公开(公告)号：WO03034988A2

公开(公告)日：2003-05-01

申请号：PCT/US0233300

申请日：2002-10-18

Applicant: IDEXX LAB INC ,  MURTHY YERRAMILLI V S N ,  SUVA ROBERT

Inventor： MURTHY YERRAMILLI V S N ,  SUVA ROBERT

IPC: A61K9/00 ,  A61K9/10 ,  A61K31/137 ,  A61K31/138 ,  A61K31/165 ,  A61K31/18 ,  A61K31/245 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/505 ,  A61K31/65 ,  A61K31/7036 ,  A61K31/7048 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61P23/02 ,  A61P31/04 ,  A61K

CPC classification number: A61K31/00 ,  A61K9/0019 ,  A61K9/0024 ,  A61K31/24 ,  A61K31/496 ,  A61K31/65 ,  A61K31/7034 ,  A61K31/7048 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K2300/00

Abstract: The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C8-C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a periods of up to 15 days or even longer. Many compounds can be administered according to the present invention including, but not limited to, tilmicosin, oxytetracycline, metoprolol, fluoxetine, roxithromycin, and turbinafine.

Abstract translation: 本发明提供用于延长释放时间和降低药理活性化合物毒性的组合物和方法。 所述化合物包含药理活性化合物与亲脂性抗衡离子的盐和药学上可接受的水溶性溶剂混合在一起以形成可注射组合物。 亲脂平衡离子可以是饱和或不饱和C 8 -C 22脂肪酸，并且优选可以是饱和或不饱和C 10 -C 18脂肪酸。 当注射到哺乳动物中时，至少一部分组合物随时间沉淀并释放活性化合物。 因此，该组合物在哺乳动物中形成活性化合物的缓释药物贮库。 因此，本发明使得能够提供控制剂量的活性化合物给药达最多15天甚至更长的时间。 根据本发明可以施用许多化合物，包括但不限于替米考星，土霉素，美托洛尔，氟西汀，罗红霉素和透明颤菌素。

公开(公告)号：ES2561108T3

公开(公告)日：2016-02-24

申请号：ES02802160

申请日：2002-10-18

Applicant: IDEXX LAB INC

Inventor： MURTHY YERRAMILLI V S N ,  SUVA ROBERT

IPC: A01N37/18 ,  A61K9/08 ,  A61K9/00 ,  A61K9/10 ,  A61K31/137 ,  A61K31/138 ,  A61K31/165 ,  A61K31/18 ,  A61K31/24 ,  A61K31/245 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/505 ,  A61K31/65 ,  A61K31/7034 ,  A61K31/7036 ,  A61K31/7048 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61P23/02 ,  A61P31/04

Abstract: Una composición para administración de un compuesto farmacológicamente activo a un mamífero que comprende una sal de un compuesto farmacológicamente activo básico y un ácido lipófilo, en la que el ácido lipófilo está seleccionado del grupo que consiste en ácidos grasos saturados o insaturados, ácidos cólicos, ácidos fosfatídicos, ácidos dicarboxílicos (como ácido sebácico), ácido polisebácico y ácido polibenzoico; y un disolvente farmacéuticamente aceptable orgánico, en el que el disolvente farmacéuticamente aceptable está seleccionado del grupo que consiste en uno o una combinación de: pirrolidona, N-metilpirrolidona, polietilenglicol, propilenglicol, glicerol formal, éter dimetílico de isosorbida, etanol, sulfóxido de dimetilo, alcohol tetrahidrofurfurílico y triacetina; combinados juntos para formar una composición inyectable, en la que la composición forma un precipitado cuando la composición se introduce o inyecta en un entorno acuoso y en la que la composición libera el compuesto activo con el tiempo cuando se introduce o inyecta en el entorno acuoso.

公开(公告)号：EP1446103A4

公开(公告)日：2011-01-12

申请号：EP02802160

申请日：2002-10-18

Applicant: IDEXX LAB INC

Inventor： MURTHY YERRAMILLI V S N ,  SUVA ROBERT

IPC: A61K9/00 ,  A61K9/10 ,  A61K31/137 ,  A61K31/138 ,  A61K31/165 ,  A61K31/18 ,  A61K31/245 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/505 ,  A61K31/65 ,  A61K31/7036 ,  A61K31/7048 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61P23/02 ,  A61P31/04 ,  A01N37/18

CPC classification number: A61K31/00 ,  A61K9/0019 ,  A61K9/0024 ,  A61K31/24 ,  A61K31/496 ,  A61K31/65 ,  A61K31/7034 ,  A61K31/7048 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K2300/00

公开(公告)号：NZ531460A

公开(公告)日：2005-05-27

申请号：NZ53146002

申请日：2002-10-18

Applicant: IDEXX LAB INC

Inventor： MURTHY YERRAMILLI ,  SUVA ROBERT

IPC: A61K9/10 ,  A61K9/00 ,  A61K31/137 ,  A61K31/138 ,  A61K31/165 ,  A61K31/18 ,  A61K31/245 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/505 ,  A61K31/65 ,  A61K31/7036 ,  A61K31/7048 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61P23/02 ,  A61P31/04

Abstract: Provided are compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C8-C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. When injected into a non-human mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, controlled dose administration of the active compound is provided for a period of up to 15 days or longer. Many compounds can be administered including, but not limited to, tilmicosin, oxytetracycline, metoprolol, fluoxetine, roxithromycin, and turbinafine. Figure 3 is a graphical depiction illustrating that the rate of release of the pharmacologically active compound, tilmicosinm is affected by the chain length of the fatty acid selected. Solvent: N-methyl pyrrolidone; lipophilic counterion: decanoic acid and lauric acid.

公开(公告)号：BR0213425A

公开(公告)日：2004-12-14

申请号：BR0213425

申请日：2002-10-18

Applicant: IDEXX LAB INC

Inventor： MURTHY YERRAMILLI V S N ,  SUVA ROBERT

IPC: A61K9/00 ,  A61K9/10 ,  A61K31/137 ,  A61K31/138 ,  A61K31/165 ,  A61K31/18 ,  A61K31/245 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/505 ,  A61K31/65 ,  A61K31/7036 ,  A61K31/7048 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61P23/02 ,  A61P31/04 ,  A01N37/18

Abstract: The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C 8 -C 22 fatty acid, and preferably may be a saturated or unsaturated C 10 -C 18 fatty acid. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a periods of up to 15 days or even longer. Many compounds can be administered according to the present invention including, but not limited to, tilmicosin, oxytetracycline, metoprolol, fluoxetine, roxithromycin, and turbinafine.

公开(公告)号：CA2463896A1

公开(公告)日：2003-05-01

申请号：CA2463896

申请日：2002-10-18

Applicant: IDEXX LAB INC

Inventor： MURTHY YERRAMILLI V S N ,  SUVA ROBERT

IPC: A61K9/00 ,  A61K9/10 ,  A61K31/137 ,  A61K31/138 ,  A61K31/165 ,  A61K31/18 ,  A61K31/245 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/505 ,  A61K31/65 ,  A61K31/7036 ,  A61K31/7048 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61P23/02 ,  A61P31/04 ,  A01N37/18

Abstract: The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compound s. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solven t combined together to form an injectable composition. The lipophilic counteri on may be a saturated or unsaturated C8-C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depo t of the active compound in the mammal. Therefore, the present invention enabl es one to provide a controlled dose administration of the active compound for a periods of up to 15 days or even longer. Many compounds can be administered according to the present invention including, but not limited to, tilmicosin , oxytetracycline, metoprolol, fluoxetine, roxithromycin, and turbinafine.

公开(公告)号：MXPA04003608A

公开(公告)日：2004-07-27

申请号：MXPA04003608

申请日：2004-04-16

Applicant: IDEXX LAB INC

Inventor： SUVA ROBERT

IPC: A61K9/10 ,  A61K31/137 ,  A61K31/138 ,  A61K9/00 ,  A61K31/165 ,  A61K31/18 ,  A61K31/245 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/505 ,  A61K31/65 ,  A61K31/7036 ,  A61K31/7048 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61P23/02 ,  A61P31/04 ,  A01N37/18

Abstract: La presente invencion provee composiciones y metodos para prolongar el tiempo de liberacion y reducir la toxicidad de compuestos farmacologicamente activos; los compuestos comprenden una sal del compuesto farmacologicamente aceptable, combinados para formar una composicion inyectable; el contraion lipofilico puede ser un acido graso saturado o insaturado C8C22 y de preferencia un acido graso saturado o insaturado de C10-C18; cuando se le inyecta a un mamifero, por lo menos una porcion de la composicion precipita y libera el compuesto activo a trabes del tiempo; de esta manera, la composicion forma un deposito del compuesto activo que se libera lentamente en el mamifero; por lo tanto, la presente invencion permite proveer una administracion de dosis controlada del compuesto activo durante periodos de hasta 15 dias o incluso mas largos; muchos compuestos se pueden administrar de acuerdo con la presente invencion, incluyendo sin limitacion tilmicosin, oxitetraciclina, metropolol, fluxotina, raxitromicina y turbinafina.

公开(公告)号：CA2463896C

公开(公告)日：2010-05-04

申请号：CA2463896

申请日：2002-10-18

Applicant: IDEXX LAB INC

Inventor： MURTHY YERRAMILLI V S N ,  SUVA ROBERT

IPC: A61K9/00 ,  A01N37/18 ,  A61K9/10 ,  A61K31/137 ,  A61K31/138 ,  A61K31/165 ,  A61K31/18 ,  A61K31/245 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/505 ,  A61K31/65 ,  A61K31/7036 ,  A61K31/7048 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61P23/02 ,  A61P31/04

Abstract: The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C8-C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a periods of up to 15 days or even longer. Many compounds can be administered according to the present invention including, but not limited to, tilmicosin, oxytetracycline, metoprolol, fluoxetine, roxithromycin, and turbinafine.

公开(公告)号：AU2002335077B2

公开(公告)日：2006-09-07

申请号：AU2002335077

申请日：2002-10-18

Applicant: IDEXX LAB INC

Inventor： MURTHY YERRAMILLI V S N ,  SUVA ROBERT

IPC: A61K9/00 ,  A61K9/10 ,  A61K31/137 ,  A61K31/138 ,  A61K31/165 ,  A61K31/18 ,  A61K31/245 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/505 ,  A61K31/65 ,  A61K31/7036 ,  A61K31/7048 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61P23/02 ,  A61P31/04

Abstract: The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C 8 -C 22 fatty acid, and preferably may be a saturated or unsaturated C 10 -C 18 fatty acid. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a periods of up to 15 days or even longer. Many compounds can be administered according to the present invention including, but not limited to, tilmicosin, oxytetracycline, metoprolol, fluoxetine, roxithromycin, and turbinafine.