AR045973A1 - COMPOSITIONS OF CONTROLLED RELEASE AND ITS MANUFACTURING METHODS - Google Patents

COMPOSITIONS OF CONTROLLED RELEASE AND ITS MANUFACTURING METHODS

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Publication number
AR045973A1
AR045973A1 ARP030103927A AR045973A1 AR 045973 A1 AR045973 A1 AR 045973A1 AR P030103927 A ARP030103927 A AR P030103927A AR 045973 A1 AR045973 A1 AR 045973A1
Authority
AR
Argentina
Prior art keywords
amylose
agent
controlled release
matrix
rich
Prior art date
Application number
Other languages
Spanish (es)
Original Assignee
Labopharm Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Labopharm Inc filed Critical Labopharm Inc
Publication of AR045973A1 publication Critical patent/AR045973A1/en

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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

Se describe una formulación de dosificación sólida para la liberación controlada de un agente farmacológico. La formulación incluye un núcleo que comprende un agente farmacológico dispersado en una primera matriz de liberación controlada que comprende un agetne farmacológico dispersado en una primera matriz de liberación controlada que comprende almidón reticulado rico en amilosa, donde la velocidad de liberación del agente de la matriz es relativamente baja. También hay un recubrimiento formado alrededor del núcleo, que incluye dicho agente dispersado en una segunda matriz de liberación controlada, donde la velocidad de liberación del agente de la matriz es relativamente alta. Preferiblemente, la segunda matriz de liberación controlada es una mezcla física de acetato de polivinilo y polivinilpirrolidona, y la liberación del agente de la matriz del núcleo es relativamente lenta en comparación con la liberación del agente de la matriz del recubrimiento. El agente en el núcleo y el recubrimiento puede, en caulquier realización, ser el mismo o diferentes. En una realización preferida, la formulación incluye un único agente, que es tramadol. Preferiblemente las composiciones farmacéuticas de tramadol son adecuadas para una administración una vez por día que comprende una cantidad efectiva de tramadol o una sal farmacéuticamente aceptable del mismo, que provee después de una única administración in vivo, una mediana del tiempo hasta alcanzar la concentración media en plasma (tmax) de entre 2 y 8 horas, y concentraciones medias máximas de tramadol en plasma (Cmax) que son menores que tres veces de la concentración media en plasma obtenida 24 horas de la administración (C24) de una única dosis de la composición. EN una realización preferida, la formulación es una tableta, y donde dicho almidón reticulado rico en amilosa comprende un almidón reticulado rico en amilosa modificado químicamente preparado a través de un método que comprende: ( a) reticular almidón rico en amilosa, seguido por (b) modificar químicamente el almidón reticulado rico en amilosa, seguido por (c) gelatinización, y (d) secar para obtener un polvo de dicho excipiente de liberación controlada; donde dicho almidón reticulado en gel, la altura del pico que corresponde a la amilosa en dicho almidón reticulado rico en amilosa es al menos 90% de la altura del pico que corresponde a la amilosa en dicho almidón reticulado rico en amilosa de (a). Dichas formulaciones de liberación controlada reducen la frecuencia requerida de administración de la droga.A solid dosage formulation for the controlled release of a pharmacological agent is described. The formulation includes a core comprising a pharmacological agent dispersed in a first controlled release matrix comprising a pharmacological agetne dispersed in a first controlled release matrix comprising crosslinked starch rich in amylose, where the release rate of the matrix agent is relatively low There is also a coating formed around the core, which includes said agent dispersed in a second controlled release matrix, where the rate of release of the matrix agent is relatively high. Preferably, the second controlled release matrix is a physical mixture of polyvinyl acetate and polyvinyl pyrrolidone, and the release of the agent from the core matrix is relatively slow compared to the release of the agent from the coating matrix. The agent in the core and the coating may, in any embodiment, be the same or different. In a preferred embodiment, the formulation includes a single agent, which is tramadol. Preferably, the pharmaceutical compositions of tramadol are suitable for once-daily administration comprising an effective amount of tramadol or a pharmaceutically acceptable salt thereof, which provides after a single administration in vivo, a median time to reach the average concentration in plasma (tmax) between 2 and 8 hours, and maximum mean plasma tramadol concentrations (Cmax) that are less than three times the average plasma concentration obtained 24 hours after administration (C24) of a single dose of the composition . In a preferred embodiment, the formulation is a tablet, and wherein said amylose rich crosslinked starch comprises a chemically modified amylose crosslinked starch prepared through a method comprising: (a) crosslinking amylose rich starch, followed by (b ) chemically modifying the crosslinked starch rich in amylose, followed by (c) gelatinization, and (d) drying to obtain a powder of said controlled release excipient; wherein said gel cross-linked starch, the height of the peak corresponding to the amylose in said cross-linked starch rich in amylose is at least 90% of the height of the peak corresponding to the amylose in said cross-linked starch rich in amylose of (a). Such controlled release formulations reduce the required frequency of drug administration.

ARP030103927 2002-10-25 2003-10-27 COMPOSITIONS OF CONTROLLED RELEASE AND ITS MANUFACTURING METHODS AR045973A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US2812602A 2002-10-25 2002-10-25
US51000003P 2003-10-10 2003-10-10

Publications (1)

Publication Number Publication Date
AR045973A1 true AR045973A1 (en) 2005-11-23

Family

ID=42778486

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030103927 AR045973A1 (en) 2002-10-25 2003-10-27 COMPOSITIONS OF CONTROLLED RELEASE AND ITS MANUFACTURING METHODS

Country Status (1)

Country Link
AR (1) AR045973A1 (en)

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