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1. WO2013034927 - COMPOSITIONS OF LOPINAVIR AND RITONAVIR

Publication Number WO/2013/034927
Publication Date 14.03.2013
International Application No. PCT/GB2012/052210
International Filing Date 07.09.2012
IPC
A61K 9/19 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders
19lyophilised
A61K 9/51 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
48Preparations in capsules, e.g. of gelatin, of chocolate
50Microcapsules
51Nanocapsules
A61K 31/536 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
536ortho- or peri-condensed with carbocyclic ring systems
CPC
A61K 31/427
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
425Thiazoles
427not condensed and containing further heterocyclic rings
A61K 31/513
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
513having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 38/55
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
55Protease inhibitors
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 9/19
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders, ; Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
19lyophilised ; , i.e. freeze-dried, solutions or dispersions
A61K 9/5138
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
48Preparations in capsules, e.g. of gelatin, of chocolate
50Microcapsules ; having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
51Nanocapsules; Nanoparticles;
5107Excipients; Inactive ingredients
513Organic macromolecular compounds; Dendrimers
5138obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
Applicants
  • THE UNIVERSITY OF LIVERPOOL [GB]/[GB] (AllExceptUS)
  • GIARDIELLO, Marco Norman [GB]/[GB] (UsOnly)
  • MCDONALD, Thomas Oliver [GB]/[GB] (UsOnly)
  • OWEN, Andrew [GB]/[GB] (UsOnly)
  • RANNARD, Steven Paul [GB]/[GB] (UsOnly)
  • MARTIN, Philip, John [GB]/[GB] (UsOnly)
  • SMITH, Darren, Lee [GB]/[GB] (UsOnly)
Inventors
  • GIARDIELLO, Marco Norman
  • MCDONALD, Thomas Oliver
  • OWEN, Andrew
  • RANNARD, Steven Paul
  • MARTIN, Philip, John
  • SMITH, Darren, Lee
Agents
  • HARRISON GODDARD FOOTE
Priority Data
1115635.309.09.2011GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) COMPOSITIONS OF LOPINAVIR AND RITONAVIR
(FR) COMPOSITIONS À BASE DE LOPINAVIR ET DE RITONAVIR
Abstract
(EN)
The present inventions relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drugs lopinavir and ritonavir. 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).
(FR)
La présente invention concerne une composition solide et une dispersion aqueuse contenant des nanoparticules des médicaments antirétroviraux que sont le lopinavir et le ritonavir. Ladite composition solide et ladite dispersion aqueuse contiennent, en outre, un mélange associant un polymère hydrophile et un tensioactif. Le tensioactif est choisi parmi les composés suivants : complexe vitamine-E-polyéthylèneglycol-succinate (Vit-E-PEG-succinate), ester d'acide gras de polyoxyéthylènesorbitane, chlorure de N-alkyldiméthylbenzylammonium, désoxycholate de sodium, sulfosuccinate dioctylique de sodium, complexe polyéthylèneglycol-12-hydroxystéarate, alcool polyvinylique (PVA) et copolymère séquencé de polyoxyéthylène et de polyoxypropylène, ou une combinaison de ces composés. Le polymère hydrophile peut, quant à lui, être choisi, de façon tout à fait appropriée, parmi les composés suivants : alcool polyvinylique (PVA), copolymère greffé alcool polyvinylique-polyéthylèneglycol, copolymère séquencé de polyoxyéthylène et de polyoxypropylène, polyéthylèneglycol, hydroxypropylméthylcellulose (HPMC) et polyvinylpyrrolidone, ou une combinaison de ces composés. La présente invention concerne également des procédés de préparation tant de la composition solide que de la dispersion aqueuse, ainsi que leur utilisation thérapeutique en vue du traitement et/ou de la prévention d'infections rétrovirales comme celle provoquée par le virus de l'immunodéficience humaine (VIH).
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