Stable gastrodin crystal with high bioavailability for oral administration as well as preparation method, preparation and application thereof
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A gastrodin, utilization technology, applied in the field of medicine, to achieve the effect of high purity, good stability and high bioavailability
Active Publication Date: 2015-03-25
KPC PHARM INC
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At present, there are many gastrodin crystals that improve the stability of gastrodin, improve the bioavailability, or even some gastrodin crystals, but they are still far from meeting people's market needs.
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[0043] The preparation method of the stable gastrodin crystal with high oral bioavailability of the present invention comprises the following steps:
[0044] A, take gastrodin crude product, add the solvent that mass volume ratio is 1:1~200 to fully dissolve, filter and separate;
[0045] B. Add ethyl acetate with a volume ratio of 1:1 to 50 to the filtrate obtained in step A, stir, then stand for crystallization, and obtain the target product after centrifugation.
[0046] The solvent is one or more of water, 50-100% ethanol or 50-100% methanol.
[0047] The crystallization temperature is -10-40° C., and the crystallization time is 2-80 hours.
[0048] The preparation of the present invention is prepared into tablets or capsules by adding pharmaceutically acceptable carriers and auxiliary materials to the gastrodin crystals.
[0049] The application of the present invention is the application of the stable gastrodin crystal with high oral bioavailability in the preparation ...
Embodiment 1
[0072] Take 1kg of gastrodin to be refined, add 2L of water, heat to fully dissolve, and filter. Add 5L of ethyl acetate to the filtrate and stir well, then let it stand at 4°C for 20 hours to slowly precipitate crystals, filter, wash, and dry under reduced pressure at 60°C to obtain 0.78 kg of refined gastrodin. The recovery rate of the refining process is 78%, and the content is 99.07%.
Embodiment 2
[0074] Take 1kg of gastrodin to be refined, add 2L of 50% methanol aqueous solution, heat to fully dissolve, and filter. Add 5L of ethyl acetate to the filtrate and stir thoroughly, then stand at 25°C for 75 hours to slowly precipitate crystals, centrifuge the product, filter, wash, and dry under reduced pressure at 60°C to obtain 0.85 kg of refined gastrodin. The recovery rate of the refining process is 85%, and the content is 99.97%.
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Abstract
The invention discloses a stable gastrodin crystal with high bioavailability for oral administration as well as a preparation method, a preparation and an application thereof. X-ray powder diffraction analysis, DSC and TG-DTA analysis and HPLC analysis show that the gastrodin crystal is a new crystal form. The preparation method comprises the steps that gastrodin crude products are dissolved with solvents for performing filtering separation, and ethyl acetate is added into the filtering liquid and is crystallized and separated to obtain a target. The preparation is a tablet or a capsule prepared by adding pharmaceutically acceptable carriers and auxiliaries into the gastrodin crystal. The application of the gastrodin crystal is an application of the stable gastrodin crystal with high bioavailability for oral administration in the preparation of medicines for preventing and/or treating cardiovascular and cerebrovascular diseases. The gastrodin crystal is high in purity, stable against light, moisture, heat and the like, high in stability in alkali solutions and high in in-vivo bioavailability; the preparation method is easy to carry out; compared with the existing crystallizing method, the used crystallized solvent has the advantages of less using amount of crystallized solvents, low production cost and easiness for industrial production; moreover, the content is more than 99 percent.
Description
technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a stable gastrodin crystal with high oral bioavailability, a preparation method, preparation and application thereof. Background technique [0002] Gastrodia elata Bl is the dry tuber of Gastrodia elata Bl. Also known as Chijian, Limu, Guiduyou, Shencao, Duyaozhi, Chijianzhi, Dingfengcao, Helicao, Duyao, Automatic Grass, and Water Potato. It is excavated after the beginning of winter and before the Qingming Festival of the following year (winter hemp is better), and it is a famous Chinese medicinal material. It has been used as medicine as early as more than 2,000 years ago, and those produced in Zhaotong, Yunnan are the best. Rich in gastrodin, vanillin, protein, amino acid, trace elements. Its property is pungent, warm and non-toxic. Its functions and indications are recorded in "Chinese Pharmacopoeia" as follows: anti-epileptic, anti-palpitation, anti-rheumatis...
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