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Preparation method of syringopicroside (SYR) poly(lactide-co-glycolide) (PLGA) nanoparticles

A technology of syringoside and -PLGA, which is applied in the field of preparation of syringoside PLGA nanoparticles, can solve the problems of large oral dose of syringoside, affecting the effect of liver disease, poor compliance of patients taking medicine, etc. Good sealing rate and drug loading, and the effect of increasing bioavailability

Inactive Publication Date: 2013-10-23
李永吉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] At present, the problem of syringpicroside in the treatment is that its oral dose is large, and the patient's medication compliance is poor.
After intravenous injection, the body eliminates quickly, the half-life is short, the bioavailability is not high, and the drug concentration in the liver is low
Affect its effect in treating liver disease

Method used

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  • Preparation method of syringopicroside (SYR) poly(lactide-co-glycolide) (PLGA) nanoparticles
  • Preparation method of syringopicroside (SYR) poly(lactide-co-glycolide) (PLGA) nanoparticles
  • Preparation method of syringopicroside (SYR) poly(lactide-co-glycolide) (PLGA) nanoparticles

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Embodiment 1

[0022] Embodiment 1 First, in order to achieve the above object, the technical scheme adopted in the present invention is: first, take PLGA (LA:GA=50:50) and join in the mixed solution of dichloromethane and ethyl acetate 1:1, obtain Concentration is the PLGA solution of 15mg / ml, then syringin is dissolved in distilled water, makes the medicine solution of 8mg / ml; Secondly, according to the volume ratio of 1:3, medicine is added in the PLGA solution, ultrasonic emulsification, makes Colostrum, then, inject this colostrum into poloxamer at a mass concentration of 0.5% 188 The aqueous solution forms the primary double emulsion, and then the primary double emulsion is added to 0.5% poloxamer according to the volume of 1:6 times 188 After 1-2 hours of magnetic stirring at 800r / min, the mixed solution of dichloromethane and ethyl acetate was rotated under reduced pressure for 45-60min to volatilize to form a colloidal solution. After freeze-drying, syringin-PLGA Nanoparticles

Embodiment 2

[0023] Embodiment 2 First, in order to achieve the above object, the technical scheme adopted by the present invention is: first, take PLGA (LA:GA=50:50) and join in the mixed solution of dichloromethane and ethyl acetate 1:2, obtain Concentration is the PLGA solution of 20mg / ml, then syringin is dissolved in distilled water, makes the medicine solution of 10mg / ml; Secondly, according to the volume ratio of 1:11, medicine is added in the PLGA solution, ultrasonic emulsification, makes Colostrum, then, inject the colostrum to a mass concentration of 0.5% poloxamer 188 The aqueous solution forms the primary double emulsion, and then the primary double emulsion is added to 1% poloxamer according to the volume of 1:11 times 188 After 1-2 hours of magnetic stirring at 800r / min, the mixed solution of dichloromethane and ethyl acetate was rotated under reduced pressure for 45-60min to volatilize to form a colloidal solution. After freeze-drying, syringin-PLGA Nanoparticles

Embodiment 3

[0024] Embodiment 3 First, in order to achieve the above object, the technical scheme adopted by the present invention is: first, take PLGA (LA:GA=50:50) and join in the mixed solution of dichloromethane and ethyl acetate 1:3, obtain Concentration is the PLGA solution of 18mg / ml, then syringin is dissolved in distilled water, makes the medicine solution of 15mg / ml; Secondly, according to the volume ratio of 1:4, medicine is added in the PLGA solution, ultrasonic emulsification, makes Colostrum, then, inject this colostrum into poloxamer at a mass concentration of 0.5% 188 The aqueous solution forms the primary double emulsion, and then the primary double emulsion is added to 0.75% poloxamer according to the volume of 1:10 times 188 After 1-2 hours of magnetic stirring at 800r / min, the mixed solution of dichloromethane and ethyl acetate was rotated under reduced pressure for 45-60min to volatilize to form a colloidal solution. After freeze-drying, syringin-PLGA Nanoparticles ...

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Abstract

The invention relates to a preparation method of syringopicroside (SYR) poly(lactide-co-glycolide) (PLGA) nanoparticles. The preparation method comprises the following steps of: weighing SYR and dissolving SYR into distilled water to serve as an internal aqueous phase; weighing PLGA and dissolving PLGA into an organic solvent consisting of ethyl acetate and dichloromethane to serve as an organic phase; slowly adding the aqueous phase into the organic phase dropwise under magnetic stirring and performing ultrasonic treatment in ice-water bath to obtain SYR primary emulsion (W / O); injecting the prepared primary emulsion into an aqueous phase containing an emulsifier poloxamer188 and stirring to form SYR primary multiple emulsion; quickly injecting the multiple emulsion into an external aqueous phase solution comprising poloxamer188, rotationally evaporating the multiple emulsion at a certain temperature and under reduced pressure until the mixed solvent of the ethyl acetate and the dichloromethane is volatilized completely to obtain a nanoparticle colloidal solution; freeze-drying to obtain the SYR-PLGA nanoparticles. The SYR-PLGA nanoparticles prepared by the method can be used for improving the stability of the SYR, prolonging the drug action time, overcoming the defect of high metabolism velocity, most importantly, achieving targeted and slow-release effects, and improving the bioavailability.

Description

technical field [0001] The invention relates to a preparation method of medicine, in particular to a preparation method of syringpicroside PLGA nanoparticles. Background technique [0002] Hepatitis B is a worldwide, infectious disease caused by hepatitis B virus (HBV). Although hepatitis B vaccination has become an important means of prevention, millions of people are still infected with HBV every year. Looking for HBV There is an urgent need for specific drugs for the treatment of hepatitis. However, it is difficult for traditional hepatitis drugs to enter the liver cells and play a role, and the amount that can really enter the liver cells is not enough to inhibit HBV. How to combine anti-hepatitis B drugs with carriers and deliver them to the diseased liver, so that the carrier particles can be selectively concentrated in liver parenchymal cells, increase the concentration of drugs in the liver, and reduce the side effects of other organs. It has become one of the entr...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/7048A61K47/34A61P1/16
Inventor 李永吉
Owner 李永吉
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