| 摘要 |
The present invention relates to novel microparticles of amphiphilic polyamino acids that transport active ingredient(s) - AI(s) -, in particular protein and peptide active ingredient(s), and also to novel modified-release pharmaceutical formulations containing said microparticles of AI. The objective of the invention is to develop novel microparticles loaded with AI, obtained by aggregation of nanoparticles of amphiphilic polyamino acids, and having improved properties, in particular in dry solid form, with regard to their capacity for dispersion and, as regards the reconstituted suspension, with regard to its stability and its ability to be readily handled and injected. In a first aspect, the invention relates to microparticles of amphiphilic polyamino acid (PO) containing at least one AI (associated noncovalently), spontaneously forming a colloidal suspension of nanoparticles in water, at pH 7.0, under isotonic conditions; wherein said microparticles are characterized a. in that they are obtained by atomization of a colloidal suspension or solution of PO comprising at least one AI, b. by a size of between 0.5 and 100 µm, and c. in that they are dispersible in a colloidal suspension. The invention also relates to the method for preparing these microparticles, to a liquid formulation comprising a suspension of these PO/AI microparticles, to a method and a kit for reconstituting this formulation, and to a dry form of this formulation. |
