Patent ID: 8568778

Claim:
An oral multiparticulate pharmaceutical form comprising pellets having an average diameter in the range from 50 to 2500 μm, the pellets comprising a) an inner matrix layer comprising nanoparticles, wherein the nanoparticles comprise a nucleic acid active ingredient and are embedded into a matrix of a polymer having a mucoadhesive effect, wherein the matrix may optionally comprise pharmaceutically acceptable excipients, and b) an outer film coating comprising an anionic polymer or copolymer which may optionally be formulated with pharmaceutically acceptable excipients, wherein the multiparticulate pharmaceutical form is formulated so that the pellets are released in the pH range of the stomach, the outer film coating is adjusted through the choice of the anionic polymer or copolymer and its formulation with the excipients and its layer thickness so that the outer film coating dissolves in a pH range from 4.0 to 8.0 in the intestine within 15 to 60 min so that the inner matrix layer is exposed and can bind to the intestinal mucosa and release the nucleic acid active ingredient into the intestinal mucosa, wherein the polymer having a mucoadhesive effect exhibits a mucoadhesive effect of at least η b =150 to 1000 mPa·s and a water uptake of from 10 to 750% in 15 min in a range of +/−0.5 pH units relative to the pH at which the outer film coating starts to dissolve, and the nucleic acid active ingredient of the nanoparticles in the inner matrix layer is a maximum of 40% by weight of the content of the polymers having a mucoadhesive effect wherein the nucleic acid active ingredient in the nanoparticles is present in the form of a complex with a cationic substance that is a cationic lipid, a cationic polypeptide or a cationic polymer and an anionic (meth)acrylate copolymer.