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Cyclodextrin clathrate of breviscapine and its prepn

A technology of cyclodextrin inclusion compound and breviscapine, which is applied in the field of medicine, can solve the problems of easy slow hydrolysis, oxidation and precipitation, instability, poor content, etc., to improve bioavailability, stability, and solubility Effect

Inactive Publication Date: 2006-03-01
张红军
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Breviscapine injection has poor stability and is prone to slow hydrolysis, oxidation and precipitation, making it difficult to solve the problems of poor clarity and unstable content
In order to improve the stability, there is a patent (publication number: CN1187365 Stable prescription and process of breviscapine injection) that adds antioxidants such as sodium bisulfite to the injection, or makes it into a freeze-dried powder (published No.: CN1095934 Breviscapine Powder Injection and Preparation Method; Publication No.: CN1133180 Breviscapine Freeze-dried Agent for Injection and Preparation Method), however, by preparing inclusion compound of breviscapine, cyclodextrin and its derivatives or by adding cyclodextrin Dextrin and its derivatives to improve the solubility of scutellarin in water, increase the stability of scutellarin, and then improve the bioavailability of scutellarin has not been reported

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Weigh 10g of hydroxypropyl-β-cyclodextrin, put it in a beaker, add 200ml of distilled water to dissolve, add 3g of scutellarin powder, adjust the pH value to 7 with 0.1mol NaOH, stir to dissolve, continue stirring for 1 hour, and use 0.1 molHCl to adjust the pH value to 6, filter, freeze-dry the filtrate, or spray-dry, and the obtained solid is scutellarin cyclodextrin inclusion compound. The X-ray diffraction pattern shows that the crystal peak of scutellarin disappears, and scutellarin forms an inclusion complex with cyclodextrin.

Embodiment 2

[0016] Weigh 10g of hydroxypropyl-β-cyclodextrin, put it in a 100ml beaker, add 50ml of distilled water to dissolve, add 2g of scutellarin powder, ultrasonically oscillate for 1 hour, filter, freeze-dry the filtrate, or spray-dry, and the obtained solid is Scutellarin cyclodextrin inclusion complex. The X-ray diffraction pattern shows that scutellarin can form an inclusion complex with cyclodextrin. The hydroxypropyl-β-cyclodextrin in the example can be replaced by SBE-β-cyclodextrin, and the operation remains unchanged.

Embodiment 3

[0018] Weigh 10g of β-cyclodextrin, put it in a beaker, add 200ml of distilled water, heat in a water bath to dissolve, add 3g of scutellarin powder, adjust the pH value to 7 with 0.1mol NaOH, stir to dissolve, continue stirring for 1 hour, and use 0.1 molHCl to adjust the pH value to 6, filter, freeze-dry the filtrate, or spray-dry, and the obtained solid is scutellarin cyclodextrin inclusion compound. The X-ray diffraction pattern shows that the crystal peak of scutellarin disappears, and scutellarin forms an inclusion complex with cyclodextrin.

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PUM

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Abstract

The present invention is cyclodextrin clathrate of breviscapine and its preparation. Cyclodextrin or its derivative is used to include breviscapine or added into breviscapine to raise the dissolubility of breviscapine in water, raise the stability of breviscapine and raise the bioavailability of breviscapine. The molar ratio between cyclodextrin or its derivative and breviscapine is 1-10. The present invention may be prepared into tablet, capsule, granule, dripping pill or suppository with relatively high bioavailability, and may be also prepared into oral liquid, injection or other preparation form with high stability.

Description

Technical field [0001] The present invention relates to the technical field of medicine, specifically utilizes cyclodextrin and its derivatives to form inclusion complexes with scutellarin or add cyclodextrin and its derivatives to improve the solubility and stability of scutellarin in water to prepare Forming breviscapine cyclodextrin inclusion compound and its preparation. Background technique [0002] Breviscapine is a class of flavonoids isolated from Breviscapine, mainly containing Breviscarpine, a small amount of scutellarin and other flavonoids. Pharmacological studies have shown that breviscapine has the following effects: increase cerebral blood flow, reduce vascular resistance, improve blood-brain barrier permeability; resist platelet aggregation and hyperviscosity caused by adenosine diphosphate, inhibit thrombosis; effectively reduce Plasma viscosity, hematocrit, platelet aggregation rate and fibrinogen in patients with cerebral infarction, inhibit abnormal lipo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K47/40A61K9/00A61P9/10
Inventor 张红军
Owner 张红军
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