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High-purity gastrodin crystal as well as preparation method and application thereof

A gastrodin and high-purity technology, applied in the field of high-purity gastrodin crystals and their preparation, can solve the problems of drug preparation dissolution rate or bioavailability improvement, etc., and achieve rich crystal form research, high purity and high bioavailability Effect

Pending Publication Date: 2022-06-03
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The above-mentioned reports on the crystalline forms of gastrodin are all hemihydrates, and the dissolution rate or bioavailability of the prepared pharmaceutical preparations need to be further improved

Method used

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  • High-purity gastrodin crystal as well as preparation method and application thereof
  • High-purity gastrodin crystal as well as preparation method and application thereof
  • High-purity gastrodin crystal as well as preparation method and application thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0076] Preparation of gastrodin Form1 samples

[0077] 3.0 g of the raw material FormA crystal form gastrodin hemihydrate was weighed, placed in an oven at 115° C. for about 15 minutes, cooled to room temperature, and the obtained solid was the gastrodin Form1 crystal form crystal compound.

[0078] For the preparation method of FormA crystal form gastrodin hemihydrate, refer to the Chinese patent with the application number of 201410379348.6.

[0079] The X-ray powder diffraction pattern of gastrodin FormA crystal form hemihydrate is as follows Figure 10 shown.

[0080] The X-ray powder diffraction pattern of gastrodin Form1 crystal form is as follows Figure 11 shown.

Embodiment 1

[0081] Example 1 Preparation of gastrodin Form4 crystal form

[0082] Take about 200mg of gastrodin Form1 sample, add 0.8mL methanol to dissolve the clear, add 6.4mL isopropyl ether dropwise with stirring at room temperature, a solid is precipitated, continue to stir for about 30 minutes, centrifuge, and vacuum dry at room temperature overnight to obtain Form4 crystal form sample, record for sample 1.

Embodiment 2

[0083] The preparation of embodiment 2 gastrodin Form4 crystal form

[0084] Take about 200mg gastrodin Form1 sample, add 0.8mL methanol to dissolve the clear, stir the solution dropwise into 6.4mL isopropyl ether at room temperature, a solid is precipitated, continue stirring for about 30 minutes, centrifuge, and vacuum dry at room temperature overnight to obtain Form4 crystals type sample, denoted as sample 2.

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Abstract

The invention provides a novel gastrodin crystal form, the crystal form is found for the first time according to an X-ray powder diffraction pattern obtained by Cu-K alpha ray measurement, and the research on the crystal form of gastrodin is enriched. The preparation process is simple, the obtained crystal form compound is high in purity, good in solubility and high in bioavailability, the application scene of gastrodin is greatly widened, and the medication compliance of a patient is improved.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a high-purity gastrodin crystal and a preparation method and application thereof. Background technique [0002] Gastrodia elata Bl is the dry tuber of orchid Gastrodia elata, also known as Chijian, Limu, Guiduyou, Shencao, Duyazhi, Chijianzhi, Dingfengcao, Helicao, Duyao, automatic Grass, water potato. From the beginning of winter to the next year before Qingming, it is a famous Chinese medicinal material. It has been used as medicine more than 2,000 years ago, and the ones produced in Zhaotong, Yunnan are the best. Rich in gastrodin, vanillin, protein, amino acids, and trace elements. Its properties are pungent, warm and non-toxic. The "Chinese Pharmacopoeia" records its functions and indications as: anti-epileptic, anti-palpitation, anti-rheumatic; Function Indications: Pinggan, relieving wind and relieving spasm. For headache dizziness, limb numbness, epilepsy...

Claims

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Application Information

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IPC IPC(8): C07H15/203C07H1/06A61K31/7034A61P9/00A61P25/00
CPCC07H15/203C07H1/06A61P9/00A61P25/00C07B2200/13
Inventor 李志朋陈云建董艳萍李滢
Owner KPC PHARM INC