公开(公告)号：US5650172A

公开(公告)日：1997-07-22

申请号：US479143

申请日：1995-06-07

申请人： Saburo Matsuda ,  Shigeyuki Ishikawa ,  Akira Suzuki ,  Kenji Tsujihara ,  Motoaki Ohashi

发明人： Saburo Matsuda ,  Shigeyuki Ishikawa ,  Akira Suzuki ,  Kenji Tsujihara ,  Motoaki Ohashi

IPC分类号： A61K9/107 ,  A61K9/14 ,  A61K9/19 ,  A61K47/12 ,  A61K47/18 ,  A61K47/26 ,  A61K9/10 ,  A61K9/16

CPC分类号： A61K9/14 ,  A61K9/1075 ,  A61K9/19 ,  Y10S514/937 ,  Y10S514/938

摘要： A preparation comprising a fat emulsion of fat microparticles wherein said emulsion contains a stabilizer consisting essentially of a fatty acid, a basic amino acid and a saccharide is provided. In the preparation comprising a fat emulsion of fat microparticles of the present invention, said microparticles having a mean particle diameter of at most 100 nm are stable, and so the microparticles remain in blood without being uptaken by liver. Therefore in case of administering a pharmaceutical preparation prepared by using the above-mentioned preparation of the present invention, the pharmacological activity may be expressed at a desired site. Thus the preparation is extremely useful as a drug carrier for drug delivery system. Furthermore, the pharmaceutical preparation of the present invention which is lyophilized can be easily and rapidly reconstituted into the pharmaceutical preparation comprising a fat emulsion of stable fat microparticles having a mean particle diameter of about at most 100 nm by adding distilled water, even after a long-term storage.

摘要翻译： 提供了包含脂肪微粒的脂肪乳液的制剂，其中所述乳液含有基本上由脂肪酸，碱性氨基酸和糖组成的稳定剂。 在包含本发明的脂肪微粒的脂肪乳剂的制剂中，平均粒径为100nm以下的微粒是稳定的，因此微粒保留在血液中而不被肝吸收。 因此，在施用通过使用本发明的上述制剂制备的药物的情况下，可以在期望的部位表达药理活性。 因此，该制剂作为药物递送系统的药物载体非常有用。 此外，冻干的本发明的药物制剂可以通过添加蒸馏水容易且迅速地重构成包含平均粒径为大约100nm的稳定脂肪微粒的脂肪乳剂的药物制剂，即使经过长时间 -term存储。

公开(公告)号：US4963365A

公开(公告)日：1990-10-16

申请号：US267085

申请日：1988-11-04

申请人： Masayoshi Samejima ,  Kazuo Noda ,  Masao Kobayashi ,  Shigeyuki Ishikawa

发明人： Masayoshi Samejima ,  Kazuo Noda ,  Masao Kobayashi ,  Shigeyuki Ishikawa

IPC分类号： A61K9/22 ,  A61K9/50 ,  A61K9/54 ,  A61K9/62

CPC分类号： A61K9/5078

摘要： A controlled release dosage form which consists essentially of a core containing a medicament; an inner coating layer composed of ethylcellulose and a hydrophobic substance; and an outer coating layer containing a medicament are disclosed. Said dosage form shows rapid increase in blood concentration of the medicament and at the same time maintains the high level of the blood concentration over a prolonged period time.

公开(公告)号：US5137733A

公开(公告)日：1992-08-11

申请号：US723031

申请日：1991-06-28

申请人： Kazuo Noda ,  Masao Kobayashi ,  Takashi Osawa ,  Shigeyuki Ishikawa

发明人： Kazuo Noda ,  Masao Kobayashi ,  Takashi Osawa ,  Shigeyuki Ishikawa

IPC分类号： A61K9/28 ,  A61K9/32 ,  A61K9/50 ,  A61K9/52 ,  A61K9/54 ,  A61K9/58 ,  A61K47/12 ,  A61K47/32

CPC分类号： A61K9/2846 ,  A61K9/5078 ,  Y10S514/963

摘要： A controlled release pharmaceutical preparation comprising a core containing a medicinal compound and a coating layer containing a water-repellent salt and a water-insoluble and slightly water-permeable acrylic polymer having trimethylammoniumethyl group. Said preparation releases a medicinal compound in a sigmoid type dissolution pattern irrespective of the PH of a dissolution medium.