Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid
Patent
1994-12-27
1997-03-04
Nutter, Nathan M.
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
Organic pressurized fluid
424434, 424435, A61K 914
Patent
active
056076622
DESCRIPTION:
BRIEF SUMMARY
This invention relates to pharmaceutical compositions for administration by inhalation, more particularly to non-pressurised powder compositions.
Many medicaments, especially those for the treatment of diseases of the respiratory tract, are administered by inhalation. However, some medicaments, such as reproterol hydrochloride, have an undesirable taste when administered by inhalation, this being due to that proportion of medicament which is; deposited in the mouth and throat of the patient. Thus, it would be desirable to modify the taste of inhalation compositions by incorporating a flavouring agent, as this may result in improved patient compliance especially if the patients are young children.
Medicaments for inhalation are commonly administered in the form of powders, either from pressurised canisters containing the powder in admixture with a liquefied gas aerosol propellant, or as non-pressurised dry powder compositions.
In the former case it is known to include flavouring and/or sweetening agents in the composition to improve the taste of the composition and/or to give the composition a recognisable flavour so that the patient realises when a dose has been inhaled, as disclosed in EP-A-365119. However, such compositions suffer from the disadvantage that the propellant may comprise a chlorofluorocarbon (CFC) which is thought to be harmful to the environment generally and the ozone layer in particular. Furthermore, the flavouring agent may be inhaled into the lung.
It would be desirable to incorporate flavouring agents into non-pressurised dry powder pharmaceutical compositions. However, flavouring agents usually exist as oils or sticky solids at room temperature. This renders them unsuitable for use in dry powder formulations, for example, because they have poor flow properties and could cause the powdered medicament to agglomerate thus reducing dispersion to the lung.
We now provide a pharmaceutical inhalation composition which overcomes or substantially mitigates these disadvantages.
We have now found that by entrapping the flavouring agent in a polysaccharide, the flavouring agent may be kept sufficiently free flowing to be incorporated into non-pressurised powder inhalation compositions.
Thus, according to the invention, we provide a non-pressurised pharmaceutical inhalation composition comprising a therapeutically effective amount of a particulate inhalation medicament having a mass median diameter in the range 0.01 to 15 .mu.m and a particulate polysaccharide entrapped flavouring agent having a mass median diameter in the range 10 to 200 .mu.m.
Polysaccharide entrapped flavouring agents are known for use in the food industry. In addition to the flavouring agent and polysaccharide, food flavourings generally contain other excipients, for example emulsifying agents, e.g. acacia gum which is the gummy exudate from the stem and branches of Acacia senegal and other species of Acacia. However, we have found that the presence of excipients, such as emulsifying agents, may cause the polysaccharide entrapped flavouring agent to be sticky or otherwise render it unsuitable for use in non-pressurised pharmaceutical inhalation compositions. Therefore, we prefer the particulate polysaccharide entrapped flavouring agents used in the compositions according to the invention to contain a minimum amount of, and preferably no, excipients in addition to the flavouring agent and polysaccharide.
Any conventional pharmaceutically acceptable flavouring agents may be used, particular flavouring agents which may be mentioned include volatile oils, e.g. peppermint oil; and menthol. The proprietary product known by the tradename DENTOMINT.TM. flavouring agent, which contains both peppermint oil and menthol, may also be used. We prefer the flavouring agent to be peppermint oil BP/Ph. Eur.
Polysaccharides in which the flavouring agent is entrapped include, for example, polyglucoses. We prefer the polysaccharide to be a dextran or a dextrin. We particularly prefer the polysaccharide to be a dextrin, especially maltodextrin. De
REFERENCES:
patent: 5254330 (1993-10-01), Ganderton et al.
Baskeyfield Lewis J.
Jay Graham F.
Wright Paul
Fisons plc
Nutter Nathan M.
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