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Method for improving biological activity of flavonoid compounds

A composition and drug technology, applied in the field of medicine, can solve problems such as differences, bioavailability that has not been further studied and verified, and irregularity, etc., and achieve the effects of simple process, improving anti-tumor activity, and promoting dissolution and absorption

Inactive Publication Date: 2022-08-05
FUJIAN HEALTH COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

That is to say, the metabolic process of different drugs is affected by excipients in different ways, and there is no uniform regularity.
So far, there have been no relevant reports on the influence and mechanism of excipients on the metabolism of prestaphyllin in the body, and the influence of excipients on the oral bioavailability of prestaphyllin has not been further studied and verified

Method used

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  • Method for improving biological activity of flavonoid compounds
  • Method for improving biological activity of flavonoid compounds
  • Method for improving biological activity of flavonoid compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1: The effect of different excipients on the metabolism of lepidopterin in rat liver microsomes

[0042] Select 6 kinds of excipients (polyoxyethylene hydrogenated castor oil 40, Tween-80, hydroxypropyl-β-cyclodextrin, Pluronic F68, povidone K30, PEG400), and add them to the rat liver according to a certain amount. In the microbody (protein concentration 1.0 mg / ml) incubation system, after shaking at 100 rpm in a 37°C water bath for 15 min, ependin (80 μmol / l) and NADPH coenzyme (1 mmol / l) were added to start the reaction, and after 10 min, three The reaction was terminated by twice the volume of ice methanol, vortexed for 1 min, centrifuged in a low-temperature high-speed centrifuge (4°C, 13000 rpm) for 8 min, the supernatant was collected, and the remaining amount of spleen was detected by LC-MS / MS.

[0043] The result is as figure 1 As shown, both low and high doses (20, 40 μg / ml) of polyoxyethylene hydrogenated castor oil RH40, Tween-80, hydroxypropyl-β-cyc...

Embodiment 2

[0044] Example 2: Determination of IC50 value of five kinds of adjuvants for inhibition of staphylococcus metabolism

[0045] 5 kinds of excipients were divided into different concentration ranges: polyoxyethylene hydrogenated castor oil 40 (1.0-40.0μg / ml), Tween-80 (10.0-200.0μg / ml), hydroxypropyl-β-cyclodextrin ( 4.0-100.0μg / ml), Pluronic F68 (10.0-200.0μg / ml), povidone K30 (4.0-100.0μg / ml), respectively added to rat liver microsomes (protein concentration 1.0mg) / ml) incubation system, after shaking at 100rpm in a 37°C water bath for 15min, respectively, add escarpone (80μmol / l) and NADPH coenzyme (1mmol / l) to start the reaction, after 10min, add three times the amount of ice methanol to stop the reaction, Vortex for 1 min, centrifuge for 8 min in a low-temperature high-speed centrifuge (4°C, 13000 rpm), take the supernatant, detect and compare the remaining amount of splendens by LC-MS / MS, and calculate the IC50 value of each excipient (see Table 1). The results showed th...

Embodiment 3

[0048] Example 3: Pharmacokinetics comparison of adjuvant for oral administration of staphylococcus

[0049] A certain proportion of metabolism-inhibiting excipients (polyoxyethylene hydrogenated castor oil 40, Tween-80, hydroxypropyl-β-cyclodextrin, pluronic F68, povidone K30) and a certain concentration of spleen Mix to make a solution. The rats were administered by gavage with the single use of staphylococcus as the control, and blood was collected from the orbit to determine the drug concentration in the plasma at each time point. The operation is as follows:

[0050] Rats (male, body weight 180-220 g) were randomly divided into 6 groups of 5 rats each. Fasting overnight before administration and drinking water ad libitum. The same doses of adjuvant mixed solution with staphylococcus and separate staphylococcus solution (dissolving staphylococcus in an aqueous solution containing dimethyl sulfoxide) (50 mg / kg) were administered by intragastric administration, respective...

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Abstract

The invention discloses a method for improving biological activity of flavonoid compounds, belongs to the technical field of medicines, particularly relates to the technical field of pharmaceutical compositions such as pharmaceutical dosage forms and preparations, and relates to a method for improving or improving oral absorption bioavailability of ampelopsin. The preparation is characterized in that the ampelopsin and an auxiliary material with a metabolic enzyme inhibition effect are jointly prepared into the preparation, and the concentration of the ampelopsin in plasma in a body can be effectively improved or increased, so that the oral curative effect of the ampelopsin is improved. The invention also relates to a method for improving the biological activity of the flavonoid compound. The invention has excellent technical effects as described in the specification.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a method for improving the biological activity of flavonoids, in particular, to a method for improving the biological activity of flavonoids, flavonoids, wherein the biological activities include but are not limited to anti- tumor activity. The biological activity of such flavonoids can be significantly improved by the method of the present invention. Background technique [0002] As described in CN112353793A (Chinese Patent Application No. 202011273451.4), lepidopterin is also known as dihydromyricetin, and this compound was first obtained by Kotake and Kubota in 1940 from the Vitis vinifera plant Fujian tea, namely the neem leaf jade grape A. Meliaefolia. It was isolated from the leaves and named as splendens. It has been proven to have anti-tumor, antioxidant, hypolipidemic, anti-inflammatory, antibacterial and other effects. Apoptosis is a dihydroflavonol compound with no s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/353A61P35/00A61K31/198A61K31/191
CPCA61K31/353A61K31/198A61K31/191A61K9/0053A61P35/00A61K2300/00
Inventor 黄仁杰鄢雪梨林燕喃
Owner FUJIAN HEALTH COLLEGE
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