmaceutical classification syst...

Claims

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Application Information

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IPC IPC(8): C07D407/04C07D213/82
CPCC07D213/82C07D407/04
Inventor 高缘杨思彤钱帅张建军
Owner CHINA PHARM UNIV
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