公开(公告)号：US5139786A

公开(公告)日：1992-08-18

申请号：US814218

申请日：1991-12-20

申请人： Pier G. Ferrini ,  Carlo Voellmy ,  Peter H. Stahl ,  Jonathan Green

发明人： Pier G. Ferrini ,  Carlo Voellmy ,  Peter H. Stahl ,  Jonathan Green

IPC分类号： A61K9/70 ,  A61K31/66

CPC分类号： A61K9/7053 ,  A61K31/66 ,  A61K9/7061 ,  A61K9/7069 ,  A61K9/7084 ,  A61K9/7092

摘要： The invention relates to topically administrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein R.sub.1 and R.sub.2 are hydrogen or C.sub.1 -C.sub.3 alkyl.

摘要翻译： 本发明涉及含有药学上可接受的式（I）的甲基二膦酸衍生物及其盐的局部施用的药物制剂，其中R 1和R 2是氢或C 1 -C 3烷基。

公开(公告)号：US4353887A

公开(公告)日：1982-10-12

申请号：US177028

申请日：1980-08-11

申请人： Hans Hess ,  Carlo Voellmy

发明人： Hans Hess ,  Carlo Voellmy

IPC分类号： A61J3/10 ,  A61K9/20 ,  A61K9/22 ,  A61K9/24 ,  A61K9/28

CPC分类号： A61J3/10 ,  A61K9/2072

摘要： Divisible tablet having controlled and delayed release of the active substance and consisting of a compact that is optionally provided with a coating and is formed by at least one active substance in an adjunct composition that effects a delayed and controlled release of the active substance and optionally one or more additional adjunct compositions that optionally contain active substances and are arranged in longitudinal layers, the compact being of an oblong shape in which the ratio of length to width to depth is approximately 2.5 to 5: approximately 0.9 to 2:1 and the width constitutes at most 2/3 of the length, and in which one or more relatively deep dividing grooves are present which run perpendicularly to the length and the depth and have a total depth constituting from approximately 1/3 to approximately 1/2 of the depth of the tablet, but are at least so deep that one fracture surface area multiplied by the number of possible fragments constitutes a maximum of 15% of the surface area of the undivided tablet, the base and top faces independently of one another are planar or are convexly curved about the longitudinal axis or about parallels to this axis, the side faces are planar, the end faces can be of any shape and edges are optionally bevelled or rounded.

摘要翻译： 可分散的片剂具有受控和延迟释放的活性物质，并由任选地具有涂层的压块组成，并由辅助组合物中的至少一种活性物质形成，所述活性物质可以延缓和控制活性物质的释放， 或更多另外的辅助组合物，其任选地含有活性物质并且被布置成纵向层，所述压块长椭圆形，其中长度与宽度之比约为2.5至5：约0.9至2:1，宽度构成 长度的至多2/3，并且其中存在一个或多个相对较深的分隔槽，其垂直于长度和深度延伸，并且具有构成距离的深度的大约1/3至大约1/2的总深度 片剂，但是至少如此深，使得一个骨折表面积乘以可能碎片数量构成最大15％ 不平面片的基部和顶面彼此独立地是平面的或者围绕纵向轴线或与该轴线平行的方式凸起地弯曲，侧面是平面的，端面可以是任何形状，并且边缘是 可选地斜切或圆形。

公开(公告)号：US5133972A

公开(公告)日：1992-07-28

申请号：US546345

申请日：1990-06-29

申请人： Pier G. Ferrini ,  Carlo Voellmy ,  Peter H. Stahl ,  Jonathan Green

发明人： Pier G. Ferrini ,  Carlo Voellmy ,  Peter H. Stahl ,  Jonathan Green

IPC分类号： A61K9/00 ,  A61K9/70 ,  A61K31/66 ,  A61K31/675 ,  A61P17/00 ,  A61P43/00 ,  C07F9/38

CPC分类号： A61K9/7053 ,  A61K31/66 ,  A61K31/675 ,  A61K9/7061 ,  A61K9/7076 ,  A61K9/7084

摘要： The invention relates to topically adminstrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein each of R.sub.1 and R.sub.2 is halogen, or wherein R.sub.1 is hydrogen and R.sub.2 is Ar--S-- or Het.sub.1 --NH--, in which Ar is unsubstituted or substituted phenyl and Het.sub.1 is unsubstituted or substituted, monocyclic, 5- or 6-membered monoaza-, diaza- or thiaza-aryl that is bonded via a ring carbon atom, or wherein R.sub.1 is hydrogen or hydroxy and R.sub.2 is --A--R.sub.3, in which A is alkylene and, on the one hand, R.sub.3 is Het.sub.2, which is Het.sub.1 bonded via a ring carbon or ring nitrogen atom, or, on the other hand, R.sub.3 is hydrogen, or amino that is unsubsituted or mono- or di-substituted by identical or different substituents selected from alkyl, cycloalkyl, Ar-alkyl, Ar-O-alkyl, Ar-S-alkyl and Het.sub.1 -alkyl, or that is disubstituted by optionally Ar-containing alkylene, wherein two alkylene carbon atoms mar additionally be linked to one another via alkylene and Ar and Het.sub.1 are each as defined above, with the proviso that when R.sub.2 is --A--R.sub. 3, A is ethylene and R.sub.3 is unsubstituted or C.sub.1 -C.sub.3 alkyl-substituted amino, R.sub.1 is other than hydroxy.

摘要翻译： 本发明涉及含有药学上可接受的式（I）的甲二膦酸衍生物及其盐的局部给药药物制剂，其中R1和R2各自为卤素，或其中R1为氢，R2为Ar-S-或Het1- NH-，其中Ar是未取代或取代的苯基，Het1是未经取代或取代的单环，5或6元单氮杂，二氮杂 - 或噻唑基 - 芳基，其通过环碳原子键合，或其中R1是氢或 羟基和R 2是-A-R 3，其中A是亚烷基，一方面，R 3是Het 2，其是通过环碳或环氮原子键合的Het1，或者另一方面，R 3是氢，或 未被取代或被相同或不同的选自烷基，环烷基，Ar-烷基，Ar-O-烷基，Ar-S-烷基和Het1 - 烷基的取代基取代或被取代的氨基，或被任意Ar- 其中两个亚烷基碳原子另外与一个a连接 通过亚烷基，Ar和Het1各自如上所定义，条件是当R 2是-A-R 3时，A是亚乙基，R 3是未取代的或C 1 -C 3烷基取代的氨基，R 1不是羟基。