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Mangiferin aglycone crystal forms, and composition, preparation method and application thereof

An aglycone crystal and composition technology, applied in the field of medicinal chemistry, can solve the problems of appearance, physical and chemical properties and biological activity differences, affecting drug stability, solubility and bioavailability, affecting preparation processing performance, etc.

Active Publication Date: 2012-02-15
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patents CN10127787, CN102002031A and CN201110004591.6 disclose its preparation and synthesis methods, but do not involve its crystal form
Different crystal forms of the same compound have the same chemical composition but different microscopic crystal structures, which lead to differences in their appearance, physicochemical properties and biological activities
These characteristics directly affect the preparation performance of the drug, and will affect the stability, solubility and bioavailability of the drug, which in turn will affect the quality, safety, effectiveness and application of the drug

Method used

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  • Mangiferin aglycone crystal forms, and composition, preparation method and application thereof
  • Mangiferin aglycone crystal forms, and composition, preparation method and application thereof
  • Mangiferin aglycone crystal forms, and composition, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1: Preparation of Form I (Form I was prepared with 70% ethanol without adding seed crystals)

[0047] Add 500mL of 70% ethanol and 150g of water to 5.5g of mangiferin aglycone, heat and reflux for 2 hours, stop heating, let it cool down to 50°C naturally, control the temperature at 45±5°C for 2 hours, the product begins to have a small amount of crystallization, The temperature was lowered to 10±5° C. at a cooling rate of 10-20° C. per hour, and the crystallization was continued for 8 hours. The crystals were filtered out, washed with a small amount of absolute ethanol, and vacuum-dried at 70±5° C. to obtain 5.1 g of mangiferin aglycone crystal form I, with a yield of 93%.

[0048] Carry out X-ray powder diffraction and infrared spectrum detection to the obtained mangiferin aglycone crystal form I, the results are shown in figure 1 and image 3 . Infrared spectrum of mangiferin aglycon form I at 3346, 3272, 1609, 1478, 1423, 1288, 1189, 1170, 1075, 812 and 56...

Embodiment 2

[0051] Example 2: Preparation of Form I (Form I was prepared with absolute ethanol without adding seed crystals)

[0052] Add 500mL of absolute ethanol to 10g of mangiferin aglycone, heat to reflux to dissolve, stop heating, let it cool down to 45°C naturally, control the temperature at 45±5°C for 2 hours, and then drop it by 10-20°C per hour The cooling rate brought the temperature down to 10±5°C, at which temperature crystallization was continued for 6 hours. The crystals were filtered out, washed with a small amount of absolute ethanol, and vacuum-dried at 70±5° C. to obtain 8.9 g of mangiferin aglycone crystal form I, with a yield of 89%. X-ray diffraction and infrared spectrum detection are consistent with the results of Example 1.

Embodiment 3

[0053] Example 3: Preparation of crystal form I (preparation of crystal form I with 90% methanol without adding seed crystals)

[0054] Add 400mL of 90% methanol to 10g of mangiferin aglycone, heat to reflux to dissolve it, stop heating, let it cool down to 30°C naturally, put it in the refrigerator and lower the temperature to 5±2°C at a cooling rate of 15-20°C per hour After 10 hours of crystallization, the crystals were filtered out, washed with a small amount of anhydrous methanol, and dried in vacuum at 60±5° C. to obtain 8.7 g of mangiferin aglycone crystal form I, with a yield of 87%. X-ray diffraction and infrared spectroscopic analysis are consistent with the results of Example 1.

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Abstract

The invention relates to the field of pharmaceutical chemistry, and discloses mangiferin aglycone crystal forms I and II, and a pharmaceutical composition, preparation method and application thereof. The mangiferin aglycone crystal form I or crystal form II provided by the invention has the advantages of single crystal form, high purity, high stability, high solubility and high bioavailability, can lower the serum uric acid concentration, and can be used for preparing medicines for preventing and treating hyperuricemia. The preparation method of the mangiferin aglycone crystal form I or crystal form II has the advantages of accessible raw materials and low production cost, and is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to the crystal form of mangiferin aglycon, its composition, preparation method and application. Background technique [0002] Mangiferin, English name norathyriol, its structural formula is as follows: [0003] [0004] In recent years, studies have found that mangiferin is an active metabolite of mangiferin, which has pharmacological effects such as anti-oxidation, inhibition of PTP1B activity, anti-tumor, lowering uric acid and anti-gout. Chinese patents CN10127787, CN102002031A and CN201110004591.6 disclose its preparation and synthesis methods, but do not involve its crystal form. So far, there are no reports at home and abroad on the crystal form of mangiferin aglycon, its preparation method and use. [0005] Crystal form is one of the important factors affecting the quality, curative effect and processing performance of pharmaceuticals. Polymorphism refers to the pheno...

Claims

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Application Information

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IPC IPC(8): C07D311/86A61K31/352A61P19/06
Inventor 周荣光杨兆祥普俊学
Owner KPC PHARM INC
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