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Ginsenoside RZ1 solid dispersion and preparation method thereof

A technology of solid dispersion and ginsenosides, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve the problems of poor water solubility and low bioavailability of ginsenosides, and achieve improved Solubility, stability improvement effect

Active Publication Date: 2017-11-24
YANTAI NEW ERA HEALTH IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] First, ginsenoside RZ 1 Poor water solubility and low bioavailability;

Method used

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  • Ginsenoside RZ1 solid dispersion and preparation method thereof
  • Ginsenoside RZ1 solid dispersion and preparation method thereof
  • Ginsenoside RZ1 solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Preparation of Ginsenoside RZ by Supercritical Antisolvent Method 1 Solid dispersion

[0028] The granulation equipment is the Helix supercritical crystallization granulation system produced by Applied Separations, USA.

[0029] Ginsenoside RZ 1 Self-made, the purity is greater than 98%.

[0030] Preparation process:

[0031] Start the device, and after the temperature of the crystallization tank reaches 55°C, the CO 2 Compressed by a high-pressure pump and preheated by a preheater, it is passed into the crystallization kettle from the top of the kettle to 14MPa. After the temperature and pressure in the kettle are stabilized, open the CO2 at the bottom of the kettle. 2 Outlet valve, and adjust the fine-tuning valve to the predetermined volume flow rate of 3L / min.

[0032] Ginsenoside RZ 1 Dissolve PVP-K30 in a mixed solvent of acetone and dichloromethane (volume ratio of acetone and dichloromethane 1:1) in a mass ratio of 1:3 to prepare ginsenoside R...

Embodiment 2

[0033] Embodiment 2 Solvent stirring method prepares ginsenoside RZ 1 Solid dispersion

[0034] A certain amount of ginsenoside RZ 1 Dissolve in absolute ethanol with povidone K-30 at a mass ratio of 1:3 to configure ginsenoside RZ 1 The solution with a mass concentration of 15mg / mL was magnetically stirred at room temperature for 3h (100r / min), and the solvent was removed by rotary evaporation at 50°C under reduced pressure, dried in vacuum for 24h, crushed through a No. 5 sieve, and stored in a desiccator for future use.

Embodiment 3

[0035] Embodiment 3 Comparative Examples

[0036] Replace the solid carrier with β-cyclodextrin, and the others are the same as in Example 2.

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PUM

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Abstract

The invention relates to a ginsenoside RZ1 solid dispersion and a preparation method thereof. A solid carrier is povidone K-30. A supercritical anti-sovent method comprises the following preparation steps: step A, starting a device, introducing CO2 from the top of a kettle into a crystallization kettle to a preset pressure when the temperature of the crystallization kettle reaches a preset value, and adjusting the flow of a CO2 outlet valve to a set value; step B, pumping ginsenoside RZ1 and a povidone K-30 solution at a set volume flow into the crystallization kettle, wherein the solvent-containing CO2 enters a separation kettle, and the solvent is recovered in the separation kettle, CO2 is discharged, and then eluting the solution for 20-30min after the solution is fed; and step C, closing the CO2 inlet valve, emptying gas in the kettle, and opening the crystallization kettle to take out microparticles. The solvent method comprises the following preparation steps: stirring the ginsenoside RZ1 and the povidone K-30 solution at normal temperature; evaporating the mixture at a reduced pressure to remove the solvent; and drying and crushing the mixture. The povidone K-30 not only can improve the solubility of RZ1 in water, but also can inhibit isomerization of the ginsenoside RZ1.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a ginsenoside RZ 1 Solid dispersion and method for its preparation. Background technique [0002] The applicant's research found that ginsenoside RZ 1 It can effectively promote the osteogenic differentiation of bone marrow mesenchymal stem cells. Ginsenoside RZ 1 It was first isolated from heat-processed ginseng by Korean scholar SangMyung LEE (reference: Ginsenosides from Heat Processed Ginseng, Chem PharmBull, 2009), and its source is derived from ginsenoside RG 3 Dehydrated. [0003] Ginsenoside RZ 1 There are two isomers, ginsenoside RK 1 and RG 5 , the chemical structural formulas and biodegradation pathways of the three are as follows: [0004] [0005] Ginsenoside RG 3 Ginsenoside RK is obtained by elimination reaction of C20 hydroxyl and C21 hydrogen 1 , Ginsenoside RG 3 The C20 hydroxyl group and the C22 hydrogen are eliminated to obtain ginsenos...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/32A61K31/704
CPCA61K9/146A61K31/704
Inventor 孙玉鹤杨勇彭雨泽
Owner YANTAI NEW ERA HEALTH IND
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