Nasal Chitosan Microspheres Of Galanthamine Hydrobromide Preparation Process And Preliminary Targeting Evaluation

This research establishes assay method of galanthamine hydrobromidedetermination in vitro. Emulsion crosslinking method was adopted to preparethe galanthamine hydrobromide chitosan microsphere, using the sizedistrbution of microspheres, drug loading，entrapped efficiency as combinedindex to optimize the prescription and technology. Directly observe theappearance and the size distribution of microspheres by light microscope andscanning electron microscope. Using rats as experimental animal model, weresearch the pharmacokinetics and brain targeting distribution of chitosanmicrospheres of galanthamine hydrobromide following intranasaladministration.The optimized chitosan concentration was4%, oil-water ratio was5:1，thedosage of formaldehyde was3ml and the dispersing stirring speed was200r/min. The chitosan microspheres of galanthamine hydrobromide preparedaccording to the optimized formula and preparation technology were toroid withuniformity disposition of particle size, mean particle diameter was30?70li m, the proportion of an average of74.86%, average entrapped efficiency ratewas67.53%and drug loading of the average of14.66%. The microsphereadhesiveness was favorable and no nasal toxicity. It was stable inhyperthermy、 high humidity and for long-term storage. Compared with oraladministration, the chitosan microspheres were taken following intranasal administration. Pharmacokinetics test indicated that the drug plasma halflife became177.02min from46.98min and the AUC value in plasma obtainedfollowing intranasal administration was12.13times of that following oraladministration. The results possessed the good ability of brain targeting.