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Application of tristilbeside in the preparation of drugs for improving microcirculation disorder

A technology of tristilbeside and stilbene, which is applied in the field of application of tristilbene in the preparation of drugs for improving blood microcirculation disorders, and can solve the problems of single function, large toxic and side effects, and large side effects

Active Publication Date: 2016-08-31
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In view of the shortcomings of the current drugs for the treatment of microcirculation disorders, such as single function, poor curative effect, and large toxic and side effects, people pay more attention to finding, researching and developing ideal drugs for treating microcirculation disorders from traditional medicine herbal medicines
Although polydatin or its salt, Panax notoginseng saponins, and ginsenoside monomer Rb have also been developed successively in recent years. 2 , calcium dobesilate and kudzu root flavonoid composition, ginsenoside and breviscapine composition, etc. are used in the treatment of microcirculation disorders, but there are still some aspects such as insignificant clinical effect, large side effects, and difficulty in controlling addiction lack of

Method used

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  • Application of tristilbeside in the preparation of drugs for improving microcirculation disorder
  • Application of tristilbeside in the preparation of drugs for improving microcirculation disorder
  • Application of tristilbeside in the preparation of drugs for improving microcirculation disorder

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] formula

[0028] Add 60% of the prepared water for injection into the preparation tank, heat to 95°C and slightly boil, keep warm to 80°C, start the vacuum and start stirring for 10 minutes at the same time, use nitrogen gas to bring the tristilbene glycoside and gastrodin together according to the prescription amount Put it into the preparation tank, dissolve tristilbeside in about 5 minutes, remove the vacuum and nitrogen, adjust the pH to 5.0-7.0 and add water to the full amount to complete the preparation process, followed by sterile filtration, filling, and freeze-drying according to the conventional process made into injections.

Embodiment 2

[0030] formula

[0031] Add 60% of the water for injection in the preparation tank, heat to 95°C and slightly boil, keep warm to 80°C, start the vacuum and stir for 10 minutes at the same time, use nitrogen gas to weigh the tristilbene, gastrodin, and hydroxy Propyl-β-cyclodextrin is brought into the preparation tank together, about 5 minutes to dissolve tristilbene, remove the vacuum and nitrogen, adjust the pH to 6.0-7.0 and add water to the full amount to complete the preparation process, and then follow the routine The process is aseptic filtration, filling, and freeze-drying to make injections.

Embodiment 3

[0033] formula

[0034] Add 60% of the prepared water for injection into the preparation tank, heat to 95°C for a slight boil, keep warm to 80°C, start the vacuum and stir for 10 minutes at the same time, use nitrogen gas to weigh the tristilbene and hydroxypropyl- Bring β-cyclodextrin into the preparation tank together, and it will dissolve tristilbene in about 5 minutes. Remove the vacuum and nitrogen, adjust the pH to 5.5-7.0 and add water to the full amount to complete the preparation process, and then follow the normal process of aseptic Filtration, filling, and freeze-drying to make injections.

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Abstract

The invention discloses an application of tristilbene in the preparation of a drug for improving microcirculation disorder, using tristilbene as an effective active ingredient, and its structural formula is: adding one or more pharmaceutically acceptable auxiliary agents, In particular gastrodin and / or water soluble cyclodextrin derivatives as well as PEG400 and mannitol. Using trizaperine as an effective active ingredient, it is used to improve the disorder caused by cerebral microvascular injury and / or the disorder caused by ischemia-reperfusion injury and / or the disorder caused by leukocyte adhesion damage and / or the disorder caused by peroxide. The application of the drug causing the disorder. The present invention uses normal mice of Kunming species and artificially induced microcirculation disorder model mice, injects administration through tail vein, and observes contraction of arterioles and venules and capillary network under a microcirculation microscope and shows that: all blood vessels of normal mice have The obvious expansion effect can obviously resist the contraction of arterioles and venules and the reduction of the opening number of capillary network in the model mice of microcirculation disorder, and can obviously resist the slowing down of blood flow velocity.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to an application of tristilbene in the preparation of medicines for improving blood microcirculation disorders. Background technique [0002] Microcirculation refers to the circulation of blood between arterioles and venules. The basic function of microcirculation is to exchange substances between blood and interstitial fluid. Under normal circumstances, the blood flow of the microcirculation adapts to the metabolic level of tissues and organs, ensuring the blood perfusion of various tissues and organs and regulating the amount of blood returned to the heart. If the microcirculation is disturbed, it will directly affect the physiological functions of various organs. The walls of arterioles, posterior arterioles, capillary anterior sphincters, and venules mainly contain smooth muscles, and their diastolic and contractile activities directly affect the blood flow in t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7034A61P9/14
CPCA61K31/7034A61K47/10A61K47/26A61K47/40A61K9/0019A61K31/724A61P9/00A61P9/10A61P9/14A61K2300/00
Inventor 陈云建刘一丹朱泽杨兆祥尚建华杨旭娟
Owner KPC PHARM INC
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