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Method for induding andrographolide by cyclodextrin and medicinal preparation

A technology of andrographolide and cyclodextrin, which is applied in the inclusion process of andrographolide, and the field of cyclodextrin inclusion andrographolide, which can solve the problem of reducing the drug activity of andrographolide, low bioavailability of active ingredients, Improve drug toxicity and side effects, etc., to achieve the effect of ensuring pharmacological activity, small hemolysis, and good water solubility

Inactive Publication Date: 2003-08-27
侯文阁
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But these medicines have changed the structure of andrographolide compound, because of the change of its structure has reduced the drug active effect of andrographolide, and has improved drug side effect; Andrographis paniculata crude extract human body direct medicine, composition is complex and effective Low bioavailability of ingredients, bitter taste

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Preparation of andrographolide for injection

[0016] Proportion: 1. HP-β-CYD................................................ 2000g 2. Andrographolide ................................. 400g 3. Medicinal ethanol .............................................. 100ml 4. For injection Distilled water...................................2000ml 5. Low molecular weight dextran..... ..............................200 g

[0017] Prepare an ethanol solution with a concentration of 40-60% with distilled water for injection, add andrographolide into the alcohol solution, heat to 60-75°C to dissolve it; dissolve HP-β-CYD cyclodextrin with distilled water for injection and add Put it into the andrographolide alcohol solution, move it to an ultrasonic generator and vibrate ultrasonically for 30-45 minutes, control the temperature below 45°C, and identify the inclusion end point by thin-layer chromatography.

[0018] Prepare a low-molecular dextran solution, pour it into the andrograph...

Embodiment 2

[0020] Preparation of small-volume andrographolide injection 1, BE-β-CYD or HP-β-CYD........................... 12000 g 2, lindenolactone...................................4000 g 3. Medicinal ethanol ................................. 300ml 4. Injection With distilled water ................................. 5000ml

[0021] Prepare an ethanol solution with a concentration of 40-60% with distilled water for injection, add andrographolide into the alcohol solution, heat to 60-75°C to dissolve it: dissolve SEB-β-CYD cyclodextrin with distilled water for injection and add Put it into the andrographolide alcohol solution, move it to an ultrasonic generator and vibrate ultrasonically for 30-45 minutes, control the temperature below 45°C, and identify the inclusion end point by thin-layer chromatography.

[0022] Calculated on the basis of 10,000 vials, each 100ml (containing 400mg andrographolide) filling volume, make up distilled water for injection to 10,000,000ml, use 0.2μm micro...

Embodiment 3

[0024] Preparation of andrographolide oral agent 1, HP-β-CYD (or SBE-β-CYD) .......... 500 Gram 2, andrographolide ............................................. 100 g 3 , medicinal ethanol .................................................. 50ml4 , distilled water...................................2000ml5 , starch .............................................. 150 ~300g 6. Powdered sugar................................... ....50g 7. Edible essence................................... ...50 grams

[0025] Prepare an ethanol solution with a concentration of 4-60% with distilled water, add andrographolide into the alcohol solution, and heat to 60-75° C. to dissolve it. Prepare HP-β-CYD cyclodextrin solution (concentration: 600-700g / L), add it to andrographolide alcohol solution, move it to an ultrasonic generator for ultrasonic oscillation for 30-45 minutes, control the temperature below 45°C, thin layer Chromatographic identification of inclusion endpoints.

[0026] Accordin...

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PUM

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Abstract

The present invention discloses a method for including andrographolide by using cyclodextrin and its medicinal preparation. The andrographolide is an importent active extract of medicinal plant andrographis. Its inclusion method includes: adding 10-60g of cyclodextrin or its derivative into distilled water and dissolving it; adding 6g of andrographolide extract into 5-10 ml of medicinal methyl alcohol, heating and dissolving it; pouring the cyclodextrin aqueous solution into andrographolide ethyl alcohol solution; ultrasonic vibrating mixed solution in ultrasonic generator for 20-30 min., adopting thin-layer chromatography to identify the cyclodextrin-andrographolide inclusion quality. It does not change chemical property and effective activity of the andrographolide, can be prepared intovarious dosage forms.

Description

Technical field: [0001] The invention relates to an inclusion technology of andrographolide, specifically discloses a method and a medicinal preparation for inclusion of andrographolide with cyclodextrin, and belongs to the technical field of natural medicines. Background technique: [0002] Andrographis paniculata is a plant of the Acanthaceae family, which has heat-clearing and detoxifying properties, and is mainly used to treat diarrhea and dysentery, cold and fever, sore throat, aphtha of the mouth and tongue, and carbuncle sores. Andrographolide is an important extract and active ingredient of the medicinal plant Andrographis paniculata. Its chemical structural formula is: diterpene bicyclic core and its five-membered lactone ring structure are the basic skeleton for clearing away heat and detoxifying. Because the andrographolide compound is insoluble in water, all adopt the way of chemical structure modification to introduce hydrophilic group to prepare various androgr...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P1/12A61P11/02A61P29/00A61P31/00
Inventor 侯文阁赵国斌秦剑飞张春滨
Owner 侯文阁
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