Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid
Patent
1997-07-21
2000-11-28
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
Organic pressurized fluid
424 46, 514957, 514958, A61K 912
Patent
active
061531731
DESCRIPTION:
BRIEF SUMMARY
This invention relates to aerosol formulations of use in 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 CCl.sub.3 F (propellant 11) in admixture with CCl.sub.2 F.sub.2 (propellant 12) and CF.sub.2 Cl.CF.sub.2 Cl (propellant 114). 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 hydrogen-containing chlorofluorocarbons and fluorocarbons and a number of medicinal aerosol formulations using such propellant systems have been disclosed in, for example, EP 0372777, WP91/04011, W091/11173, W091/11495, W091/14422, W092/00061, W092/00062 and W092/00107.
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. These applications all propose the addition of a wide range 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 to minimise potential ozone damage.
Surprisingly, we have now found that mixtures of a non ozone-depleting propellant and a specific fluorinated hydrocarbon may be employed as propellant systems suitable for use in pharmaceutical aerosol compositions.
There is thus provided in one aspect of the invention an aerosol formulation comprising: 1,1,1,2,3,3,3-heptafluoro-n-propane (CF.sub.3 CHFCF.sub.3) or mixtures thereof as propellant;
Generally, the ratio of propellant: co-propellant is in the range of about 30:70 to about 95:5, preferably 50:50 to 90:10 by weight, especially 50:50 to 80:20, for example 75:25 (w/w).
Medicaments which may be administered in aerosol formulations according to the invention include any drugs useful in inhalation therapy which may be presented in a form which is substantially completely insoluble in the selected propellant system. Appropriate medicaments may thus be selected from, for example, analgesics, e.g. codeine, dihydromorphine, ergotamine, fentanyl or morphine; anginal preparations, e.g. dilitiazem; antiallergics, e.g. cromolyn, cromogylcate or nedocromil; antibiotics, e.g. cephalosporins, penicillins, streptomycin, sulphonamides or tetracyclines; antihistamines, e.g. methapyrilene; anti-inflammatories, e.g. beclomethasone, flunisolide, fluticasone, tipredane, budesonide, triamcinolone acetonide; antitussives, e.g. noscapine; bronchodilators, e.g. ephedrine, epinephrine, fenoterol, formoterol, isoprenaline, isoproterenol, metaproterenol, phenylephrine, phenylpropanolamine, pirbuterol, repoterol, rimiterol, salbutamol, salmeterol, terbutaline or (-)-4-amino-3,5-dichloro-.alpha.-[[[6-[2-(2-pyridinyl) ethoxy]hexyl]amino]methyl]benzenemethanol; diuretics, e.g. amiloride, anticholinergics e.g. ipratropium bromide; hormones, e.g. cortisone, hydrocortisone or prednisolone; and therapeutic proteins and peptides, e.g. glucagon or insulin. It will be clear to a person skilled in the art that, where appropriate, the medicaments will be used in the form of salts (e.g. as alkali metal or amine salts or as acid addition salts) or as esters (e.g. lower alkyl esters) or as solvates (eg hydrates) to optimise the activity and/or stability of the medicament and/or to minimise the solubility of the medicament in the propellant.
Particularly preferred medicaments fo
REFERENCES:
patent: 5314926 (1994-05-01), Robin et al.
patent: 5376359 (1994-12-01), Johnson
Sapsford Andrew
Savage Andrew Patrick
Channavajjala Lakshmi
Glaxo Group Limited
Page Thurman K.
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