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Application of 3,5,4'-trihydroxy-stilbyl-3'-O-glucoside in preparation of microcirculatory disturbance improvement medicines

A technology of microcirculation disorder and tristilbene, which is applied in the field of application of tristilbene in the preparation of drugs for improving blood microcirculation disorder, can solve the problems of insignificant clinical treatment effect, large side effects, poor curative effect, etc.

Active Publication Date: 2014-01-15
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 3,5,4'-trihydroxy-stilbyl-3'-O-glucoside in preparation of microcirculatory disturbance improvement medicines
  • Application of 3,5,4'-trihydroxy-stilbyl-3'-O-glucoside in preparation of microcirculatory disturbance improvement medicines
  • Application of 3,5,4'-trihydroxy-stilbyl-3'-O-glucoside in preparation of microcirculatory disturbance improvement medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] formula 1 2 3 4 5 Tristilbene 5g 5g 5g 10g 20g gastrodin 0.5g 80g 400g 80g 200g sodium hydroxide or hydrochloric acid Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Water for Injection 1000ml 1000ml 1000ml 1000ml 1000ml

[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 1 2 Tristilbene 25g 50g gastrodin 80g 100g Hydroxypropyl-β-cyclodextrin 30g 30g sodium hydroxide or hydrochloric acid Appropriate amount Appropriate amount Water for Injection 1000ml 1000ml

[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 1 2 3 4 Tristilbene 5g 10g 10g 20g Hydroxypropyl-β-cyclodextrin 30g 30g 50g 50g sodium hydroxide or hydrochloric acid Appropriate amount Appropriate amount Appropriate amount Appropriate amount Water for Injection 1000ml 1000ml 1000ml 1000ml

[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 3,5,4'-trihydroxy-stilbyl-3'-O-glucoside in the preparation of microcirculatory disturbance improvement medicines. The microcirculatory disturbance improvement medicines comprise 3,5,4'-trihydroxy-stilbyl-3'-O-glucoside as an effective active component, and one or more pharmaceutically acceptable auxiliary agents, especially gastrodin and / or water-soluble cyclodextrin derivatives and PEG400 and mannitol, wherein the structural formula of 3,5,4'-trihydroxy-stilbyl-3'-O-glucoside is shown in the specification. The microcirculatory disturbance improvement medicines treat 3,5,4'-trihydroxy-stilbyl-3'-O-glucoside as the effective active component, and are used for improving disturbances caused by cerebral microvascular damages and / or disturbances caused by ischemia reperfusion damages and / or disturbances caused by leukocyte adhesion damages, and / or disturbances caused by peroxides. Normal mice of Kunming species and artificially induced microcirculatory disturbance model mice undergo tail vein injection treatment, and results of the observation of arteriole and venule systole and capillary network under a microcirculatory microscope show that 3,5,4'-trihydroxy-stilbyl-3'-O-glucoside has an obvious expansion effect on the blood vessels of the normal mice, can obviously resist the reduction of the arteriole and venule systole and capillary network opening number of the microcirculatory disturbance model mice and can obviously resist the reduction of the blood flow speed.

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 Applications(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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