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.
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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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