Pharmaceutical formulation based on antibiotic in...

A - Human Necessities – 61 – K

Patent

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A61K 31/43 (2006.01) A61K 9/50 (2006.01)

Patent

CA 2571045

The invention concerns oral antibiotic medicines. The invention aims at limiting, even stopping, antibiotic resistance, without sacrificing the requirements (a) of increasing the efficacy of oral antibiotics, in particular for pediatric applications, (b) of tolerance, (c) of broad spectra of activity and (d) strict patient compliance. Therefor, the invention concerns the use of microcapsules with modified release, which comprise a core containing at least one active principle (PA1) consisting of at least one antibiotic and a coating of said core regulating the modified release of said active principle, to produce a drinkable or orodispersible antibiotic pharmaceutical formulation, enabling the increase or antibiotic resistance of target germs to be reduced; said formulation: being adapted to be administered in one or two daily doses, preferably two; and being defined as follows, relative to an immediate release oral formulation (FLI*) comprising at least one active principle (PA1) and for a similar dose D of PA1 and FLI*: Tcmi > T*cmi of FLI*.

L'invention concerne des médicaments antibiotiques oraux. Le but visé par l'invention est de limiter, voire de stopper, l'augmentation de l'antibiorésistance, et ce sans sacrifier aux exigences (a) d'augmentation de l'efficacité des antibiotiques oraux, en particulier pour des applications pédiatriques, (b) de tolérance, (c) de larges spectres d'activité et (d) de bonne observance par les patients. Ce but est atteint par l'invention qui propose l'utilisation de microcapsules à libération modifiée, qui comprennent un coeur contenant au moins un principe actif PA1 formé par au moins un antibiotique et un enrobage dudit coeur régissant la libération modifiée de ce principe actif, pour fabriquer une formulation pharmaceutique antibiotique orale buvable ou orodispersible, permettant de limiter l'augmentation de l'antibiorésistance des germes cibles; cette formulation: - étant administrable en une ou deux prises quotidiennes, de préférence deux, - et étant définissable comme suit, par rapport à une formulation orale à libération immédiate (FLI*) comprenant au moins un principe actif PA1 et pour une même dose D en PA1 que FLI*: Tcmi > T*cmi de FLI*

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