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Puerarin anhydrous spherical crystal and preparation method and application thereof

A technology of spherical crystals and puerarin, applied in the field of medicine, can solve problems such as unfavorable development of solid preparations, achieve good development prospects, simple operation, and improve fluidity and compressibility

Active Publication Date: 2020-10-30
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In order to solve the technical problem that the existing puerarin monohydrate crystals are not conducive to the development of solid preparations, the present invention provides a method for preparing spherical puerarin anhydrate crystals by the anti-solvent method, which does not require additional bridging agents and seed crystals Wait, it's easy to operate

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  • Puerarin anhydrous spherical crystal and preparation method and application thereof
  • Puerarin anhydrous spherical crystal and preparation method and application thereof
  • Puerarin anhydrous spherical crystal and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0049] Preparation of Spherical Crystals of Puerarin Anhydrate

[0050] Add 150 mL of acetonitrile to the crystallization container, place it in a constant temperature water bath to keep the temperature at 30°C, turn on the stirrer and keep the speed at 250 rpm; weigh about 1 g of puerarin, put it in a vial, add 10 mL of methanol, and ultrasonically dissolve the drug Dissolved, the resulting solution was added dropwise to the crystallization container, and the timer was started after the dropwise addition was completed, and the stirring was kept for 60 min. Suction filtration was performed on the suspension, and the solid was vacuum-dried at 25°C for 24 h, and the obtained dried solid particles were the product.

[0051] The appearance of the product is spherical, the Carr index is 10.92%, the angle of repose is 24.7°, and the average particle size is 75 μm.

Embodiment 2

[0053] Preparation of Spherical Crystals of Puerarin Anhydrate

[0054] Add 50 mL of acetonitrile to the crystallization vessel, place it in a constant temperature water bath to keep the temperature at 35 °C, turn on the stirrer and keep the speed at 500 rpm; weigh about 0.2 g of puerarin, put it in a vial, add 10 mL of methanol, and ultrasonically dissolve the drug Dissolved, the resulting solution was added dropwise to the crystallization container, and the timer was started after the dropwise addition was completed, and the stirring was kept for 90 min. The suspension was suction filtered, and the solid was vacuum-dried at 30°C for 12 h, and the obtained dried solid particles were the product.

[0055] The appearance of the product is spherical, the Carr index is 15.43%, the angle of repose is 28.7°, and the average particle size is 43 μm.

Embodiment 3

[0057] Preparation of Spherical Crystals of Puerarin Anhydrate

[0058] Add 150 mL of acetonitrile to the crystallization vessel, place it in a constant temperature water bath to keep the temperature at 20°C, turn on the stirrer and keep the rotation speed at 100 rpm; weigh about 1 g of puerarin, put it in a vial, add 5 mL of methanol, and ultrasonically dissolve the drug Dissolved, the resulting solution was added dropwise to the crystallization vessel, and the timer was started after the dropwise addition was completed, and the stirring was kept for 10 min. The suspension was suction filtered, and the solid was vacuum-dried at 20°C for 48 h, and the obtained dried solid particles were the product.

[0059] The appearance of the product is spherical, the Carr index is 18.48%, the angle of repose is 29.5°, and the average particle size is 84 μm.

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Abstract

The invention discloses a puerarin anhydrous spherical crystal and a preparation method and application thereof, and belongs to the technical field of medicines. By selecting a proper solvent system and controlling a proper temperature and a stirring rate, the puerarin anhydrous spherical crystal can be formed, the crystallization process is simple, convenient and fast, and the obtained sphericalproduct is round and smooth in particle, has a Karl index of about 10-18% and a repose angle of 24-31 degrees, and is good in flowability and compressibility. The anhydrous spherical crystal is different from commercially available puerarin monohydrate crystals in powder X-ray diffraction spectrogram, DSC spectrogram, TGA spectrogram and infrared spectrogram, and is a new solid form of puerarin. The invention provides an important practical value for the puerarin crystal form research and spherical crystal production and application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to spherical crystals of puerarin anhydrate and a preparation method and application thereof. Background technique [0002] Puerarin is an isoflavone compound that can be extracted from the dried roots of Pueraria lobata and Pueraria mirifica, and its chemical name is 8-β-D-glucopyranose-4′,7-dihydroxy Isoflavones, molecular formula C 21 h 20 o 9 , the chemical structure is as formula Ⅰ: [0003] . [0004] Studies have shown that puerarin has a wide range of pharmacological effects, such as: expanding coronary blood vessels, enhancing myocardial contractility, improving microcirculation; reducing blood sugar and blood lipids, scavenging free radicals; inhibiting the degradation of articular cartilage, protecting nerve cells, etc. Clinically, it is widely used in the treatment of hypertension, myocardial infarction, angina pectoris, ischemic stroke, diabetes and ...

Claims

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Application Information

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IPC IPC(8): C07D407/04A61K31/352A61P9/08A61P9/04A61P9/10A61P9/12A61P9/00A61P3/10A61P3/06A61P39/06A61P25/00A61P19/08
CPCC07D407/04A61P9/08A61P9/04A61P9/10A61P9/12A61P9/00A61P3/10A61P3/06A61P39/06A61P25/00A61P19/08C07B2200/13
Inventor 张建军孟文卉薛一凡钱帅高缘魏元锋
Owner CHINA PHARM UNIV
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