Composiciones de lopinavir

Una composición sólida de lopinavir que comprende nanopartículas de lopinavir dispersas en una mezcla sólida de al menos un polímero hidrofílico y al menos un tensioactivo; en donde el polímero hidrofílico es PVA y el tensioactivo es vitamina-E-polietilenglicol-succinato (Vit-E-PEG-succinato) y en d...

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Bibliographische Detailangaben
Hauptverfasser: MARTIN, Philip John, McDONALD, Thomas Oliver, OWEN, Andrew, SMITH, Darren Lee, GIARDIELLO, Marco Norman, LONG, James, RANNARD, Steven Paul
Format: Patent
Sprache:spa
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Zusammenfassung:Una composición sólida de lopinavir que comprende nanopartículas de lopinavir dispersas en una mezcla sólida de al menos un polímero hidrofílico y al menos un tensioactivo; en donde el polímero hidrofílico es PVA y el tensioactivo es vitamina-E-polietilenglicol-succinato (Vit-E-PEG-succinato) y en donde la composición comprende: 40 a 80 % de lopinavir, 10 a 40 % en peso de PVA y 2 a 20 % en peso de vitamina -E-polietilenglicol-succinato (Vit-E-PEG-succinato). The present invention relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drug lopinavir. The solid composition and aqueous dispersion additionally comprise a mixture of a hydrophilic polymer and a surfactant. The surfactant is selected from vitamin-E-polyethylene glycol-succinate (Vit-E-PEG-succinate), a polyoxyethylene sorbitan fatty acid ester, N-alkyldimethylbenzylammonium chloride, sodium deoxycholate, dioctyl sodium sulfosuccinate, polyethyleneglycol-12-hydroxystearate, polyvinyl alcohol (PVA), and a block copolymer of polyoxyethylene and polyoxypropylene, or a combination thereof. The hydrophilic polymer is suitably selected from polyvinyl alcohol (PVA), a polyvinyl alcohol-polyethylene glycol graft copolymer, a block copolymer of polyoxyethylene and polyoxypropylene, polyethylene glycol, hydroxypropyl methyl cellulose (HPMC), and polyvinylpyrrolidone, or a combination thereof. The present invention also relates to processes for preparing both the solid composition and the aqueous dispersion, as well as to their use in therapy for the treatment and/or prevention of retroviral infections such as human immunodeficiency virus (HIV).