Nebulised antibiotics for inhalation therapy

Abstract

The present invention provides pharmaceutical aerosols which are useful for the prevention or treatment of infectious diseases of the airways, such as the lungs, the bronchi, or the sinunasal cavities. The aerosols comprise an active agent selected from the group of quinolone antibiotics. Also disclosed are liquid and solid compositions suitable for being converted into the aerosols, and kits comprising such compositions.

Description

technical field [0001] The present invention relates to a medical aerosol suitable for preventing or treating infectious diseases of the trachea, such as the lung, bronchi or sinus cavity. The invention also relates to solid or liquid pharmaceutical compositions and kits for the preparation of said aerosols. Background technique [0002] The delivery of therapeutic compounds to the bronchi and lungs is primarily used for topical treatment of diseases and conditions of the respiratory system, such as asthma and bronchitis. More recently, pulmonary administration of systemic drugs (eg, insulin) has been proposed and has been actively investigated in product development programs, taking advantage of the large surface area of ​​the lung for absorption. [0003] Typically the drug substance can be delivered to the respiratory system as an aerosolized dry powder or as a liquid in the form of a solution or dispersion, such as a drug suspension. Various devices have been developed...

AI Technical Summary

Problems solved by technology

Depending on the particular active compound chosen, one or more disadvantages may be related to its teachings

[0015] First, water-soluble active compounds can be difficult to effectively associate with lipid-based colloidal drug carrier systems

Second, pharmaceutical compositions for inhalation use must be sterile for safety reasons, and the proposed formulation comprising a lipid-based colloidal drug carrier system is difficult to manufacture in a sterile form

Third, the proposed carrier particle size range is up to 2 microns, which presents considerable difficulties in converting the formulation to an aerosol with a particle size distribution in the range suitable for aerosol delivery to the lungs

Fourth, lipid-based colloidal drug delivery systems typically require large excipient loadings relative to the content of the active ingredient; and if, as in the case of many anti-infective compounds, the dose of the active ingredient is relatively high (e.g. , compared to corticosteroids or betamimetics for inhalation), then the resulting level of excipients (especially amphiphilic lipids) in any water-based liquid formulation would produce excessive viscosity Therefore, it is impossible to effectively aerosolize

On the other hand, if the formulation is diluted to reduce viscosity and allow for more efficient aerosolization, the liquid volume will increase, potentially increasing the required inhalation time beyond acceptable limits

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