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Medicinal composition with imidazoline receptor agonist activity and preparation method and application

A technology of imidazoline receptors and compositions, which is applied in the field of pharmaceutical compositions with imidazoline receptor agonistic activity and its preparation and application, and can solve the problems that the antihypertensive effect is not stronger than that of clonidine, and the antihypertensive effect, etc.

Inactive Publication Date: 2008-01-09
BEIJING UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

(2) with α 2 Drugs with stronger R affinity than clonidine have no stronger antihypertensive effect than clonidine
(3) Histidine receptor H 2 The blocking agents cimetidine and alpha 1 / α 2 The R antagonist phentolamine is ineffective in reducing blood pressure orally but is effective when administered on the RVLM

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Crush 5g of Prunella vulgaris, 5g of Gentiana, 10g of Motherwort, 5g of Radix Paeoniae Alba, and 25g of Glycyrrhizae into coarse powder, extract with water or ethanol containing water, filter and concentrate to obtain an extract with a relative density of 1.2-1.5 (40-80°C); The obtained extract is precipitated with 50-80% ethanol, the precipitate is filtered off, and the supernatant is concentrated into an extract of 1.2-1.5 (40-80° C.). The obtained extract is determined by high performance liquid chromatography, including (by weight) 5-15 parts of ursolic acid, 10-50 parts of gentiopicroside, 20-70 parts of stachydrine, 100-200 parts of paeoniflorin, licorice 30-100 parts of acid; the antihypertensive effect of the obtained extract, the antagonism experiment of efaxan and the RVLM microinjection experiment showed that the tablet has the activity of stimulating imidazoline receptors.

Embodiment 2

[0051] Crush 30g of Prunella vulgaris, 15g of Gentiana, 10g of Motherwort, 5g of Radix Paeoniae Alba, and 3g of Glycyrrhiza licorice into coarse powder, extract with water or ethanol containing water, filter and concentrate into an extract with a relative density of 1.2-1.5 (40-80°C); The obtained extract is precipitated with 50-80% ethanol, the precipitate is filtered off, and the supernatant is concentrated into an extract of 1.2-1.5 (40-80° C.). The obtained extract is determined by high performance liquid chromatography, including (by weight) 5-15 parts of ursolic acid, 10-50 parts of gentiopicroside, 20-70 parts of stachydrine, 100-200 parts of paeoniflorin, licorice 30-100 parts of acid; the antihypertensive effect of the obtained extract, the antagonism experiment of efaxan and the RVLM microinjection experiment showed that the tablet has the activity of stimulating imidazoline receptors.

Embodiment 3

[0053] Grind 10 grams of Prunella vulgaris, 3 grams of Gentiana, 10 grams of Motherwort, 10 grams of Radix Paeoniae Alba, and 6 grams of Licorice Root into coarse powder, filter and concentrate with water to form an infusion with a relative density of 1.2-1.5 (40-80°C). Cream; the obtained extract is precipitated with 50-80% ethanol, the precipitate is filtered off, and the supernatant is concentrated into an extract of 1.2-1.5 (40-80° C.) to carry out the antihypertensive effect and the antagonism of efalaxane Experiments and RVLM microinjection experiments, the results show that the tablet has the activity of stimulating imidazoline receptors.

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PUM

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Abstract

The present invention relates to a medicine composite with imidazoline acceptor excitation activity, and preparation method of said medicine composite and its application. Said medicine composite contains the extracts of Chinese medicinal materials of prunella spike, gentian root, leonurus, white peony root and licorice. Said medicine composite can be used for preparing the medicines for curing heart failure, arrhythmia, dementia for curing heart failure, arrhythmia, dementia and reducing blood pressure, etc.

Description

technical field [0001] The invention relates to a pharmaceutical composition with imidazoline receptor agonistic activity, as well as a preparation method and application of the composition. Background technique [0002] The imidazoline receptor is a new type of receptor that has been gradually recognized in recent years. In 1962, German scientist H. Stahle synthesized and discovered that clonidine (clonidine) had a hypotensive effect in the process of searching for a drug for treating nasal congestion. Clonidine began to be used clinically as an antihypertensive drug in the 1960s and was widely used in the 1970s. Clonidine has become one of the main prototype drugs of central antihypertensive drugs, and other central antihypertensive drugs have been synthesized on this basis, such as guanabenz (1962), guanfacine (1975), but these drugs have dry mouth, unresponsiveness, Side effects such as drowsiness, sedation, decreased heart rate, and inhibition of salivation. How to o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/71A61P9/04A61P9/06A61K31/352A61K31/56A61K31/7048
Inventor 赵琰屈会化王庆国李宇航曲荣波汤尔群
Owner BEIJING UNIV OF CHINESE MEDICINE
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