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Production technology of petasites lactone compound

A technology of butterbur lactone and production process is applied in the field of production technology of butterbur lactone compounds, and achieves the effects of less energy consumption for extraction and short extraction period

Inactive Publication Date: 2012-08-29
苏州宝泽堂医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, no literature has reported the use of supercritical CO 2 Extraction technology Process method for preparing butterbur lactone compounds from plants of the genus Ligularia or Butterbur

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Take Ligularia sagitta (Maxim.) Matt.25kg and crush it to 10-30 mesh, put it into a supercritical extraction tank, extract for 2 hours under the condition of extraction temperature of 50°C and pressure of 13MPa, and introduce CO 2 The flow rate is 18L / h. After the environment in the extraction tank is stable, adjust the temperature of the first-stage separation ax to 38°C and the pressure to 6MPa, the temperature of the second-stage separation ax to 25°C, and the pressure to 5MPa, and desorb the extract to obtain butterbur. 70.7g of the ester extract was stirred and dissolved with saturated saline, extracted 4 times with ether, the ether layer was distilled under reduced pressure to recover the reagent, and dried in vacuum at low temperature to obtain 20.4g of the product, with a total content of butterbur lactone of 88.7%.

Embodiment 2

[0018] Take Ligularia diciyoneura (Franch.) Hand.-Mazz. 25kg and pulverize it to 20-40 mesh, put it into a supercritical extraction tank, and extract it for 3 hours under the condition of extraction temperature of 20°C and pressure of 28MPa. Into CO 2 The flow rate is 17L / h. After the environment in the extraction tank is stable, adjust the temperature of the first-stage separation ax to 46°C and the pressure to 10MPa, the temperature of the second-stage separation ax to 28°C, and the pressure to 6MPa, and desorb the extract to obtain butterbur. 63.7g of the ester extract was stirred and dissolved with saturated saline, extracted 6 times with ether, the ether layer was distilled under reduced pressure to recover the reagent, and dried in vacuum at low temperature to obtain 16.7g of the product, with a total content of butterbur lactone of 88.9%.

Embodiment 3

[0020] Take butterbur Petasites japonicus (Sieb.et Zucc.) Fr Schmidt 35kg and pulverize to 30-50 mesh, put it into a supercritical extraction tank, extract for 2.5 hours under the condition of extraction temperature of 25°C and pressure of 23MPa, and introduce CO 2 The flow rate is 15L / h. After the environment in the extraction tank is stabilized, adjust the temperature of the first-stage separation ax to 42°C and the pressure to 8MPa, and the temperature of the second-stage separation ax to 37°C and the pressure to 7MPa, and desorb the extract to obtain butterbur. 98.9 g of the ester extract was stirred and dissolved with saturated brine, extracted 3 times with ether, the ether layer was distilled under reduced pressure to recover the reagent, and dried in vacuum at low temperature to obtain 28.6 g of the product, with a total content of butterbur lactone of 83.5%.

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Abstract

The invention belongs to the field of pharmaceutical chemistry and relates to a production technology of a petasites lactone compound. The production technology comprises the following steps: extracting a petasites lactone substance by a supercritical carbon dioxide technology; dissolving an extraction solution into saturated saline; extracting by using ethyl ether; drying at a low temperature; and thus obtaining the petasites lactone compound. The production technology is simple in process, low in cost and high in yield.

Description

Technical field: [0001] The invention belongs to the field of medicinal chemistry and relates to a production process of butterbur lactone compounds. Background technique: [0002] Sesquiterpene lactone compounds are biologically active components of a large group of medicinal plants, which are widely found in plants such as Acanthaceae, Umbelliferae, Euphorbiaceae, Magnoliaceae, Fangaceae and Compositae. Sesquiterpene lactones exhibit cytotoxic activity and antitumor activity, antiulcer activity, cardiotonic activity, antimigraine effect, and antimalarial effect, etc. [0003] Butterbur lactones are a class of sesquiterpene lactones isolated from Ligularia plants of the genus Ligularia and Petasites plants of the genus Butterbur. It has been reported that butterburide G and H have inhibitory effects on platelet activating factor (PAF), and deisobutyryl butterburide H has inhibitory effects on platelet aggregation induced by arachidonic acid (AA) and collagen ; Butterbur l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/28C07D307/94A61P1/00A61P11/00A61P11/02A61P11/06A61P17/00A61P17/04A61P17/06A61P19/02A61P27/02A61P27/16A61P25/00A61P29/00A61P37/08A61P39/02
CPCY02P20/54
Inventor 李法庆刘东锋
Owner 苏州宝泽堂医药科技有限公司
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