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Refined bear gall powder with improved bioavailability and preparation method thereof

A technology of bear bile powder and tauroursodeoxycholic acid, applied in the field of medicine, can solve the problems of low content of active ingredients, unstable properties, and many impurities

Active Publication Date: 2019-11-29
江西天元药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] CN1311002A (00102073.0, Shi Lixia) discloses a refined bear bile powder and a preparation method thereof, which belongs to the field of pharmacy. Common bear bile powder is easy to absorb moisture and agglomerate, has a sticky tooth feeling, extremely fishy smell, extremely bitter taste, many impurities, and slow absorption. The property is unstable and easy to be corrupted, and the content of active ingredients is low, which limits the application range of bear bile powder. Oral application often adds flavoring agents to reduce the stench

Method used

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  • Refined bear gall powder with improved bioavailability and preparation method thereof
  • Refined bear gall powder with improved bioavailability and preparation method thereof
  • Refined bear gall powder with improved bioavailability and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Embodiment 1: prepare refined bear bile powder

[0081] (1) the bear bile collected (without tube drainage method) (when it is dried under reduced pressure to obtain powder, measure the content of tauroursodeoxycholic acid and taurochenodeoxycholic acid in this powder, be respectively 22.63% And 16.31%, this data is the percentage content of two kinds of materials in bear bile solids) add water dilution (add 2.5 times of volume water dilutions), filter with 80 mesh screens, 80 mesh screens are filtered gained filtrate and use 1M hydrochloric acid Solution adjusts its pH=3.3, then adds 1.2% sodium chloride in the filtrate, obtains crude bear bile fluid (this crude bear bile fluid is dried under reduced pressure to obtain powder, measure tauroursodeoxycholic acid and taurine angiosperm in this powder The content of deoxycholic acid is 28.47% and 20.33% respectively, which shows that the ratio of the two is basically unchanged before filtration, but it is concentrated du...

Embodiment 2

[0101] Embodiment 2: prepare refined bear bile powder

[0102] Steps (1) to (4) are carried out according to Example 1; in step (5), the ethyl acetate-ether (5:1) mixture used is changed to ethyl acetate, and the precipitate is dried under reduced pressure to remove the solvent to obtain refined Bear bile powder. It was determined that the melting point of the refined bear bile powder was 162-163° C., and the difference in melting point indicated that it had a different crystal form from the refined bear bile powder in Example 1.

Embodiment 3

[0103] Embodiment 3: prepare refined bear bile powder

[0104] Steps (1) to (4) are carried out according to Example 1; in the step (5), the ethyl acetate-ether (5:1) mixed solution used is changed to ether, and the precipitate is dried under reduced pressure to remove the solvent to obtain refined bear bile pink. It is determined that the melting point of the refined bear bile powder is 173-175° C., and the difference in melting point shows that it has a different crystal form from the refined bear bile powder in Example 1.

[0105] The above results of Example 2 and Example 3 show that in step (5) the mixture of ethyl acetate-ether (5:1) can be used to obtain the T crystal form with a melting point of 187-189°C, instead of using this mixture The crystals obtained are different.

[0106]Place 3 months at 45 ℃ of temperature places to embodiment 1~3 gained three kinds of refined bear bile powders, then measure their fusing points, the fusing points of three batches of refi...

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Abstract

The invention relates to refined bear gall powder with improved bioavailability and a preparation method thereof. Specifically, the invention relates to a compound represented by a formula (I). The diffraction peaks represented by 2[theta] angles of the compound in a powder X-ray diffraction spectrogram under the alpha irradiation of Cu-K are 8.53 + / - 0.20 degrees, 10.96 + / - 0.20 degrees, 12.03 + / - 0.20 degrees, 13.14 + / - 0.20 degrees, 14.82 + / - 0.20 degrees, 17.26 + / - 0.20 degrees, 22.53 + / - 0.20 degrees, 24.21 + / - 0.20 degrees, 26.68 + / - 0.20 degrees, 29.42 + / - 0.20 degrees, and 31.24 + / - 0.20 degrees. The compound has excellent biological properties such as excellent bioavailability and has the same physiological activity of bear gall powder or tauroursodeoxycholic acid.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a bear bile powder product and a preparation method thereof. The bear bile powder product presents excellent biological effects. Background technique [0002] Bear bile has been used as medicine for more than 1,000 years. It is known as the "gold in medicine" and ranks first among the four major animal medicinal materials: bear bile, tiger bone, bezoar, and musk. At present, there are 153 kinds of Chinese patent medicines made from bear bile powder alone and compound Chinese patent medicine preparations containing bear bile powder, involving 183 drug manufacturers. Its comprehensive effects cannot be replaced by other drugs. Among the 660 classics of traditional Chinese medicine (including more than 80,000 traditional prescriptions) from the Han Dynasty to the Qing Dynasty, about 366 works recorded the efficacy and application of bear bile and the compatibility of prescriptions....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J9/00C07C277/08C07C279/14
CPCC07B2200/13C07C277/08C07J9/005C07C279/14
Inventor 傅金荣付金洪
Owner 江西天元药业有限公司
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