Pharmaceutical composition for drug delivery

Inventors

Sävmarker, Jonas • Rönn, Robert • Fischer, Andreas

Assignees

Orexo AB

Abstract

According to the invention, there is provided a pharmaceutically-acceptable composition which is preferably in the form of a spray-dried powder comprising a mixture of: (a) a pharmacologically-effective dosage amount of at least one pharmaceutically-active compound; and(b) a pharmaceutically-acceptable carrier material, which carrier material comprises a combination of a disaccharide and a polymeric material. Compositions are suitable for, for example, transmucosal drug delivery, including sublingual and nasal delivery. In the case of nasal delivery, said compositions may be loaded into single- or multiple-use nasal applicators. Preferred pharmaceutically-acceptable carriers in this regard include lactose or trehalose and dextrins (e.g. cyclodextrins or maltodextrins), which may be spray-dried together in combination. Compositions may further comprise one or more alkyl saccharides. Preferred alkyl saccharides include sucrose esters, such as sucrose monolaurate.

Core Innovation

The invention relates to a nasal applicator device for intranasal delivery of a composition to nasal mucosa. The device includes a reservoir containing an amorphous powder and is free of liquid propellant, such that actuation deposits an effective dose to the nasal mucosa. The amorphous powder is an amorphous composite containing epinephrine or a pharmaceutically-acceptable salt thereof embedded with a carrier material.

In the amorphous powder, epinephrine or its pharmaceutically-acceptable salt is the sole active ingredient, and the carrier material comprises a combination of a disaccharide and a polymeric material. The polymeric material includes a dextrin and/or hydroxypropylmethyl cellulose, and the particles comprise an amorphous composite of epinephrine or the salt and the carrier material.

The powder particle size is configured so that, upon actuation of the nasal applicator device, an effective dose of epinephrine or salt is deposited to the nasal mucosa. The disclosed compositions further emphasize amorphous spray-dried mono-particulate powder compositions for transmucosal delivery and include stability-oriented constraints described in terms of glass transition temperature under controlled humidity and moisture/water barrier packaging.

Claims Coverage

The independent claim is directed to a nasal applicator device for intranasal delivery of an amorphous epinephrine powder without liquid propellant, using a specific amorphous composite particle design with a disaccharide/polymeric carrier and particle sizing configured for nasal deposition. Dependent claims further refine the composition and device delivery properties with additional quantitative constraints, including carrier component relationships, glass transition temperature conditions, dosage amount, particle size distribution metrics, and single-use/single-dose reservoir configuration.

Overall claim coverage centers on an intranasal nasal applicator device that delivers an amorphous mono-particulate powder free of liquid propellant, with epinephrine or a pharmaceutically-acceptable salt as the sole active ingredient. The particles are an amorphous composite with a carrier made from a disaccharide and a polymeric material comprising dextrin and/or hydroxypropylmethyl cellulose, and the particle size is configured to deposit an effective epinephrine dose to nasal mucosa upon actuation. Dependent claim refinements include single-use/single-dose reservoir configuration and additional quantitative constraints described in the partial content as glass transition temperature and particle size distribution metrics.

Stated Advantages

Documented Applications