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Pharmaceutical application and pharmaceutical composition of lignan compounds

A technology of lignans and compounds is applied in the field of medicine to achieve the effect of preventing the formation of osteoporosis

Inactive Publication Date: 2015-11-18
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Chinese patent CN102557893A and GangNi et al. (Journaloforganicchemistry, 2011, 76:2056‐2061) reported that the lignan compounds isolated from Acorus calamus have glucokinase activation and can be used for the treatment of diabetes, but the lignans Whether the compound has the effect of inhibiting osteoclastogenesis, and further has the effect of inhibiting bone resorption has not been reported yet

Method used

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  • Pharmaceutical application and pharmaceutical composition of lignan compounds
  • Pharmaceutical application and pharmaceutical composition of lignan compounds
  • Pharmaceutical application and pharmaceutical composition of lignan compounds

Examples

Experimental program
Comparison scheme
Effect test

preparation example

[0058] Preparation example: extraction method of lignans

[0059] The lignans compound of the present invention is extracted from the rhizome of Acorus calamus, and its extraction method comprises the following steps:

[0060] (1) Take 10 kg of the traditional Chinese medicine Acorus calamus, grind it, extract twice with 95% ethanol under reflux, combine the two extracts, concentrate under reduced pressure, and dry in vacuum to obtain 700 g of extract.

[0061] (2), mix and suspend the above-mentioned extract with about 5 times the amount of water (the quality of water is 5 times of the quality of the extract), extract with petroleum ether, chloroform and n-butanol successively, and after recovering the solvent, obtain each part of the extract.

[0062] (3) The chloroform extraction part (total 190g) was chromatographed on a 100-200 mesh silica gel column, and the petroleum ether-acetone solution with a volume ratio of 5:1 was used as the mobile phase for gradient elution to o...

Embodiment 1

[0132] The pharmaceutical composition in this example is made into tablets by using lignan compound I, excipients and fillers. The mass percentage of the lignan compound I is 70%, the mass percentage of the excipient is 20%, and the mass percentage of the filler is 10%.

Embodiment 2

[0134] The pharmaceutical composition in this example is made into an injection by using the lignan compound II, a diluent and an absorption enhancer.

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Abstract

The invention provides pharmaceutical application and a pharmaceutical composition of lignan compounds, wherein the lignan compounds, which are extracted from roots and stems of rhizoma acori graminei, can be used for preparing medicines capable of treating osteoporosis; the pharmaceutical composition contains effective dosage of the lignan compounds, and the pharmaceutical composition can be prepared into pharmaceutical preparations of various types; experimental results of the invention prove that the extracted lignan compounds can be used for significantly inhibiting a differentiation process of bone marrow derived monocytes and macrophages into osteoclasts and inhibiting the formation of bone resorption lacunae, and the inhibiting effect is related to TRAP, Cts K and MMP-9; in addition, the lignan compounds, which are free from a remarkable cytotoxic effect on bone marrow derived macrophages, can be used for preparing medicines for preventing or treating osteoporosis; therefore, the lignan compounds have good prospect of medical application.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to the pharmaceutical application and pharmaceutical composition of lignan compounds. Background technique [0002] Osteoporosis (Osteoporosis) is a common bone metabolic disease, characterized by low bone mass and microarchitectural degeneration of bone tissue, accompanied by symptoms such as increased bone fragility and susceptibility to fracture. [0003] According to statistics from the International Osteoporosis Foundation, osteoporosis affects about 1 / 3 of women over 50 years old and 1 / 5 of men over 50 years old in the world, and its incidence rate has jumped to the 7th among common chronic diseases in the world. , becoming one of the main causes of bone pain and fracture, disability and death due to fracture in middle-aged and elderly women (Qin Ling, et al. Chinese Journal of Osteoporosis, 2002, 8:90-93). [0004] With the development of society and economy, people's living standards ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/09A61K31/341A61P19/10A61P19/02A61P29/00
Inventor 王红兵李珊周若愚张营营陈威
Owner TONGJI UNIV