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Scutellarin aglycone crystal forms and preparation method thereof

A technology of scutellarin aglycone and crystal form, which is applied in the field of medicine and chemical industry, and can solve the problems of complex components, poor oral absorption of scutellarin, and low oral utilization rate

Active Publication Date: 2015-05-06
YUNNAN INST OF MATERIA MEDICA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The problem with the administration of scutellarin is that scutellarin itself is a mixture of scutellarin, scutellarin isomers-isobaicalin and others, the composition is complex, and there are some problems in quality control
However, scutellarin is the main component of scutellarin, which is the result of technological advancement, but the oral absorption of scutellarin is poor, and the oral utilization rate is not high

Method used

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  • Scutellarin aglycone crystal forms and preparation method thereof
  • Scutellarin aglycone crystal forms and preparation method thereof
  • Scutellarin aglycone crystal forms and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0191] Example 1 Preparation of scutellarin aglycone crystal form A

[0192]Take by weighing 100 grams of scutellarin (purchased from Yunnan Botanical Pharmaceutical Co., Ltd.), put it into a 5000ml round bottom flask, add 4000ml of propylene glycol or ethylene glycol, stir and heat to reflux, heat preservation and reflux to completely dissolve scutellarin; 20ml of 5% hydrochloric acid solution was slowly added dropwise to the solution; the reflux was continued for 6-16 hours, and the hydrolysis reaction was completed. After the solution is cooled, a large amount of precipitates are precipitated, filtered, and the filter cake is washed with propylene glycol or ethylene glycol and water respectively, dried and pulverized to obtain scutellarin aglycone crystal form A with a content (as determined by HPLC) of not less than 96%.

[0193] The typical XRPD figure of the crystal form A prepared according to this method is shown in figure 1 , the peak information of its spectrum is s...

Embodiment 2

[0265] Example 2 Preparation of scutellarin aglycon crystal form B

[0266] Weigh about 10 mg of scutellarin aglycone crystal form A into a 3 mL glass bottle, add 0.5 to 1.25 mL of pyridine / water (volume ratio 3:1) or pyridine / acetonitrile (volume ratio 3:1) or pyridine / ethyl acetate ester (volume ratio 3:1), to ensure complete dissolution of the sample to obtain a clear solution. The obtained solution was slowly evaporated at room temperature, and the crystal form B was obtained after the solvent was evaporated.

[0267] Method 1: Use pyridine / water (volume ratio 3:1) as a solvent to obtain Form B, and its spectrum peak information is shown in Table 21.

[0268] Table 21 XRPD peak information of scutellarin aglycone crystal form B

[0269]

[0270] Method 2: Use pyridine / acetonitrile (volume ratio 3:1) as a solvent to obtain Form B, and its spectrum peak information is shown in Table 22.

[0271] Table 22 XRPD peak information of scutellarin aglycone crystal form B

[...

Embodiment 3

[0280] Example 3 Preparation of scutellarin aglycon crystal form C

[0281] Method 1: Weigh about 15 mg of scutellarin aglycone crystal form A into a 3 mL glass bottle, add 0.2 mL of pyridine to completely dissolve the solid, then slowly add 0.2-2 mL of heptane to the pyridine solution dropwise, if there is precipitation, put A solid sample was isolated by precipitation. If there is no precipitation, it evaporates rapidly at room temperature to obtain Form C, and its spectrum peak information is shown in Table 25.

[0282] Table 25 XRPD peak information of scutellarin aglycone crystal form C

[0283]

[0284]

[0285] Method 2: Weigh about 15 mg of scutellarin aglycone crystal form A into a 3 mL glass bottle, add 0.2 mL of pyridine to completely dissolve the solid. Slowly add the above clear solution dropwise to 5°C heptane, if there is precipitation, separate the precipitation to obtain a solid sample. If there is no precipitation, conduct a rapid volatilization test...

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Abstract

Belonging to the field of pharmaceutical chemical engineering, the invention in particular relates to a variety of scutellarin aglycone crystal forms and a preparation method thereof. The invention also relates to application of the scutellarin aglycone crystal forms in preparation of drugs preventing and / or treating cardiovascular and cerebrovascular diseases, rheumatism arthritis, stroke sequelae and the like. The scutellarin aglycone crystal forms provided by the invention have good stability, and can overcome the poor oral absorption and low bioavailability problems of scutellarin.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to various crystal forms of scutellarin aglycone and a preparation method thereof. The present invention also relates to the use of the crystal form of scutellarin aglycone in the preparation of medicines for preventing and / or treating cardiovascular and cerebrovascular diseases, rheumatoid arthritis or stroke sequelae. Background technique [0002] Scutellarin (also known as scutellarin) has the functions of improving cerebral blood circulation, increasing cerebral blood flow, reducing blood viscosity and anti-platelet aggregation. Scutellarin is widely used clinically, mainly for cardiovascular and cerebrovascular diseases, such as residual paralysis caused by occlusive cerebrovascular, coronary heart disease, angina pectoris, etc. Scutellarin has significant curative effect in the treatment of cardiovascular and cerebrovascular diseases, rheumatoid arthr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/30A61K31/352A61P9/10A61P19/02A61P13/12A61P27/02A61P3/10A61P1/16A61P25/02A61P27/16
CPCC07D311/30C07B2200/13A61K31/7048A61P1/16A61P13/12A61P19/02A61P25/02A61P27/02A61P27/16A61P3/10A61P9/00A61P9/10A61K31/352
Inventor 王泽人徐俊王明辉朱兆云王京昆梅双喜孙文强崔涛
Owner YUNNAN INST OF MATERIA MEDICA
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