公开(公告)号：US4828839A

公开(公告)日：1989-05-09

申请号：US149901

申请日：1988-01-29

申请人： Berthold Stemmle ,  Alexander Wirl ,  Fritz Demmer

发明人： Berthold Stemmle ,  Alexander Wirl ,  Fritz Demmer

IPC分类号： A61K9/20 ,  A61K31/715

CPC分类号： A61K31/715 ,  A61K9/2004 ,  A61K9/2009

摘要： The present invention provides a composition containing guar flour in the form of tablets for oral administration, said tablets having been produced by dry pressing guar flour with a particle size of 60 to 500 .mu.m. in admixture with 5 to 30% of highly dispersed silica gel.

摘要翻译： 本发明提供一种含有用于口服给药的片剂形式的瓜尔豆粉的组合物，所述片剂是通过干燥粒径为60-500μm的瓜耳粉制成的。 与5至30％的高度分散的硅胶混合。

公开(公告)号：US5840330A

公开(公告)日：1998-11-24

申请号：US357143

申请日：1994-12-15

申请人： Berthold Stemmle ,  Klaus Budde ,  Alexander Wirl ,  Fritz Demmer

发明人： Berthold Stemmle ,  Klaus Budde ,  Alexander Wirl ,  Fritz Demmer

IPC分类号： A61K9/22 ,  A61K20060101 ,  A61K9/20 ,  A61K31/19 ,  A61K47/00 ,  A61P3/06

CPC分类号： A61K9/2095 ,  A61K9/2077

摘要： Process for the preparation of shaped, compressed controlled-release unit-dosage forms from a therapeutic active substance exhibiting a self-retarding release that depends on the magnitude of the force used for the compression. The process gives unit-dosage forms for which the release of the active substance is highly uniform, reproducibly identical and largely linear. To achieve this, the active substance and an additive charge that inhibits or compensates for the self-retardation of its release are processed into particles in the first stage of production, so that the preliminary compressed objects made from these particles without any further additives exhibit a rapid release (in comparison with the required controlled release) over the range of the force of compression envisaged for the production of the unit-dosage form in question, after which the particles are compressed in the second stage of production with a release-retarding agent to obtain the unit-dosage forms. The invention also relates to the unit-dosage forms thus obtained.

摘要翻译： 从治疗活性物质制备成形的，压缩的控制释放单位剂型的方法，其表现出取决于用于压缩的力的大小的自我缓解释放。 该方法给出了单位剂型，其中活性物质的释放是高度均匀的，可重复地相同的并且在很大程度上是线性的。 为了达到这个目的，在生产的第一阶段，抑制或补偿其释放的自我延迟的活性物质和添加剂被加工成颗粒，使得由这些颗粒制成的预先压制的物体没有任何其它添加剂显示出 在生产所述单位剂量形式的压缩力的范围内快速释放（与所需的控制释放相比），然后在第二阶段用释放阻滞剂压缩颗粒 以获得单位剂型。 本发明还涉及由此获得的单位剂型。

公开(公告)号：US4859472A

公开(公告)日：1989-08-22

申请号：US134047

申请日：1987-12-17

申请人： Fritz Demmer ,  Berthold Stemmle

发明人： Fritz Demmer ,  Berthold Stemmle

IPC分类号： A61K9/20 ,  A61K9/48 ,  A61K31/66 ,  A61K9/14

CPC分类号： A61K31/66 ,  A61K9/2059 ,  A61K9/2095 ,  Y10S514/96

摘要： The present invention provides a medicament containing 80 to 95% clodronate, 2 to 10% filling material and 1 to 10% lubricant.The present invention also provides a process for the production of a clodronate-containing medicament containing 80 to 95% clodronate, 2 to 10% filling material and 1 to 10% lubricant, wherein the dry components are mixed, moist granulated with an aqueous binding agent and the granulate obtained subsequently dried, a lubricant being additionally admixed with the final granulate in an amount of from 1 to 5% and the mixture thus obtained pressed into tablets or filled into capsules which have a rate of dissolving of >90% after 30 minutes.

摘要翻译： 本发明提供含有80〜95％氯膦酸盐，2〜10％填充材料和1〜10％润滑剂的药物。 本发明还提供一种含有氯膦酸盐的药物的方法，所述药物含有80-95％的氯膦酸盐，2-10％的填充材料和1-10％的润滑剂，其中将干组分混合，用含水结合剂 然后将得到的颗粒随后干燥，将润滑剂另外与最终颗粒混合1至5％，并将所得混合物压制成片剂或填充至胶囊中，30分钟后溶解速率> 90％ 。

公开(公告)号：US5378462A

公开(公告)日：1995-01-03

申请号：US109051

申请日：1993-08-19

申请人： Bernd Boedecker ,  Friederike Henninges ,  Klaus-Juergen Koelln ,  Guenther Kuhnow ,  Guenter-Josef Peschke ,  Manfred Rehburg ,  Alwin Sobe ,  Berthold Stemmle

发明人： Bernd Boedecker ,  Friederike Henninges ,  Klaus-Juergen Koelln ,  Guenther Kuhnow ,  Guenter-Josef Peschke ,  Manfred Rehburg ,  Alwin Sobe ,  Berthold Stemmle

IPC分类号： A61J3/07 ,  A61K9/16 ,  A61K9/36 ,  A61K9/50 ,  A61K38/46 ,  A61K38/54 ,  A61K37/62 ,  A01N25/34 ,  C12N11/08 ,  C12N11/18

CPC分类号： A61K9/1694 ,  A61K9/1641 ,  A61K9/5042

摘要： Pancreatin-containing micropellet cores which can be coated with a gastric juice-resistant film are prepared by extruding a mixture containing pancreatin, polyethylene glycol 4000 and a lower alcohol such as propan-2-ol to produce extrudates which break by themselves into fragments, rounding the fragments with the addition of highly liquid paraffin and drying. Propan-2-ol may be present with the paraffin during rounding. The micropellet cores contain 65-85% pancreatin, and have a bulk density of 0.6 g/ml to 0.85 g/ml, a spherical to ellipsoidal shape with a minor axis in the range of 0.7-1.4 mm and a particle size distribution in which at least 80% of the micropellet cores have a minor axis to major axis ratio in the range from 1:1 to 1:2.

摘要翻译： 通过挤压含有胰酶，聚乙二醇4000和低级醇如丙-2-醇的混合物制备可涂覆有耐胃酸膜的含胰蛋白酶的微丸芯，制备出自己断裂成碎片的挤出物 片中加入高度液体石蜡并干燥。 丙烯醇可能在四舍五入期间与石蜡一起存在。 微丸芯含有65-85％的胰酶，其体积密度为0.6g / ml至0.85g / ml，球形至椭圆形的短轴为0.7-1.4mm，粒径分布为 至少80％的微芯线芯具有在1：1至1：2的长轴比的短轴。