INHALED ANTIBACTERIAL FORMULATIONS FOR TREATING LUNG INFECTIONS

Smart overview of the Invention

The patent application introduces a new formulation of tigecycline for treating lung infections. The composition is a carrier-free, micronized powder with a mean particle size of less than 7 μm, designed for inhalation. This formulation addresses the limitations of traditional antibiotic therapies by delivering the drug directly to the lungs, enhancing its concentration at the infection site, and reducing systemic side effects.

Background

Traditional treatments for pulmonary infections often rely on intravenous or oral antibiotics, which require high doses to reach effective concentrations in the lungs. This can lead to poor therapeutic outcomes and increased toxicity. Inhalation therapy offers an alternative by delivering drugs directly to the lungs, improving efficacy and reducing adverse effects. Tigecycline, a broad-spectrum antibiotic, is effective against various bacteria but faces challenges like chemical instability and high dose requirements when administered systemically.

Composition Details

The innovative formulation is a dry powder composed of micronized tigecycline with specific particle size distributions. It is free from stabilizing excipients, which can act as nutrients for bacteria. The powder is designed for pulmonary administration through various devices such as dry powder inhalers or nasal sprays. This approach not only enhances stability and ease of use but also eliminates the need for reconstitution.

Stability and Administration

The composition demonstrates significant stability under various conditions, maintaining its integrity at temperatures up to 40°C and relative humidity levels up to 75% for extended periods. The method of treatment involves administering micronized tigecycline via inhalation devices, offering an initial dose ranging from 5 mg to 15 mg, with maintenance doses adjusted accordingly. This method targets both gram-negative and gram-positive bacterial infections effectively.

Therapeutic Application

This novel inhalation formulation allows for reduced dosing compared to traditional systemic administration, with initial doses as low as 10 mg. It provides superior aerosol performance and drug stability, making it particularly suitable for treating infections caused by resistant bacteria like Stenotrophomonas maltophilia and others. The method also supports the concurrent use of additional active agents to enhance therapeutic outcomes.