KAGAKU KOGAKU RONBUNSHU, Vol.30, No.1, 43-46, 2004
Adding effect of saccharides to microsuspension particle sizes of griseofulvin-lipid mixtures subjected freeze-drying and rehydration
Preparation and stabilization of particle sizes of microsuspensions of the practically insoluble drug griseofulvin (GF) and hydrogenated soybean lecithin mixtures were investigated to improve drug dissolution. Particle sizes in the suspension gradually decreased with increasing pass number through an interaction chamber, and reached an average of 60 nm at the pass number 20, when the suspension became transparent. Polydispersion index (dw/dn) also decreased with increasing pass number to a value of 1-2. The microsuspension could be preserved for about 1 month in a refrigerator, but it gradually became opaque after two weeks of strage at room temperature. Particle sizes in a rehydrated freeze-dried microsuspension were practically restored to those of the original microsuspension, when a saccharide such as xylitol, treharose or sucrose was added at more than 5, 3 and 3 wt%, respectively, before the freezing procedure. The restration of nano-size particles restoring is related to the molecular interactions among saccharides, drug and water molecules. The results obtained above provide valuable information for proposing practically liquid dosage forms for drug delivery.
Keywords:freeze-dry rehydration;improving drug dissolution;microsuspension of drug and lecithin mixtures;preserving nano-size suspension by saccharide addition