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BRPI0711179A2 - composição farmacêutica contendo composto inibidor de dpp iv e processo para a sua preparação - Google Patents

composição farmacêutica contendo composto inibidor de dpp iv e processo para a sua preparação Download PDF

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Publication number
BRPI0711179A2
BRPI0711179A2 BRPI0711179-7A BRPI0711179A BRPI0711179A2 BR PI0711179 A2 BRPI0711179 A2 BR PI0711179A2 BR PI0711179 A BRPI0711179 A BR PI0711179A BR PI0711179 A2 BRPI0711179 A2 BR PI0711179A2
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pharmaceutical composition
composition according
agent
diluent
disintegrating agent
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BRPI0711179-7A
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Kohlrausch Anja
Romer Patrick
Seifert Gerd
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Boehringer Ingelheim International Gmbh
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Publication of BRPI0711179A2 publication Critical patent/BRPI0711179A2/pt
Publication of BRPI0711179B1 publication Critical patent/BRPI0711179B1/pt

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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

COMPOSIçãO FARMACêUTICA CONTENDO COMPOSTO INIBIDOR DE DPP IV E PROCESSO PARA SUA PREPARAçãO. A presente invenção refere-se a composições farmacêuticas de inibidores de DPP IV com um grupo amino, à preparação das mesmas e ao uso das mesmas para tratar diabetes mellitus.

Description

Relatório Descritivo da Patente de Invenção para "COMPOSIÇÃOFARMACÊUTICA CONTENDO COMPOSTO INIBIDOR DE DPP IV E PRO-CESSO PARA SUA PREPARAÇÃO".
A presente invenção refere-se a composições farmacêuticas deinibidores de DPP IV selecionados, à preparação dos mesmos e ao uso dosmesmos para tratar estados de saúde médicos selecionados.
A enzima DPP-IV (dipeptidil peptidase IV) também conhecida comoCD26 é uma serina protease conhecida por levar à clivagem de um dipeptídeopartindo da extremidade N-terminal de um número de proteínas que possuemem sua extremidade N-terminal um resíduo de prolina ou de alanina. Devido aesta propriedade, os inibidores de DPP-IV interferem no nível plasmático depeptídeos bioativos incluindo o peptídeo GLP-1 e são considerados como sendofármacos promissores para o tratamento de diabetes mellitus.
Em tentativas de preparar composições farmacêuticas de inibido-res de DPP-IV selecionados foi observado, que os inibidores de DPP-IV comum grupo amino primário ou secundário exibem incompatibilidades, proble-mas de degradação ou problemas de extração com um número de excipien-tes costumeiros tais como celulose microcristalina, amido glicolato de sódio,croscarmelose de sódio, ácido tartárico, ácido cítrico, glicose, frutose, saca-rose, lactose, maltodextrinas. Embora os próprios compostos sejam muitoestáveis, reagem com muitos excipientes utilizados em formas de dosagemsólidas e com impurezas dos excipientes, especialmente em contato íntimofornecidos em comprimidos e em altas proporções de excipiente/fármaco. Ogrupo amino parece reagir com açúcares redutores e com outros gruposcarbonila reativos e com grupos funcionais de ácido carboxílico formados,por exemplo, na superfície de celulose microcristalina através da oxidação.Estas dificuldades inesperadas são primariamente observadas em faixas dedosagem baixas que são requeridas devido á potência surpreendente dosinibidores selecionados. Assim, são necessárias composições farmacêuticaspara solucionar estes problemas técnicos associados com a potência ines-perada de compostos inibidores de DPP-IV selecionados.
Uma composição farmacêutica de acordo com a presente invençãoé pretendida para o tratamento para atingir o controle glicêmico em um pacientecom diabetes mellitus do tipo 1 ou do tipo 2 e compreende um inibidor deDPP-IV com um grupo amino, especialmente um grupo amino livre ou primá-rio, como um ingrediente ativo, um primeiro e um segundo diluentes, um a-5 gente aglutinante, um agente de desintegração e um agente lubrificante. Umagente de desintegração adicional e um agente de deslizamento adicionalconstituem uma opção adicional. Adicionalmente, as composições podemser utilizadas para tratar artrite reumatóide, obesidade e osteoporose assimcomo para sustentar o transplante de aloenxerto.
Os diluentes adequados para uma composição farmacêutica deacordo com a invenção são pó de celulose, fosfato de cálcio dibásico anidro,fosfato de cálcio dibásico diidratado, eritritol, hidroxipropil celulose substituí-da inferior, manitol, amido pré-gelatinizado ou xilitol. Entre estes diluentes omanitol e o amido pré-gelatinizado são preferidos.
Os diluentes preferidos como o segundo diluente são os diluen-tes mencionados anteriormente amido pré-gelatinizado e hidroxipropilcelulo-se substituída inferior (L-HPC) que exibem propriedades aglutinantes adicio-nais.
Os agentes lubrificantes adequados para uma composição far-macêutica de acordo com a invenção são talco, polietilenoglicol, behenatode cálcio, estearato de cálcio, óleo de mamona hidrogenado ou estearato demagnésio. O agente lubrificante preferido é/o estearato de magnésio.
Os agentes aglutinantes adequados para uma composição far-macêutica de acordo com a invenção são copovidona (co-poliperizados deVinilpirrolidona com outros derivados de vinila), hidroxipropil metilcelulose(HPMC), hidroxipropilcelulose (HPC), polivinilpirrolidona (povidona), amidopré-gelatinizado, hidroxipropilcelulose substituída inferior (L-HPC), a copovi-dona e o amido pré-gelatinizado sendo os preferidos.
Os agentes aglutinantes mencionados anteriormente amido pré-gelatinizado e L-HPC exibem propriedades diluentes e de desintegração adi-cionais e podem também ser utilizados como o segundo diluente ou o agen-te de desintegração.Os agentes de desintegração adequados para uma composiçãofarmacêutica de acordo com a presente invenção são amido de milho, cros-povidona, hidroxipropilcelulose substituída inferior (L-HPC) ou amido pré-gelatinizado, o amido de milho sendo o preferido.
Como um agente de deslizamento opcional pode ser utilizado odióxido de silício coloidal.
Um exemplo de composição de acordo com a presente invençãocompreende o diluente manitol, amido pré-gelatinizado como um diluentecom propriedades de agente aglutinante adicionais, o agente aglutinantecopovidona, o agente de desintegração amido de milho e o estearato demagnésio como o agente lubrificante.
As formas de dosagem preparadas com as composições farma-cêuticas de acordo com a presente invenção contêm ingredientes ativos nasfaixas de dosagem de 0,1-100 mg. As dosagens preferidas são 0,5 mg, 1mg, 2,5 mg, 5 mg e 10 mg.
As composições farmacêuticas típicas compreendem (% em peso)
0,5-20 % de ingrediente ativo
40-88 % de diluente 1,
3-40 % de diluente 2,
20 1-5% de agente aglutinante,
5-15% de agente de desintegração e
0,1-4% de agente lubrificante.
As composições farmacêuticas preferidas compreende (% empeso)
25 0,5-7 % de ingrediente ativo
50-75 % de diluente 1,
5-15 % de diluente 2,
2-4 % de agente aglutinante,
8-12 % de agente de desintegração e
0,5-2 % de agente lubrificante
As composições farmacêuticas de acordo com a invenção sãopretendidas para uso oral e podem ser utilizadas na forma de dosagem deuma cápsula, um comprimido ou de um comprimido revestido com filme. Ti-picamente o revestimento de filme representa 2-4%, preferencialmente 3%da composição e compreende um agente formador de filme, um agente deplastificação, um agente de deslizamento e opcionalmente um ou mais pig-mentos. Um exemplo de composição de revestimento pode compreenderhidroxipropilmetilcelulose (HPMC), polietileno glicol (PEG), talco, dióxido detitânio e opcionalmente óxido de ferro.
Os ingredientes ativos preferidos no contexto da presente inven-ção são inibidores de DPP-IV com um grupo amino primário e sais dosmesmos taLcomo qualquer inibidor de DPP-IV e sal do mesmo definido pelafórmula (I)
<formula>formula see original document page 5</formula>
ou fórmula (II)
<formula>formula see original document page 5</formula>
em que R1 é ([1,5]naftiridin-2-il)metila, (quinazolin-2-il)metila, (quinoxalin-6-il)metila, (4-Metil-quinazolin-2-il)metila, 2-Ciano-benzila, (3-Ciano-quinolin-2-il)metila, (3-Ciano-piridin-2-il)metila, (4-Metil-pirimidin-2-il)metila ou (4,6-Dimetil-pirimidin-2-il)metila e R2 é 3-(fl)-amino-piperidin-1-ila, (2-amino-2-metil-pro-pil)-metilamino ou (2-(S)-amino-propil)-metilamino.
Os compostos inibidores de DPP IV preferidos são os compos-tos a seguir e os sais dós mesmos:
1 -[(4-metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1 -il)-8-(3-(fi)-amino-pipe-ridin-1 -il)-xantina (comparar com WO 2004/018468, exemplo 2(142)):<formula>formula see original document page 6</formula>
1·[(Π ,5]naftiridin-2-il)metil]-3-metil-7-(2-b1-il)-xantina (comparar com WO 2004/018468, exemplo 2(252)):
<formula>formula see original document page 6</formula>
|-3-metil-7-(2-butin-1 -il)-8-((f?)-3-amino-piperidin-1 ->m WO 2004/018468, exemplo 2(80)):
<formula>formula see original document page 6</formula>
2-((R)-3-Amino^iperidin-1-il)-3-(but-2-rinil)-5-(4-metil-quinazolin-2-ilmetil)-3,5-dihidro-imidazo[4,5-d]piridazin-4-ona (comparar com WO 2004/050658,exemplo 136):
<formula>formula see original document page 6</formula>
1-[(4-Metil·quinazolin-2-il)metil]-3-metil-7-(2-butiin-1-il)-8-[(2-amino-2-metil-propil)-metilamino]-xantina (comparar com WO 2006/029769, exemplo 2(1)):1-[(3-Ciano-quinolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((fO-3-amino-piperidin-1 -il)-xantina (comparar com WO 2005/085246, exemplo 1 (30)):
<formula>formula see original document page 7</formula>
1 -(2-Ciano-benzil)-3-metil-7-(2-butin-1 -il)-8-((fl)-3-amino-piperidin-1 -il)-xantina (comparar com WO 2005/085246, exemplo 1 (39)):
<formula>formula see original document page 7</formula>
1-[(4-Metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1 -il)-8-[(S)-(2-amino-pro-pil)-metilamino]-xantina (comparar com WO 2006/029769, exemplo 2(4)):
<formula>formula see original document page 7</formula>
1-[(3-Ciano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((fí)-3-amino-pipe--ridin-1 -il)-xantina (comparar com WO 2005/085246, exemplo 1 (52)):
<formula>formula see original document page 7</formula>
1-[(4-Metil-pirimidin-2-M)metil]-3-metil-7-(2-butin-1-il)-8-((/^ridin-1-il)-xantina (comparar com WO 2005/085246, exemplo 1(81)):<formula>formula see original document page 8</formula>
• 1 -[(4,6-Dimetil-pirimidin-2-il)metil]-3-metil-7-(2-butin-1 -il)-8-((fi)-3-amino-piperidin-1 -il)-xantina (comparar com WO 2005/085246, exemplo 1(82)):
<formula>formula see original document page 8</formula>
• 1 -[(Quinoxalin-6-il)metil]-3-metil-7-(2-butin-1 -il)-8-((fí)-3-amino-piperidin-1 -il)-xantina (comparar com WO 2005/085246, exemplo 1(83)):
<formula>formula see original document page 8</formula>
Para preparar as composições de acordo com a invenção, umgranulado pode ser preparado através de um processo de granulação úmi-da. Os métodos alternativos para a granulação de ingrediente ativo e excipi-entes com um líquido de granulação são a granulação em leito fluidizado oua granulação em um recipiente.
No processo de granulação úmida o líquido de granulação é umsolvente tal como água, etanol, metanol, isopropanol, acetona, preferencial-mente água purificada e contém um agente aglutinante tal como copovidona.O solvente é um componente volátil, que não permanece no produto final. Oingrediente ativo e os cfutros excipientes com a exceção do agente Iubrifican-te são pré-misturados e granulados com o líquido aquoso de granulação uti-lizando um granulador de alto cisalhamento. A etapa de granulação úmida éseguida por uma etapa de peneiração úmida opcional, secagem e peneira-ção seca dos grânulos. Por exemplo, uma secadora em leito fluidizado podeser então utilizada para a secagem.
Os grânulos secos são peneirados através de uma peneira apro-priada. Após a adição dos outros excipientes com a exceção do agente lubri-ficante a mistura é misturada em uma misturadora convencional adequadatal como uma misturadora de queda livre seguida pela adição do agente lu-brificante tal como estearato de magnésio e pela mistura final na misturadora.
Assim, um exemplo de processo de granulação úmida para apreparação de uma composição farmacêutica de acordo com a presente in-venção compreende
a. dissolver um agente aglutinante tal como copovidona-em um
solvente tal como água purificada à temperatura ambiente para produzir um
líquido de granulação;
b. misturar um inibidor de DPP-IV1 um diluente e um agente de
desintegração em uma misturadora adequada para produzir uma pré-mistura;
c. umedecer a pré-mistura com o líquido de granulação e a gra-
nulação subseqüente da pré-mistura umedecida, por exemplo, em uma mis-turadora de alto cisalhamento;
d. peneirar opcionalmente a pré-mistura granulada através de
uma peneira com um tamanho de trama de pelo menos 1,0 mm e preferen-cialmente 3 mm;
e. secar o granulado à temperatura de ar de entrada de aproxi-madamente 40-75°C e preferencialmente 55-65°C, por exemplo, em umasecadora em leito fluidizado até que a perda desejada no valor de secagemde 1 -5 % seja obtida;
f. desagregar o granulado seco, por exemplo, peneirando atravésde uma peneira com um tamanho de trama de 0,6 mm-1,6 mm, preferenci-almente 1,0 mm; e
g. adicionar, preferencialmente o agente lubrificante peneirado nogranulado para a mistura final, por exemplo, em uma misturadora de cuba.
Em um processo alternativo, parte dos excipientes tal como partede um agente de desintegração (por exemplo, amido de milho) ou um diluen-te (por exemplo, amido pré-gelatinizado) ou um agente de desintegraçãoadicional (crospovidona) pode ser adicionada de forma extragranular antesdo final da mistura da etapa g.
Em uma outra versão alternativa do processo o granulado pro-duzido nas etapas a até e é produzido em um processo de granulação dealto cisalhamento em um recipiente e a secagem subseqüente é em um gra-nulador de um recipiente.
Para a preparação de cápsulas, a mistura final é preenchida den-tro de cápsulas.
Para a preparação de comprimidos ou núcleos de comprimidos,a mistura-final é adicionalmente=comprimida em comprimidos do peso donúcleo de comprimido-alvo com tamanho e força de compressão apropria-dos, utilizando uma prensa de comprimidos apropriada.
Para a preparação de comprimidos revestidos com filme é prepa-rada uma suspensão de revestimento e os núcleos de comprimidos compri-midos são revestidos com a suspensão de revestimento até um ganho depeso de aproximadamente 2-4 %, preferencialmentè aproximadamente 3%,utilizando um aparato de revestimento com filme padronizado. O solvente derevestimento com filme é um componente volátil, que não fica no produtofinal. Para reduzir a quantidade requerida de agente lubrificante nos compri-midos é uma opção utilizar um sistema de lubrificação externa.
Exemplos
Exemplo 1 - Formulação para compressão direta
Um ingrediente inibidor de DPP IV ativo com um grupo aminoprimário e todos os outros excipientes com a exceção de esteaj-ato de mag-nésio são misturados em uma misturadora de alto cisalhamento. A pré-mistura é peneirada através de uma peneira de 1 mm. Após a adição de es-tearato de magnésio, a pré-mistura é misturada em uma misturadora dequeda livre para produzir a mistura final. A mistura final é comprimida emcomprimidos utilizando uma prensa de comprimidos adequada. Podem serobtidas as composições a seguir:<table>table see original document page 11</column></row><table>
Exemplo 2 - Formulação alternativa para compressão direta
Um ingrediente inibidor de DPP IV ativo com um grupo aminoprimário e todos os outros excipientes com a exceção de estearato de mag-nésio são misturados em uma misturadora de alto cisalhamento. Esta pré-mistura é peneirada através de uma peneira de 1 mm. Após a adição de es-tearato de magnésio, a pré-mistura é misturada em uma misturadora dequeda livre para produzir a mistura final. A mistura final é comprimida emcomprimidos utilizando uma prensa de comprimidos adequada. Podem serobtidas as composições a seguir:
<table>table see original document page 11</column></row><table><formula>formula see original document page 12</formula>
Exemplo 3 - Formulação de comprimido
A copovidona é dissolvida em água purificada ã temperaturaambiente para produzir um líquido de granulação. Um ingrediente inibidor deDPP IV ativo com um grupo amino primário, manitol e parte do amido pré-gelatinizado são misturados em uma misturadora adequada, para produziruma pré-mistura. A pré-mistura é umedécida com o Ifqujdo de granulação egranulada subseqüentemente. O granulado umedecido é opcionalmente pe-neirado através de uma peneira com um tamanho de trama de 1,6-3,0 mm.O granulado é seco a 55 0C em uma secadora adequada até um teor de u-midade residual correspondendo a 2-5 % de perda na secagem. O granula-do seco é peneirado através de uma peneira com um tamanho de trama de1,0 mm. O granulado é misturado com parte do amido pré-gelatinizado emuma misturadora adequada. O estearato de magnésio é adicionado a estamistura após passar através de uma peneira de 1,0 mm para desagregação.
Subseqüentemente, a mistura final é produzida através da mistu-ra final em uma misturadora adequada e comprimida em comprimidos. Podeser obtida a composição de comprimido a seguir
<table>table see original document page 12</column></row><table><table>table see original document page 13</column></row><table>
Exemplo 4 - Formulação de comprimido revestido
A copovidona é dissolvida em água purificada à temperaturaambiente para produzir um líquido de granulação. Um ingrediente inibidor deDPP IV ativo com um grupo amino primário, manitol, amido pré-gelátinizadoe amido de milho são misturados em, uma misturadora adequada para pro-duzir a pré-mistura. A pré-mistura é umedecida com o líquido de granulaçãoe granulada subseqüentemente utilizando uma misturadora de alto cisalha-mento. O granulado umedecido é opcionalmente peneirado através de umapeneira com tamanho de trama de 1,6-3,0 mm. O granulado é seco a apro-Ximaclamente 60 0C em uma secadora em leito fluidizado até que uma perdano valor de secagem de 2-4 % seja obtida. A mistura final é comprimida emnúcleos de comprimido.
A hidroxipropil metilcelulose, o polietileno glicol, o talco, o dióxidode titânio e o oxido de ferro são suspensos em água purificada em uma mis-turadora adequada à temperatura ambiente para produzir uma suspensão derevestimento. Os núcleos de comprimidos são revestidos com uma suspen-são de revestimento até um ganho de peso de aproximadamente 3 % paraproduzir comprimidos revestidos com filme. Podem ser obtidas as composi-ções de comprimido a seguir:
<table>table see original document page 13</column></row><table><table>table see original document page 14</column></row><table>
Exemplo 5 - Formulação de comprimido
A copovidona é dissolvida em água purificada à temperaturaambiente para produzirum líquido de granulação. Um ingrediente inibidor de.DPP IV ativo com um grupo amino primário, manitol e amido pré-gelatinizadosão misturados em uma misturadora adequada para produzir uma pré-mistura. A pré-mistura é umedecida com o líquido de granulação e subse-qüentemente granulada. O granulado umedecido é opcionalmente peneiradoatravés de uma peneira adequada. O granulado é seco a aproximadamente50°C em uma secadora adequada até que uma perda no valor de secagemde 3-5% seja obtida. O granulado seco é peneirado através de uma peneiracom tamanho de trama de 1,0 mm.
O estearato de magnésio é passado através de uma peneira de1,0 mm e adicionado no granulado. Subseqüentemente, a mistura final éproduzida através da mistura final e uma misturadora adequada e a mistura-ção final é comprimida em comprimidos. Podem ser obtidas as composiçõesde comprimido a seguir:
<table>table see original document page 14</column></row><table>Exemplo 6 - Variações de formulações de comprimido
A copovidona é dissolvida em água purificada à temperaturaambiente para produzir um líquido de granulação. Um ingrediente inibidor deDPP IV ativo com um grupo amino primário e uma parte do manitol, amidopré-gelatinizado e amido de milho são misturados em uma misturadora ade-quada, para produzir uma pré-mistura. A pré-mistura é umedecida com olíquido de granulação e subseqüentemente granulada. O granulado umede-cido é peneirado através de uma peneira adequada. O granulado é seco àtemperatura do ar de entrada a aproximadamente 60 0C em uma sécadoraem leito fluidizado até que uma-perda no valor de secagem de 1-4 % sejaobtida. O granulado seco é peneirado através de uma peneira com tamanhode trama de 1,0 mm.
O estearato de magnésio é passado através de uma peneira pa-ra a desagregação e é adicionado no granulado. Adicionalmente, a parterestante dos excipientes é adicionada de forma extragranular nesta etapa doprocesso. Subseqüentemente, a mistura final é produzida através da mistu-ração final em uma misturadora adequada e comprimida em núcleos decomprimido.
A hidroxipropil metilcelulose, o polietileno glicol, o talco, o dióxidode titânio e o óxido de ferro são suspensos em água purificada em uma mis-turadora adequada à temperatura ambiente para produzir uma suspensão derevestimento. Os núcleos de comprimido são revestidos com a suspensãode revestimento até um ganho de peso de aproximadamente 3 % para pro-duzir comprimidos revestidos com filme. Podem ser obtidas as^yariações deformulações a seguir:
Exemplo 6.1 - Variações de formulação com excipientes extragranulares
<table>table see original document page 15</column></row><table><table>table see original document page 16</column></row><table>
Exemplo 6.2 - Variações de formulação com agente de desintegraçãoextragranuiar adicional
<table>table see original document page 16</column></row><table>Exemplo 6.3 - Formulações D de dose alta
<table>table see original document page 17</column></row><table>

Claims (20)

1. Composição farmacêutica, caracterizada pelo fato de quecompreendo como um ingrediente ativo um composto inibidor de DPP IVcom um grupo amino ou um sal do mesmo, um primeiro diluente, um segun-do diluente, um agente aglutinante, um agente de desintegração e um agen-te lubrificante.
2. Composição farmacêutica de acordo com a reivindicação 1,caracterizada pelo fato de que compreende um agente de desintegraçãoadicional.
3. Composição farmacêutica de acordo com a reivindicação 1 ou 2, caracterizada pelo fato de que compreende um agente de deslizamentoadicional.
4. Composição farmacêutica de acordo com a reivindicação 1,caracterizada pelo fato de que o diluente é pó de celulose, fosfato de cálciodibásico anidro, fosfato de cálcio dibásico diidratado, eritritol, hidroxipropilcelulose substituída inferior, manitol, amido pré-gelatinizado ou xilitol.
5. Composição farmacêutica de acordo com a reivindicação 1,caracterizada pelo fato de que o agente lubrificante é talco, polietilenoglicol,behenato de cálcio, estearato de cálcio, óleo de mamona hidrogenado ou es-tearato de magnésio.
6. Composição farmacêutica de acordo com a reivindicação 2,caracterizada pelo fato de que o agente aglutinante é copovidona (co-polimerizados de vinilpirrolidona com outros derivados de vinila), hidroxipro-pil metilcelulose (HPMC), hidroxipropilcelulose (HPC) ou polivinilpirrolidona(Povidona).
7. Composição farmacêutica de acordo com a reivindicação 1,caracterizada pelo fato de que o agente de desintegração é amido de milho.
8. Composição farmacêutica de acordo com a reivindicação 2,caracterizada pelo fato de que o agente de desintegração adicional é cros-povidona.
9. Composição farmacêutica de acordo com a reivindicação 1,caracterizada pelo fato de que o agente de deslizamento opcional é dióxidode silício coloidal.
10. Composição farmacêutica de acordo com a reivindicação 1,caracterizada pelo fato de que o primeiro diluente é manitol, o segundo diluenteé amido pré-gelatinizado, o agente aglutinante é copovidona, o agente de de-sintegração é amido de milho e o agente lubrificante é estearato de magnésio.
11. Composição farmacêutica de acordo com a reivindicação 1,caracterizada pelo fato de que compreende-0,5-20 % de ingrediente ativo-40-88 % de diluente 1,-3-40% de diluente 2,-1-5 % de agente aglutinante,-5-15 % de agente de desintegração e-0,1-4% de agente lubrificante
12. Composição farmacêutica de acordo com a reivindicação 1,caracterizada pelo fato de que compreende-0,5-7 % de ingrediente ativo-50-75% de diluente 1,-5-15% de diluente 2,-2-4 % de agente aglutinante,-8-12% de agente de desintegração e-0,5-2 % de agente lubrificante
13. Composição farmacêutica de acordo com a reivindicação 1,caracterizada pelo fato de que está na forma de dosagem de uma cápsula,de um comprimido ou de um comprimido revestido com filme.
14. Composição farmacêutica de acordo com a reivindicação 13,caracterizada pelo fato de que compreende 2-4 % de revestimento de filme.
15. Composição farmacêutica de acordo com a reivindicação 1,caracterizada pelo fato de que o revestimento de filme compreende um a-gente formador de filme, um agente de plastificação, um agente de desliza-mento e opcionalmente um ou mais pigmentos.
16. Composição farmacêutica de acordo com a reivindicação 15,caracterizada pelo fato de que o revestimento de filme compreende hidroxi-propilmetilcelulose (HPMC), polietileno glicol (PEG), talco, dióxido de titânioe óxido de ferro.
17. Processo para a preparação de uma composição farmacêuti-ca como definida na reivindicação 1, caracterizado pelo fato de que compre-endea dissolver um agente aglutinante em um solvente para produzirum líquido de granulação;b. misturar um inibidor de DPP-IV, um diluente e um agente dedesintegração para produzir uma pré-mistura;c. umedecer a pré-mistura com o líquido de granulação e granu-Iar subseqüentemente a pré-mistura umedecida;d. peneirar opcionalmente a pré-mistura granulada através deuma peneira com um tamanho de trama de pelo menos 1,0 mm;e. secar o granulado a aproximadamente 40-75°C até que a per-da desejada no valor de secagem na faixa de 1-5 % seja obtida;f. peneirar o granulado seco através de uma peneira com umtamanho de trama de pelo menos 0,6 mm;g. adicionar o agente lubrificante no granulado para a mistura final.
18. Processo de acordo com a reivindicação 17, caracterizadopelo fato de que compreende aindaa. comprimir a mistura final em núcleos de comprimido;b. preparar uma suspensão de revestimento;c. revestir os núcleos de comprimido com a suspensão de reves-timento até um ganho de peso de aproximadamente 2-4 % para produzircomprimidos revestidos com filme.
19. Processo de acordo com a reivindicação 17, caracterizadopelo fato de que parte dos excipientes é adicionada de forma extragranularantes da mistura final da etapa g.
20. Processo de acordo com a reivindicação 17, caracterizadopelo fato de que o granulado produzido nas etapas a-e é produzido em umprocesso de granulação de alto cisalhamento em um recipiente e através dasecagem subseqüente em um granulador de um recipiente.
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