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Icariin sustained and controlled release nano-particle and method for preparing same

An icariin and nanoparticle technology is applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., which can solve the problems of low bioavailability, poor oral absorption, Difficulty and other problems, to achieve the effect of good repeatability, improved solubility, simple and cheap materials

Inactive Publication Date: 2017-12-22
ZUNYI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, icariin is poorly soluble in water, has poor oral absorption and low bioavailability

Method used

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  • Icariin sustained and controlled release nano-particle and method for preparing same
  • Icariin sustained and controlled release nano-particle and method for preparing same
  • Icariin sustained and controlled release nano-particle and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Dissolve 10 mg of icariin raw material drug and 30 mg of PLGA in 10 ml of methanol / dichloromethane solution (1:1 volume ratio), and prepare an icariin / PLGA solution with a concentration of 1.0 mg / ml; Dissolve 300 mg of PVA in 10 ml of water to prepare a PVA solution with a concentration of 30 mg / ml. Measure 0.75 ml of icariin / PLGA solution and add it to 2.25 ml of PVA solution, and then perform ultrasonic emulsification on the mixture; the ultrasonic frequency is 20-25 KHz, the power is 250 W, the ultrasonic time is 6 min, and each ultrasonic wave is 5 s , with an interval of 10 s. The emulsified solution was transferred to a rotary evaporator, and the methanol, dichloromethane, and chloroform were completely evaporated by rotary evaporation at room temperature for 10 minutes, and then the sample was centrifuged at high speed for 30 minutes (4°C, 20,000 rpm) to collect the precipitate and add Resuspend in deionized water and centrifuge again. The operation was repeate...

Embodiment 2

[0027] Dissolve 20 mg icariin raw material drug and 200 mg PLGA in 10 ml methanol / dichloromethane solution (volume ratio 5:1), and prepare icariin / PLGA solution with a concentration of 2.0 mg / ml; Dissolve 300 mgPVA in 10 ml of water to prepare a PVA solution with a concentration of 30 mg / ml. Measure 0.75 ml of icariin / PLGA solution and add it to 2.25 ml of PVA solution, and then carry out ultrasonic emulsification of the mixture; the ultrasonic frequency is 20-25 KHz, the power is 100 W, the ultrasonic time is 6 min, every ultrasonic 5 s, The interval is 10 s. The emulsified solution was transferred to a rotary evaporator, and the methanol, dichloromethane, and chloroform were completely evaporated by rotary evaporation at room temperature for 10 minutes, and then the sample was centrifuged at high speed for 30 minutes (4°C, 20,000 rpm) to collect the precipitate and add Resuspend in deionized water and centrifuge again. The operation was repeated 5 times, and the nanopartic...

Embodiment 3

[0029] Dissolve 30 mg icariin raw material drug and 10 mg PLGA in 10 ml methanol / ethyl acetate solution (volume ratio 9:1), and prepare icariin / PLGA solution with a concentration of 3.0 mg / ml; Dissolve 300 mgPVA in 10 ml of water to prepare a PVA solution with a concentration of 30 mg / ml. Measure 0.75 ml of icariin / PLGA solution and add it to 2.25 ml of PVA solution, and then carry out ultrasonic emulsification of the mixture; the ultrasonic frequency is 20-25 KHz, the power is 400 W, the ultrasonic time is 6 min, every ultrasonic 5 s, The interval is 10 s. The emulsified solution was transferred to a rotary evaporator, and the methanol, dichloromethane, and chloroform were completely evaporated by rotary evaporation at room temperature for 10 minutes, and then the sample was centrifuged at high speed for 30 minutes (4°C, 20,000 rpm) to collect the precipitate and add Resuspend in deionized water and centrifuge again. The operation was repeated 5 times, and the nanoparticles...

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Abstract

The invention discloses an icariin sustained and controlled release nano-particle and a method for preparing the same. The method includes preparing icariin / PLGA (polylacticcoglycollic acid) solution and PVA (polyvinyl alcohol) solution; adding the icariin / PLGA solution into the PVA solution; uniformly mixing the icariin / PLGA solution and the PVA solution to obtain mixed solution and then emulsifying and treating the mixed solution; removing organic solvents by means of evaporating; centrifuging and washing the mixed solution; centrifuging and washing the mixed solution again; carrying out repeated operation to obtain the icariin sustained and controlled release nano-particle. The icariin sustained and controlled release nano-particle and the method have the advantages that the average hydrodynamic diameter of the icariin sustained and controlled release nano-particle prepared by the aid of the method ranges from 100 nm to 600 nm, the solubility of the icariin sustained and controlled release nano-particle in water is improved by 100 times at least as compared with icariin crude medicines, and the dispersibility of the icariin sustained and controlled release nano-particle can be obviously improved; icariin can be slowly released to prolong the action time, and accordingly the bioavailability and the efficacy of the sustained and controlled release nano-particle can be effectively improved; materials used in the method are simple and inexpensive, preparation procedures are easy and convenient to operate, and the method is good in repeatability.

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicine pharmacy, and in particular relates to an icariin sustained and controlled release nanoparticle and a preparation method thereof. technical background [0002] Icariin is an effective active ingredient extracted from the traditional Chinese medicine Epimedium. It is a flavonoid glycoside compound that has pharmacological activities such as anti-tumor, promoting bone cell proliferation and differentiation, protecting brain hypoxia, and regulating body immunity. However, icariin is poorly soluble in water, has poor oral absorption and low bioavailability. Drug absorption requires appropriate water solubility and lipid solubility in order to penetrate the lipid bilayer of biological membranes. Using modern nanotechnology to nanometerize insoluble drugs can greatly improve solubility and dispersibility, enhance biological activity and target utilization; at the same time reduce t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K9/51A61K31/7048A61K47/34A61K47/32A61P35/00A61P37/02A61P39/00
CPCA61K9/5031A61K9/0002A61K9/5026A61K31/7048
Inventor 姜建芳
Owner ZUNYI MEDICAL UNIVERSITY
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