RADEMAKER, Bernardus,MINNAARD, Willem Adriaan,VAN ZWIETEN, Eduard Johannes,WIELING, Jacob
申请号：
NL2019050384
公开号：
WO2019245373A1
申请日:
2019.06.21
申请国别(地区):
NL
年份:
2019
代理人:
摘要：
The invention relates, among others, to methods for preparing pharmaceutical compositions that can be provided to the subject in oral form, comprising as an active ingredient: a protein with a mass of 10 kilodalton or more, a nucleic acid molecule of 15 nucleotides or more, or a combination thereof. The one or more active ingredients are distributed in particles in a way that facilitates the uptake of the particles by the intestine and the release of the active ingredient(s) into the blood stream. Methods for preparing such pharmaceutical compositions comprise preparing an aqueous composition comprising one or more active ingredients； a mono- or disaccharide； one or more further compounds and chitosan； and spraying the prepared aqueous composition into an anti-solvent and/or supercritical fluid in which the water fraction of the composition is soluble or miscible and in which the solutes of the composition are not soluble, thereby precipitating the solutes and producing particles with an average diameter of 50 nanometers (nm) to 20 micrometers (urn)； collecting said particles； and preparing the pharmaceutical composition comprising said particles. Also provided are collections of particles with an average diameter of 50 nm to 20 um comprising a homogeneous distribution of indicated ingredients. Also provided is a pharmaceutical formulation in oral dosage form comprising such a collection of particles for use in the treatment of a disease.L'invention concerne, entre autres, des procédés de préparation de compositions pharmaceutiques qui peuvent être fournies au patient sous forme destinée à la voie orale, comprenant en tant que principe actif : une protéine dont la masse est de 10 kilodaltons ou plus, une molécule d'acide nucléique de 15 nucléotides ou plus, ou une combinaison de ceux-ci. Le ou les principes actifs sont répartis dans des particules d'une manière qui facilite l'absorption des particules par l'intestin et la libération du ou des principes actifs dans l
