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Hydroxyl asiatic acid salt, preparation method and application thereof

A technology of centella asiatic acid and tromethamine oxalate, which is applied in the biological field and can solve the problems of low bioavailability, poor transdermal absorption, and poor solubility of centella asiatica salt

Active Publication Date: 2015-08-12
SHANGHAI INST OF PHARMA IND CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Therefore, the technical problem to be solved by the present invention is that the existing Centella asiatica salt has poor solubility, extremely low bioavailability, poor transdermal absorption, and it is difficult to use Centella asiatica salt for the development of cosmetics and medicines. Provided is a kind of madecassate and its preparation method and use

Method used

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  • Hydroxyl asiatic acid salt, preparation method and application thereof
  • Hydroxyl asiatic acid salt, preparation method and application thereof
  • Hydroxyl asiatic acid salt, preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0049] Preparation and Identification of Embodiment 1 Madecassic Acid Choline Salt

[0050] 1. Preparation of Madecassic Acid

[0051] Weigh 5 g of madecassoside (purchased from Guangxi Nanning Lichuang Biotechnology Co., Ltd.), of which the content of madecassoside is 35.5%, add a solution containing 4% NaOH and 50% ethanol, and reflux for 4 hours; Add hydrochloric acid to adjust the pH value to 2-3, and let stand overnight. Centrifuge the sample, discard the filtrate, wash the solid with water and 30% ethanol in turn until the filtrate is colorless to transparent; add absolute ethanol to the solid after washing, add to dissolve, add granular activated carbon, and reflux for 1 hour for decolorization; Add deionized water and let it stand overnight; centrifuge to get the total acid of madecassica (namely intermediate I, mainly madecassic acid and its isomer termi-nolic acid), in which the content of madecassica acid is 55 % (using HPLC method to detect); take an appropriate ...

Embodiment 2

[0065] Embodiment 2 prepares madecassate choline salt

[0066] Mix 1g (1.98mmol) of madecassic acid prepared in Example 1 with absolute ethanol at room temperature, heat to 60°C until completely dissolved, add 0.3g (2.48mmol) of choline to the solution, and stir at this temperature for 2 After 1 hour, a clear solution was obtained. The stirring speed was 100 rpm. The solvent was evaporated at normal temperature, and the product was put into a vacuum oven at 50° C. for drying to obtain 1.15 g of light brown solid hydroxyasiatic acid choline salt. The obtained hydroxyasiatica The purity of choline oxalate is 97%.

Embodiment 3

[0067] Embodiment 3 prepares madecassate choline salt

[0068] Mix 1g (1.98mmol) of madecassic acid prepared in Example 1 with absolute ethanol at room temperature, heat to 65°C until completely dissolved, add 0.28g (2.46mmol) of choline to the solution, and stir at this temperature for 1.5 After 1 hour, a clear solution was obtained. The stirring speed was 50 rpm. The solvent was evaporated at normal temperature, and the product was put into a vacuum oven at 50° C. for drying to obtain 1.1 g of light brown solid hydroxyasiatic acid choline salt, and the obtained hydroxyasiatica The purity of choline oxalate is 97%.

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Abstract

The invention discloses a hydroxyl asiatic acid choline salt, a preparation method and an application thereof, a hydroxyl asiatic acid glucosamine salt, a preparation method and an application thereof, and a hydroxyl asiatic acid trometamol salt, a preparation method and an application thereof. A hydroxyl asiatic acid salt solution is high in purity, is wide in concentration range, is abundant in selectable drug delivery approaches, and can be used for preparing medicines and cosmetics for preventing or treating fibrosis and resisting aging. Compared with free hydroxyl asiatic acid or other forms of the hydroxyl asiatic acid salt, the hydroxyl asiatic acid salt is greatly enhanced in water solubility and is easy to prepare into an injection or various solution agents. Through the proper preparation method, the bioavailability of the medicine is effectively improved so that the effect of the medicine is greatly improved. The medicine can be used for treating various fibrosis diseases and preventing or treating scar hyperplasia and also has an anti-aging function.

Description

technical field [0001] The invention belongs to the field of biotechnology, and in particular relates to a madecassate and its preparation method and application. Background technique [0002] Centella asiatica is the dry whole herb of Centella asiatica (L.) . Madecassic acid is one of the active ingredients in Centella asiatica. It has a wide range of pharmacological effects. It is often used to treat burns or chronic ulcers, skin deformation caused by tuberculosis or leprosy, and has certain effects on cardiovascular diseases and liver poisoning. Efficacy. [0003] Although there are hydrophilic groups in the molecular structure of madecassic acid, it has poor wettability and is almost insoluble in water. The formulation of madecassic acid for topical use, especially hydrophilic formulations, requires a unique approach and specific excipients. Furthermore, skin absorption is mainly transepidermal (intracellular and through cells) and is mainly controlled by the action o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00C07C239/12C07H5/06C07H1/00C07C215/10C07C213/02A61K31/56A61K8/63A61Q19/00A61Q19/08A61P11/00A61P1/16A61P13/12A61P1/18A61P29/00A61P17/02A61P17/00A61P9/00A61P39/06
CPCA61K8/63A61Q19/00A61Q19/08C07C213/00C07C215/10C07C239/12C07H1/00C07H5/06C07J63/008
Inventor 刘珉宇年四昀刘英黄晓玲张瑱蔡立肖璘姚玉龙潘绵立邓轶方刘晓慧王国平刘全海吴彤
Owner SHANGHAI INST OF PHARMA IND CO LTD
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