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delayed formulation of 3 - (- dimethylaminomethyl cyclohexyl) phenol
专利权人:
GRUENENTHAL GMBH
发明人:
TOBIAS JUNG,JOHANNES BARTHOLOMAUS
申请号:
BRPI0621466
公开号:
BRPI0621466A2
申请日:
2006.09.15
申请国别(地区):
BR
年份:
2012
代理人:
摘要:
DELAYED FORMULATION OF 3 - (- DIMETHYLAMINOMETIL CYCLOHEXIL) PHENOL. The invention relates to a dosage form for the controlled release of the active ingredient 3- (2-dimethylaminomethylcyclohexyl) phenol, preferably (1 R, 2R) -3- (2-dimethylaminomethylcyclohexyl) phenol, or one of the pharmaceutically acceptable salts thereof. same, which in vivo reaches the plasma level peak of the active ingredient after 2 to 10 h, and / or in vitro, measured according to European Pharmacopels with a paddle mixer in a buifer at a pH value of 6.8 (preferably 900 ml), a temperature of 370 ° C and 75 rpm releases - after 0.5 hours 3.0 to 37% weight, - after 1 hour 5.0 to 56% weight, - after 2 hours 10 to 77% weight, - after 3 hours 15 to 88% by weight, - after 6 hours at least 30% by weight, - after 12 hours at least 50% by weight, - after 18 hours at least 70% by weight and - after 24 hours at least 80% by weight of the active ingredient originally contained in the form DosingFORMULAçãO RETARDADA DE 3-(-DIMETILAMINOMETIL CICLOHEXIL) FENOL. A invenção relaciona-se com uma forma de dosage para a liberação controlada do ingrediente ativo 3-(2-dimetilaminometilciclohexil)fenol, preferentemente (1 R,2R)-3-(2-dimetilaminometilciclohexil)fenol, ou umas das sais farmacéuticamente aceitáveis do mesmo, a qual in vivo alcança o peak de nível do plasma do ingrediente ativo depois de 2 a 10 h, e/ou in vitro, medida de acordo à Farmacopéis Européia com um aparelho misturador de pá num buifer a um valor de pH de 6.8 (preferentemente 900 ml),uma temperatura de 370C e 75 rpm libera - após 0.5 horas 3.0 a 37 %peso, - após 1 hora 5.0 a 56 %peso, - após 2 horas 10 a 77%peso, - após 3 horas 15 a 88 %peso, - após 6 horas ao menos 30 %peso, - após 12 horas ao menos 50 %peso,- após 18 horas ao menos 70 %peso e - após 24 horas ao menos 80 % peso do ingrediente ativo originalmente contido na forma de dosagem.
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