Extract containing evodiamine (EVO) and rutaecarpin (RUT) and preparation method and application thereof

A technology for evodiamine and evodiamine, which is applied to the application field of analgesia, can solve the problems that the preparation method does not contain, cannot infer the preparation method of the extract, etc., and achieves low cost, good production and development value, and simple and acceptable process. control effect

Inactive Publication Date: 2012-10-31
CHANGSHA JINGYI PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Chinese patent CN 1931271A patent provides an extract of Evodia rutaecarpa and its preparation method, pharmaceutical composition and use, but its preparation method does not include and cannot infer the preparation method of the extract of the present invention

Method used

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  • Extract containing evodiamine (EVO) and rutaecarpin (RUT) and preparation method and application thereof
  • Extract containing evodiamine (EVO) and rutaecarpin (RUT) and preparation method and application thereof
  • Extract containing evodiamine (EVO) and rutaecarpin (RUT) and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 Preparation of Evodiamine and Evodiamine Extract

[0027] A. Extraction

[0028] (A) Add 60% ethanol solution to the raw material by adding 60% ethanol solution to the raw material according to the volume fraction ratio of raw material and 60% ethanol solution of 1:10-12, and then mix the mixture of the two Heat to 70-100°C, keep warm for 3 hours, take liquid from filter residue.

[0029] (B) Add 60% ethanol solution to the slag filtered out in step A (A) according to the volume fraction ratio of Evodia rutaecarpa raw material and 60% ethanol solution of 1: 8-10, and heat the mixture to 70- 100°C, after 3 hours of heat preservation, the liquid was taken from the filter residue.

[0030] (C) Add 60% ethanol solution to the slag filtered out in step A (B) according to the volume fraction ratio of Evodia rutaecarpa raw material and 60% ethanol solution of 1:8-10, and heat the mixture to 70- 100°C, after 3 hours of heat preservation, the liquid was taken from t...

Embodiment 2

[0036] Pharmacokinetic comparison in rats of different purity extracts of embodiment 2

[0037] The high, medium and low purity Evodia rutaecarpa extracts obtained by the method in Example 1 were respectively suspended in 0.5% CMC-Na solution to prepare a suspension. 18 healthy SD rats were fasted for 12 hours before the experiment, without water, and were given high, medium and low purity Evodia rutaecarpa extract suspension by intragastric administration at a dose of 40 mg kg -1 (EVO), 31mg·kg -1 (RUT). At 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, and 4 hours after gavage, 0.5 ml of blood was collected from the retro-orbital venous plexus, and placed in a heparin-anticoagulated plastic centrifuge tube. The blood sample was immediately extracted by liquid-liquid extraction Processing, sample injection analysis, see the results figure 2 , 3 .

[0038] C of EVO in the high-purity group max It is 2.1 times of the middle purity group, 3.8 times of the low purity group, and the C...

Embodiment 3

[0039] Embodiment 3 Comparison of pharmacokinetics in rats with different ratios of EVO and RUT

[0040] In order to confirm the effect of the ratio of EVO and RUT on drug absorption in vivo, the chemical synthesis products of EVO and RUT were mixed in the ratio of 20:1, 10:1, 5:1, 1:1, 1:5 and suspended in 0.5% CMC-Na ethanol solution to make a suspension. Thirty healthy SD rats were fasted for 12 hours before the experiment, without water, and given the above suspension by intragastric administration. At 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, and 4 hours after gavage, 0.5 ml of blood was collected from the retro-orbital venous plexus, and placed in a heparin-anticoagulated plastic centrifuge tube. The blood sample was immediately extracted by liquid-liquid extraction Processing, sample injection analysis, see the results Figure 4 , 5 .

[0041]CMC-Na ethanol solution was used to increase drug absorption to reflect the effect of the ratio of EVO and RUT on the in vivo absor...

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Abstract

The invention relates to an extract containing evodiamine (EVO) and rutaecarpin (RUT) and a preparation method thereof. The invention further relates to a medical application of the extract. The ratio of the EVO to the RUT in the extract containing EVO and RUT provided by the invention is (1-10):(1-5). Compared with a chemically-synthesized monomer, the extract in a specific ratio has the advantages: the absorption of EVO and RUT can be improved remarkably, and the bioavailability of EVO and RUT is increased; and the extract is purity-dependent. The extract disclosed by the invention can be used for alleviating pain.

Description

Technical field: [0001] The invention relates to a method for preparing an extract containing evodiamine and evodiamine, and the invention also includes the application of the extract in analgesia. Background technique: [0002] Evodiamine (EVO) and rutaecarpine (RUT) are the main active ingredients of traditional Chinese medicine Evodia rutaecarpine, which have antihypertensive, vasodilation, anti-allergic, anti-inflammatory, and analgesic effects. VR with EVO and RUT 1 The agonistic effect can promote the synthesis and release of neurotransmitters (CGRP, substance P, etc.). Experiments have confirmed that high doses of EVO can desensitize isolated mouse ileal neurons and exert an analgesic effect. It is speculated that the analgesic mechanism of EVO may be related to Capsaicin-like, by interacting with VR on peripheral sensory afferent fibers 1 binds, activates the membrane ion channel coupled to it, and makes Ca 2+ channel open, cytoplasmic Ca 2+ Elevated concentratio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/756A61P29/00
Inventor 丁劲松胡长平周应军徐世希陈菲罗芳梅
Owner CHANGSHA JINGYI PHARM TECH CO LTD
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