公开(公告)号：US06458824B1

公开(公告)日：2002-10-01

申请号：US09661577

申请日：2000-09-14

申请人： Motokazu Iwata ,  Teruaki Kuriyama ,  Megumi Fujita ,  Keiichi Fujiwara ,  Shiro Kato ,  Hiroshi Harada ,  Akihito Fujii ,  Osamu Odai ,  Hitoshi Kawashima

发明人： Motokazu Iwata ,  Teruaki Kuriyama ,  Megumi Fujita ,  Keiichi Fujiwara ,  Shiro Kato ,  Hiroshi Harada ,  Akihito Fujii ,  Osamu Odai ,  Hitoshi Kawashima

IPC分类号： A61K3140

CPC分类号： C07D209/16

摘要： The present invention provides a solid preparation comprising a crystal of [3-[(2R)-[[(2R)-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1H-indol-7-yloxy]acetic acid (Compound A), especially a crystal of Compound A having a particle size of not larger than 100 &mgr;m at the cumulative weight distribution value of 50%, and not larger than 200 &mgr;m at the cumulative weight distribution value of 95%, preferably a solid preparation having the excellent stability and the content uniformity of Compound A, which is prepared by preparing granules of the crystal of Compound A with fillers, disintegrants and binders, and then followed by mixing said granules with external excipients.

摘要翻译： 本发明提供包含[3 - [（2R） - [[（2R） - （3-氯苯基）-2-羟乙基]氨基]丙基] -1H-吲哚-7-基氧基]乙酸的晶体的固体制剂 （化合物A），特别是在累积重量分布值为50％，粒径不大于100μm的化合物A的晶体，累积重量分布值为95％以下为200μm以下，优选为固体 通过用填料，崩解剂和粘合剂制备化合物A的晶体颗粒，然后将所述颗粒与外部赋形剂混合制备的具有优异的化合物A的稳定性和含量均匀性的制剂。

公开(公告)号：US20050267222A1

公开(公告)日：2005-12-01

申请号：US10531915

申请日：2003-10-21

申请人： Motokazu Iwata ,  Megumi Fujita ,  Hideo Kurita ,  Kenichiro Kiyoshima

发明人： Motokazu Iwata ,  Megumi Fujita ,  Hideo Kurita ,  Kenichiro Kiyoshima

IPC分类号： A61K9/20 ,  A61K31/11

CPC分类号： A61K9/2018 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/2095

摘要： The present invention provides a composition containing a substance being capable of supplying aldehyde-like substances to be used in the field of medicaments, cosmetics, hair care products, etc., that contains a low-molecular weight active substance the stability of which is impaired by the effects of aldehydes and a stabilizer having an amine structure and being capable of absorbing aldehydes, and has an improved stability to aldehyde of said low-molecular weight active the stability of which is impaired by the effects of aldehydes substance; and a method for stabilizing such a low-molecular weight active substance. An example of said stabilizer is an aminosugar or a polymer thereof, an aminosugar alcohol or a polymer thereof, an amino acid or a polymer thereof, a protein or a hydrolysate thereof, an alkylamine, a hydroxyalkylamine, or a salt thereof.

摘要翻译： 本发明提供一种含有能够供给用于药物，化妆品，护发产品等领域的醛类物质的物质的组合物，其含有稳定性受损的低分子量活性物质 通过醛和具有胺结构并且能够吸收醛的稳定剂的作用，并且对于所述低分子量活性物的醛的稳定性具有改善的稳定性，其稳定性受到醛类物质的影响; 和稳定这种低分子量活性物质的方法。 所述稳定剂的实例是氨基糖或其聚合物，氨基糖醇或其聚合物，氨基酸或其聚合物，蛋白质或其水解产物，烷基胺，羟烷基胺或其盐。

公开(公告)号：US5288502A

公开(公告)日：1994-02-22

申请号：US779173

申请日：1991-10-16

申请人： James W. McGinity ,  Motokazu Iwata

发明人： James W. McGinity ,  Motokazu Iwata

IPC分类号： A61K9/16 ,  A61K9/50 ,  A61K31/135 ,  A61K31/165 ,  A61K31/54 ,  A61K38/00 ,  A61K38/04 ,  A61K38/21 ,  A61K38/22 ,  A61K38/44 ,  A61K38/46 ,  A61K39/00 ,  A61K47/30 ,  A61K9/14 ,  B32B5/16

CPC分类号： A61K9/1694 ,  A61K9/1647 ,  A61K9/5031 ,  A61K9/5089 ,  Y10T428/2984 ,  Y10T428/2985 ,  Y10T428/2987

摘要： Multi-phase polymeric microspheres containing a molecular compound dispersed in a polymeric matrix are described. Methods for preparing the multi-phase microspheres are also described, which includes a multiple emulsion solvent evaporation technique. Drug loading efficiencies between 80 to 100% were achieved using the described methods. Particular ratios of the W/O emulsion to polymer, and concentration of surfactant and dispersion media (mineral oil) provide highly efficient multi-phase microspheres. In particular embodiments, the multi-phase microspheres feature a high loading efficiency of water-soluble drugs, and also eliminates partitioning of the water soluble agent into the polymer acetonitrile (solvent) phase, thus preventing low encapsulation efficiency. The described multi-phase microspheres possess efficient drug loading, release properties, and drug stability, and also provide a vehicle for long term therapeutic release of a biologically active molecule for therapeutically effective periods of time. Molecular compounds which may be incorporated within the multi-phase microspheres include both water-soluble and water-insoluble drugs, proteins (e.g. TNF), peptides, and chemicals. The molecular compound is protected within an oily droplet, and contact with polymer, surfactant, organic solvents, and other potentially denaturing agents is prevented.

摘要翻译： 描述了分散在聚合物基质中的分子化合物的多相聚合物微球。 还描述了制备多相微球的方法，其包括多重乳液溶剂蒸发技术。 使用所述方法实现了80至100％之间的药物负载效率。 W / O乳液与聚合物的比例以及表面活性剂和分散介质（矿物油）的浓度提供了高效的多相微球。 在具体实施方案中，多相微球体具有高的水溶性药物的负载效率，并且还消除了水溶性剂分解成聚合物乙腈（溶剂）相，从而防止低的包封效率。 所描述的多相微球具有有效的药物加载，释放性质和药物稳定性，并且还提供用于治疗有效时间段的生物活性分子的长期治疗性释放的载体。 可以掺入多相微球体的分子化合物包括水溶性和水不溶性药物，蛋白质（例如TNF），肽和化学物质。 分子化合物在油滴中被保护，并且防止与聚合物，表面活性剂，有机溶剂和其它潜在的变性剂接触。