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1. WO2013034925 - COMPOSITIONS OF EFAVIRENZ

Publication Number WO/2013/034925
Publication Date 14.03.2013
International Application No. PCT/GB2012/052208
International Filing Date 07.09.2012
IPC
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
48
Preparations in capsules, e.g. of gelatin, of chocolate
50
Microcapsules
51
Nanocapsules
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
10
Dispersions; Emulsions
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
14
Particulate form, e.g. powders
19
lyophilised
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
536
ortho- or peri-condensed with carbocyclic ring systems
A61K 9/51 (2006.01)
A61K 9/10 (2006.01)
A61K 9/19 (2006.01)
A61K 31/536 (2006.01)
CPC
A61K 31/536
A61K 9/10
A61K 9/14
A61K 9/1682
A61K 9/19
A61K 9/5138
Applicants
  • THE UNIVERSITY OF LIVERPOOL [GB/GB]; Foundation Building 765 Brownlow Hill Liverpool L69 7ZX, GB (AllExceptUS)
  • GIARDIELLO, Marco Norman [GB/GB]; GB (UsOnly)
  • McDONALD, Thomas Oliver [GB/GB]; GB (UsOnly)
  • OWEN, Andrew [GB/GB]; GB (UsOnly)
  • RANNARD, Steven Paul [GB/GB]; GB (UsOnly)
  • MARTIN, Philip John [GB/GB]; GB (UsOnly)
  • SMITH, Darren Lee [GB/GB]; GB (UsOnly)
Inventors
  • GIARDIELLO, Marco Norman; GB
  • McDONALD, Thomas Oliver; GB
  • OWEN, Andrew; GB
  • RANNARD, Steven Paul; GB
  • MARTIN, Philip John; GB
  • SMITH, Darren Lee; GB
Agents
  • HARRISON GODDARD FOOTE; 4th Floor, Merchant Exchange 17-19 Whitworth Street West Manchester M1 5WG, GB
Priority Data
1115633.809.09.2011GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) COMPOSITIONS OF EFAVIRENZ
(FR) COMPOSITIONS D'ÉFAVIRENZ
Abstract
(EN)
The present inventions relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drug efavirenz. 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 porte sur une composition solide et une dispersion aqueuse comprenant des nanoparticules du médicament antirétroviral éfavirenz. La composition solide et la dispersion aqueuse comprennent de plus un mélange d'un polymère hydrophile et d'un tensioactif. Le tensioactif est choisi parmi le succinate de tocophéryle polyoxyéthylénique (TPGS), un ester d'acide gras et de sorbitane polyoxyéthylénique, un chlorure de N- alkyldiméthylbenzylammonium, le désoxycholate de sodium, le sulfosuccinate de sodium et de dioctyle, un 12-hydroxystéarate polyoxyéthylénique, le poly(alcool vinylique) (PVA) et un copolymère séquencé de polyoxyéthylène et de polyoxypropylène, ou une association de ceux-ci. Le polymère hydrophile est de façon appropriée choisi parmi le poly(alcool vinylique) (PVA), un copolymère greffé de poly(alcool vinylique)-polyéthylèneglycol, un copolymère séquencé de polyoxyéthylène et de polyoxypropylène, le polyéthylèneglycol, l'hydroxypropylméthylcellulose (HPMC) et la polyvinylpyrrolidone, ou une association de ceux-ci. La présente invention porte également sur des procédés pour la préparation aussi bien de la composition solide que de la dispersion aqueuse, ainsi que sur leur utilisation en thérapie pour le traitement et/ou la prévention d'infections rétrovirales telles qu'une infection au virus de l'immunodéficience humaine (VIH).
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