The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Apr. 17, 2018
Filed:
Jun. 18, 2014
Pharmathen S.a., Pallini Attikis, GR;
Evangelos Karavas, Pallini Attikis, GR;
Efthymios Koutris, Pallini Attikis, GR;
Sotiria Haitidou, Pallini Attikis, GR;
Theofanis Mantourlias, Pallini Attikis, GR;
Georgia Papanikolaou, Pallini Attikis, GR;
PHARMATHEN S.A., Pallini-Attikis, GR;
Abstract
The present invention relates to preparation of biodegradable microparticles formed from polylactide-polyglycolide copolymers (PLGA) polymer and how to achieve sigmoidal release of active pharmaceutical compound from the microparticles. In particular, the present invention relates to emulsification of an inner/oil phase to an outer/water phase followed by quenching and a single drying step for the preparation of microparticles having a preferred release profile of preferably basic/nucleophilic compounds such as risperidone. Alternatively the present invention is also suitable for hydrophobic compounds that have poor water-solubility and a high drug loading of >20% w/w is required. The release profile can be controlled by adjusting the degree of saturation of the outer/water phase with the organic solvent used in the inner/oil phase, the polymer concentration of the inner/oil phase and the temperature at the quenching step. In particular, an initial lag phase and a substantially sigmoidal release profile are achieved by using an outer aqueous phase over saturated with the solvent used in the inner phase at emulsification step, in combination with a low temperature during quenching.