Novel aerosol formulation containing a polar fluorinated molecule
OwnerPhilippe Roguedainventor
Life of this patent
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Abstract
The present invention relates to a stable pharmaceutical aerosol formulation intended for inhalation. The formulation contains an active substance, an aerosol propellant, a polar flurorinated molecule and an excipient. The preferred propellant is HFA 134a or HFA 227 or a mixture thereof.
Claims18
A pharmaceutical formulation comprising a drug, an aerosol propellant, a polar fluorinated molecule and an excipient.
A pharmaceutical aerosol formulation as claimed in any preceding claim, wherein the excipient is a PEG co-polymer.
A pharmaceutical aerosol formulation as claimed in any preceding claim, wherein the excipient is a PEG-phospholipid.
A pharmaceutical aerosol formulation as claimed in any preceding claim, wherein the excipient is selected from:
- Acrylidone 1005, Crodesta F160, Methoxy PEG Amine, Methoxy PEG carboxymethyl, 4 arms PEG, Cholic acid, MYRJ 52 P, APG-810-XL, APG-1014-XL, Glucopon 215, Glucopon 600, Brij 52, Gum Xanthan, Salicylic Acid, D-Lacotose monohydrate, α Lactose monohydrate, Lecithin egg, Carrageean, Sokalan CO5, Eudragit RLPO, Eudragit RSPO, Eudragit E100, Eudragit S100, Eudragit L100, Poly (DL-lacide coGlycolide), Gantrez S-97 BF, Gantrez AN-119, Gantrez AN-169, Myrisitic acid, Poly (lactide EO Lactid), Poly (methyl methacrylate-β-ethylene oxide), Lactose, Carboxymethyl cellulose Sodium Salt, 1-O-n-Octyl β D glucopyranoside, AOT DI-CF4H, Dioctyl-sulfosuccinate sodium salt (AOT), Phospholipon 100, Crodesta F10, Crodesta SL 40, APG 3399, Methoxy-PEG-DSPE MW 2000, Methoxy-PEG-DSPE MW 5000, N Dodecyl β D Maltoside, N Octyl β D Glucopyranoside, α cyclodextrin, β cyclodextrin hydrate, β cyclodextrin, γ cyclodextrin hydrate, γ cyclodextrin, γ cyclodextrin hydrate, Deoxycholic acid, Taurocholic acid, D-Mannitol, Poly (Methyl Methacrylate), Montanov 202, Montanov 68 EC, n Dodecyl β D Glucopyranoside, N Decyl β D Glucopyranoside, n Decyl β D Maltopyranoside, Glucamate DOE-120, Glucate SS, Glucamate SSE-20, Glucam DOE-120, Glucam P10, Glucam E20, Glucam P20 disteared, Glucam P20, Glucquat 125, Brij 30, Brij 96, Crodasinic LS 30, Crossential L99, Copolymer VC 713, Copolymer 958, Glucopon 650 EC, α Tocopherol, PVP K30, K25 and Plasdone K-29/32, PEG 600 and 1000, Three-Arm Poly (ethylene glycol),
- lactose based compounds (eg Poly (lactide-co glycolide), Lactitol, Lactose, Cellulose based compounds (e.g. Carboxymethylcellulose, Cellulose, Hydroxypropyl cellulose), Faty acids (e.g. Castor oil), PEG and derivatives (e.g. Star PEG), Sugar compounds (e.g. Alkyl polyglucosides, Methyl glucosides, Sucrose esters, such as Berol AG6202, Glucopon chemical range, Montanov 68, Montanov 202, Grilloten LSE87, Crodesta chemical range), Poly(ethylene Oxide) compounds (e.g. Hydroxy terminated Three-Arm Polyethylene oxide, Hydroxy terminated Eight-Arm Polyethylene oxide, Carboxy terminated Eight-Arm Poyethylene Oxide, 4 Arms Star Polythylene Oxide, Poly(methyl methacrylate b-ethylene oxide), Poly(t-butyl methacrylate-b-ethylene oxide), Poly(lactide-ethylene oxide-lactide triblock copolymer), Ω-Diacrylonyl terminated poly(lactide-ethylene oxide-lactide) triblock copolymer, Poly(lactone-β-ethylene oxide-β-lactone) triblock copolymer, Poly(ethylene oxide-β-caprolactone), Poly(ethylene oxide-β-propylene oxide) also known as PEO-PPO copolymers, Poly(methy methacrylate-β-ethylene oxide) also known as PMMA-PEO copolymers)). Further examples include Citric acid, Dibutyl Sebacate, Edetic acid, Glyceryl monooleate & monostearate, Glycofinol, Crodamol chemical range, Maltitol, Maltodextrin, Triglyceride, Polymethacrylate, Polyosyethylene alkyl ether, Sodium citrate dihydrate, Sorbitol, Mirj and Brij chemical range, Pluronic chemical range, Acrylidone 1005, Fluorinated AOT with different degrees of fluorination, Cholic acid, Copolymer 958, Copolymer VC713, Crossential L99, Crodasinic LS30, AOT Sodium salt, Phospholipon 100H, Salycilic acid, Sokalan CO5, Poly (lactide co glycolide), Poly(ethylene-β-methyl methacrylate), Poly(ethylene-β-2-vinyl pyridine), Poly(ethylene-β-4-vinyl pyridine), Poly(methyl methacrylate-β-sodium acrylate), Poly(methyl methacrylate-β-sodium methacrylate), PEG derivative compounds (Amino acid-PEG, Carboxyl-PEG copolymers, Methoxy PEG amine, Methoxy PEG carboxymethyl, Branched PEG 4 arms, star PEG, PEG-PLA-PEG triblock copolymer), sugar branched cyclodextrins derivatives, PEO cyclodextrins derivatives, and Dendrimer-PEO-Dendrimer triblock-copolymers, Methoxy-PEG-DSPE MW 5000, Eudragit E100, Glucamate DOE 120, Methoxy-PEG-DSPE MW 2000, Acrylidone 1005, Crodesta F160, Methoxy PEG Amine, Methoxy PEG carboxymethyl, 4 arms PEG, Cholic acid, MYRJ 52 P, APG-810-XL, APG-1014-XL, Glucopon 215, Glucopon 600, Brij 52, Gum Xanthan, Salicylic Acid, D-Lacotose monohydrate, α Lactose monohydrate, Lecithin egg, Carrageean, Sokalan CO5, Eudragit RLPO, Eudragit RSPO, Eudragit E100, Eudragit S100, Eudragit L100, Poly (DL-lacide coGlycolide), Gantrez S-97 BF, Gantrez AN-119, Gantrez AN-169, Myristic acid, Poly (lactide EO Lactid), Poly (methyl methacrylate-β-ethylene oxide), Lactose, Carboxymethyl cellulose Sodium Salt, 1-O-n-Octyl β D glucopyranoside, AOT DI-CF4H, Dioctyl-sulfosuccinate sodium salt (AOT), Phospholipon 100, Crodesta F10, Crodesta SL 40, APG 3399, Methoxy-PEG-DSPE MW 2000, Methoxy-PEG-DSPE MW 5000, N Dodecyl β D Maltoside, N Octyl β D Glucopyranoside, α cyclodextrin, β cyclodextrin hydrate, β cyclodextrin, gamma cyclodextrin hydrate, gamma cyclodextrin, gamma cyclodextrin hydrate, Deoxycholic acid, Taurocholic acid, D-Mannitol, Poly (Methyl Methacrylate), Montanov 202, Montanov 68 EC, n Dodecyl β D Glucopyranoside, N Decyl β D Glucopyranoside, n Decyl β D Maltopyranoside, Glucamate DOE-120, Glucate SS, Glucamate SSE-20, Glucam DOE-120, Glucam P10, Glucam E20, Glucam P20 disteared, Glucam P20, Glucquat 125, Brij 30, Brij 96, Crodasinic LS 30, Crossential L99, Copolymer VC 713, Copolymer 958, Glucopon 650 EC, α Tocopherol, PVP K30, K25 and Plasdone K-29/32, PEG 600 and 1000, Three-Arm Poly (ethylene glycol).
The use of a polar fluorinated molecule in conjunction with an excipient to reduce deposition and creaming of a pharmaceutical aerosol formulation, and obtain a very fine stable suspension comprising a hydrofluoroalkane propellant having dispersed therein drug particulates.
Dependencies are inferred from the claim text.