The Study Of Alprostadil Long-Circulating Proliposome

Alprostadil(PGE₁), belonging to hormone,has extensive biological function,which includes:opening vacular smooth muscle,inhibiting blood platelet aggregation and gastric acid output,stimulating intestinal and uterine smooth muscle.but PGE₁ metabolizes fastly in vivo,about 80% inactivate in lung in one circulational progress.The object of this study was to obtain alprostadil preparation which activates for long circulating time in vivo . Expectably, the new dosage can prolong the retention time and weakean the clinical stimulation of the blood vessels.The research seperated liposome and dissociative drug by ultrafilter film way, founded a method to determine drug content and encapsulation efficiency by HPLC.Selecting encapulation efficiency and particle size as index ,we compared the different ways and membrane meterials to obtain the alprostadil liposomal preparation ,and found the best method—injection method. Through studying the many factor during injection,we adopted ethanol injection method to prepare directly liposome of the small size successfully.During this process,it was not applied to reduce the particle size of lipomes by ultrasonic or homogemizer.Through safety periments of the final products, we found the clinical blood vessel stimulation of alprostadil had improved obviously. The final products had no haemolytic reaction and Pyrogen reaction,It fit for requirement of intravenous injection.