Near-infrared responsive pramipexole-loaded degradable microsphere preparation

A near-infrared and microsphere technology, applied in the field of medicine, can solve the problems of inconvenient and rapid drug delivery, and achieve good application prospects

Inactive Publication Date: 2019-08-06
南京锐利施生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, PLGA microspheres will not be controlled by external conditions during the slow release of drugs. When applied to the treatment of neurodegenerative diseases such as Parkinson's, although the sustained release of microspheres can greatly reduce the drug However, patients still face problems such as tremors, muscle stiffness, and slow movements in case of sudden illness, which are inconvenient for rapid drug administration.

Method used

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  • Near-infrared responsive pramipexole-loaded degradable microsphere preparation
  • Near-infrared responsive pramipexole-loaded degradable microsphere preparation
  • Near-infrared responsive pramipexole-loaded degradable microsphere preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] 1) Dissolve 0.12mM cobalt chloride, 0.1mM sodium citrate, and 0.4mM polyvinylpyrrolidone in 200mL deionized water, and dissolve under magnetic stirring;

[0033] 2) Quickly add 0.1 mM sodium borohydride solution to the solution in step 1) under the protection of argon, and stir magnetically for 1 h;

[0034] 3) Add 0.0012mM chloroauric acid to the solution obtained in step 2), and stir magnetically for 2 hours;

[0035] 4) Centrifuge and wash the solution obtained in step 3) for 3 times, collect HGNS, and resuspend HGNS with 0.15% polyvinylpyrrolidone solution, quickly cool down the HGNS suspension to 4°C in the dark, and use power 4W, Ultrasonic treatment for 1 min, freeze-drying;

[0036] 5) Weigh 20mg of pramipexole and dissolve in dimethyl sulfoxide, weigh 200mg of PLGA and dissolve in dichloromethane, ultrasonically dissolve, and combine as the organic phase; weigh 1mg of HGNS protected by polyvinylpyrrolidone obtained in step 4) As a solid phase, colostrum is fo...

Embodiment 2

[0039] 1) Dissolve 0.12mM cobalt chloride, 0.1mM sodium citrate, and 0.4mM polyvinylpyrrolidone in 200mL deionized water, and dissolve under magnetic stirring;

[0040] 2) Quickly add 0.5mM sodium borohydride solution to the solution in step 1) under the protection of argon, and stir magnetically for 1 hour;

[0041] 3) Add 0.0012mM chloroauric acid to the solution obtained in step 2), and stir magnetically for 2 hours;

[0042] 4) Centrifuge and wash the solution obtained in step 3) for 3 times, collect HGNS, and resuspend HGNS with 0.15% polyvinylpyrrolidone solution, quickly cool down the HGNS suspension to 4°C in the dark, and use power 4W, Ultrasonic treatment for 1 min, freeze-drying;

[0043] 5) Weigh 20mg of pramipexole and dissolve in dimethyl sulfoxide, weigh 200mg of PLGA and dissolve in dichloromethane, ultrasonically dissolve, and combine as the organic phase; weigh 1mg of HGNS protected by polyvinylpyrrolidone obtained in step 4) As a solid phase, colostrum is ...

Embodiment 3

[0046] 1) Dissolve 0.12mM cobalt chloride, 0.1mM sodium citrate, and 0.4mM polyvinylpyrrolidone in 200mL deionized water, and dissolve under magnetic stirring;

[0047]2) Quickly add 0.1 mM sodium borohydride solution to the solution in step 1) under the protection of argon, and stir magnetically for 1 h;

[0048] 3) Add 0.0012mM chloroauric acid to the solution obtained in step 2), and stir magnetically for 2 hours;

[0049] 4) Centrifuge and wash the solution obtained in step 3) for 3 times, collect HGNS, and resuspend HGNS with 0.15% polyvinylpyrrolidone solution, quickly cool down the HGNS suspension to 4°C in the dark, and use power 4W, Ultrasonic treatment for 1 min, freeze-drying;

[0050] 5) Weigh 40mg of pramipexole and dissolve in dimethyl sulfoxide, weigh 200mg of PLGA and dissolve in dichloromethane, ultrasonically dissolve, and combine as the organic phase; weigh 1mg of HGNS protected by polyvinylpyrrolidone obtained in step 4) As a solid phase, colostrum is for...

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Abstract

The invention discloses a near-infrared responsive pramipexole-loaded degradable microsphere preparation. The near-infrared responsive pramipexole-loaded microspheres (PRX / HGNS-PLGA MS) are prepared by using HGNS as a photothermal effect material and by a polyvinylpyrrolidone protective technology, and a near-infrared controlled-release microsphere drug delivery system is formed. Pramipexole whichis administered three times a day is optimized to be the microsphere preparation which is administered once every two weeks, and the instantaneous rapid drug release can be achieved by a near-infrared button in PD patients with sudden illness. The constructed near-infrared responsive pramipexole-loaded biodegradable microsphere preparation is an excellent drug delivery system, has good application prospect and is expected to be applied to the treatment of PD.

Description

technical field [0001] The invention discloses a near-infrared responsive pramipexole-loaded degradable microsphere preparation, and also provides a preparation method of the microsphere preparation, which belongs to the technical field of medicine. Background technique [0002] Pramipexole is a new generation of non-ergot dopamine receptor agonists, which binds to the D2 subfamily of dopamine receptors with high selectivity and specificity, has preferential affinity for D3 receptors, and has complete intrinsic activity. Pramipexole alleviates the movement disorder in patients with Parkinson's disease (PD) by stimulating the dopamine receptors in the striatum, amplifies the neural effects of dopaminergic neurons, reduces the short-term and long-term motor complications of patients, and improves the quality of life of patients. However, it is difficult for pramipexole tablets to maintain a long-term drug effect and stable blood concentration, and taking the drug multiple time...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/34A61K31/428A61K41/00A61P25/16
CPCA61K9/0019A61K9/5031A61K31/428A61K41/0042A61P25/16
Inventor 李又欣孙凤英李爽刘佳欣李鸽滕乐生
Owner 南京锐利施生物技术有限公司
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