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Stevioside crystal with crystal form A and its preparation method and application

A steviol and crystal form technology, applied in the field of medicinal chemistry, can solve problems affecting drug stability, bioavailability and curative effect, appearance, solubility, melting point, dissolution, different biological effectiveness, steviol research, etc., to achieve The crystallization process is easy to control, the crystallinity is high, and the effect of easy operation

Active Publication Date: 2017-09-22
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Drug polymorphism exists widely in the process of drug development. It is an inherent characteristic of small organic molecules and one of the important factors affecting drug quality and clinical efficacy. Different crystal forms of the same drug have different effects on appearance, solubility, melting point, dissolution rate, Bioavailability and other aspects may be significantly different, thereby affecting the stability, bioavailability and efficacy of the drug
At present, there is no report to study the crystal form of steviol

Method used

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  • Stevioside crystal with crystal form A and its preparation method and application
  • Stevioside crystal with crystal form A and its preparation method and application
  • Stevioside crystal with crystal form A and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Mix 25g of steviol with a purity of 80% and 100mL of water, stir at 30rpm at 10°C for 24h to obtain a suspension of steviol; filter the above suspension, and dry the resulting solid in vacuum at 40°C to obtain a crystal form Form A white steviol crystals.

[0033] The filtrate obtained after filtering the above suspension was cooled to 40°C, and a white solid was precipitated, and the solid was dried at 100°C to obtain steviol crystals in the form of crystal form A.

Embodiment 2

[0035] Mix 15 g of steviol with a purity of 99.5% and 100 mL of 95% methanol aqueous solution, and stir at 10 rpm at 20°C for 1 hour to obtain a suspension of steviol; centrifuge the above suspension, and dry the obtained solid under vacuum at 25°C. White steviol crystals having the Form A form were obtained.

[0036] The filtrate obtained after the above suspension was centrifuged was cooled to 4°C, and a white solid was precipitated, and the solid was vacuum-dried at 25°C to obtain steviol crystals in the form of crystal form A.

Embodiment 3

[0038] Mix 35 g of steviol with a purity of 55% and 100 mL of 97% isopropanol, and stir at 20 rpm for 0.5 h at 40°C to obtain a suspension of steviol; centrifuge the above suspension, and dry the resulting solid under vacuum at 45°C Thereafter, white steviol crystals in the form of crystal form A were obtained.

[0039] Then the clear solution obtained by centrifuging the suspension was cooled to 10°C, and a white solid was precipitated, and the filtered solid was vacuum-dried at 45°C to obtain steviol crystals in the form of crystal form A.

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Abstract

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a stevioside crystal with the crystal form A and its preparation method and application. The stevioside crystal with the crystal form A is subjected to X-ray powder diffraction analysis by using Cu-Kalpha rays, the 20 angle expressed in degrees at least has obvious characteristic diffraction peaks at 7.76, 12.12, 14.18, 15.66, 16.04, 16.62, 19.2, 20.78, 24.00, 27.08, 31.72, 35.32 and 35.70 positions. XRD, DSC, TGA and other solid chemical analysis means are applied to show characteristics of the crystal, it is found that the crystal has the advantages of being high in crystallinity, high in stability and the like, and the crystal is suitable for more extensive application areas. The preparation method of the crystal is simple and easy to operate, the crystallization process is easy to control, the selectivity is good, and the target crystal form can be stably obtained.

Description

【Technical field】 [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a steviol crystal with crystal form A, its preparation method and application. 【Background technique】 [0002] Stevioside is a representative compound group in the natural, high-sweet, non-nutritive sweetener family. It enjoys the reputation of the third sugar source in the world. The sweetness component is endo-kaurenoic acid / ester Tetracyclic diterpenoids, which have the same tetracyclic diterpenoid structure aglycone steviol (steviol), the structural formula is as follows: [0003] [0004] Steviol is a high value-added drug synthesis intermediate, and it also has certain biological activities, such as tumor suppression, through the inhibition of lipopolysaccharide LPS-mediated release of TNF-α, IL-1β and IL-6 , and through the IκBα / NF-κB signal transduction pathway to affect the gene expression of cytokines, weaken the release of LPS-induced infl...

Claims

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Application Information

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IPC IPC(8): C07C51/43C07C62/32A61P3/10A61P29/00A61P35/00
CPCC07B2200/13C07C51/43C07C62/32
Inventor 夏咏梅陈俊名张童童方云彭庆蕤
Owner JIANGNAN UNIV
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