US 12,419,838 B2
Pharmaceutical formulation with improved solubility and bioavailability
Jose Maria Lagaron Cabello, Valencia (ES); Cristina Prieto Lopez, Lugo (ES); Jose Manuel Valle Baz, Castellon de la Plana (ES); David Galan Nevado, Malaga (ES); and Julia Hrakovsky, Gdynia (PL)
Assigned to Consejo Superior de Investigaciones Cientificas (CSIC), Madrid (ES); and BIOINICIA, S.L., Valencia (ES)
Filed by Consejo Superior de Investigaciones Cientificas (CSIC), Madrid (ES); and BIOINICIA, S.L., Valencia (ES)
Filed on Oct. 24, 2022, as Appl. No. 17/972,172.
Application 17/972,172 is a division of application No. 17/255,680, abandoned, previously published as PCT/EP2019/067342, filed on Jun. 28, 2019.
Claims priority of application No. 18382484 (EP), filed on Jun. 29, 2018.
Prior Publication US 2023/0040719 A1, Feb. 9, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/10 (2006.01); A61K 9/14 (2006.01); A61K 9/16 (2006.01); A61K 9/50 (2006.01); A61K 45/06 (2006.01); B82Y 5/00 (2011.01); B82Y 30/00 (2011.01); B82Y 40/00 (2011.01)
CPC A61K 9/146 (2013.01) [A61K 9/1611 (2013.01); A61K 9/1652 (2013.01); A61K 9/1694 (2013.01); A61K 45/06 (2013.01); B82Y 5/00 (2013.01); B82Y 30/00 (2013.01); B82Y 40/00 (2013.01)] 3 Claims
OG exemplary drawing
 
1. A method to prepare sub-micron particles between 1 and 800 nm of at least one active pharmaceutical ingredient or pharmaceutical acceptable salt thereof encapsulated into microparticles between 1 and 100 μm comprising excipients, the method practiced in a facility comprising:
an injection unit, which is an electronebulizer, comprising at least:
one inlet for an emulsion;
one inlet for injection gas; and
one outlet for droplets through which sprayed droplets of emulsion are released, a drying unit, which is arranged after the injection unit, and
a collection unit, arranged after the drying unit;
the method comprises the following steps:
a) preparing of an emulsion comprising:
at least one active pharmaceutical ingredient or pharmaceutically acceptable salt thereof to be encapsulated,
one or more excipients;
at least two non-miscible or partially miscible solvents or two miscible solvents that by solubilizing the API or the excipients become non-miscible or partially miscible solvents,
b) forming droplets of nano-embedded microparticles in only one step by the electronebulizer from the emulsion obtained in stage (a) in the presence of an injection gas flow that creates the droplets and applying a voltage of between 0.1 kV and 500 kV at the outlet of the injection unit,
c) drying the droplets obtained in stage (b) in the drying unit at a controlled room temperature to obtain the microparticles; and
d) collecting the microparticles obtained in stage (c) by means of the collection unit.