Patent ID: 6207178
Filing Date: 2001-03-27
Classification: A01N,A61K,A61Q,B01F,B82Y,Y10S,Y10T

Abstract:
A suspension stable for at least about 12 months of particles of bioactive agents (PBAs) manufactured by an emulsifying process having the following steps:(a) melting at least one solid bioactive agent;(b) heating a dispersion medium to approximately the same temperature as said at least one molten solid bioactive agent formed by step (a);(c) adding at least one highly mobile water-soluble or dispersible stabilizer, which does not form a separate phase in the dispersion medium, to the dispersion medium in an amount effective after emulsification to stabilize newly created surfaces during recrystallization, and optionally adding at least one lipid-soluble or dispersible stabilizer to said at least one molten bioactive agent;(d) premixing said at least one molten bioactive agent and the dispersion medium, and subsequently homogenizing said mixture by high pressure homogenization, micro-fluidization and/or ultrasonication; and(e) allowing the homogenized dispersion to cool until solid particles are formed by recrystallization of the dispersed bioactive agents,wherein the PBAs consist of a single phase, and include a drug having a low bioavailability and/or being poorly absorbed from the intestinum, and having a melting point below about 100.degree. C. or which can be decreased to below about 100.degree. C. or which can be decreased to below about 100.degree. C. by addition of an adjuvant, which drug is selected from the group consisting of an anesthetic, a narcotic, an anticholinergic, an antidepressive, a physychostimulant, a neuroleptic, an antiepileptic, an antiphlogistic, a bronchodilator, a cardiovascular drug, a cytostatic, a hyperemic drug, a lipid reducer, a spasmolytic, a testosterone derivative, a tranquilizer, a virustatic, a vitamin A derivative, a vitamin E derivative, menadione, cholecalciferol, an insecticide, a pesticide, and a herbicide.