Hydrofluorocarbon propellant containing medicinal aerosols

A - Human Necessities – 61 – K

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A61K 9/12 (2006.01) A61K 9/00 (2006.01)

Patent

CA 2187447

1,1,1,2,3,3,3-heptafluoropropane (HFC-227) has been identified as a highly polar propellant. Surfactants which have an elevated value (9.6 or greater) for their hydrophilic-lipophilic balance (HLB) can be used as suspending, wetting, and lubricating agents or cosolvents in metered dose inhaler (MDI) formulations pressurized with HFC-227 or propellant blends that contain HFC-227. Particularly, preferred surfactants include polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan mono-oleate, polyethylene glycol 300, propoxylated polyethylene glycol, polyoxyethylene 4 lauryl ether, and diethylene glycol monoethyl ether.

On a découvert que le 1,1,1,2,3,3,3-heptafluoropropane (HFC-227) constitue un agent propulseur hautement polaire. Des agents tensioactifs qui présentent une valeur d'équilibre hydrophile-lipophile élevée (9,6 ou plus) s'utilisent comme agents de mise en suspension, d'humidification et de lubrification ou comme co-solvants dans des formulations pour inhalateurs à doses mesurées mises sous pression avec le HFC-227 ou des mélanges d'agents propulseurs le contenant. Les agents tensioactifs nettement préférés incluent le polyoxyéthylène sorbitan monolaurate, le polyoxyéthylène sorbitan mono-oléate, le polyéthylène-glycol 300, le polyéthylène-glycol propoxylaté, le polyoxyéthylène 4 lauryl éther, et le diéthylène-glycol monoéthyl éther.

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