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A plurality of antineoplastic sapogenin and its injection preparation method

An injection and anti-tumor technology, applied in the direction of anti-tumor drugs, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of low bioavailability, no anti-tumor effect research, and poor utilization of resources, etc. problem, achieve the effect of saving production cost and reducing usage

Inactive Publication Date: 2007-05-16
王丹
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no research on the antitumor effect of its combined use
[0007] 3. At present, most of the ginseng anti-tumor products used clinically are taken orally, such as Shenyi Capsules. As we all know, the bioavailability of oral products is quite low, resulting in poor utilization of resources. The existing patents related to ginsenoside injections, such as : CN1182433; Injection CN1526407A of protopanaxadiol, no injection of protopanaxadiol and protopanaxatriol compound

Method used

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  • A plurality of antineoplastic sapogenin and its injection preparation method

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Experimental program
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Effect test

Embodiment 1

[0041]Dissolve 100g of Panax notoginseng saponins in 1.5L of anhydrous n-butanol, add 40g (1.73mol) of sodium particles while stirring rapidly until there are no bubbles, then continue to feed oxygen, heat to 90°C, and react for 24 hours. , cooled to room temperature, washed three times with 1L of n-butanol saturated water to remove excess alkali and salts generated, then recover n-butanol under reduced pressure, disperse the reactant (about 73g) in 1L of aqueous solution, and use 1L of Ethyl acetate was extracted three times, and ethyl acetate was recovered and dried to obtain 40 g of ethyl acetate extract. The ethyl acetate extract was subjected to silica gel column chromatography, and CHCl 3 - MeOH (100:1 ~ 100:6) gradient elution to obtain 4.6 g of protopanaxadiol and 11.0 g of protopanaxatriol.

[0042] Its NMR data are respectively:

[0043] Protopanaxadiol 1 H-NMR (300MHz, CDCl 3 )δ: 1.70(3H, s), 1.64(3H, s), 1.20(3H, s), 0.99(3H, s), 0.98(3H, s), 0.89(6H, s), 0.78(3...

Embodiment 2

[0049] Dissolve 100g of total ginsenosides in 1.3L of anhydrous n-butanol, add 36g (1.57mol) of sodium particles while stirring rapidly until there are no bubbles, then continue to feed oxygen, heat to 95°C, and react for 18h. After the reaction, Cool to room temperature, wash with 1L of n-butanol-saturated water three times to remove excess alkali and generated salt, then recover n-butanol under reduced pressure, disperse the reactant (about 70 g) in 1L of aqueous solution, and wash with 1L of n-butanol Ethyl acetate was extracted three times, and ethyl acetate was recovered and dried to obtain 43g of ethyl acetate extract. The ethyl acetate extract was subjected to macroporous adsorption column chromatography, and EtOH-H 2 Gradient elution with O (50%-100%) yielded 12 g of protopanaxadiol and 3.8 g of protopanaxatriol.

[0050] Its NMR data is consistent with the literature, and the total TLC of the reference substance is a spot.

Embodiment 3

[0052] Panax ginseng total saponins 100g, dissolved in 1.1L anhydrous n-butanol, add 46g (2mol) of sodium particles while stirring rapidly until there are no bubbles, then continue to feed oxygen, heat to 95°C, react for 15h, after the reaction is completed, cool to room temperature, washed three times with 1L of n-butanol saturated water to remove excess alkali and salt produced, then recover n-butanol under reduced pressure, disperse the reactant (about 80g) in 1L of aqueous solution, wash with 1L of ethyl acetate Ethyl acetate was extracted three times, ethyl acetate was recovered, dried to obtain 47g ethyl acetate extract, ethyl acetate extract was subjected to ODS column chromatography, and EtOH-H 2 Gradient elution with O (50%-100%) yielded 10.7 g of protopanaxadiol and 3.0 g of protopanaxatriol.

[0053] Its NMR data is consistent with the literature, and the total TLC of the reference substance is a spot.

[0054] 2 preparation of injection

[0055] Example 1

[005...

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Abstract

The invention discloses a saponin compound to prevent tumour preparing method of its agent, which comprises the following steps: adopting panaxoside, American ginseng saponin, Notoginsen triterpenes and gynostemma pentaphylla saponin as raw material; dissolving in the high-boiling point organic solvent; aerating oxygen to do oxide alkaline degradation; adsorbing product through column chromatography to obtain protopanaxadiol, protopanaxatriol and Octoid.

Description

technical field [0001] 1: The present invention relates to the preparation method of protopanaxadiol and protopanaxatriol. Protopanaxadiol and protopanaxadiol are prepared by using total ginsenosides, total saponins of American ginseng, total saponins of Panax notoginseng and total saponins of gypenosides as raw materials, and by oxidation and alkali degradation at room temperature. Protopanaxatriol: the present invention also relates to protopanaxadiol and protopanaxatriol as an antitumor drug, when the dosage is fixed, its combined application shows a better effect than the single application; the present invention also relates to protopanaxatriol An injection of compound panaxadiol and protopanaxatriol and a preparation method thereof. Background technique [0002] 1. In the 1980s, Japanese scholars reported the anti-tumor effects of protopanaxadiol and protopanaxatriol. However, since the protopanaxadiol or triol in natural ginseng, American ginseng and other plants exis...

Claims

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Application Information

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IPC IPC(8): C07J9/00A61K31/575A61K9/08A61K9/10A61K9/19A61P9/00A61P35/00
Inventor 王丹
Owner 王丹
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