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Astragaloside cyclodextrin clathrate, its prepn. and preparing mehtod

The technology of cyclodextrin inclusion complex and astragaloside IV is applied in the directions of non-active components of polymer compounds, pharmaceutical formulations, pharmaceutical combinations, etc., and can solve the problems of limited wide use, difficulty in preparing injections, low oral bioavailability, and the like, Achieve the effect of expanding application prospects, enriching formulation varieties, improving solubility and bioavailability

Inactive Publication Date: 2006-06-14
NANJING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low solubility of astragaloside in water, the oral bioavailability is very low, and it is difficult to prepare injections, thus limiting its wide use

Method used

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  • Astragaloside cyclodextrin clathrate, its prepn. and preparing mehtod
  • Astragaloside cyclodextrin clathrate, its prepn. and preparing mehtod

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Preparation of astragaloside β-cyclodextrin inclusion compound

[0042] Weigh 5.0g of astragaloside IV, add 1250ml of ethanol and heat to dissolve; weigh another 7.2g of β-cyclodextrin, add 360ml of distilled water, heat and stir to dissolve; slowly add astragaloside IV ethanol solution dropwise while stirring, and keep the temperature at 50°C , continue to stir for half an hour, stop heating, let it gradually drop to room temperature, continue to stir until the remaining 1 / 5 of the solution, and dry under reduced pressure to obtain. The clathrate solubility reaches 82.5μg / ml.

Embodiment 2

[0044] Preparation of astragaloside β-cyclodextrin inclusion compound

[0045] Weigh 5.0 g of astragaloside IV, add 950 ml of methanol and heat to dissolve; weigh another 7.2 g of β-cyclodextrin, add 360 ml of distilled water, and heat to dissolve; slowly add astragaloside IV methanol solution dropwise under ultrasound, maintaining the temperature at 40 °C, Continue to sonicate for half an hour, stop heating, let it drop to room temperature gradually, continue to sonicate until the remaining 1 / 5 of the solution, and dry under reduced pressure to obtain the product. The clathrate solubility reaches 80.9μg / ml.

Embodiment 3

[0047] Preparation of astragaloside β-cyclodextrin inclusion compound

[0048] Weigh 5.0g of astragaloside IV, add about 1250ml of ethanol and heat to dissolve; weigh another 14.4g of β-cyclodextrin, add 720ml of distilled water, heat and stir to dissolve; slowly add astragaloside IV ethanol solution dropwise while stirring, and maintain the temperature at 50 ℃, continue to stir for 1 hour, stop heating, let it gradually lower to room temperature, continue to stir until the remaining 1 / 10 of the solution, and dry under reduced pressure to obtain. The clathrate solubility reaches 195.6μg / ml.

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Abstract

An inclusion compound used as medicine is prepared from astragaloside A and cyclodextrin through including the astragaloside A by cyclodextrin. Its preparing process is also disclosed. It has the improved solubility and biological utilization rate.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a cyclodextrin inclusion compound of natural medicine astragaloside IV, a preparation and a preparation method thereof. Background technique [0002] Astragalus membranacevs (Fisch.) Bge.Var.mongolicus (Bge.) Hsiao is a commonly used traditional Chinese medicine, mainly produced in Shanxi, Gansu, Heilongjiang, Inner Mongolia and other places. muscle function. Astragaloside IV is the main active ingredient in Astragalus, the English name is Astragaloside IV, and its molecular formula is C 41 h 68 o 14 . Modern pharmacology and traditional Chinese medicine chemistry studies have shown that astragaloside IV has various pharmacological effects such as enhancing the body's immune function, anti-inflammation, enhancing the positive inotropic effect of the heart, and lowering blood pressure. It is clinically used to treat cardiovascular and cerebrovascular diseases such as...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K9/00A61K36/481A61K47/40A61P1/16A61P9/00A61P35/00
Inventor 陈国广李学明陈振华孙视
Owner NANJING UNIV OF TECH
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