公开(公告)号：US4338306A

公开(公告)日：1982-07-06

申请号：US149132

申请日：1980-05-12

申请人： Kazuhiko Kitao ,  Ken-ichi Nishimura

发明人： Kazuhiko Kitao ,  Ken-ichi Nishimura

IPC分类号： A61K9/02 ,  A61K47/12 ,  A61K31/43 ,  A61K31/54 ,  A61K37/26 ,  A61K47/00

CPC分类号： A61K9/02 ,  A61K47/12 ,  Y10S424/15 ,  Y10S514/946 ,  Y10S514/966

摘要： Fatty acids having 8 to 14 carbon atoms, leucinic acid and nontoxic salts thereof promote the absorption of a pharmacologically-active substance through the rectum into the blood stream and effectively raise the concentration of such active substance in the blood stream even when said active substance is one which is usually absorbable through the rectum only with considerable difficulty.

摘要翻译： 碳原子数为8〜14的脂肪酸，亮氨酸及其无毒盐促进药物活性物质通过直肠向血液中的吸收，并有效地提高血液中的活性物质的浓度，即使所述活性物质为 通常通过直肠可以吸收的是相当困难的一种。

公开(公告)号：US4485033A

公开(公告)日：1984-11-27

申请号：US365021

申请日：1982-04-02

申请人： Kazuhiko Kitao ,  Ken-ichi Nishimura

发明人： Kazuhiko Kitao ,  Ken-ichi Nishimura

IPC分类号： A61K9/02 ,  A61K47/12 ,  B01J13/00 ,  A01N61/02 ,  A61K31/20 ,  A61K47/00

CPC分类号： A61K9/02 ,  A61K47/12 ,  Y10S424/15 ,  Y10S514/946 ,  Y10S514/966

摘要： Fatty acids having 8 to 14 carbon atoms, leucinic acid and nontoxic salts thereof promote the absorption of a pharmacologically-active substance through the rectum into the blood stream and effectively raise the concentration of such active substance in the blood stream even when said active substance is one which is usually absorbable through the rectum only with considerable difficulty.

摘要翻译： 碳原子数为8〜14的脂肪酸，亮氨酸及其无毒盐促进药物活性物质通过直肠向血液中的吸收，并有效地提高血液中此类活性物质的浓度，即使所述活性物质为 通常通过直肠可以吸收的是相当困难的一种。

公开(公告)号：US4442090A

公开(公告)日：1984-04-10

申请号：US246953

申请日：1981-03-24

申请人： Nobuharu Kakeya ,  Kazuhiko Kitao ,  Ken-ichi Nishimura

发明人： Nobuharu Kakeya ,  Kazuhiko Kitao ,  Ken-ichi Nishimura

IPC分类号： A61K9/02 ,  A61K47/18 ,  A61K37/26 ,  A61K31/425 ,  A61K31/54 ,  A61K37/00

CPC分类号： A61K9/02 ,  A61K47/183 ,  Y10S424/15

摘要： Compounds satisfying four specific requirements, namely: (1) a log P value in the range of from 2.5 to 6, (2) a molecular structure with at least one carboxyl group, (3) a pKa value for the carboxyl group of not less than 2.5 and (4) absence of halo substitution, and nontoxic salts thereof promote absorption of pharmacologically-active substance through the rectum into the bloodstream and are effective to raise the concentration of such active substance in the bloodstream even when the active substance is usually unabsorbable or absorbable through the rectum only with considerable difficulty. The compounds are combined with pharmacologically-active ingredients, with pharmaceutical bases suitable for rectal administration of drugs and with appropriate combinations of both.

摘要翻译： 满足四个具体要求的化合物，即：（1）log值在2.5至6的范围内，（2）具有至少一个羧基的分子结构，（3）羧基的pKa值不低于 超过2.5和（4）不存在卤素取代，并且其无毒盐促进药物活性物质通过直肠吸收到血液中，并且有效地提高这种活性物质在血流中的浓度，即使活性物质通常是不可吸收的 或通过直肠吸收只有相当大的困难。 将化合物与药理学活性成分组合，其中适合于直肠给药的药物基质和两者的适当组合。

公开(公告)号：US4277465A

公开(公告)日：1981-07-07

申请号：US67451

申请日：1979-08-17

申请人： Akira Kamada

发明人： Akira Kamada

IPC分类号： A61K9/00 ,  A61K9/02 ,  A61K9/48 ,  A61K38/00 ,  A61K47/18 ,  C07D207/16 ,  C07D233/64 ,  C07D307/58 ,  C07K5/06 ,  A61K37/26

CPC分类号： C07K5/06026 ,  A61K47/183 ,  A61K9/02 ,  C07D207/16 ,  C07D307/58 ,  A61K38/00 ,  A61K9/0031 ,  A61K9/4858 ,  Y10S424/15 ,  Y10S514/924 ,  Y10S514/925 ,  Y10S514/926 ,  Y10S514/946

摘要： The enamine derivatives having following formula ##STR1## promote absorption of therapeutically active substances through the digestive tract into the blood stream and are able to effectively elevate the concentration of such active substances in the blood stream even when said active substances are usually absorbable through the digestive tract only with considerable difficulty.

摘要翻译： 具有以下结构式的烯胺衍生物促进治疗活性物质通过消化道的吸收进入血流，并且能够有效地提高血液中这些活性物质的浓度，即使所述活性物质通常通过消化系统吸收 只有相当的困难。