Long acting sustained-release formulation containing dopamine-receptor stimulant medicine and its preparation process

The technology of a receptor agonist and a sustained-release preparation is applied in the field of long-acting sustained-release preparations containing dopamine receptor agonists and their preparation technology, and can solve the problems of no disclosure of composition and ratio.

Active Publication Date: 2006-04-26
SHANDONG LUYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although it is mentioned in CN1531428A that microparticles or microcapsules (i.e. sustained-release microspheres in the present invention) of roticotin can be prepared by citing earlier documents EP0625069 (CN1090172A), for the microcapsules of roticotin , Sustained-release microspheres, etc. are not publicly disclosed
[0008] Above-mentioned CN1531428A and CN1090172A do not have any disclosure for the slow-release preparation and adjuvant of dopamine receptor agonist medicine, therefore, actually comprise the long-acting slow-release preparation of dopamine receptor agonist medicine of roticotin (dosing interval is long up to 1 or 2 weeks or even more than a month) is still unknown

Method used

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  • Long acting sustained-release formulation containing dopamine-receptor stimulant medicine and its preparation process
  • Long acting sustained-release formulation containing dopamine-receptor stimulant medicine and its preparation process
  • Long acting sustained-release formulation containing dopamine-receptor stimulant medicine and its preparation process

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0127] Dissolve 0.1g of roticotine and 0.9g of polylactide-glycolide (lactide:glycolide=50:50, molecular weight 25,000) in 5ml of dichloromethane, under vigorous stirring (1200-1600rpm) Drop it into 250ml of 0.5% PVA aqueous solution, continue stirring vigorously for 3-10 minutes after dropping, then reduce the stirring speed to 300rpm, volatilize the solvent for 4-6 hours, filter, wash the microspheres with distilled water three times, and freeze-dry. The particle size of the microspheres measured by a laser particle size analyzer is 1-250 μm, and the particle size distribution is as follows: figure 2 shown, and then sieved to remove microspheres with a particle size greater than 150 microns, and subpackaged. image 3 It is the scanning electron micrograph of the slow-release microsphere gained in embodiment 1.

Embodiment 2

[0129] Take by weighing roticotine 0.1g, polylactide-glycolide (lactide: glycolide=50:50, molecular weight 13000) 0.9g, prepare by the method for embodiment 1 and contain medicine 10% particle size is 1-250 μm microspheres. Sieve to remove microspheres with a particle size greater than 150 microns, and divide into packages.

Embodiment 3

[0131] Take by weighing roticotine 0.2g, polylactide-glycolide (lactide: glycolide=50:50, molecular weight 25000) 0.8g, prepare by the method for embodiment 1 containing drug 20%, particle diameter For microspheres of 1-250 μm, but with 250 ml of 0.5% carboxymethylcellulose in water instead of 0.5% PVA in water. Sieve to remove microspheres with a particle size greater than 150 microns, and divide into packages.

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Abstract

The invention relates to a long acting sustained-release formulation containing dopamine-receptor stimulant medicine, which comprises 5-5- wt% of effective dose of dopaminergic acceptor medicaments, and 50-95 wt% of medicinal macromolecular auxiliary materials.

Description

technical field [0001] The present invention relates to a long-acting sustained-release preparation of a dopamine receptor agonist drug, more specifically, the present invention relates to a sustained-release microsphere for injection of a dopamine drug, an implant, a gel for injection and a preparation method thereof, and the use of this The preparation of similar compounds is used for the treatment or auxiliary treatment of diseases related to dopamine receptors and the long-acting sustained-release preparations for the treatment of Parkinson's diseases such as Parkinson's disease or Parkinson's syndrome (hereinafter collectively referred to as Parkinson's disease). is the method of microspheres. Background technique [0002] Dopamine receptor agonists are an important class of drugs for the treatment of Parkinson's disease. The currently clinically used dopamine receptor agonists dopamine agonist drugs are rotigotine, pramipexole, and ropinil. Ropinirole, pergolide, terg...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/08A61K9/16A61K31/136A61K31/341A61K31/381A61K31/40A61K47/34A61P25/16
Inventor 张路平
Owner SHANDONG LUYE PHARMA CO LTD
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