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Application of rotigotine microspheres in preparation of medicine for treating inflammatory pain

An inflammatory pain, microsphere technology for biomedical applications

Inactive Publication Date: 2020-06-16
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the research on rotigotine mainly includes the preparation method, analysis method, application, new preparation of rotigotine and its derivatives, and the treatment of Parkinson's disease, Parkinson-plus syndrome, depression caused by dopaminergic nervous system damage. There are no reports on the analgesic effect of rotigotine microsphere preparations in these aspects.

Method used

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  • Application of rotigotine microspheres in preparation of medicine for treating inflammatory pain
  • Application of rotigotine microspheres in preparation of medicine for treating inflammatory pain

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Analgesic effect and results of rotigotine microspheres on carrageenan-induced inflammatory pain

[0022] Materials and Reagents

[0023] Rotigotine Microspheres (Specification: 42mg / bottle, made by Shandong Luye Pharmaceutical Co., Ltd.); Rotigotine Microspheres Vehicle (made by Shandong Luye Pharmaceutical Co., Ltd.); Carrageenan (Sigma-Aldrich, USA)

[0024] Animals: SPF grade SD rats, male, weighing 180-220 g, provided by Jinan Pengyue Experimental Animal Breeding Co., Ltd., certificate number: SCXK (Lu) 2019 0003.

[0025] Instruments: YLS-6B intelligent hot plate instrument (Jinan Yiyan Technology Development Co., Ltd.); 7200 tenderness instrument (UGO Basile, Italy); AL204 electronic balance (Mettler, Switzerland)

[0026] Thermal stimulation was measured on the YLS-6B intelligent hot plate instrument. During the experiment, the temperature of the hot plate was kept at 52±0.2 °C. The timing was started from the time of contact, and the time until the...

Embodiment 2

[0029] Example 2: Determination results of rotigotine microspheres on carrageenan-induced inflammatory tissue pain-causing substances

[0030] Materials and Reagents

[0031] Rotigotine Microspheres (Specification: 42 mg / bottle, made by Shandong Luye Pharmaceutical Co., Ltd.); Rotigotine Microspheres Vehicle (made by Shandong Luye Pharmaceutical Co., Ltd.); Chloral Hydrate (Sinopharm Chemical Reagent Co., Ltd.) ; Carrageenan (Sigma-Aldrich, USA); Rat PGE2 ELISA Kit (Shanghai Enzyme Biotechnology Co., Ltd.)

[0032] Animals: SPF grade SD rats, male, weighing 180-220 g, provided by Jinan Pengyue Experimental Animal Breeding Co., Ltd., certificate number: SCXK (Lu) 2019 0003.

[0033] Instruments: VCX130PB ultrasonic breaker (SONICS, USA); AL204 electronic balance (METTLER, Switzerland); SpectraMax M3 multifunctional microplate reader (Molecular Devices, USA); Beckman Allegra X-22R high-speed centrifuge (Beckman Coulter, USA)

[0034] After the three groups of rats in Example 1...

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PUM

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Abstract

The invention discloses an application of rotigotine microspheres in preparation of a medicine for treating inflammatory pain. Rotigotine is a dopamine receptor agonist, and the long-acting sustained-release microsphere can obviously prolong the recession incubation period of the rat posterior claw to thermal stimulation and mechanical stimulation after carrageenan inflammation; the rotigotine microsphere is capable of inhibiting the expression of inflammatory tissue PGE2 and proving that the rotigotine microsphere has an analgesic effect on inflammatory pain, can be used for treating exercisesymptoms of Parkinson's disease and treating the pain of the Parkinson's disease or accompanied diseases, and the analgesic effect can be maintained for 4 days after one-time administration.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to the application of rotigotine microspheres in the preparation of medicines for treating inflammatory pain. Background technique [0002] Rotigotine is a non-ergot dopamine receptor agonist that produces anti-parkinsonian effects by stimulating dopamine D3 / D2 / D1 receptors. In primate and rodent Parkinsonian models induced by 6-hydroxydopa and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, rotigotine exhibited significant anti-Parkinsonism Jinsen effect and neuroprotection, and continuous administration of rotigotine can reduce the occurrence of motor complications compared with pulsed administration of levodopa and rotigotine. [0003] Rotigotine Sustained-release Microspheres for Injection (LY03003) developed by Luye Pharma has completed phase I clinical trials in China and the United States respectively and has been exempted from phase II clinical trials, and is currently ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/381A61K9/52A61P19/02A61P25/16A61P29/00
CPCA61K9/5031A61K31/381A61P19/02A61P25/16A61P29/00
Inventor 李珂珂傅风华王天
Owner YANTAI UNIV
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