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1. (WO2015039199) MICRO- AND NANOSTRUCTURED PHARMACEUTICAL AND VETERINARY COMPOSITIONS, CONTAINING BENZNIDAZOLE AND DERIVATIVES THEREOF, WHICH FORM MICRO- AND NANOSTRUCTURES IN THE GASTROINTESTINAL TRACT, AND BIOLOGICAL USES THEREOF
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2015/039199    International Application No.:    PCT/BR2014/000304
Publication Date: 26.03.2015 International Filing Date: 26.08.2014
IPC:
A61K 31/4168 (2006.01), A61K 9/51 (2006.01), A61P 33/02 (2006.01)
Applicants: UNIVERSIDADE FEDERAL DE OURO PRETO - UFOP [BR/BR]; Rua Diogo de Vasconcelos, 122, Bairro Pilar CEP 35.400-000 - Ouro Preto/MG (BR)
Inventors: MOSQUEIRA, Vanessa Carla Furtado; (BR).
OLIVEIRA, Liliam Teixeira; (BR).
CASTANHEIRA, Raquel Gomes; (BR)
Priority Data:
BR 102013023902-0 18.09.2013 BR
Title (EN) MICRO- AND NANOSTRUCTURED PHARMACEUTICAL AND VETERINARY COMPOSITIONS, CONTAINING BENZNIDAZOLE AND DERIVATIVES THEREOF, WHICH FORM MICRO- AND NANOSTRUCTURES IN THE GASTROINTESTINAL TRACT, AND BIOLOGICAL USES THEREOF
(FR) COMPOSITIONS PHARMACEUTIQUES ET VÉTÉRINAIRES MICRO- ET NANOSTRUCTURÉES CONTENANT DU BENZNIDAZOLE ET DES DÉRIVÉS ASSOCIÉS, QUI FORMENT DES MICRO- ET NANOSTRUCTURES DANS LE TUBE DIGESTIF, ET LEURS UTILISATIONS BIOLOGIQUES
(PT) COMPOSIÇÕES FARMACÊUTICAS E VETERINÁRIAS NAS FORMAS MICRO E NANOESTRUTURADAS E QUE FORMAM MICRO E NANOESTRUTURAS NO TRATO GASTROINTESTINAL CONTENDO BENZNIDAZOL E SEUS DERIVADOS E SUAS APLICAÇÕES BIOLÓGICAS
Abstract: front page image
(EN)The present invention describes methods for preparing micro- and nano-scale polymeric pharmaceutical forms encapsulating benznidazole for parenteral administration, and pharmaceutical forms for oral administration, which self-emulsify in contact with biological fluids, forming micro- or nanoemulsions. Microcapsules, microspheres, microemulsions, nanocapsules, nanospheres, nanoemulsions, solid, semi-solid and liquid lipid nanoparticles, lipid-core nanocapsules and self-emulsifying systems, which form micro- and nanoemulsions, are included. The formulations sought to be patented include pharmaceutical forms having a structure of emulsified globules, optionally coated with polymers, containing a benznidazole and/or nitroimidazole derivative. The pharmaceutical compositions developed improve the dissolution profile of benznidazole, control drug release and increase plasmatic bioavailability, with a consequent improvement in pharmacological activity.
(FR)La présente invention concerne des procédés pour préparer des formes pharmaceutiques polymères à l'échelle micrométrique et nanométrique encapsulant du benznidazole pour une administration par voie parentérale, et des formes pharmaceutiques pour une administration orale, qui s'auto-émulsionnent en contact avec des liquides biologiques, formant des micro- ou nanoémulsions. On peut citer des microcapsules, des microsphères, des microémulsions, des nanocapsules, des nanosphères, des nanoémulsions, des nanoparticules lipidiques solides, semi-solides et liquides, des nanocapsules à noyau lipidique et des systèmes auto-émulsifiants, qui forment des micro- et nanoémulsions. Les formulations faisant l'objet de l'invention comprennent des formes pharmaceutiques possédant une structure de globules émulsifiés, éventuellement revêtues par des polymères, contenant un benznidazole et/ou un dérivé nitroimidazole. Les compositions pharmaceutiques développées améliorent le profil de dissolution du benznidazole, contrôlent la libération de médicament et améliorent la biodisponibilité plasmatique, avec une amélioration conséquente dans l'activité pharmacologique.
(PT)A presente invenção descreve os métodos de preparo de formas farmacêuticas poliméricas micro e nanométricas encapsulando o benznidazol para uso parenteral e de formas farmacêuticas de uso oral que se autoemulsionam em contato com fluidos biológicos, formando micro ou nanoemulsões. Incluem microcápsulas, microesferas, microemulsões, nanocápsulas, nanoesferas, nanoemulsões, nanopartículas lipídicas sólidas, semi-solidas e líquidas, nanocápsulas de núcleo lipídico e sistemas autoemulsionáveis, que formam micro e nanoemulsões. As formulações a serem patenteadas incluem formas farmacêuticas que possuem estrutura de glóbulos emulsionados revestidos ou não por polímeros contendo o Benznidazol e/ou um de derivados nitroimidazólicos. As composições farmacêuticas desenvolvidas melhoram o perfil de dissolução do benznidazol, controlam a liberação do fármaco e promovem aumento da biodisponibilidade plasmática, com consequentemente melhoria da atividade farmacológica.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG).
Publication Language: Portuguese (PT)
Filing Language: Portuguese (PT)