Ampelopsin oral preparation with high bioavailability

A technology for oral preparations of staphylosin, which is applied in the field of improving or enhancing the bioavailability of oral absorption of staphylosin, which can solve problems such as differences, bioavailability that has not been further studied and verified, and irregularity, etc., to achieve simple process, Effect of promoting dissolution and absorption and easy industrialization

Inactive Publication Date: 2021-02-12
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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  • Ampelopsin oral preparation with high bioavailability
  • Ampelopsin oral preparation with high bioavailability

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Effects of different excipients on the metabolism of staphylophyllin in rat liver microsomes

[0026] 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 liver of rats in a certain amount. In the microbody (protein concentration 1.0 mg / ml) incubation system, shake at 100 rpm for 15 minutes in a water bath at 37°C, add staphylophyllin (80 μmol / l) and NADPH coenzyme (1 mmol / l) to start the reaction, and after 10 minutes, add three Double the amount of ice methanol to terminate the reaction, vortex for 1 min, and centrifuge in a low-temperature high-speed centrifuge (4°C, 13,000 rpm) for 8 min, take the supernatant, and compare the remaining staphylophyll by LC-MS / MS.

[0027] The result is as figure 1 As shown, low and high doses (20, 40 μg / ml) of polyoxyethylene hydrogenated castor oil RH40, Tween-80, hydroxypropyl-β-cyclodextrin, pluronic F68...

Embodiment 2

[0028] Example 2 Determination of the IC50 value of five kinds of excipients on the inhibition of staphyloclin metabolism

[0029]Five kinds of excipients were used in different concentration ranges: polyoxyethylene hydrogenated castor oil 40 (1.0-40.00 μg / ml), Tween-80 (10.0-200.0 μg / ml), hydroxypropyl-β-cyclodextrin ( 4.0-100.0μg / ml), Pluronic F68 (10.0-200.0μg / ml), povidone K30 (4.0-100.0μg / ml), were added to rat liver microsomes (protein concentration 1.0 mg / ml) incubation system, after shaking at 100rpm in a 37°C water bath for 15min, add staphylophyllin (80μmol / l) and NADPH coenzyme (1mmol / l) to start the reaction, and after 10min, add three times the amount of ice methanol to terminate the reaction. Vortex for 1 min, then centrifuge in a low-temperature high-speed centrifuge (4°C, 13,000 rpm) for 8 min, take the supernatant, and compare the remaining amount of staphylophyll by LC-MS / MS, and calculate the IC50 value of each excipient (see Table 1). The results showed t...

Embodiment 3

[0032] Embodiment 3 The pharmacokinetics comparison of adjuvant to the oral administration of staphylocoxine

[0033] Mix a certain proportion of metabolic inhibitory excipients (polyoxyethylene hydrogenated castor oil 40, Tween-80, hydroxypropyl-β-cyclodextrin, pluronic F68, povidone K30) with a certain concentration of staphylophyllin Mix to make a solution. Taking prednisin alone as a control, the rats were administered by intragastric administration, blood was collected from the orbit, and the concentration of the drug in plasma was measured at each time point. The operation is as follows:

[0034] Rats (male, body weight 180-220 g) were randomly divided into 6 groups, 5 rats in each group. Fasted overnight before administration and had free access to water. The mixed solution of adjuvant and staphylophyll of the same dosage was given by intragastric administration respectively, and a separate saponin solution (the hydrotrope was dissolved in the aqueous solution contai...

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PUM

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Abstract

The invention discloses an ampelopsin oral preparation with high bioavailability, belongs to the technical field of pharmaceutical dosage forms and preparations, and relates to a method for improvingor increasing oral absorption bioavailability of ampelopsin, which is characterized in that ampelopsin and auxiliary materials with a metabolic enzyme inhibition effect are prepared into the preparation together. The concentration of ampelopsin in in-vivo plasma can be effectively improved or increased, so that the oral curative effect of ampelopsin is improved. The ampelopsin oral preparation ischaracterized in that ampelopsin and auxiliary materials with a metabolic enzyme inhibition effect are prepared into the preparation together, so that the purpose of increasing the oral absorption amount of ampelopsin is achieved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical dosage forms and preparations, and relates to a method for improving or increasing the bioavailability of oral absorption of staphylophyllin, that is, making preparations of staphylophyllin and auxiliary materials with inhibitory effects on metabolic enzymes, which can effectively improve or increase the bioavailability of staphylophyllin in blood plasma. Increase the concentration of staphylosin, thereby improving the oral efficacy of staphylosin. Background technique [0002] Staphylin, also known as dihydromyricetin, was first isolated by Kotake and Kubota in 1940 from the leaves of A. Meliaefolia, a plant of the genus Vitis vinifera in the family Vitis genus, and named as staphylophyll. Staphylococcus has been proven to have various effects such as anti-tumor, anti-oxidation, lowering blood fat, anti-inflammatory, and antibacterial. Staphylococcus is a dihydroflavonol compound, in the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K9/00A61K47/10A61K47/40A61K47/26A61K47/44A61K47/32A61P35/00A61P29/00A61P39/06A61P3/06
CPCA61K9/0053A61K31/352A61K47/10A61K47/26A61K47/32A61K47/40A61K47/44A61P3/06A61P29/00A61P35/00A61P39/06
Inventor 黄仁杰鄢雪梨肖健邓昌良
Owner FUJIAN HEALTH COLLEGE
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