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Application of asiatic acid and madecassic acid in preparation of alpha-glucosidase inhibitor drugs

A technology of madecassic acid and glucosidase, which is applied in the field of medicine and can solve problems such as time-consuming, laborious, cumbersome, and large solvents

Inactive Publication Date: 2011-03-30
赵全成
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In the past, asiatic acid and madecassic acid were prepared by isolating asiaticoside and madecassoside as a single component from plants, and then performing hydrolysis and purification to obtain a single component of asiatic acid and madecassic acid; another method is directly from Extracted from Centella asiatica, obtained through cumbersome extraction, layering and other separation processes, it is time-consuming and laborious, and consumes a large amount of solvent, and the yield is low

Method used

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  • Application of asiatic acid and madecassic acid in preparation of alpha-glucosidase inhibitor drugs
  • Application of asiatic acid and madecassic acid in preparation of alpha-glucosidase inhibitor drugs
  • Application of asiatic acid and madecassic acid in preparation of alpha-glucosidase inhibitor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 , the preparation of asiatic acid and hydroxy asiatic acid

[0044] Take Centella asiatica medicinal material 1kg, and extract 3 times with 8 times the amount of 70% ethanol containing 0.2% calcium oxide under reflux. Each time for 2 hours, combine the extracts, add 50g of medicinal activated carbon, stir, filter, and the filtrate directly passes through the treated D101 macroporous resin column, elutes 1200ml with 70% ethanol, collects the effluent and eluent, and recovers Concentrate the solvent to 500ml; add 1000ml of 1mol / l sodium hydroxide solution, and hydrolyze at 100°C for 3 hours. Let cool, adjust the pH value to 4 with dilute hydrochloric acid, filter, discard the hydrolyzate, wash the filter cake with deionized water until neutral; then heat to boiling with 1500ml of 90% ethanol, add 5g of medicinal activated carbon, stir, and filter while hot After drying, the filtrate was concentrated under reduced pressure and recovered until there was no alcoh...

Embodiment 2

[0045] Example 2 , the preparation of asiatic acid and hydroxy asiatic acid

[0046] Take 1 kg of Centella asiatica medicinal material, and reflux extract twice with 10 times the amount of 60% ethanol containing 0.2% calcium oxide. 3 hours each time, combine the extracts, add 25g of medicinal activated carbon, stir, filter, and the filtrate directly passes through the treated D201 macroporous resin column, elutes 18000ml with 50% ethanol, collects the effluent and eluent, and recovers the solvent , concentrated to 500ml; add 1000ml of 0.2mol / l potassium hydroxide solution, and hydrolyze at 100°C for 5 hours. Let it cool, adjust the pH value to 2 with dilute hydrochloric acid, filter, discard the hydrolyzate, wash the filter cake with deionized water until neutral; then heat it to boiling with 95% ethanol, add 8g of activated carbon in the volume of the liquid medicine, and filter while hot After filtration, the filtrate was concentrated under reduced pressure and recovered ...

Embodiment 3

[0047] Example 3 , the preparation of asiatic acid and hydroxy asiatic acid

[0048] Take 1 kg of Centella asiatica medicinal material, and use 6 times the amount of 80% ethanol containing 0.2% calcium oxide to reflux extract for 3 times. 3h each time, combine the extracts, add 50g of medicinal activated carbon, stir, filter, the filtrate directly passes through the treated AB-8 macroporous resin column, elutes 9000ml with 80% ethanol, collects the effluent and eluent, Recover the solvent, concentrate to 500ml; add 1000ml of 2mol / l sodium carbonate solution, and hydrolyze at 100°C for 4 hours. Let it cool, adjust the pH value to 6 with dilute hydrochloric acid, filter, discard the hydrolyzate, wash the filter cake with deionized water until neutral; then heat to boiling with 85% ethanol, add 5g of activated carbon in the volume of the liquid medicine, and filter while hot After filtration, the filtrate was concentrated under reduced pressure and recovered until there was no...

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Abstract

Asiatic acid and madecassic acid are extracted and prepared from Centella asiatica (L.) Urban, and pharmacological experiments prove that the asiatic acid and the madecassic acid have the activity of inhibiting alpha-glucosidase. The invention discloses a new use of the asiatic acid and the madecassic acid in the preparation of alpha-glucosidase inhibitor drugs, and the asiatic acid, the madecassic acid or a composition containing the asiatic acid and the madecassic acid can be used for preparing the alpha-glucosidase inhibitor drugs. The invention simultaneously discloses a new preparation method of the asiatic acid and the madecassic acid.

Description

technical field [0001] The invention relates to a method for extracting asiatic acid and madecassic acid from traditional Chinese medicine, which has new medical application as proved by pharmacological experiments. Specifically, it is the application of asiatic acid and hydroxyasiatic acid as alpha-glucosidase inhibitors in the preparation of hypoglycemic drugs. It belongs to the field of medical technology. Background technique [0002] Diabetes mellitus is a group of clinical syndromes caused by the interaction of genetic and environmental factors. It is due to the absolute or relative insufficiency of insulin secretion and the decreased sensitivity of target tissues to insulin, which causes a series of metabolism in the body such as sugar, fat, protein, water and electrolytes. Disorder, clinically with hyperglycemia as the main common sign. Prolonged illness can cause multi-system damage, and acute metabolic disorders such as ketoacidosis can occur when the condition i...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P3/10
Inventor 南敏伦赫玉芳陈声武赵全成马吉胜赵文杰
Owner 赵全成
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