Applications of stilbene compounds

A compound and drug technology, applied in the field of medicine, can solve problems such as poor curative effect and aggravated disease

Inactive Publication Date: 2013-12-04
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Clinical practice has also proved that a treatment has obvious effects o

Method used

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  • Applications of stilbene compounds
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  • Applications of stilbene compounds

Examples

Experimental program
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Effect test

Embodiment 1

[0022] Embodiment 1: the preparation of trizastilbene glycoside

[0023] Materials: Lhasa rhubarb medicinal material (purchased in Lhasa, Tibet, batch number 20110308, content 4.8%), remove impurities, clean, crushed into coarse powder; D101 macroporous adsorption resin (Cangzhou Baoen Adsorption Material Co., Ltd.) pretreated according to the instructions .

[0024]Preparation: Take 1Kg of Lhasa rhubarb crude powder, calculated as Kg / L, add 8 times the volume (W / V) of ethanol to extract 3 times, 2 hours / time, filter, combine the filtrates, concentrate until there is no alcohol smell, add 1L of water, mix Evenly, leave for 24 hours. Take about 900mL of the supernatant, put it on the D101 macroporous adsorption resin (the resin column is about 2000mL), elute with 3 times the column volume of water (V / V), and then use 6 times the column volume of 25% ethanol (V / V V) Elution, collect 0.5-6 times the ethanol eluent, concentrate to dryness, add 100mL water, mix well, and crystall...

Embodiment 2

[0026] Embodiment 2: the inspection of tristilbene raw material

[0027] Take an appropriate amount of stilbeneside (No. 20110401) prepared in Example 1, and conduct an inspection according to the regulations under the item of U injection in Appendix I of "Chinese Pharmacopoeia".

[0028] Properties: Off-white powder with bitter taste.

[0029] Loss on drying: According to the provisions of Appendix IX G of the 2010 edition of "Chinese Pharmacopoeia", trizastilbene glycosides were taken, and phosphorus pentoxide was used as a desiccant, and dried under reduced pressure at room temperature to constant weight, and the weight loss was 1.2%.

[0030] Residue on ignition: According to the provisions of Appendix IX J of the 2010 edition of "Chinese Pharmacopoeia", take an appropriate amount of trizastilbeside for inspection, and the residue on ignition is 0.1%.

[0031] Related substances: take an appropriate amount of tristilbene, according to the provisions of Appendix IX S of th...

Embodiment 3

[0042] Example 3: Acute Toxicity Test of Trizastilbene

[0043] 1. Experimental animals

[0044] 50 SPF grade ICR mice (provided by the Experimental Animal Center of Kunming Pharmaceutical Group), weighing 18-22 g, half male and half male. The pre-experiment animals were acclimatized indoors for one week at a room temperature of 18-25°C. They were housed in rack cages and fed with standard feed.

[0045] 2. Preparation of test drug

[0046] The tristilbene (No. 20110401) prepared in Example 1 was prepared into a 40 mg / mL tristilbene test drug solution with relevant excipients. 0.45um microporous membrane filtration for standby.

[0047] 3. Experimental methods and results

[0048] 50 mice were weighed and marked, and randomly divided into 5 different dosage groups of trizaperoside (10 mice in each group). According to the results obtained in the pilot experiment, the 0% (Dn) and 100% (Dm) lethal doses of the tested drug trizaperone were 0.51 g and 1.13 g, respectively. ...

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Abstract

The invention relates to the field of medicine, and discloses a novel application of stilbene compounds in preparation of drugs for curing ischemia stroke in the acute phase. The effective time windows of rhubarb stilbene glucoside and piceatannol can last for 6 hours; the rhubarb stilbene glucoside and piceatannol can decrease the water content in the rat brain tissues during the cerebral ischemia process of a rat, and improve the rat nerve function scores. The mechanism is that rhubarb stilbene glucoside and piceatannol have strong functions of oxidation resistance and clearance of oxygen free radicals, and have a brain protection function. The piceatannol has stronger functions of oxidation resistance and clearance of oxygen free radicals than those of the rhubarb stilbene glucoside in vitro. So the invention provides applications of rhubarb stilbene glucoside and piceatannol in preparation of drugs for curing ischemia stroke in the acute phase.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of stilbene compounds in the preparation of medicines for treating acute ischemic stroke. Background technique [0002] Stroke, commonly known as cerebral apoplexy, is a sudden-onset cerebral blood circulation disorder disease, also known as cerebrovascular accident, which refers to patients with cerebrovascular disease causing cerebral artery stenosis, occlusion or Rupture, resulting in acute cerebral blood circulation disorder, clinically manifested as symptoms and signs of transient or permanent brain dysfunction. Stroke is divided into ischemic stroke and hemorrhagic stroke. The morbidity, morbidity and mortality of stroke are all high, and its treatment is quite complicated, especially for the most common ischemic stroke, so far there is no recognized and universally applicable treatment method. [0003] Ischemic stroke is a generalized cerebral infarction, which re...

Claims

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Application Information

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IPC IPC(8): A61K31/7034A61K31/05A61P9/10
Inventor 龚云麒刘一丹陈锦锌方芳
Owner KPC PHARM INC
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