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Method for extracting PiPerlonguminine and drug combination comprising same

An extraction method, the technology of peronine, which is applied in the field of extraction of peronine and the pharmaceutical composition containing peronine, can solve the problems of difficult, unacceptable and harmful extraction of piperonamide-like substances, and achieve stable protection Sexuality and bioavailability, simple and easy extraction method, rich economic resources

Inactive Publication Date: 2010-10-20
INNER MONGOLIA MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been found through research that this type of compound not only has a blood lipid-lowering effect similar to that of piperine, but also has very low toxicity. For example, the Chinese patent application CN1634029A discloses the application of isobutylpiperamide in the preparation of blood lipid-lowering drugs or health products. However, Because the existing technology is difficult to extract the piperonamides from Piper longum, the extraction rate of the conventional method is low and the extraction cost is high, the patent application CN1634029A adopts the method of chemically synthesizing the compound to obtain high-purity isobutyl pepper Amides, which not only require strict synthesis conditions, but are expensive to synthesize
More importantly, highly toxic methanol is used as a solvent in the synthesis. Since methanol is banned in the pharmaceutical industry, its use in medicine is harmful and not allowed

Method used

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  • Method for extracting PiPerlonguminine and drug combination comprising same
  • Method for extracting PiPerlonguminine and drug combination comprising same
  • Method for extracting PiPerlonguminine and drug combination comprising same

Examples

Experimental program
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Effect test

Embodiment 1

[0034] The extraction of embodiment 1 perineline

[0035]According to the following steps to extract peronine from longan longan:

[0036] (1) Take 500g of longan longan medicinal material granules (14 mesh) and place them in a reflux device, add 3000ml of absolute ethanol, heat and reflux at 50°C for 4 hours, then cool to room temperature, and filter through a filter membrane (100-200μm) to obtain the filtrate. Add 1000 ml of absolute ethanol to the filter residue, heat and reflux at 50° C. for 1 hour, then cool to room temperature, filter through a filter membrane (100-200 μm) to obtain a filtrate; combine the two filtrates, recover ethanol, and obtain an alcohol extract;

[0037] (2) The obtained ethanol extract was subjected to 100 mesh silica gel column chromatography, using 1.5:1 (v / v) n-hexane-ethyl acetate as the eluent, and eluted at a constant speed (4.0ml / min) (through high-efficiency liquid Phase chromatography analysis) obtains 6 kinds of components successively:...

Embodiment 2

[0053] The extraction of embodiment 2 perinerine

[0054] (1) Take 500g of longan longan medicinal material granules (16 mesh) and place them in a reflux device, add 3500ml of absolute ethanol, heat and reflux at 45°C for 4 hours, then cool to room temperature, and filter (100-200μm pore size filter membrane) to obtain the filtrate. Add 1000 ml of absolute ethanol to the filter residue, heat and reflux at 45° C. for 1 hour, then cool to room temperature, and filter to obtain the filtrate; combine the two filtrates, recover ethanol, and obtain the ethanol extract;

[0055] (2) The obtained ethanol extract was subjected to 100 mesh silica gel column chromatography, using 1.5:1 (v / v) n-hexane-ethyl acetate as the eluent, and eluted at a constant speed (4.0ml / min) (through high-efficiency liquid Phase chromatography analysis) obtains 6 kinds of components successively: reclaim eluent, obtain solid state F 1 ~F 6 , where F 4 with F 5 exists in the form of a mixture;

[0056] (...

Embodiment 3

[0061] The extraction of embodiment 3 perinerine

[0062] (1) Take 500g of Piper longum granules (20 mesh) and place them in a reflux device, add 3000ml of absolute ethanol, heat and reflux at 48°C for 4.5 hours, then cool to room temperature, and filter to obtain the filtrate. Add 1000ml of absolute ethanol to the filter residue, heat and reflux at 48°C for 1 hour, then cool to room temperature, and filter to obtain the filtrate; combine the two filtrates, recover ethanol, and obtain the ethanol extract;

[0063] (2) The ethanol extract obtained is subjected to 200 mesh silica gel column chromatography, with 1.5: 1 (v / v) n-hexane-ethyl acetate as the eluent, uniformly eluted (analyzed by high performance liquid chromatography), Obtain 6 kinds of components successively: Recover eluent, obtain solid state F 1 ~F 6 , where F 4 with F 5 exists in the form of a mixture;

[0064] (3) put F 4+5 The mixture was subjected to 200-mesh silica gel column chromatography again, with...

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Abstract

The invention provides a method for extracting PPA (PiPerlonguminine), which comprises the following steps: firstly, extracting by using absolute alcohol to obtain alcohol extract; and further carrying out continuous separation by using silica gel columns for two times to obtain pure PPA crystal after crystallization. The method of the invention can remove a large amount of impurities, thus obtaining the PPA with the purity thereof being as high as 85% to 95%; moreover, the method of the invention has the advantages of low cost and high extraction efficiency, dispenses with toxic reagents in short supply and technically complex equipment and facilitates the batch production; and particularly, the PPA obtained by the method of the invention is low in toxicity and high in activity. The invention further provides a drug preparation comprising the PPA, a preparation method thereof and an application thereof in preparing drugs for treating hyperlipidaemia.

Description

technical field [0001] The present invention relates to a method for extracting peronerine, a pharmaceutical composition containing peronerine obtained according to the extraction method and its application in the pharmaceutical composition for treating hyperlipidemia. Background technique [0002] Longum longum (Piper longum L.) belongs to the pepper family and is a commonly used medicinal material in Mongolian medicine. Mongolian medicine theory believes that: it belongs to the treatment of "Badakan" medicine, which tastes pungent, warm in nature, greasy, sharp, light, and dry; it can regulate stomach fire, dispel "Badakan Heyi", nourish and strengthen, and relieve asthma , expectorant, pain relief, tune yuan, and other effects. The Mongolian medicine Wuwei Qingzhuo Powder, which uses Piper longum as medicine, is mainly used to treat the decline of stomach fire, the syndrome of unseparated clear and turbidity, and no desire to eat. The so-called non-separation syndrome o...

Claims

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Application Information

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IPC IPC(8): C07D317/60A61K31/36A61P3/06A61P9/10A61P1/16
Inventor 那生桑胡日乐巴根包勒朝鲁乌兴荣侯峰
Owner INNER MONGOLIA MEDICAL COLLEGE
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