Aqueous suspension for nasal administration

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/56 (2006.01) A61K 9/00 (2006.01) A61K 9/12 (2006.01) A61K 31/565 (2006.01) A61K 47/38 (2006.01) A61P 37/08 (2006.01)

Patent

CA 2278025

Loteprednol etabonate having excellent antiinflammatory and antiallergic activities is expected to be developed as a drug for external application but when it is formulated into an aqueous suspension, the aggregation and precipitation of particles tend to take place. According to the present invention, long-term stabilization of the suspension was successfully achieved by formulating loteprednol etabonate with microcrystalline cellulose carmellose sodium. Moreover, the resulting suspension features a remarkably improved intranasal retention and no dermal or mucosal irritation.

On pensait pouvoir utiliser l'étabonate de loteprednol comme médicament à usage externe présentant d'excellentes propriétés anti-inflammatoires et anti-allergiques; mais lorsqu'il est préparé en solution aqueuse, il est l'objet d'une agglutination et d'une précipitation des particules. La présente invention a réussi à obtenir une stabilité à long terme de la suspension en y associant de la cellulose carmelose sodique microcristalline, la suspension résultante présente de plus une rétention intranasale remarquablement améliorée sans produire d'irritation de la peau ou des muqueuses.

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