Research And Preparation Of MAT-Freeze-Drying Liposomal Injection

Objective: To explore the industrial preparation method of liposome, and utterly raise the entrapment efficiency (EE,%) , resolve the poor stabilization , enhance the therapy concentration of drug matrine (matrine ,MAT) in liver ,this task used freeze-drying technology package MAT with liposome ,and prepared the injection pharmaceutical of MAT-freeze -drying liposome .Methods: Based with pretrival ,we used freeze-drying method ,choosing the single factors firstly ,optimized method by orthogonall design and came out the best technology.Weighed by appearance , particle size distribution , dissolubility and entrapment efficiency (EE,%) of MAT in liposome et ,we prepared the MAT-Freeze-Drying liposomal injection. EE was determined with ultraviolet spectrophotometery of continuous flowing liquid from the column of Sephadex G50. In this paper , we monitored the EE with the high liquid chromatography, observed the appearance by TEM with negative staining, measured the particle diameter by granulometry apparatus ,examined the dissolution profiles in vivo using dynamoic dialyzetion ,checked the concentration of drug by HPLC, measured the targeting capability by observing the drug concentration in mice.Results: The results showed that using the defined method ,we prepared good MAT-Freeze-Drying liposomal injection :it has cream colored, full, loose appearance; good dissolubility ; round and oval granule appearance through TEM, well-distributed particle size distribution,as 96%-99% is during 50nm-400nm,and the equally diameter is 120±20nm;Research indicated , the EE measuration is reliable ,and measured the average EE is 88.3%, drug loading ratio is 36.79%; Using HPLC, we found both the peak figure of drug and the standard curve were ideal, and the average concentration is 49.22mg; In vivo experiment showed that the relation of culminateve drug and time accord to Higuchi equation; we also setup the preliminary quality standard of MAT-Freeze-Drying liposmal injection . The initial stability test displayed that the product is stable. In the vein injection experiment on animal, the drug percentage 40%-50% detained the liver showed that they have good distinct targeting capacity.