公开(公告)号：US09592294B2

公开(公告)日：2017-03-14

申请号：US14649721

申请日：2014-01-13

Applicant: Dow Global Technologies LLC

Inventor： Mladen Ladika ,  Jin Zhao ,  Michael L. Tulchinsky ,  Thomas H. Kalantar ,  J. Keith Harris

IPC: A61K47/10 ,  A61K31/095 ,  A61K31/10 ,  A61K9/48 ,  A61K31/192 ,  A61K31/58 ,  C08G65/20 ,  A61K31/343 ,  C08L71/02

CPC classification number: A61K47/10 ,  A61K9/4866 ,  A61K31/095 ,  A61K31/10 ,  A61K31/192 ,  A61K31/343 ,  A61K31/58 ,  C08G65/20 ,  C08L71/02

Abstract: The present invention relates to the use of polyalkoxylated alcohols of the formula R—O-(AO)—H, wherein R is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl or heterocyclic group having 7 to 25 carbon atoms, (AO) is a polyoxyalkylene moiety of the composition (BO)m(EO)n(DO)r with random or blockwise arrangement of the constituting oxyalkylene units, wherein m, n and r represent the average number of oxybutylene (BO) units, oxyethylene (EO) units and oxyalkylene units derived from at least one epoxide selected from styrene oxide and alkylene oxides having from 5 to 10 carbon atoms (DO) per molecule of the polyalkoxylated alcohol, respectively, m being a number greater than or equal to 1, n being a number greater than or equal to 1 and r being a number in the range from 0 to 50 under the proviso that (m+n+r) is less than or equal to 200 and the ratio n/(m+r) is in the range of 1 to 20, as excipients in pharmaceutical compositions. Said polyalkoxylated alcohols enable very effective solubilization of poorly soluble active pharmaceutical ingredients in aqueous media. Solid or semi-solid pharmaceutical compositions comprising one or more such polyalkoxylated alcohol combined with at least one active pharmaceutical ingredient are further long term stable under typical storage conditions and can be readily provided in various dosage forms such as tablets and filled capsules.

Abstract translation: 本发明涉及式R-O-（AO）-H的聚烷氧基化醇的用途，其中R是具有7至25个碳原子的取代或未取代的烷基，烯基，炔基，芳基，芳烷基或杂环基，（ AO）是组成（BO）m（EO）n（DO）r的聚氧化烯部分，其具有构成的氧化烯单元的无规或块状排列，其中m，n和r表示氧化丁烯（BO）单元的平均数，氧化乙烯 （EO）单元和衍生自至少一种选自氧化苯乙烯和每分子聚烷氧基化醇具有5至10个碳原子的氧化烯（DO）的环氧化物的氧化烯单元，m分别大于或等于1， n是大于或等于1的数，r是0至50的数，条件是（m + n + r）小于或等于200，并且比率n /（m + r） 在1至20的范围内，作为药物组合物中的赋形剂。 所述聚烷氧基化的醇使得难溶性活性药物成分非常有效地溶解在水性介质中。 包含一种或多种这样的多烷氧基化醇与至少一种活性药物成分组合的固体或半固体药物组合物在典型的储存条件下进一步长期稳定，并且可以容易地以各种剂型例如片剂和填充的胶囊提供。

公开(公告)号：US20180244552A1

公开(公告)日：2018-08-30

申请号：US15757546

申请日：2016-09-02

Applicant: Dow Global Technologies LLC ,  The Board of Trustees of the Univesity of Illinois ,  Rohm and Haas Company

Inventor： Larisa Mae Q. Reyes ,  J. Keith Harris ,  Joshua S. Katz ,  Christopher J. Tucker ,  Steven C. Zimmerman ,  Brittany A. Walker

IPC: C02F5/10 ,  C07C57/34

Abstract: A method of scale inhibition treatment of a water system comprising introducing an aqueous scale inhibiting composition into the water system wherein the aqueous scale inhibiting composition comprises a carboxylated hyperbranched polyglycerol.

公开(公告)号：US20150374823A1

公开(公告)日：2015-12-31

申请号：US14649721

申请日：2014-01-13

Applicant: DOW GLOBAL TECHNOLOGIES LLC

Inventor： Mladen Ladika ,  Jin Zhao ,  Michael L. Tulchinsky ,  Thomas H. Kalantar ,  J. Keith Harris

IPC: A61K47/10 ,  A61K31/095 ,  A61K31/343 ,  A61K31/192 ,  A61K31/58

CPC classification number: A61K47/10 ,  A61K9/4866 ,  A61K31/095 ,  A61K31/10 ,  A61K31/192 ,  A61K31/343 ,  A61K31/58 ,  C08G65/20 ,  C08L71/02

Abstract: The present invention relates to the use of polyalkoxylated alcohols of the formula R—O-(AO)—H, wherein R is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl or heterocyclic group having 7 to 25 carbon atoms, (AO) is a polyoxyalkylene moiety of the composition (BO)m(EO)n(DO)r with random or blockwise arrangement of the constituting oxyalkylene units, wherein m, n and r represent the average number of oxybutylene (BO) units, oxyethylene (EO) units and oxyalkylene units derived from at least one epoxide selected from styrene oxide and alkylene oxides having from 5 to 10 carbon atoms (DO) per molecule of the polyalkoxylated alcohol, respectively, m being a number greater than or equal to 1, n being a number greater than or equal to 1 and r being a number in the range from 0 to 50 under the proviso that (m+n+r) is less than or equal to 200 and the ratio n/(m+r) is in the range of 1 to 20, as excipients in pharmaceutical compositions. Said polyalkoxylated alcohols enable very effective solubilisation of poorly soluble active pharmaceutical ingredients in aqueous media. Solid or semi-solid pharmaceutical compositions comprising one or more such polyalkoxylated alcohol combined with at least one active pharmaceutical ingredient are further long term stable under typical storage conditions and can be readily provided in various dosage forms such as tablets and filled capsules.

Abstract translation: 本发明涉及式R-O-（AO）-H的聚烷氧基化醇的用途，其中R是具有7至25个碳原子的取代或未取代的烷基，烯基，炔基，芳基，芳烷基或杂环基，（ AO）是组成（BO）m（EO）n（DO）r的聚氧化烯部分，其具有构成的氧化烯单元的无规或阻塞排列，其中m，n和r表示氧丁烯（BO）单元的平均数，氧化乙烯 （EO）单元和衍生自至少一种选自氧化苯乙烯和每分子聚烷氧基化醇具有5至10个碳原子的氧化烯（DO）的环氧化物的氧化烯单元，m分别大于或等于1， n是大于或等于1的数，r是0至50的数，条件是（m + n + r）小于或等于200，并且比率n /（m + r） 在1至20的范围内，作为药物组合物中的赋形剂。 所述聚烷氧基化的醇使得难溶性活性药物成分在水性介质中非常有效地溶解。 包含一种或多种这样的多烷氧基化醇与至少一种活性药物成分组合的固体或半固体药物组合物在典型的储存条件下进一步长期稳定，并且可以容易地以各种剂型例如片剂和填充的胶囊提供。