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    • 1. 发明申请
    • Phenylephrine Pharmaceutical Formulations and Compositions for Colonic Absorption
    • 去氧肾上腺素药物制剂和用于结肠吸收的组合物
    • US20080020055A1
    • 2008-01-24
    • US11756881
    • 2007-06-01
    • David MonteithJohn O'MullaneJoseph ReoRobert NowakJiansheng WanMohammed KabirMalaz AbutarifGlenn Fritz
    • David MonteithJohn O'MullaneJoseph ReoRobert NowakJiansheng WanMohammed KabirMalaz AbutarifGlenn Fritz
    • A61K31/137A61K31/4545A61K9/14A61P11/02A61P31/16A61P37/00
    • A61K31/137A61K9/167A61K9/2054A61K9/209A61K9/5026A61K9/5042A61K31/4545A61K47/12A61K47/38
    • The invention discloses a pharmaceutical composition comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is for oral administration wherein the composition delivers phenylephrine or a pharmaceutically acceptable salt thereof via absorption in the colon. The pharmaceutical composition comprises a core comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is in a time-dependent, pH-dependent, or colon-specific enzyme-dependent erodible layer that degrades to expose the core to release phenylephrine in the colon. In one preferred embodiment, the erodible layer encases the core. The composition optionally further comprises phenylephrine in the erodible layer or other additional layer(s). The pharmaceutical composition can further comprise one or more additional therapeutically active agents selected from one or more of the group consisting of antihistamines, analgesics, anti-pyretics, and non-steroidal anti-inflammatory agents. The invention also discloses methods of administering phenylephrine via the colon, thereby increasing the bioavailable amount of therapeutically active unconjugated phenylephrine relative to the total phenylephrine in the plasma.
    • 本发明公开了一种药物组合物,其包含去氧肾上腺素或其药学上可接受的盐和用于口服给药的可溶性层,其中所述组合物通过在结肠中的吸收递送苯肾上腺素或其药学上可接受的盐。 药物组合物包含包含去氧肾上腺素或其药学上可接受的盐的核心和可溶性层,其处于时间依赖性,依赖于pH或结肠特异性的酶依赖性可溶解层,其降解以暴露核心以释放出去氧肾上腺素 结肠。 在一个优选实施例中,可侵蚀层包裹芯。 所述组合物任选地还包含可腐蚀层或其它附加层中的去氧肾上腺素。 药物组合物还可以包含一种或多种另外的治疗活性剂,其选自抗组胺剂,止痛剂,抗热解剂和非甾体抗炎剂中的一种或多种。 本发明还公开了通过结肠施用苯肾上腺素的方法,从而相对于血浆中的总去氧肾上腺素增加了治疗活性的非共轭去氧肾上腺素的生物可利用量。
    • 2. 发明授权
    • Resealable container for powdered materials
    • 可重复使用的粉末容器
    • US5597115A
    • 1997-01-28
    • US644305
    • 1996-05-10
    • Joseph Reo
    • Joseph Reo
    • B65D5/54B65D5/70
    • B65D5/541B65D5/701
    • A three-dimensional resealable container for dispensing powdered or particulate material comprising a top portion, a bottom portion and at least one side portion, the top portion being comprised of an inner section with a die-cut piece, an intermediate section contiguous to said inner section and provided with a hinged flap portion adapted to open and close the container with the die-cut piece secured to the hinged flap, and an outermost section with a pattern of perforations such that a removable segment of such section which covers the hinged flap can be manually removed.
    • 一种用于分配粉末或颗粒材料的三维可再密封容器,包括顶部,底部和至少一个侧部,所述顶部由具有模切件的内部部分组成,与所述内部部分相邻的中间部分 并且设置有适于打开和关闭容器的铰接翼片部分,其中模切件固定到铰接翼片,以及具有穿孔图案的最外部分,使得覆盖铰接翼片的这种部分的可移除部分可以 手动删除
    • 5. 发明申请
    • Sustained-release tablet composition comprising a dopamine receptor agonist
    • 包含多巴胺受体激动剂的缓释片剂组合物
    • US20050020589A1
    • 2005-01-27
    • US10871646
    • 2004-06-18
    • Loksidh GanorkarJoseph ReoAlice MartinoGregory AmidonConnie Skoug
    • Loksidh GanorkarJoseph ReoAlice MartinoGregory AmidonConnie Skoug
    • A61K31/496A61K31/498A61K31/5377A61K31/538
    • A61K31/5377A61K31/496A61K31/498A61K31/538
    • A sustained-release pharmaceutical composition in a form of an orally deliverable tablet comprises as active pharmaceutical agent a compound of formula or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are the same or different and are H, C1-6 alkyl (optionally phenyl substituted), C3-5 alkenyl or alkynyl or C3-10 cycloalkyl, or where R3 is as above and R1 and R2 are cyclized with the attached N atom to form pyrrolidinyl, piperidinyl, morpholinyl, 4-methylpiperazinyl or imidazolyl groups; X is H, F, Cl, Br, I, OH, C1-6 alkyl or alkoxy, CN, carboxamide, carboxyl or (C1-6 alkyl)carbonyl; A is CH, CH2, CHF, CHCl, CHBr, CHI, CHCH3, C═O, C═S, CSCH3, C═NH, CNH2, CNHCH3, CNHCOOCH3, CNHCN, SO2 or N; B is CH, CH2, CHF, CHCl, CHBr, CHI, C═O, N, NH or NCH3, and n is 0 or 1; and D is CH, CH2, CHF, CHCl, CHBr, CHI, C═O, O, N, NH or NCH3. The agent is. dispersed in a matrix comprising a hydrophilic polymer and a starch having a tensile strength of at least about 0.15 kN cm−2 at a solid fraction representative of the tablet. The composition exhibits sustained-release properties effective for treatment of Parkinson's disease. The tablet is optionally coated. Tablets of the invention have improved resistance to attrition or erosion during manufacture, packaging and handling.
    • 口服递送片剂形式的持续释放药物组合物包含式(I)化合物或其药学上可接受的盐作为活性药剂,其中R 1,R 2和R 3相同或不同 并且是H,C 1-6烷基(任选被取代的苯基),C 3-5烯基或炔基或C 3-10环烷基,或其中R 3如上,R 1和R 2与所附连接的环 形成吡咯烷基,哌啶基,吗啉基,4-甲基哌嗪基或咪唑基; X是H,F,Cl,Br,I,OH,C 1-6烷基或烷氧基,CN,羧酰胺,羧基或(C 1-6烷基)羰基; A是CH,CH 2,CHF,CHCl,CHBr,CHI,CHCH 3,C = O,C = S,CSCH 3,C = NH,CNH 2,CNHCH 3,CNHCOOCH 3,CNHCN,SO 2或N; B是CH,CH 2,CHF,CHCl,CHBr,CHI,C = O,N,NH或NCH 3,n是0或1; 且D为CH,CH 2,CHF,CHCl,CHBr,CHI,C = O,O,N,NH或NCH 3。 代理人是。 分散在包含亲水性聚合物的基质和具有至少约0.15kN cm -2的拉伸强度的淀粉中,其表示片剂的固体分数。 该组合物显示出有效治疗帕金森病的持续释放性质。 片剂可任选地包衣。 本发明的片剂在制造,包装和处理过程中具有改善的抵抗磨损或侵蚀的能力。
    • 7. 发明申请
    • Sustained-release tablet composition comprising a dopamine receptor agonist
    • 包含多巴胺受体激动剂的缓释片剂组合物
    • US20050079217A1
    • 2005-04-14
    • US10626274
    • 2003-07-24
    • Loksidh GanorkarJoseph ReoAlice MartinoGregory AmidonConnie Skoug
    • Loksidh GanorkarJoseph ReoAlice MartinoGregory AmidonConnie Skoug
    • A61K9/22A61K9/20A61K31/428A61K31/4745A61K47/36A61K47/38A61P15/10A61P25/16A61P43/00
    • A61K31/428A61K9/2054A61K9/2059A61K31/4745
    • A sustained-release pharmaceutical composition in a form of an orally deliverable tablet comprises as active pharmaceutical agent a compound of formula or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are the same or different and are H, C1-6 alkyl (optionally phenyl substituted), C3-5 alkenyl or alkynyl or C3-10 cycloalkyl, or where R3 is as above and R1 and R2 are cyclized with the attached N atom to form pyrrolidinyl, piperidinyl, morpholinyl, 4-methylpiperazinyl or imidazolyl groups; X is H, F, Cl, Br, I, OH, C1-6 alkyl or alkoxy, CN, carboxamide, carboxyl or (C1-6 alkyl)carbonyl; A is CH, CH2, CHF, CHCl, CHBr, CHI, CHCH3, C═O, C═S, CSCH3, C═NH, CNH2, CNHCH3, CNHCOOCH3, CNHCN, SO2 or N; B is CH, CH2, CHF, CHCl, CHBr, CHI, C═O, N, NH or NCH3, and n is 0 or 1; and D is CH, CH2, CHF, CHCl, CHBr, CHI, C═O, O, N, NH or NCH3. The agent is dispersed in a matrix comprising a hydrophilic polymer and a starch having a tensile strength of at least about 0.15 kN cm−2 at a solid fraction representative of the tablet. The composition exhibits sustained-release properties effective for treatment of Parkinson's disease. The tablet is optionally coated. Tablets of the invention have improved resistance to attrition or erosion during manufacture, packaging and handling.
    • 口服递送片剂形式的持续释放药物组合物包含式(I)化合物或其药学上可接受的盐作为活性药剂,其中R 1,R 2和R 3相同或不同 并且是H,C 1-6烷基(任选被取代的苯基),C 3-5烯基或炔基或C 3-10环烷基,或其中R 3如上,R 1和R 2与所附连接的环 形成吡咯烷基,哌啶基,吗啉基,4-甲基哌嗪基或咪唑基; X是H,F,Cl,Br,I,OH,C 1-6烷基或烷氧基,CN,羧酰胺,羧基或(C 1-6烷基)羰基; A是CH,CH 2,CHF,CHCl,CHBr,CHI,CHCH 3,C = O,C = S,CSCH 3,C = NH,CNH 2,CNHCH 3,CNHCOOCH 3,CNHCN,SO 2或N; B是CH,CH 2,CHF,CHCl,CHBr,CHI,C = O,N,NH或NCH 3,n是0或1; 且D为CH,CH 2,CHF,CHCl,CHBr,CHI,C = O,O,N,NH或NCH 3。 在代表片剂的固体分数下,将试剂分散在包含亲水性聚合物和抗拉强度为至少约0.15kN cm -2的淀粉的基质中。 该组合物显示出有效治疗帕金森病的持续释放性质。 片剂可任选地包衣。 本发明的片剂在制造,包装和处理过程中具有改善的抵抗磨损或侵蚀的能力。