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Quzhazhigan crystal and preparation method and application thereof

A technology for tristilbene and crystals, applied in the field of tristilbene crystals and their preparation, can solve the problems affecting drug quality, safety and effectiveness, affecting drug stability, solubility and bioavailability, affecting drug processing and Production and other problems, to achieve the effect of high solubility and bioavailability, single crystal form, and low production cost

Active Publication Date: 2013-12-11
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These characteristics directly affect the processing and production of the drug, and will affect the stability, solubility and bioavailability of the drug, so the polymorphic form of trizapereside affects the quality, safety and effectiveness of the drug, and is not suitable for use as a drug

Method used

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  • Quzhazhigan crystal and preparation method and application thereof
  • Quzhazhigan crystal and preparation method and application thereof
  • Quzhazhigan crystal and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: X-ray powder diffraction, infrared spectroscopic analysis and differential scanning calorimetry analysis conditions

[0025] X-ray powder diffraction analysis: the detection instrument is D / max-3A X-ray diffractometer; the detection conditions are Cu target Kα1 ray, voltage 35kV, current 25mA, divergence slit 1°, anti-scatter slit 1°, receiving slit The slits are 0.3mm and 0.3mm, and the 2θ range is 3° to 60°; the detection basis is the general rules of X-ray diffraction methods for polycrystals with rotating targets JY / T009-1996.

[0026] Infrared spectroscopy (IR) analysis: the detection instrument is a Perkin Elmer FT-IR spectrophotometer; the detection condition is KBr pellets.

[0027] Differential scanning calorimetry (DSC) analysis: The detection instrument is DSC204 differential scanning calorimeter from NETZSCH, Germany; the detection condition is N2 as the atmosphere, 20mL / min, the temperature is raised from room temperature to 250°C at 10°C / min,...

Embodiment 2

[0028] Embodiment 2: Preparation of Trizaperoside crystals

[0029] Take P 2 o 5 Add 120mL of water, then add 1.5% (that is, 0.3g) needle active boiled for 3min, filter while hot, stand at 4°C for 6h, and pump out the crystallization solution Filter, P 2 o 5 The desiccant was dried under reduced pressure for 12 hours to obtain 17.1 g of tristilbene crystals, and the yield of tristilbene crystals was 85.5%. Carry out X-ray powder diffraction, infrared spectrum analysis and differential scanning calorimetry analysis to the obtained trizapereside crystal, the results are shown in Figure 1~3 . Wherein, the calculation formula of the tristilbeside crystal yield is: tristilbene crystal yield=tristilbene crystal amount / tristilbene input amount×100%.

[0030] Depend on figure 1It can be seen that the X-ray powder diffraction pattern of the tristilbene crystal prepared in the present invention is 5.8, 6.7, 8.4, 9.3, 12.8, 13.5, 14.0, 15.2, 17.4, 18.7, 19.4, 23.6, 25.7, 27.0, 27...

Embodiment 3

[0032] Take P 2 o 5 As a desiccant, add 120 mL of the solvent listed in Table 1 to 20 g of tristilbene raw material (purity 98%) after vacuum drying for 12 hours, then add 1.5% (ie 0.3 g) of the active needle and boil for 3 minutes. Filter, stand at 4°C for 6h, suction filter the crystallization solution, P 2 o 5 The desiccant was dried under vacuum and reduced pressure for 12 hours to obtain tristilbene crystals, the yield and yield of tristilbene crystals were calculated, and the obtained tristilbene crystals were analyzed by differential scanning calorimetry and X-ray Diffraction and infrared spectroscopic analysis, the results are shown in Table 1. X-ray diffraction and infrared spectroscopic analysis are consistent with the results of Example 2, not shown here.

[0033] Table 1 Solvent Selection

[0034]

[0035] As can be seen from the results in Table 1, when using 15% ethanol, 30% ethanol, 45% ethanol, 15% methyl alcohol, 30% methyl alcohol, 45% methyl alcohol ...

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PUM

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Abstract

The invention relates to the pharmaceutical chemistry field, and discloses a quzhazhigan crystal and a preparation method and an application thereof. The quzhazhigan crystal of the invention has a single crystal form, high purity, good stability, high solubility and bioavailability. The preparation method of the quzhazhigan crystal of the invention has simple operation, easily available raw materials, low production cost, continuous operation, and is applicable to mass preparation of the quzhazhigan crystal.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a tristilbene crystal, a preparation method and application thereof. Background technique [0002] Tristilbene, whose chemical name is (E)-1-(3,5-dihydroxyphenyl)-2-(4-hydroxy-3-O-β-D-glucopyranosephenyl)ethylene or 3, 5,3',4'-Tetrahydroxystilbene-3'-O-β-glucoside, also known as Quzha in Tibetan medicinal materials because of its plant source Lhasa rhizome Technology Press, 2004), so the compound is called tristilbeside. The structure is shown in formula I, [0003] [0004] It can be seen from its structural formula that the glycoside substitution of tristilbene is located on the non-meta-hydroxyl-substituted benzene ring, which is similar to the series of stilbenes obtained from rhubarb, deoxyreverin, polydatin and Polygonum multiflorum. There are structural differences in the glycoside substitution positions of stilbene glycosides and other stilbene glycosides, and comp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H15/203C07H1/06A61K31/7034A61P9/10
Inventor 龚云麒陈锦锌胡琳
Owner KPC PHARM INC
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