Slow release microsphere preparation of derivative of 3,3 ¿C diphenyl propylamine as receptor antagon of toadstool alkali in use for injection
A technology of diphenylpropylamine derivative and sustained-release microsphere preparation, applied in 3 as a muscarinic receptor antagonist, can solve problems such as increased treatment cost, inability to long-act sustained release, and low bioavailability
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Embodiment 1
[0061] 0.6g (R)-N, N-diisopropyl-3-(2-hydroxyl-5-hydroxymethylphenyl)-3-phenylpropylamine (compound Ia), 9.4g polylactide-glycolide Ester (lactide: glycolide = 50:50, molecular weight 25,000) was dissolved in 50ml of dichloromethane, under vigorous stirring (1200-1600rpm), it was dripped into 2500ml of 0.5% PVA aqueous solution, and continued to vigorously Stir for 3-10 minutes, then reduce the stirring speed to 300 rpm, evaporate the solvent for 4-6 hours, filter, wash the microspheres with distilled water three times, and freeze-dry. The particle size is 1-200 μm, the drug content is 3.8%, and the embedding rate is 63%.
[0062] The slow-release microspheres were tested for in vivo release in rabbits. The dose is 10 mg / kg, the microspheres are suspended in normal saline for injection, and intramuscularly administered. Within 1 to 20 days, blood is collected for HPLC-MS detection, and the blood drug concentration is 1-20 ng / ml. It is proved that the sustained-release micros...
Embodiment 2
[0064] Weigh (R)-N, N-diisopropyl-3-(2-hydroxyl-5-hydroxymethylphenyl)-3-phenylpropylamine (compound Ia) 0.5g, polylactide-glycolide (lactide:glycolide=50:50, molecular weight 13000) 9.5g, prepared by the method of Example 1, containing 4.7% of the drug microspheres with a particle size of 1-200 μm, the embedding rate was 94%.
Embodiment 3
[0066] Weigh (R)-N, N-diisopropyl-3-(2-hydroxyl-5-hydroxymethylphenyl)-3-phenylpropylamine (compound Ia) 1.0g, polylactide-glycolide (Lactide:glycolide=50:50, molecular weight 35000) 9.0g, prepared by the method of Example 1 containing 6.5% drug, microspheres with a particle size of 1-200 μm, the embedding rate was 65%.
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