Quzhazhigan crystal and preparation method and application thereof

A technology of trizaperoside and crystals, which is applied in the field of trizaperoside crystals and its preparation, can solve problems affecting drug stability, solubility and bioavailability, drug processing and production, and drug quality, safety and effectiveness. In order to achieve the effects of high solubility and bioavailability, single crystal form and low production cost

Active Publication Date: 2011-12-14
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 spectrum (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 DSC 204 differential scanning calorimeter of German NETZSCH company; the detection condition is N2 as the atmosphere, 20mL / min, from room temperature to 250°C at 10°C / min, record heating curve. ...

Embodiment 2

[0028] Embodiment 2: Preparation of Trizaperoside crystals

[0029] Take P 2 o 5 20g of tristilbeside raw material after drying under reduced pressure for 12h as a desiccant, add 120mL of water, then add 1.5% (0.3g) needle active boil for 3min, filter while hot, let stand at 4°C for 6h, 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 for the yield of tristilbeside crystals is: the yield of tristilbene crystals=the amount of tristilbene crystals / the amount of tristilbene charged×100%.

[0030] Depend on figure 1It can be seen that the X-ray powder diffraction pattern of the tristilbene crystal prepar...

Embodiment 3

[0032] Take P 2 o 5 The desiccant was vacuum-dried for 12 hours. Tristilbene glycoside raw material (purity 98%) was added to 20 g per part, respectively, 120 mL of the solvent listed in Table 1 was added, and then 1.5% (ie 0.3 g) of the needle was added and boiled for 3 min with active ingredients. Filter, stand at 4°C for 6h, suction filter the crystallization solution, P 2 o 5 The desiccant was vacuum-dried under reduced pressure for 12 hours to obtain tristilbene crystals, and the yield and yield of tristilbene crystals were calculated, and the obtained tristilbene crystals were calculated.

[0033] The glycoside crystal form was analyzed by differential scanning calorimetry, X-ray diffraction and infrared spectroscopy, and 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.

[0034] Table 1 Solvent Selection

[0035]

[0036] As can be seen from the results in Table 1...

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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, the chemical name is (E)-1-(3,5-dihydroxyphenyl)-2-(3-hydroxy-4-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 tristilbene. The structure is as 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 compa...

Claims

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Application Information

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Patent Type & Authority Applications(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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