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Glycyrrhetinic acid crystal type C, its preparation method and its application in pharmaceutical composition or health care product

A technology of glycyrrhetic acid and health care products, which is applied in the directions of drug combinations, steroids, medical preparations containing active ingredients, etc.

Active Publication Date: 2016-04-27
北京健坤和医药科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This patent relates to the method for preparing glycyrrhetinic acid by microwave technology, not the crystal form preparation of glycyrrhetinic acid

Method used

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  • Glycyrrhetinic acid crystal type C, its preparation method and its application in pharmaceutical composition or health care product
  • Glycyrrhetinic acid crystal type C, its preparation method and its application in pharmaceutical composition or health care product
  • Glycyrrhetinic acid crystal type C, its preparation method and its application in pharmaceutical composition or health care product

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preparation example Construction

[0040] According to the preparation method of glycyrrhetinic acid crystal type C according to the present invention, it is characterized in that the glycyrrhetinic acid raw material is completely dissolved at a temperature of 15°C to 80°C using a single solvent of methanol, and then heated at an ambient temperature of 4°C to 80°C. Glycyrrhetinic acid crystal type C is obtained through the recrystallization preparation process under the condition of ambient humidity of 10%-75% and normal pressure or vacuum pressure.

[0041] According to the preparation method of glycyrrhetinic acid crystal type C according to the present invention, it is characterized in that after mixing any two or more of methanol, n-hexane, cyclohexane, and water, the mixture is mixed at a temperature of 15°C to 80°C. Glycyrrhetinic acid raw materials are completely dissolved, and glycyrrhetinic acid crystal type C is obtained through a recrystallization preparation process under the conditions of ambient te...

Embodiment 1

[0049] The preparation method of glycyrrhetinic acid crystal type C sample 1 :

[0050] The preparation method of crystal type C sample of glycyrrhetinic acid is characterized in that 20 ml of methanol solvent is used to completely dissolve 500 mg of glycyrrhetinic acid raw material at 25 ° C, and the solvent is removed under vacuum conditions at a temperature of 40 ° C to prepare glycyrrhetinic acid Acid crystal type C solid sample, its powder X-ray diffraction pattern and figure 1 unanimous.

[0051] The preparation method of the crystal type C sample of glycyrrhetinic acid 2 :

[0052] The preparation method of crystal type C sample of glycyrrhetinic acid is characterized by using a mixed solvent of 20ml of methanol and 20ml of n-hexane to completely dissolve 500mg of glycyrrhetinic acid raw material at a temperature of 40°C, then standing at 25°C to precipitate a solid, and then vacuum Filter and dry, prepare and obtain glycyrrhetinic acid crystal type C solid sampl...

Embodiment 2

[0058] Glycyrrhetinic acid crystal form C absorption characteristics and blood concentration characteristics in rats :

[0059] SD rats with a body weight of 230 ± 5g were reared under conventional feeding conditions, free to drink water, and after fasting for 12 hours, the glycyrrhetinic acid crystal type C solid prepared in Example 1 was administered by intragastric administration at 200 mg / kg, before administration. And 0.083, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 (h) after administration, about 0.4ml of blood was collected from the orbit, centrifuged at 4,000rpm for 15min to prepare plasma. Take 150 μl of plasma, add 200 μl of methanol, vortex for 1 min, centrifuge at 13400 rpm for 15 min, absorb the supernatant layer, filter through a 0.45 μm microporous membrane, take 20 μl for HPLC detection, AligentXDB-C18 (150×4.6mm, 5 μm), mobile phase Methanol: 0.4% acetic acid aqueous solution = 90:10, flow rate: 1ml / min, detection wavelength: 254nm.

[0060] From the results...

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Abstract

The invention relates to a glycyrrhetinic acid crystal type C, a preparation method and use thereof in pharmaceutical compositions or health-care products. The invention further relates to use of the glycyrrhetinic acid crystal type C in preparing anti-inflammatory, antibacterial, anti-tumor, antiviral, antiallergic and anti-ulcer pharmaceutical compositions or health-care products.

Description

technical field [0001] The present invention relates to a new glycyrrhetinic acid crystal type C and its preparation method, also relates to its pharmaceutical composition or health product, and its anti-inflammatory, antibacterial, anti-tumor, anti-viral, anti-allergic, anti-inflammatory Application in pharmaceutical composition or health product for ulcer. Background technique [0002] Glycyrrhetinic acid (GlycyrrhetinicBcid) molecular structure is as follows: [0003] [0004] In the Chinese patent CN101899081A, the "synthesis method of glycyrrhetinic acid ester derivatives and deoxyglycyrrhetinic acid ester compounds" invented by Zhang Aiming et al., which involves the preparation method of glycyrrhetinic acid ester derivatives, does not involve glycyrrhetinic acid compounds . [0005] In the Chinese patent CN1563073, the "preparation method of glycyrrhetinic acid" invented by Fan Yunge et al. is recorded, which involves the preparation method of glycyrrhetinic acid...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00A61K31/56A61P29/00A61P31/04A61P35/00A61P31/12A61P37/08A61P1/04A23L33/00
Inventor 杜冠华吕扬王守宝张丽郭永辉田硕
Owner 北京健坤和医药科技有限公司
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