公开(公告)号：US5651983A

公开(公告)日：1997-07-29

申请号：US442915

申请日：1995-05-17

申请人： Gary Robert Kelm ,  Gary Lee Manring ,  Paula Denise Davis ,  Douglas Joseph Dobrozsi ,  Kenneth Gary Mandel ,  David Lee McCauley-Meyers

发明人： Gary Robert Kelm ,  Gary Lee Manring ,  Paula Denise Davis ,  Douglas Joseph Dobrozsi ,  Kenneth Gary Mandel ,  David Lee McCauley-Meyers

IPC分类号： A61K9/00 ,  A61K9/14 ,  A61K9/22 ,  A61K9/28 ,  A61K9/48 ,  A61K9/50 ,  A61K31/44 ,  A61K31/4402 ,  A61K47/48 ,  A61K9/20 ,  A61K31/715 ,  A61K47/40

CPC分类号： A61K9/145 ,  A61K31/44 ,  A61K31/4402 ,  A61K47/48969 ,  A61K9/146 ,  A61K9/2846 ,  A61K9/2886 ,  A61K9/4808 ,  A61K9/4891 ,  A61K9/5078 ,  B82Y5/00

摘要： The present invention relates to a pharmaceutical composition in a unit dosage form for peroral administration in a human or lower animal, having a gastrointestinal tract comprising a small intestine and a colon with a lumen therethrough having an inlet to the colon from the small intestine, comprising:a. a safe and effective amount of rapidly dissolving bisacodyl incorporated into or coated on the surface of a dosage form selected from the group consisting of a spherical substrate, an elliptical substrate, a hard capsule, or a compressed tablet, with a maximum diameter of about 3 mm to about 10 mm; andb. an enteric polymer coating material;wherein the dosage form has a smooth surface free from edges or sharp curves; the elliptical substrate and the hard capsule have a ratio of the long to short diameters of no greater than about 1.5; the rapidly dissolving bisacodyl is released at a point near the inlet to, or within the colon; the enteric polymer coating material begins to dissolve in an aqueous media at a pH between about 5 to about 6.3; and the enteric polymer coating material has a coating thickness of at least about 250 .mu.m.

摘要翻译： 本发明涉及一种用于人或低等动物口服给药的单位剂量形式的药物组合物，其具有胃肠道，该胃肠道包含小肠和结肠与其中具有从小肠到结肠入口的结肠，包括 ： 一个。 将安全有效量的快速溶解的双醋酸掺入或涂覆在选自球状基质，椭圆形基质，硬胶囊或压缩片剂的剂型的表面上，最大直径为约3 毫米至约10毫米; 和b。 肠溶性聚合物涂料; 其中所述剂型具有没有边缘或尖锐曲线的光滑表面; 椭圆形基底和硬胶囊具有长度与短径之比不大于约1.5; 快速溶解的bisacodyl在靠近入口处或结肠内的点处释放; 肠溶聚合物涂层材料开始在约5至约6.3之间的pH下溶于水性介质; 肠溶性聚合物涂层材料的涂层厚度为至少约250μm。

公开(公告)号：US5656290A

公开(公告)日：1997-08-12

申请号：US442914

申请日：1995-05-17

申请人： Gary Robert Kelm ,  Gary Lee Manring ,  Paula Denise Davis ,  Douglas Joseph Dobrozsi ,  Kenneth Gary Mandel

发明人： Gary Robert Kelm ,  Gary Lee Manring ,  Paula Denise Davis ,  Douglas Joseph Dobrozsi ,  Kenneth Gary Mandel

IPC分类号： A61K9/00 ,  A61K9/14 ,  A61K9/22 ,  A61K9/28 ,  A61K9/30 ,  A61K9/48 ,  A61K9/50 ,  A61K31/44 ,  A61K31/4402 ,  A61K47/48 ,  A61K9/32 ,  A61K9/36 ,  A61K9/58

CPC分类号： B82Y5/00 ,  A61K31/44 ,  A61K31/4402 ,  A61K47/48969 ,  A61K9/145 ,  A61K9/146 ,  A61K9/2846 ,  A61K9/2886 ,  A61K9/4808 ,  A61K9/4891 ,  A61K9/5078 ,  Y10S514/867 ,  Y10S514/892

摘要： The present invention relates to a pharmaceutical composition in a unit dosage form for peroral administration in a human or lower animal, having a gastrointestinal tract comprising a small intestine and a colon with a lumen therethrough having an inlet to the colon from the small intestine, comprising:a. a safe and effective amount of rapidly dissolving bisacodyl incorporated into or coated on the surface of a dosage form selected from the group consisting of a spherical substrate, an elliptical substrate, a hard capsule, or a compressed tablet, with a maximum diameter of about 3 mm to about 10 mm; andb. an enteric polymer coating material comprising at least one inner coating layer and one outer coating layer;wherein the dosage form has a smooth surface free from edges or sharp curves; the elliptical substrate and the hard capsule have a ratio of the long to short diameters of no greater than about 1.5; the rapidly dissolving bisacodyl is released at a point near the inlet to, or within the colon; each of the inner coating layer(s) is an enteric polymer that begins to dissolve in an aqueous media at a pH between about 5 to about 6.3; and the outer coating layer is an enteric polymer that begins to dissolve in an aqueous media at a pH between about 6.8 to about 7.2.

摘要翻译： 本发明涉及一种用于人或低等动物口服给药的单位剂量形式的药物组合物，其具有胃肠道，该胃肠道包含小肠和结肠与其中具有从小肠到结肠入口的结肠，包括 ： 一个。 将安全有效量的快速溶解的双醋酸掺入或涂覆在选自球状基质，椭圆形基质，硬胶囊或压缩片剂的剂型的表面上，最大直径为约3 毫米至约10毫米; 和b。 肠溶性聚合物涂层材料，其包含至少一个内涂层和一个外涂层; 其中所述剂型具有没有边缘或尖锐曲线的光滑表面; 椭圆形基底和硬胶囊具有长度与短径之比不大于约1.5; 快速溶解的bisacodyl在靠近入口处或结肠内的点处释放; 每个内部涂层是在pH约5至约6.3之间开始溶解于水性介质中的肠溶性聚合物; 并且外涂层是在约6.8至约7.2之间的pH下开始溶解于水性介质中的肠溶性聚合物。

公开(公告)号：US5670158A

公开(公告)日：1997-09-23

申请号：US558338

申请日：1995-11-15

申请人： Paula Denise Davis ,  Douglas Joseph Dobrozsi ,  Gary Robert Kelm ,  Kenneth Gary Mandel

发明人： Paula Denise Davis ,  Douglas Joseph Dobrozsi ,  Gary Robert Kelm ,  Kenneth Gary Mandel

IPC分类号： A61K9/24 ,  A61K9/14 ,  A61K9/22 ,  A61K9/28 ,  A61K9/32 ,  A61K9/48 ,  A61K9/50 ,  A61K9/52 ,  A61K9/66 ,  A61K31/44 ,  A61K31/4402 ,  A61K47/12 ,  A61K47/18 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61K47/40 ,  A61K47/48 ,  A61P1/10 ,  A61P43/00 ,  A61K9/00 ,  A61K31/715 ,  A61K47/00

CPC分类号： B82Y5/00 ,  A61K31/44 ,  A61K31/4402 ,  A61K47/48969 ,  A61K9/145 ,  A61K9/146 ,  A61K9/2846 ,  A61K9/2886 ,  A61K9/4808 ,  A61K9/4891 ,  A61K9/5078

摘要： The subject invention involves pharmaceutical compositions in dosage unit form, for peroral administration of bisacodyl to a human or lower animal having a gastrointestinal tract, with a lumen therethrough, with a small intestine and a colon with a junction therebetween, comprising: (a) a safe and effective amount of rapidly-dissolving bisacodyl means; and (b) a delivery means which prevents the release of bisacodyl from the dosage form into the lumen of the gastrointestinal tract during transport of the dosage form through the lumen until the dosage form is near the junction between the small intestine and the colon or in the colon, and which then releases the bisacodyl in the lumen near the junction between the small intestine and the colon or within the colon, The subject invention also involves methods for providing laxation for humans and lower animals in need thereof by peroral administration of such compositions.

摘要翻译： 本发明涉及以剂量单位形式的药物组合物，其用于口服给予具有胃肠道的人或更低级动物，具有通过其中的腔的比索拉昔克，具有小肠和结肠之间的连接，包括：（a） 安全有效量的快速溶解的bisacodyl手段; 和（b）递送装置，其防止在将剂型运送到内腔期间直到剂型接近小肠和结肠之间的连接处时，剂型中的双醋酸从剂型释放到胃肠道的内腔中 结肠，然后在小肠和结肠之间或结肠内的接合处的内腔中释放双歧杆菌。本发明还涉及通过口服给予这种组合物来为有需要的人和低等动物提供泻药的方法 。