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Application of isobaicalin in preparation of medicine

A technology of isoflavones and drugs, applied in the field of isobaicalein, can solve the problems of unseen pharmacokinetic studies and achieve excellent curative effect

Inactive Publication Date: 2006-08-30
史关正
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no study on the application of isobaicalein in the preparation of drugs for the prevention and treatment of cardiovascular and cerebrovascular and thrombotic diseases and the pharmacokinetics of the two isomers in vivo

Method used

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  • Application of isobaicalin in preparation of medicine
  • Application of isobaicalin in preparation of medicine
  • Application of isobaicalin in preparation of medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Take 100 kg of leaves of Sterculia foetida or Sterculia colorata, a plant of the family Sycamore, and use 60% ethanol equivalent to 15 times the weight of the leaves to reflux extract for 40 minutes, and reflux extract twice. The extracts were combined, and the ethanol was concentrated under reduced pressure, followed by extraction with petroleum ether, chloroform, ethyl acetate, and n-butanol. The n-butanol part was chromatographed on a macroporous adsorption resin, and eluted with water, 20%, 60%, and 80% ethanol successively to obtain 5 positions, and its 20% ethanol layer was chromatographed on a silica gel column, and chloroform: methanol: water (1 : 2: 2) elution, and then Sephadex LH220 chromatography, methanol: water (1: 2) elution to obtain the compound isobaicalein. The mixture of polyethylene glycol 6000: polyethylene glycol 4000 (1:2-4) is used as the base, the coolant is simethicone: liquid paraffin (3:2), and the ratio of raw material isobaicalic anhydride...

Embodiment 2

[0063] Take 1000 g of isobaicalein prepared by the method of Example 1, add an appropriate amount of water for injection, adjust the pH value to 7 with sodium carbonate, stir and dissolve, and then add manna for injection equivalent to 10-15% of isobaicalein Alcohol, sterilizing and filtering, measuring the content, dispensing to 10mg / bottle, sealing, to obtain.

Embodiment 3

[0065] Take the isobaicalein prepared by the method of Example 1, adopt the well-known infusion preparation method in the art, and prepare isobaicalein sodium chloride injection, and its specification is 250ml: 20 mg isobaicalein and sodium chloride 2.25g: Prepared into isobaicalein glucose injection, the specification of which is 250ml: 20mg isobaicalein and 12.5g glucose.

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PUM

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Abstract

An application of isoscutellarin 5,7,4'-trihydroxyflavone-6-0-glucuronicoside in preparing medicines for preventing and treating coronary heart disease, angina pectoris, myocardial ischema injury, cerebral thrombosis, cerebral infarction, etc.

Description

Technical field: [0001] The present invention relates to the use of isobaicalein (ISOSCUTELLARIN 5,7,4'-trihydroxyflavone-6-O-glucuronide), in particular to the use in the field of pharmacy. Background technique: [0002] Baicalin (SCUTELLARIN 5,6,4'-trihydroxyflavone-7--O-glucuronide) is also known as scutellarin. It has the effects of dilating blood vessels, increasing cerebral blood flow and coronary artery flow, reducing blood viscosity, and improving microcirculation [1]. Clinically, it is mainly used to treat cerebral thrombosis, cerebral infarction, paralysis after stroke, coronary heart disease, angina pectoris and other diseases. Its existing preparations are ordinary tablets, injections and injection powders. However, the oral bioavailability of ordinary tablets is extremely low, only 0.4±0.19% [2]. Ordinary injections and powder injections have a short half-life and rapid elimination in vivo[2-6]. At present, research at home and abroad is mainly focused on im...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P9/10
CPCA61K31/7048A61P7/02A61P9/00A61P9/10
Inventor 史关正
Owner 史关正
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