Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid
Patent
1997-03-27
1998-12-15
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
Organic pressurized fluid
514180, 514265, 514456, 514653, 514975, A61L 904, A61K 3156, A61K 3152, A61K 3135, A61K 31135
Patent
active
058492658
DESCRIPTION:
BRIEF SUMMARY
This application is filed pursuant to 35 U.S.C. .sctn.371 as a United States National Phase Application of International Application No. PCT/IB95/00866, filed 27 Sep. 1995, which claims priority from 9419536.9 (GB), filed 28 Sep. 1994.
This invention relates to aerosol formulations of use for the administration of medicaments by inhalation.
The use of aerosols to administer medicaments has been known for several decades. Such aerosols generally comprise the medicament, one or more chlorofluorocarbon propellants and either a surfactant or a solvent, such as ethanol. The most commonly used aerosol propellants for medicaments have been propellant 11 (CCl.sub.3 F) and/or propellant 114 (CF.sub.2 ClCF.sub.2 Cl) with propellant 12 (CCl.sub.2 F.sub.2). However these propellants are now believed to provoke the degradation of stratospheric ozone and there is thus a need to provide aerosol formulations for medicaments which employ so called "ozone-friendly" propellants.
A class of propellants which are believed to have minimal ozone-depleting effects in comparison to conventional chlorofluorocarbons comprise fluorocarbons and hydrogen-containing chlorofluorocarbons, and a number of medicinal aerosol formulations using such propellant systems are disclosed in, for example, EP 0372777, WO91/04011, WO91/11173, WO91/11495 and WO91/14422. These applications are all concerned with the preparation of pressurised aerosols for the administration of medicaments and seek to overcome the problems associated with the use of the new class of propellants, in particular the problems of stability associated with the pharmaceutical formulations prepared. The applications all propose the addition of one or more of adjuvants such as alcohols, alkanes, dimethyl ether, surfactants (including fluorinated and non-fluorinated surfactants, carboxylic acids, polyethoxylates etc) and even conventional chlorofluorocarbon propellants in small amounts intended to minimise potential ozone damage.
It is well established in the art that fluorinated surfactants may be used to stabilise micronised drug suspensions in hydrofluorocarbon propellants such as 1,1,1,2-tetrafluoroethane (P134a), see for example U.S. Pat. No. 5,126,123, WO91/11173, WO91/14422 and WO92/00062. Surprisingly, the applicants have now found that a particular group of fluorinated surfactants may be used to prepare novel aerosol formulations, and can be advantageous in terms of reducing drug deposition, increasing shelf life and like.
Thus, in one aspect the invention provides a pharmaceutical aerosol formulation which comprises particulate medicament, a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant and a surfactant of general formula (Ia) or (Ib) ##STR2## wherein: R.sup.1 represents: --(CH.dbd.CH).sub.d --(CH.sub.2).sub.e --A--; (wherein each of R.sup.6 and R.sup.7 represents C.sub.1 -C.sub.4 alkyl or hydroxyethyl), --(CH.sub.2).sub.t --, wherein t=0 or 1 or --C(O)N(R.sup.9)--(CH.sub.2).sub.q --B, wherein q is an integer from 0 to 12, B represents --O-- or --C(O)--, and R.sup.9 is hydrogen or R.sup.6, b+d is from 0 to 12 and each of f and g is from 1 to 12; following structures: and R.sub.F 1 represents CF.sub.3 --, C.sub.2 F.sub.5 -- or (CF.sub.3).sub.2 CF--, 6 and wherein each of R.sub.F 2 and R.sub.F 3 independently represents CF.sub.3 --, C.sub.2 F.sub.5 --, n-C.sub.3 F.sub.7 -- or CF.sub.3 CF.sub.2 CF(CF.sub.3)-- or R.sub.F 2 and R.sub.F 3 taken together represent --(CF.sub.2).sub.4 -- or --(CF.sub.2).sub.5 --, or atoms are replaced by one or more hydrogen or bromine atoms and/or at least two chlorine atoms in a proportion such that at least 50% of the atoms bonded to the carbon skeleton of R.sub.F are fluorine atoms, and wherein R.sub.F contains at least 4 fluorine atoms, C.sub.3 -C.sub.20 acyl; or C.sub.1 -C.sub.4 alkyl group; hydrogen atom; a C.sub.1 -C.sub.4 alkyl group, --CH.sub.2 CH.sub.2 O(CH.sub.2 CH.sub.2 O).sub.s R.sup.3, wherein s represents an integer of from 1 to 5, or R.sup.4 and R.sup.5 when taken together represent --(CH.sub.2).sub.q wherein
REFERENCES:
patent: 4352789 (1982-10-01), Thiel
patent: 5126123 (1992-06-01), Johnson
patent: 5344930 (1994-09-01), Riess et al.
Johnson Keith A.
Li-Bovet Li
Glaxo Wellcome Inc.
Jordan Kimberly
Riek James P.
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