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Berberine-glucan microcapsule as well as preparation method and application thereof

A technology of berberine and dextran, which is applied in the field of biomedicine, can solve the problems of low oral utilization efficiency of berberine and its derivatives, lack of development in clinical application and transformation, and difficulty in obtaining stable drug systems, etc. Targeting ability, improving tumor targeting and anti-tumor ability, and improving anti-cancer effect

Active Publication Date: 2016-09-07
潘元明
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because there are no really effective drugs available for the clinical treatment of pancreatic cancer, the current first-line treatment standard for metastatic pancreatic cancer is the use of a single drug gemcitabine, and the recommended dose is 1000mg / m2
However, gemcitabine does not have a particularly prominent response rate, nor can it cure pancreatic cancer. Its main role is to improve the quality of life, showing its low toxicity and pain relief, and slightly prolonging the survival of patients.
In November 2005, the U.S. Food and Drug Administration recommended the combination of targeted drug Erlotinib (Tarceva) and gemcitabine in the treatment of advanced pancreatic cancer. Discover the clear benefits it brings
Not only that, in vitro experiments have confirmed that berberine has a strong inhibitory effect on various tumor cells, such as prostate cancer and pancreatic cancer cells, but its clinical application and transformation in tumor treatment have not been developed. The main reason is Because the solubility of berberine varies greatly with temperature and solvent polarity, it is not easy to obtain a stable drug system; the oral utilization efficiency of berberine and its derivatives is extremely low, which greatly limits its clinical application in tumor prevention and treatment

Method used

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  • Berberine-glucan microcapsule as well as preparation method and application thereof
  • Berberine-glucan microcapsule as well as preparation method and application thereof
  • Berberine-glucan microcapsule as well as preparation method and application thereof

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Effect test

Embodiment 1

[0047] Embodiment 1: Preparation of berberine dextran microcapsules

[0048] At 60°C, a saturated solution of berberine was prepared. Take 1 ml of this solution, add 20 mg of dextran microcapsules therein, fully incubate for 8 hours, and swell the dextran microcapsules. During this process, the berberine molecules diffused into the dextran microcapsules and reached equilibrium.

[0049] After equilibrium, add 2ml of ethanol dropwise to the system while stirring (the speed is less than 0.4ml / min). After the dropwise addition is completed, continue to stir for 10 minutes and freeze-dry or spin dry the solvent to obtain an encapsulation efficiency above 92%. berberine dextran microcapsule powder preparation.

Embodiment 2

[0050] Embodiment 2: Preparation of berberine dextran microcapsules

[0051] At 60°C, a saturated solution of berberine was prepared. Take 10 ml of the solution, add 200 mg of dextran microcapsules therein, fully incubate for 8 hours, and swell the dextran microcapsules. During this process, the berberine molecules diffused into the dextran microcapsules and reached equilibrium. After freeze-drying or rotary evaporating the solvent to obtain the berberine dextran microcapsule powder preparation, dissolve the berberine dextran microcapsule powder preparation with 1 to 3 ml of water, or freeze-dry or rotary evaporate the solvent again The berberine dextran microcapsule powder preparation is obtained. The berberine dextran microcapsule powder preparation with an encapsulation rate of over 92% can be obtained.

Embodiment 3

[0052] Embodiment 3: Preparation of berberine dextran microcapsules

[0053] At 50°C, a saturated solution of berberine was prepared. Take 10 ml of the solution, add 200 mg of dextran microcapsules therein, fully incubate for 8 hours, and swell the dextran microcapsules. During this process, the berberine molecules diffused into the dextran microcapsules and reached equilibrium. After freeze-drying or rotary evaporating the solvent to obtain the berberine dextran microcapsule powder preparation, dissolve the berberine dextran microcapsule powder preparation with 1 to 3 ml of water, or freeze-dry or rotary evaporate the solvent again By obtaining the berberine glucan microcapsule powder preparation, the berberine dextran microcapsule powder preparation can be obtained with an encapsulation rate of over 92%.

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Abstract

The invention discloses a berberine-glucan microcapsule. The berberine-glucan microcapsule is characterized by comprising berberine and glucan, wherein the microcapsule is formed by the glucan; the berberine is encapsulated inside the glucan microcapsule; the microcapsule is a sphere or a spheroid with size of (1-6 microns)*(1-6 microns). According to the berberine-glucan microcapsule, the berberine is encapsulated inside the glucan, so that the stability of the berberine is improved, the adsorption of the berberine is enhanced, the tumor targeting capability of the berberine is improved, and the alternative medicine applied to the targeted therapy of pancreatic cancer is provided for clinic.

Description

technical field [0001] The present invention relates to the field of biomedicine. More specifically, it relates to a new formulation of berberine. Background technique [0002] According to the "Global Cancer Report 2014" released by the World Health Organization (WHO), the absolute number of new cancer cases and deaths in China still ranks first in the world. Among them, the threat of malignant gastrointestinal tumors such as pancreatic cancer is the most significant. Pancreatic cancer, which mostly occurs in the head of the pancreas, has a high degree of malignancy and is the most common malignant tumor. The average survival period is less than 6 months, and the five-year survival rate is less than 5%. It is difficult to cure and has a very high mortality rate. Become known as the "King of Cancer" by the medical profession. Generally speaking, chemotherapy is one of the most common and effective ways to kill tumors, but in clinical practice, pancreatic cancer is not sen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/4375A61K47/36A61P35/00
CPCA61K9/5036A61K31/4375
Inventor 潘元明
Owner 潘元明
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