Preparation, medical application and composition of 20S-protopanaxadiol beta-cyclodextrin inclusion compound

A technology of cyclodextrin inclusion compound and protopanaxadiol, which is applied in the fields of pharmacy and food, and can solve problems such as difficulty in preparation, affecting drug stability and safety, etc.

Active Publication Date: 2011-09-14
兰州和盛堂制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the lack of pharmaceutical specifications of hydroxypropyl-β-cyclodextrin, the inclusion compound of 20S-ppD hydroxypropyl-β-cyclodextrin is hygroscopic (affecting the stability and saf

Method used

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  • Preparation, medical application and composition of 20S-protopanaxadiol beta-cyclodextrin inclusion compound
  • Preparation, medical application and composition of 20S-protopanaxadiol beta-cyclodextrin inclusion compound
  • Preparation, medical application and composition of 20S-protopanaxadiol beta-cyclodextrin inclusion compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1: Preparation of β-cyclodextrin inclusion compound of 20S-protopanaxadiol of the present invention

[0046] A) Take 1 g of 20S-protopanaxadiol, add 1 g of β-cyclodextrin, add 6 ml of water, and grind for 3 hours. The measured inclusion rate is 84.1%, and the yield of 20S-protopanaxadiol inclusion compound is 98.2%. Before and after inclusion, the composition did not change.

[0047] B) Take 1g of 20S-protopanaxadiol, add 1g of β-cyclodextrin, add 6ml of absolute ethanol, ultrasonic power is 200W, ultrasonic time is 30min, and temperature is 30°C. Under this condition, the clathrate rate was 89.2%, and the clathrate yield was 91.2%.

[0048] C) Take 1 g of β-cyclodextrin, add 6 ml of water to dissolve at 60°C, and continuously add 20S-protopanaxadiol 1g of absolute ethanol solution to it under stirring, the inclusion time is 3 hours, and the inclusion temperature is 60°C. The clathrate rate can reach 94%, and the clathrate yield is 95.5%.

Embodiment 2

[0049] Example 2: Qualitative and quantitative analysis of the β-cyclodextrin inclusion compound of 20S-protopanaxadiol of the present invention

[0050] Chromatographic conditions and system suitability test used octadecyl bonded silica gel as filler, acetonitrile-water (85:15V / V), column temperature 30°C, flow rate 1.0ml / min. The number of theoretical plates calculated by 20S-protopanaxadiol should not be less than 2000. The separation between 20S-protopanaxadiol and adjacent peaks is greater than 1.5.

[0051] Detector: ultraviolet detection, the detection wavelength is 203nm; with mass spectrometry (MS) detector (461.4[M+H] + ) detection; time-of-flight mass spectrometry (TOF-MS) detector (461.3995[M+H] + ) detection; ultraviolet-visible diode array detector 190-203nm detection; circular dichroism (CD) detector 190-210nm detection; evaporative light scattering detector.

[0052] Configuration of the reference substance solution: Take 20S-protopanaxadiol chemical referenc...

Embodiment 3

[0055] Embodiment 3: the preparation of pharmaceutical composition

[0056] Any one of the compounds described in the present invention and a pharmaceutically acceptable carrier, or compatible with other drugs, are mixed with conventional pharmacy techniques to prepare tablets, capsules, granules, oral liquids, injections and other preparations.

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Abstract

The invention relates to a 20S-protopanaxadiol beta-cyclodextrin inclusion compound which can be used for preparing medicines and foods for resisting tumors, protecting the liver, reducing blood fat, reducing blood sugar, promoting gastric secretion, promoting appetite, improving digestion functions, enhancing immunity, resisting oxidization and resisting senescence. The invention also relates toa preparation process as well as composition of the inclusion compound.

Description

Technical field: [0001] The invention belongs to the fields of pharmacy and food, and relates to β-cyclodextrin inclusion compound of 20S-protopanaxadiol, which can be used for anti-tumor, liver protection, lipid-lowering, blood-sugar-lowering, promotion of gastric juice secretion, improvement of appetite, improvement of digestive function, Immunity enhancement, anti-oxidation, anti-aging medicine and food application, and preparation process and composition thereof. Background technique: [0002] 20S-protopanaxadiol (20S-protopanaxdiol, 20S-ppD) is a ginsenogenin obtained by extracting, separating and transforming Panax quinquefolium L or Panaxginseng. Foreign scholars have reported that PPD has a strong inhibitory effect on tumor cell growth. However, the low water solubility of 20S-ppD (less than 30 μg / mL) leads to low oral bioavailability, which limits its clinical efficacy to a certain extent. Chen Jing et al. ("Modern Drugs and Clinics" 2009, Issue 06) prepared 20S-p...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/575A23L1/29G01N30/36G01N21/33A61P1/14A61P1/16A61P3/06A61P3/10A61P11/04A61P11/14A61P17/04A61P25/04A61P25/08A61P25/16A61P25/28A61P27/12A61P29/00A61P31/04A61P31/14A61P35/00A61P37/08A61P39/06A23L33/00A61K47/69
Inventor 李国玉杨璐卢立娜于非
Owner 兰州和盛堂制药股份有限公司
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