Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1997-06-24
1999-09-21
Cook, Rebecca
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514174, 514178, 514180, 514357, 514653, 514757, 514758, 514759, 424 45, 424 46, 424489, 424499, 6048901, A01N 4304, A61K 3156, A61K 3170
Patent
active
059554398
DESCRIPTION:
BRIEF SUMMARY
This is a 371 of PCT/EP95/05085 filed Dec. 22, 1995.
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.
Surprisingly, the applicants have now found that particular sugars may advantageously be used to prepare novel aerosol formulations.
Thus, one aspect of the invention provides an aerosol formulation comprising:
In an alternative embodiment the present invention provides a pharmaceutical aerosol formulation as hereinbefore defined with the provisos that when said formulation consists essentially of human insulin, soybean lecithin S100, lactose and heptafluoropropane the weight to weight ratio of medicament to lactose is other than 1:1 and that when said formulation consists essentially of salbutamol, soybean lecithin S100, lactose and heptafluoropropane the weight to weight ratio of medicament to lactose is other than 200:1798.
The particle size of the particulate (e.g. micronised) medicament should be such as to permit substantially all of the particles to be potentially available for inhalation into the lungs upon administration of the powder composition. Thus, for example, at least 90%, preferably at least 95% by weight of the particles will have a diameter of less than 15 micrometers, preferably in the range of 1 to 10 micrometers, for example 1 to 5 micrometers.
The final aerosol formulation desirably contains 0.005-10% w/w, preferably 0.005-5% w/w, especially 0.01-1.0% w/w, of medicament relative to the total weight of the formulation.
Medicaments which may be administered in aerosol formulations according to the invention include any drug useful in inhalation therapy and which may be presented in a form which is substantially completely insoluble in the selected propellant. Appropriate medicaments may thus be selected from, for example, analgesics, e.g. codeine, dihydromorphine, ergotamine, fentanyl or morphine; anginal preparations, e.g. dilfiazem; antiallergics, e.g. cromoglycate, ketotifen or nedocromil; antiinfectives e.g. cephalosporins, penicillins, streptomycin, sulphonamides, tetracyclines and pentamidine; antihistamines, e.g. methapyrilene; anti-inflammatories, e.g. beclomethasone, flunisolide, budesonide, tipredane, triamcinolone acetonide or fluticasone; antitussives, e.g. noscapine; bronchodilators, e.g. ephedrine, adrenaline, fenoterol, formoterol, isoprenaline, metaproterenol, phenylephrine, phenylpropanolamine, pi
REFERENCES:
WPIDS AN 88-072 668, Axelsson et al, 1988.
Cook Rebecca
Glaxo Group Limited
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