Pharmaceutical preparation containing...

A - Human Necessities – 61 – K

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A61K 9/20 (2006.01)

Patent

CA 2533330

The invention relates to a pharmaceutical formulation containing 6- dimethylaminometh-yl-1-(3-methoxy-phenyl)- cyclohexane-1,3-diol or one of the pharmaceutically acceptable salts thereof in a matrix, with delayed release of active ingredients. The matrix contains 1-80 wt. % of one or several hydrophilic or hydrophobic polymers as pharmaceutically acceptable matrix formulators and exhibits the following dissolution rate in vitro: 3-35 wt % (in relation to 100 wt. % active ingredients) 6-dimethylaminomethyl-1-(3- methoxy--phenyl)-cyclohexane-1,3-diol is released after 0.5 hrs, 5-50 wt. % 6- dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1,3-diol is released after 1 hr, 10-75 wt.- % 6-Dimethylaminomethyl-1-(3-methoxy--phenyl)- cyclohexane-1,3-diol is released after 2 hrs, 15-82 wt.- % 6- dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1,3-diol is released after 3 hrs, 30-97 wt.- % 6-dimethylaminomethyl-1-(3-methoxy--phenyl)- cyclohexane-1,3-diol is released after 6 hours, more than 50 wt.- % 6- Dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1,3- diol is released after 12 hours, more than 70 wt.- % 6- dimethylaminomethyl-1-(3-methoxy- phenyl)-cyclohexane-1,3-diol is released after 18 hours, more than 80 wt.- % 6- dimethylaminomethyl-1 -(3- methoxy-phenyl)-cyclohexane-1,3-diol is released after 24 hrs.

L'invention concerne une formulation pharmaceutique à libération différée du principe actif, cette formulation contenant du 6-diméthylaminométhyl-1-(3-méthoxy-phényl)-cyclohexane-1,3-diol ou un sel pharmaceutiquement acceptable de celui-ci dans une matrice à libération différée du principe actif. Ladite matrice comprend 1 à 80 % en poids d'un ou de plusieurs polymères hydrophiles ou hydrophobes en tant qu'agents de formation de matrice pharmaceutiquement acceptables et elle présente in vitro la vitesse de dissolution suivante : 3-35 % en poids (par rapport au poids total de principe actif) du 6-diméthylaminométhyl-1-(3-méthoxy-phényl)-cyclohexane-1,3-diol libérés après ? heure, 5-50 % en poids libérés après 1 heure, 10-75 % en poids libérés après 2 heures, 15-82 % en poids libérés après 3 heures, 30-97 % en poids libérés après 6 heures, plus de 50 % en poids libérés après 12 heures, plus de 70 % en poids libérés après 18 heures, plus de 80 % en poids libérés après 24 heures.

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