公开(公告)号：US07569549B2

公开(公告)日：2009-08-04

申请号：US10390573

申请日：2003-03-17

申请人： Miljenko Dumic ,  Mladen Vinkovic ,  Marina Oresic ,  Ernest Mestrovic ,  Aleksandar Danilovski ,  Alojz Dumbovic ,  Zdravka Knezevic ,  Gorjana Lazarevski ,  Dominik Cincic ,  Darko Filic ,  Katica Lazaric ,  Dejan Kresimir Bucar

发明人： Miljenko Dumic ,  Mladen Vinkovic ,  Marina Oresic ,  Ernest Mestrovic ,  Aleksandar Danilovski ,  Alojz Dumbovic ,  Zdravka Knezevic ,  Gorjana Lazarevski ,  Dominik Cincic ,  Darko Filic ,  Katica Lazaric ,  Dejan Kresimir Bucar

IPC分类号： A61K31/70 ,  C07H17/08

CPC分类号： C07H17/00 ,  C07H17/08

摘要： Substantially pure isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A having the Formula I: wherein S is an organic solvent which is at least partially miscible with water, x is 1, 1.25, 1.5 or 2, y is 0, 0.5, or 1, the pseudopolymorph being characterized by the monoclinic space group P21 and average unit cell parameters comprising: crystal axis lengths of a=15.5-17.0 Å, b=15.5-17.0 Å, and c=17.5-19.5 Å, and angles between the crystal axes of α=γ=90° and β=106°-112°. In addition, this disclosure is directed to processes for the preparation of the substantially pure isostructural pseudopolymorphs of Formula I; to pharmaceutical compositions containing substantially pure isostructural pseudopolymorphs of Formula I; and to a method for the treatment of bacterial and protozoan infections, and inflammation-related diseases by administration of a pharmaceutical composition containing the substantially pure isostructural pseudopolymorphs of Formula I.

摘要翻译： 具有式I的9-脱氧-9a-氮杂-9a-甲基-9a-高红霉素A的基本上纯的同态结构假多晶型物：其中S是与水至少部分混溶的有机溶剂，x为1,1.25,1.5或2 ，y为0,0.5或1，所述假多晶型物的特征在于单斜晶系空间群P21和平均晶胞参数，其包括：晶轴长度a =15.5-17.0，b =15.5-17.0，c = 17.5- α=γ= 90°和β= 106°-112°的晶轴之间的角度。 此外，本公开涉及制备式I的基本上纯的同态结构假多晶型物的方法; 包含基本上纯的式I的同态假多晶型物的药物组合物; 以及用于治疗细菌和原生动物感染以及炎症相关疾病的方法，其通过施用含有基本上纯的式I的同型结构假多晶型物的药物组合物。

公开(公告)号：US20050118266A1

公开(公告)日：2005-06-02

申请号：US10504014

申请日：2002-03-27

申请人： M.Z.I. Khan ,  Aleksandra Krajacic ,  Zdravka Knezevic ,  Snjezana Vodopija-Mandic

发明人： M.Z.I. Khan ,  Aleksandra Krajacic ,  Zdravka Knezevic ,  Snjezana Vodopija-Mandic

IPC分类号： A61K9/22 ,  A61K9/16 ,  A61K9/20 ,  A61K9/28 ,  A61K9/36 ,  A61K31/196 ,  A61K31/341 ,  A61K31/64 ,  A61K31/4172 ,  A61K9/26

CPC分类号： A61K9/2077 ,  A61K9/1635 ,  A61K9/2866

摘要： A sustained/controlled release formulation with reduced risk of dose dumping and side effects combines two components: component (a) comprises a pharmaceutically active agent and a water-insoluble, but water-permeable polymer, whereas component (b) comprises a pharmaceutically active agent and a hydrophobic material. By changing the ratio of a pharmaceutically active agent and water-insoluble, but water-permeable polymer comprised in the component (a) and/or the ratio of the pharmaceutically active agent and hydrophobic material comprised in the component (b), and ideal release rate, with reduced risk of dose dumping and side effects, can easily be achieved.

摘要翻译： 具有降低的倾倒风险和副作用的持续/控释制剂组合了两个组分：组分（a）包含药物活性剂和水不溶性但水可渗透的聚合物，而组分（b）包含药物活性剂 和疏水性材料。 通过改变组分（a）中包含的药物活性剂和水不溶性但水可渗透的聚合物的比例和/或组分（b）中包含的药物活性剂和疏水性物质的比例和理想释放量 速率，减少倾倒的风险和副作用，可以很容易地实现。