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Andrographolide compound solubilizing preparing method and medicinal preparation

A technology of andrographolide and compounds, which is applied in the field of solubilization preparation of andrographolide compounds and pharmaceutical preparations, can solve the problems of reducing the drug activity of andrographolide, improve bioavailability, reduce drug side effects, and improve insoluble properties Effect

Inactive Publication Date: 2004-12-08
侯文阁
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The change in the structure of andrographolide not only reduces the drug activity of andrographolide; but also the potassium and sodium metal ions are in the same medicinal chemical structure, which limits the scope of clinical use and is prone to adverse drug reactions

Method used

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  • Andrographolide compound solubilizing preparing method and medicinal preparation
  • Andrographolide compound solubilizing preparing method and medicinal preparation
  • Andrographolide compound solubilizing preparing method and medicinal preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040]Take 3.5g of andrographolide powder with a content of 98%, 35g of β-cyclodextrin, and 20ml of 85% ethanol solution, put them together in a ball milling cup, add agate grinding balls, and decompress and vacuum to 10-30P a And maintain this vacuum, set the speed of the ball mill to run at a variable speed within the range of 500 rpm to 700 rpm, grind for 4 hours, take out the decompression to remove ethanol for later use.

[0041] Add 500ml of water for injection to the grinding mixture and put it in the solution tank of a high-frequency ultrasonic generator, feed high-purity nitrogen gas with a purity of 99.99% and maintain it, heat the solution to 60-70°C and maintain it, the ultrasonic output frequency is 150HZ, and ultrasonically oscillate for 1 hour.

[0042] After ultrasonic oscillation, 1-3‰ activated carbon is used to sterilize and remove pyrogens to obtain the complex of the andrographolide compound and the solubilizing compound cyclodextrin.

Embodiment 2

[0044] Take 3.5g of andrographolide powder with a content of 98%, 35g of hydroxypropyl-β-cyclodextrin, and 20ml of 85% ethanol solution, put them together in a colloid mill, grind for 4 hours, take out the ethanol under reduced pressure and remove it for later use.

[0045] Add 500ml of water for injection to the grinding mixture and put it in the solution tank of a high-frequency ultrasonic generator, feed high-purity nitrogen gas with a purity of 99.99% and maintain it, heat the solution to 60-70°C and maintain it, the ultrasonic output frequency is 150HZ, and ultrasonically oscillate for 1 hour.

Embodiment 3

[0047] Get 3.5g of dehydrated andrographolide powder with a content of 98%, 35g of methyl-β-cyclodextrin, and 20ml of 85% ethanol solution, put them together in a ball mill and add agate grinding balls, grind for 4 hours, take out the ethanol under reduced pressure and remove it for later use.

[0048] Add 500ml of water for injection to the grinding mixture and put it in the solution tank of a high-frequency ultrasonic generator, feed high-purity nitrogen gas with a purity of 99.99% and maintain it, heat the solution to 60-70°C and maintain it, the ultrasonic output frequency is 150HZ, and ultrasonically oscillate for 1 hour.

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PUM

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Abstract

A process for preparing the andrographolide compound (or medicine with improved solubility includes such steps as proportionally mixing the andrographolide with solubilizer (cyclodextrin, amino acid, phosphatide, water-soluble high polymer and vegetable oil), adding water or organic cosolvent, mechanical grinding, ultrasonic processing, and mixing with medicinal auxiliary.

Description

Technical field: [0001] The invention discloses a method for preparing andrographolide compound solubilization and a pharmaceutical preparation, and relates to the technical field of methods for improving the dissolution rate of andrographolide. Background technique: [0002] Andrographolide and Dehydro-Dehydroandrographolide extracted from the plant Andrographis paniculata (burm.f.) Nees have been recognized by the international pharmaceutical community and are extremely medicinal in clinical medicine. Valuable antiviral natural medicine. The andrographolide compound is a terpenoid compound composed of a five-membered lactone ring and its basic structure of a diterpene bicyclic core. The andrographolide compound is almost insoluble in water, not only the single-structure compound does not become a liquid preparation, but also the hydrophilic modified compound dehydroandrographolide succinic half-ester monopotassium salt of andrographolide and similar structure compounds ar...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P31/12
Inventor 侯文阁赵国斌侯丽娟
Owner 侯文阁
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