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1. 发明专利

JP2009137988A Sustained release formulation of erythromycin derivative 有权
标题翻译：持续释放ERYTHROMYCIN衍生物的配方
公开(公告)号：JP2009137988A
公开(公告)日：2009-06-25
申请号：JP2009001631
申请日：2009-01-07
申请人： Abbott Lab , アボット・ラボラトリーズAbbott Laboratories
发明人： AL-RAZZAK LAMAN A , CRAMPTON SHERI L , GUSTAVSON LINDA E , HUI HO-WAH , MILMAN NELLY , SEMLA SUSAN J
IPC分类号： A61K31/7048 , A61K9/20 , A61K9/22 , A61K9/36 , A61K47/12 , A61K47/26 , A61K47/30 , A61K47/32 , A61K47/34 , A61K47/38 , A61P31/04
CPC分类号： A61K31/7048 , A61K9/2018 , A61K9/2054
摘要： PROBLEM TO BE SOLVED: To provide a pharmaceutical composition sustainably releasing an erythromycin derivative in the gastrointestinal environment.
SOLUTION: The composition includes an erythromycin derivative and a pharmaceutically acceptable water-soluble polymer. When ingested orally, the composition induces statistically significantly lower Cmax in the plasma than an immediate release composition of the erythromycin derivative while maintaining bioavailability and minimum concentration substantially equivalent to that of the immediate release composition of the erythromycin derivative upon multiple dosing. The composition has an improved taste profile and reduced gastrointestinal side effects as compared to those for the immediate release composition.
COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供可持续释放红霉素衍生物在胃肠环境中的药物组合物。组合物包括红霉素衍生物和药学上可接受的水溶性聚合物。当口服摄入时，组合物比红霉素衍生物的立即释放组合物诱导血浆中Cmax的统计学显着降低，同时保持生物利用度和最小浓度基本上等同于多次给药时红霉素衍生物的速释组合物。与立即释放组合物相比，该组合物具有改善的味道特征和减少的胃肠道副作用。版权所有（C）2009，JPO＆INPIT

2. 发明专利

TR200707263T2 未知
公开(公告)号：TR200707263T2
公开(公告)日：2008-01-21
申请号：TR200707263
申请日：1998-03-06
申请人： ABBOTT LAB
发明人： AL-RAZZAK LAMAN A , CRAMPTON SHERI L , SEMLA SUSAN J , HUI HO-WAH , MILMAN NELLY , GUSTAVSON E LINDA
IPC分类号： A61K9/22 , A61K9/20 , A61K9/32 , A61K9/36 , A61K31/7048 , A61K47/30 , A61K47/32 , A61K47/38 , A61P31/04
摘要： Disclosed is a pharmaceutical composition for extended release of an erythromycin derivative in the gastrointestinal environment. The composition comprises an erythromycin derivative and a pharmaceutically acceptable polymer so that, when ingested orally, the composition induces statistically significantly lower Cmax in the plasma than an immediate release composition of the erythromycin derivative while maintaining bioavailability and minimum concentration substantially equivalent to that of the immediate release composition of the erythromycin derivative upon multiple dosing. The compositions of the invention have an improved taste profile and reduced gastrointestinal side effects as compared to those for the immediate release composition.

3. 发明专利

NZ537410A Extended release formulations of clarithromycin that minimise adverse effects and provide at least equivalent to tablet or liquid formulations 未知
公开(公告)号：NZ537410A
公开(公告)日：2007-06-29
申请号：NZ53741098
申请日：1998-03-06
申请人： ABBOTT LAB
发明人： CRAMPTON SHERI L , GUSTAVSON LINDA E , HUI HO-WAH , MILMAN NELLY , SEMLA SUSAN J , AL-RAZZAK LAMAN A
IPC分类号： A61K9/20 , A61K9/22 , A61K9/36 , A61K31/7048 , A61K47/30 , A61P31/04 , A61K31/70 , A61K9/30 , A61P31/00
摘要： Described is a pharmaceutical composition for extended release of clarithromycin in the gastrointestinal tract, to be administered orally, comprising clarithromycin, which, when administered once a day, induces a statistically significantly lower degree of fluctuation value for the clarithromycin concentration in plasma compared with an equal dosing of the immediate release composition of clarithromycin administered twice a day, while maintaining exposure (AUC0-24) substantially equivalent to the immediate release composition of clarithromycin. The composition further induces a statistically significant lower degree of fluctuation value in plasma compared with that of the controlled release formulation containing clarithromycin, a water soluble alginate salt, a complex salt of alginic acid, and an organic carboxylic acid, and, which releases clarithromycin so that after a regimen of a single 1000 mg dose on day 1 and a multiple dose regimen of 1000 mg on days 3, 4 and 5, the Cmax is about 2.45 mu g/ml, the Cmin is about 0.70 mu g/ml, the Tmax is about 8.6 hours, the AUC0-24 is about 39.6 mu g h/ml, and the fluctuation index is about 1.11. The pharmaceutical composition also has an improved taste perversion compared with an immediate release formulation containing clarithromycin when administered to a patient.

4. 发明专利

ES2199981T3 未知
公开(公告)号：ES2199981T3
公开(公告)日：2004-03-01
申请号：ES95909559
申请日：1995-02-14
申请人： ABBOTT LAB
发明人： BRISKIN JACQUELINE E , GUPTA PRAMOD K , LOYD CLAUD , KOHLER ROBERT W , SEMLA SUSAN J
IPC分类号： A61K9/16 , A61K47/44
摘要： A process for preparing fine particle pharmaceutical formulations having improved throughput and producing greater uniformity of particle size. The process relates to adding to the dry components of the formulation prior to the steps of wetting, extrusion and spheronization, an extrusion aid material selected from pharmaceutically acceptable oils and waxes having a drop point between about 15 DEG C. and 115 DEG C.

5. 发明专利

DK0973527T3 未知
公开(公告)号：DK0973527T3
公开(公告)日：2003-11-24
申请号：DK98907722
申请日：1998-03-06
申请人： ABBOTT LAB
发明人： AL-RAZZAK LAMAN A , CRAMPTON SHERI L , GUSTAVSON LINDA E , HUI HO-WAH , SEMLA SUSAN J , MILMAN NELLY
IPC分类号： A61K9/20 , A61K9/22 , A61K9/36 , A61K31/7048 , A61K47/30 , A61P31/04 , A61K31/71
摘要： Disclosed is a pharmaceutical composition for extended release of an erythromycin derivative in the gastrointestinal environment. The composition comprises an erythromycin derivative and a pharmaceutically acceptable polymer so that, when ingested orally, the composition induces statistically significantly lower Cmax in the plasma than an immediate release composition of the erythromycin derivative while maintaining bioavailability and minimum concentration substantially equivalent to that of the immediate release composition of the erythromycin derivative upon multiple dosing. The compositions of the invention have an improved taste profile and reduced gastrointestinal side effects as compared to those for the immediate release composition.

6. 发明专利

CA2387621A1 EXTENDED RELEASE FORMULATIONS OF ERYTHROMYCIN DERIVATIVES 未知
公开(公告)号：CA2387621A1
公开(公告)日：2001-04-19
申请号：CA2387621
申请日：2000-10-13
申请人： ABBOTT LAB
发明人： DEVCICH KAREN J , SEMLA SUSAN J , NOTARIO GERALD F , HOM RICHARD C , PALMER ROBERT N , ZHANG JIE
IPC分类号： A61K9/20 , A61K9/22 , A61K9/36 , A61K31/7048 , A61K47/30 , A61P31/04
摘要： Disclosed is a pharmaceutical composition for extended release of an erythromycin derivative in the gastrointestinal environment. The composition comprises an erythromycin derivative and a pharmaceutically acceptable polym er so that, when ingested orally, the composition induces statistically significantly lower Cmax in the plasma than an immediate release composition of the erythromycin derivative while maintaining bioavailability and minimum concentration substantially equivalent to that of the immediate release composition of the erythromycin derivative upon multiple dosing. The compositions of the invention have an improved taste profile and reduced gastrointestinal side effects as compared to those for the immediate release composition.

7. 发明专利

CZ9903471A3 Formulation of erythromycin derivatives with prolonged release 未知
公开(公告)号：CZ9903471A3
公开(公告)日：2000-01-12
申请号：CZ347199
申请日：1998-03-06
申请人： ABBOTT LAB
发明人： AL-RAZZAK LAMAN A , CRAMPTON SHERI L , GUSTAVSON LINDA E , HUI HO-WAH , MILMAN NELLY , SEMLA SUSAN J
IPC分类号： A61K9/20 , A61K9/22 , A61K9/36 , A61K31/7048 , A61K47/30 , A61P31/04 , A61K31/7036 , A61P1/00
CPC分类号： A61K31/7048 , A61K9/2018 , A61K9/2054

8. 发明专利

SK288127B6 Pharmaceutical formulation with extended release of clarithromycin and use thereof 未知
公开(公告)号：SK288127B6
公开(公告)日：2013-10-02
申请号：SK50212010
申请日：1998-03-06
申请人： ABBOTT LAB
发明人： AL-RAZZAK LAMAN A , CRAMPTON SHERI L , GUSTAVSON LINDA E , HUI HO-WAH , MILMAN NELLY , SEMLA SUSAN J
IPC分类号： A61K31/7048 , A61K9/20 , A61K9/22 , A61K9/36 , A61K47/30 , A61K47/38 , A61P31/04
摘要： Disclosed is a pharmaceutical formulation for oral administration, in the form of a tablet for extended release of clarithromycin in the gastrointestinal tract, which comprises clarithromycin and a pharmaceutically acceptable, hydrophilic, water-soluble polymer, which is hydroxypropyl methylcellulose 2208, with a methoxyl content of 19 to 24 %, a hydroxypropoxyl content of 7 to 12 %, viscosity of from 80 to 120 mPa.s, as a 2 % water solution, and with a particle size such that 100 % of the particles passes through the sieve with a mesh size of 595 micrometers (30 mesh), more than 99 % of the particles passes through the sieve with a mesh size of 400 micrometers (40 mesh) and more than 90 % of the particles passes through the sieve with a mesh size of 149 micrometers (100 mesh), wherein the tablet formulation comprises 500 mg clarithromycin and 100 mg of the polymer, 360 mg lactose monohydrate, 30 mg talc USP and 10 mg magnesium stearate, is obtainable by wet granulation, and releases clarithromycin so that after a regimen of a single 1000 mg dose on a day 1 and a multiple dose regimen of 1000 mg on days 3, 4 and 5 the maximum plasma concentration is reached after 6.9 + 3.3 hours and the area under the plasma concentration time curve 0-24 is 40.2 + 13.8 micrograms.h/ml, the maximum plasma concentration is 2.66 + 0.87 micrograms/ml, the minimum plasma concentration is 0.67 + 0.39 and the fluctuation index is 1.24 + 0.37. Further disclosed is a use of the aforesaid formulation for the preparation of a medicament for the treatment of a bacterial infection in a mammal.

9. 发明专利

CA2182282C PROCESS FOR PREPARING FINE PARTICLE PHARMACEUTICAL FORMULATIONS 未知
公开(公告)号：CA2182282C
公开(公告)日：2006-04-18
申请号：CA2182282
申请日：1995-02-14
申请人： ABBOTT LAB
发明人： BRISKIN JACQUELINE E , GUPTA PRAMOD K , SEMLA SUSAN J , KOHLER ROBERT W , LOYD CLAUD
IPC分类号： A61K9/16 , A61K47/44
摘要： A process for preparing fine particle pharmaceutical formulations having imp roved throughput and producing greater uniformity of particle size comprises adding to the dry components of the formulation pr ior to the steps of wetting, extrusion and spheronizatio n, an extrusion aid material selected from pharmaceutically acceptable oils and w axes having a drop point between about 15 .degree.C and 115 .degree.C.

10. 发明专利

DK0744941T3 未知
公开(公告)号：DK0744941T3
公开(公告)日：2003-09-29
申请号：DK95909559
申请日：1995-02-14
申请人： ABBOTT LAB
发明人： GUPTA PRAMOD K , BRISKIN JACQUELINE E , LOYD CLAUD , KOHLER ROBERT W , SEMLA SUSAN J
IPC分类号： A61K9/16 , A61K47/44
摘要： A process for preparing fine particle pharmaceutical formulations having improved throughput and producing greater uniformity of particle size. The process relates to adding to the dry components of the formulation prior to the steps of wetting, extrusion and spheronization, an extrusion aid material selected from pharmaceutically acceptable oils and waxes having a drop point between about 15 DEG C. and 115 DEG C.

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