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Ampelopsin nano-micelle and application thereof

A technology of staphylococcus and nanomicelles, which is applied in the directions of medical preparations containing active ingredients, organic active ingredients, anti-tumor drugs, etc. It can improve the encapsulation rate and stability, improve the effect of adjuvant therapy, and achieve obvious therapeutic effects.

Inactive Publication Date: 2014-09-17
FUJIAN HEALTH COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Staphylococcus has been proven to have anti-tumor, anti-oxidation, hypolipidemic, anti-inflammatory, antibacterial and other effects, but due to its low solubility and the possibility of being metabolized by bacteria in the intestinal tract, the bioavailability of oral administration is low
In addition, due to its low solubility in water, it is not conducive to making injection forms
These are the obstacles that affect its clinical application. At present, there are no related products of prednisone monomer used in clinical practice.
Although there are literature reports (Ruan LP, Yu BY, et.al.Improving the solubility of ampelopsin by solid dispersions and inclusion complexes.Journal ofPharmaceutical and Biomedical Analysis.2005, 38 (3): 457-64) using solid dispersion technology, cyclopaste Preparation techniques such as fine clathrate technology are used to improve the solubility of staphylocoxine, but these methods have complex preparation processes, high costs, and can only improve solubility alone, but cannot achieve the purpose of sustained release and injection
However, the use of surfactants, ethanol, dimethyl sulfoxide and other reagents to increase solubility has the disadvantage of high toxicity or irritation

Method used

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  • Ampelopsin nano-micelle and application thereof
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  • Ampelopsin nano-micelle and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Accurately weigh TPGS respectively 1000 8g, Pluronic F 127 1g, 0.45g of staphylophyllin, dissolved in an appropriate amount of methanol, the methanol was removed by a rotary evaporator at 37°C in a vacuum, and a thin uniform film was formed on the bottom and inner wall of the eggplant-shaped bottle, and 50mL of purified water was added. Hydrate in a water bath at ℃ for 30 minutes, seal and place in the refrigerator for about 6 hours, ultrasonically treat for 10 minutes, wait for the film to fall off completely, and then filter three times with 0.2 μm and 0.1 μm polycarbonate membranes respectively to obtain the steroidin nanomicelle preparation , The encapsulation efficiency is 80.1%.

Embodiment 2

[0029] Accurately weigh TPGS respectively 1000 5g, Pluronic F 127 1g, 0.3g of staphylophyllin, dissolved in an appropriate amount of methanol, the methanol was removed by a rotary evaporator at 37°C in a vacuum, and a thin uniform film was formed on the bottom and inner wall of the eggplant-shaped bottle, and 50mL of purified water was added, and the Hydrate in a water bath at ℃ for 30 minutes, seal and place in the refrigerator for about 6 hours, ultrasonically treat for 10 minutes, wait for the film to fall off completely, and then filter three times with 0.2 μm and 0.1 μm polycarbonate membranes respectively to obtain the steroidin nanomicelle preparation , the encapsulation efficiency was 74.9%.

Embodiment 3

[0031] Accurately weigh TPGS respectively 1000 8g, Pluronic F 127 1g, 0.9g of staphylophyllin, dissolved in an appropriate amount of methanol, the methanol was removed by a rotary evaporator at 37°C in a vacuum, and a thin uniform film was formed on the bottom and inner wall of the eggplant-shaped bottle, and 50mL of purified water was added, and the Hydrate in a water bath at ℃ for 30 minutes, seal and place in the refrigerator for about 6 hours, ultrasonically treat for 10 minutes, wait for the film to fall off completely, and then filter three times with 0.2 μm and 0.1 μm polycarbonate membranes respectively to obtain the steroidin nanomicelle preparation , the encapsulation efficiency was 70.7%.

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Abstract

The invention discloses an ampelopsin nano-micelle and application thereof. The ampelopsin nano-micelle is prepared from a carrier and ampelopsin, wherein the carrier is a mixture of pluronic F127 and D-alpha-tocopheryl polyethylene glycol 1000 succinate; the feeding mass ratio of the ampelopsin to the carrier is (1:10)-(1:30); the feeding mass ratio of the pluronic F127 to the D-alpha-tocopheryl polyethylene glycol 1000 succinate in the carrier is (1:3)-(1:10). The ampelopsin nano-micelle can be used for remarkably improving the solubility of ampelopsin, has a higher encapsulation efficiency and a certain sustained-release effect, can be applied to injection, and can be used for remarkably improving the treatment effect when being used for treating patients with prostatic cancer.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a staphylocene nano-micelle and an application thereof. 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 anti-tumor, anti-oxidation, hypolipidemic, anti-inflammatory, antibacterial and other effects, but due to its low solubility and the possibility of being metabolized by bacteria in the intestinal tract, the bioavailability of oral administration is low. In addition, because of its low solubility in water, it is unfavorable to be made into an injection form. These are the obstacles that affect its clinical application, and there are no related products of staphylovinyl monomer used in clinical practice. Although there are literature re...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/352A61K47/34A61P35/00
Inventor 黄仁杰倪峰狄万鹏张月芬
Owner FUJIAN HEALTH COLLEGE
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