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公开(公告)号：US08394414B2
公开(公告)日：2013-03-12
申请号：US10706243
申请日：2003-11-12
IPC分类号： A61K9/16
CPC分类号： A61K9/5146 , A61K9/0073 , A61K9/0075 , A61K9/1617
摘要： Drug delivery to the pulmonary system has been achieved by encapsulation of the drug to be delivered in microparticles having a size range between 0.5 and ten microns, preferably in the range of two to five microns, formed of a material releasing drug at a pH of greater than 6.4. In a preferred embodiment, the drug delivery system is based on the formation of diketopiperazine microparticles which are stable at a pH of 6.4 or less and unstable at pH of greater than 6.4, or which are stable at both acidic and basic pH, but which are unstable at pH between about 6.4 and 8. Other types of materials can also be used, including biodegradable natural and synthetic polymers, such as proteins, polymers of mixed amino acids (proteinoids), alginate, and poly(hydroxy acids). In another embodiment, the microparticles have been modified to effect targeting to specific cell types and to effect release only after reaching the targeted cells.
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公开(公告)号：US06428771B1
公开(公告)日：2002-08-06
申请号：US08441378
申请日：1995-05-15
IPC分类号： A61K912
CPC分类号： A61K9/5146 , A61K9/0073 , A61K9/0075 , A61K9/1617
摘要： Drug delivery to the pulmonary system has been achieved by encapsulation of the drug to be delivered in microparticles having a size range between 0.5 and ten microns, preferably in the range of two to five microns, formed of a material releasing drug at a pH of greater than 6.4. In a preferred embodiment, the drug delivery system is based on the formation of diketopiperazine microparticles which are stable at a pH of 6.4 or less and unstable at pH of greater than 6.4, or which are stable at both acidic and basic pH, but which are unstable at pH between about 6.4 and 8. Other types of materials can also be used, including biodegradable natural and synthetic polymers, such as proteins, polymers of mixed amino acids (proteinoids), alginate, and poly(hydroxy acids). In another embodiment, the microparticles have been modified to effect targeting to specific cell types and to effect release only after reaching the targeted cells.
摘要翻译： 药物递送到肺部系统已经通过将待递送的药物封装在尺寸范围在0.5至10微米之间的微粒中，优选在2至5微米的范围内，通过在pH较大的材料释放药物形成 超过6.4。 在优选的实施方案中，药物递送系统基于在pH6.4或更低的pH下稳定的二酮哌嗪微粒的形成，并且在pH大于6.4时不稳定，或者在酸性和碱性pH两者下都是稳定的 还可以使用其他类型的材料，包括可生物降解的天然和合成聚合物，如蛋白质，混合氨基酸（蛋白质类），藻酸盐和聚（羟基酸）的聚合物。 在另一个实施方案中，微粒已经被修饰以实现靶向特定细胞类型，并且仅在达到靶细胞后才能实现释放。
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公开(公告)号：US6071497A
公开(公告)日：2000-06-06
申请号：US847352
申请日：1997-04-24
IPC分类号： A61K9/00 , A61K9/12 , A61K9/14 , A61K9/16 , A61K9/50 , A61K9/51 , A61K9/72 , A61K31/727 , A61K38/28 , A61K48/00
CPC分类号： A61K9/5146 , A61K9/0073 , A61K9/0075 , A61K9/1617
摘要： Drug delivery to the pulmonary system has been achieved by encapsulation of the drug to be delivered in microparticles having a size range between 0.5 and ten microns, preferably in the range of two to five microns, formed of a material releasing drug at a pH of greater than 6.4. In a preferred embodiment, the drug delivery system is based on the formation of diketopiperazine microparticles which are stable at a pH of 6.4 or less and unstable at pH of greater than 6.4, or which are stable at both acidic and basic pH, but which are unstable at pH between about 6.4 and 8. Other types of materials can also be used, including biodegradable natural and synthetic polymers, such as proteins, polymers of mixed amino acids (proteinoids), alginate, and poly(hydroxy acids). In another embodiment, the microparticles have been modified to effect targeting to specific cell types and to effect release only after reaching the targeted cells.
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公开(公告)号：US5503852A
公开(公告)日：1996-04-02
申请号：US299842
申请日：1994-09-01
IPC分类号： C07D319/12 , A61K9/16 , A61K9/50 , A61K47/22 , C07D241/08
CPC分类号： A61K9/1617
摘要： Drug delivery systems have been developed based on the formation of diketopiperazine (or analogs) microparticles. In the preferred embodiment the microparticle is stable at low pH and disintegrates at physiological pH, and is particularly useful for oral drug delivery. In other embodiments, the microparticles are stable at high pH and disintegrate at neutral or basic pH, or are stable at neutral pH and disintegrate at high or low pH. In the most preferred embodiment the microparticles are formed in the presence of the drug to be delivered, for example, insulin, felbamate, calcitonin or heparin. The diketopiperazine synthetic intermediates are preferably formed by cyclodimerization to form diketopiperazine derivatives at elevated temperatures under dehydrating conditions, functionalized on the side chains, and then precipitated with drug to be incorporated into microparticles.
摘要翻译： 已经基于二酮哌嗪（或类似物）微粒的形成开发了药物递送系统。 在优选的实施方案中，微粒在低pH下是稳定的并且在生理pH下分解，并且对于口服药物递送特别有用。 在其它实施方案中，微粒在高pH下是稳定的，并且在中性或碱性pH下分解，或者在中性pH下是稳定的，并在高或低pH下崩解。 在最优选的实施方案中，在待递送的药物例如胰岛素，麦芽糖素，降钙素或肝素的存在下形成微粒。 二酮哌嗪合成中间体优选通过环二聚作用形成二酮哌嗪衍生物，在脱水条件下在侧链官能化的高温下形成二酮哌嗪衍生物，然后用药物沉淀以引入微粒。
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公开(公告)号：US5576436A
公开(公告)日：1996-11-19
申请号：US204559
申请日：1994-03-02
IPC分类号： G01N33/533 , G01N33/94 , C07D271/12
CPC分类号： G01N33/94 , G01N33/533
摘要： Conjugates of fluorescent labels with specific, selective, and high affinity ligands for receptors have been synthesized and used to directly measure binding to receptors.
摘要翻译： 已经合成了具有特异性，选择性和高亲和力受体配体的荧光标记物的缀合物，并用于直接测量与受体的结合。
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6.发明申请Pharmaceutical Formulations Comprising Incretin Peptide and Aprotic Polar Solvent 审中-公开包含Incretin肽和非质子极性溶剂的药物制剂公开(公告)号：US20080200383A1
公开(公告)日：2008-08-21
申请号：US11910723
申请日：2006-04-06
申请人： Robert N. Jennings , John T.H. Ong , Christopher A. Rhodes , Gregg Stetsko , Steven J. Prestrelski
发明人： Robert N. Jennings , John T.H. Ong , Christopher A. Rhodes , Gregg Stetsko , Steven J. Prestrelski
CPC分类号： A61K38/22 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K38/26 , A61K47/14 , A61K47/18 , A61K47/20 , A61K47/22
摘要： The present disclosure is directed to stable pharmaceutical formulations and uses thereof.
摘要翻译： 本公开涉及稳定的药物制剂及其用途。
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公开(公告)号：US5712269A
公开(公告)日：1998-01-27
申请号：US377667
申请日：1995-01-24
IPC分类号： A61K31/55 , A61P25/28 , C07D471/04
CPC分类号： C07D471/04 , A61K31/55
摘要： Muscarinic M.sub.2 receptor ligands are described which are suitable for the treatment of neurological disorders, and which may be administered with minimal side-effects. A method of synthesis of these compounds is also described.
摘要翻译： 描述了适用于治疗神经障碍的毒蕈碱M2受体配体，其可以以最小的副作用施用。 还描述了这些化合物的合成方法。
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