公开(公告)号：US20080132471A1

公开(公告)日：2008-06-05

申请号：US11935764

申请日：2007-11-06

申请人： Toru Hibi ,  Akira Yamamoto ,  Maria Nakatani ,  Hidemasa Katsumi

发明人： Toru Hibi ,  Akira Yamamoto ,  Maria Nakatani ,  Hidemasa Katsumi

IPC分类号： A61K31/66 ,  A61K31/675 ,  A61P9/00

CPC分类号： A61K31/66 ,  A61K31/675

摘要： The present invention provides for methods of administering by a pulmonary route an effective amount of a bisphosphonate active agent to a subject. Aspects of the invention including administering the active agent to the subject in conjunction with one or more mucosal membrane protecting agents, where the protecting agent may include one or more of a protecting enzyme and/or a protecting amino acid and/or a protecting peptide. Also provided are inhalant compositions for use in practicing methods according to embodiments of the invention. Methods and compositions according to embodiments of the invention find use in a variety of different applications, including but not limited to, the treatment of bone adsorption disease conditions.

摘要翻译： 本发明提供了通过肺部途径向受试者施用有效量的双膦酸酯活性剂的方法。 本发明的方面包括将活性剂与一种或多种粘膜保护剂联合施用于受试者，其中保护剂可包括保护酶和/或保护性氨基酸和/或保护肽中的一种或多种。 还提供了用于根据本发明的实施方案的实践方法中使用的吸入剂组合物。 根据本发明的实施方案的方法和组合物可用于各种不同的应用，包括但不限于骨吸收疾病状况的治疗。

公开(公告)号：US20100034752A1

公开(公告)日：2010-02-11

申请号：US12330749

申请日：2008-12-09

申请人： Toru Hibi ,  Akira Yamamoto ,  Hidemasa Katsumi

发明人： Toru Hibi ,  Akira Yamamoto ,  Hidemasa Katsumi

IPC分类号： A61K9/12 ,  A61K31/66

CPC分类号： A61K31/663 ,  A61K9/0078

摘要： The present invention provides for methods of administering by a pulmonary route a bisphosphonate active agent in combination with a pyrazolone derivative to a subject. Also provided are pharmaceutical compositions for use in practicing methods according to embodiments of the invention. The methods and compositions according to embodiments of the invention find use in a variety of different applications, including but not limited to, the treatment of bone absorption disease conditions.

摘要翻译： 本发明提供了通过肺部途径将双膦酸盐活性剂与吡唑啉酮衍生物组合给予受试者的方法。 还提供了用于根据本发明的实施方案的实践方法中使用的药物组合物。 根据本发明的实施方案的方法和组合物可用于各种不同的应用，包括但不限于骨吸收疾病状况的治疗。

公开(公告)号：US20100266670A1

公开(公告)日：2010-10-21

申请号：US12746594

申请日：2008-12-09

申请人： Akira Yamamoto ,  Toshiyasu Sakane ,  Hidemasa Katsumi ,  Fumio Kamiyama ,  Ying-shu Quan

发明人： Akira Yamamoto ,  Toshiyasu Sakane ,  Hidemasa Katsumi ,  Fumio Kamiyama ,  Ying-shu Quan

IPC分类号： A61K9/70 ,  A61K31/663 ,  A61P19/10 ,  A61P3/14

CPC分类号： A61K31/663 ,  A61K9/7061 ,  A61K47/10 ,  A61K47/28 ,  A61K47/32

摘要： This invention is to provide a transdermal administration type pharmaceutical preparation which has better transdermal absorptivity, safety and practical application for treatment of bone calcium metabolic diseases, such as high calcium in blood which resulted from osteoporosis, osteitis deformans and malignant tumors.A percutaneous administration type pharmaceutical preparation in tape form comprising a flexible backing, which is not permeable by the active ingredient, and an adhesive base layer formed on said flexible backing; said adhesive base layer consisting essentially of an adhesive base material of acrylic copolymer, polyhydric alcohol and bisphosphonate or its derivatives, wherein the bisphosphonate or its derivatives are in their therapeutic dose, adhesive base material and polyhydric alcohol in a concentration ratio of 100:150 to 600 by weight; said acrylic copolymer are copolymerized by acrylic acid, 2-ethylhexyl acrylate and polar monomer (except for acrylic acid) in the concentration ratio of 50 to 88%:8 to 40%:1 to 40% by weight respectively. PEG modify and antioxidants are also applicable to reduce the skin stimulation.

摘要翻译： 本发明提供一种透皮给药型药物制剂，其具有较好的经皮吸收性，安全性和实际应用，用于治疗由骨质疏松症，变形性骨畸形和恶性肿瘤引起的骨钙代谢疾病如血钙高。 一种胶带形式的经皮给药型药物制剂，其包含不能被活性成分渗透的柔性背衬和形成在所述柔性背衬上的粘合剂基层; 所述粘合剂基层主要由丙烯酸共聚物，多元醇和二膦酸盐或其衍生物的粘合剂基材组成，其中双膦酸盐或其衍生物的治疗剂量为粘合剂基材和多元醇，浓度比为100:50至 600重量份; 所述丙烯酸共聚物由丙烯酸，丙烯酸2-乙基己酯和极性单体（丙烯酸除外）以50〜88％的浓度比分别为8〜40％：1〜40重量％。 PEG修饰和抗氧化剂也适用于减少皮肤刺激。