公开(公告)号：WO2007056125A3

公开(公告)日：2007-06-28

申请号：PCT/US2006042931

申请日：2006-11-03

Applicant: EASTMAN CHEM CO

Inventor： POSEY-DOWTY JESSICA DEE ,  WATTERSON THELMA LEE ,  EDGAR KEVIN JOSEPH ,  KIRK SHANE KIPLEY ,  WELTY MICHAEL LEE ,  YUAN JINGHUA ,  SHELTON MICHAEL CHARLES ,  LINGERFELT LARRY RONNIE JR ,  WILSON ALAN KENT

IPC: A61K9/10 ,  A61K9/20 ,  A61K9/48

CPC classification number: A61K9/2054 ,  A61K9/10 ,  A61K9/2013 ,  A61K9/4808 ,  A61K31/717

Abstract: Disclosed herein are pharmaceutical compositions comprising carboxyalkylcellulose esters for sustained delivery of pharmaceutically active substances. The composition comprises: at least one pharmaceutically active agent, and at least one carboxyalkyl cellulose ester comprising an anhydroglucose repeat unit having the structure (I), wherein: R 1 -R 6 are each independently selected from -OH, -OC(O)(alkyl), and -O(CH 2 ) X C(O)OH, and pharmaceutically acceptable salts thereof, wherein x ranges from 1-3, a degree of substitution per anhydroglucose of - OH ranges from 0.1 to 0.7, a degree of substitution per anhydroglucose of -C(O)(alkyl) ranges from 0.1 to 2.7, and a degree of substitution per anhydroglucose of -O(CH 2 ) X C(O)OH ranges from 0.2 to 0.75, and wherein in pharmaceutically acceptable media, the composition exhibits sustained release of the at least one pharmaceutically active agent. Also disclosed are methods of administering the compositions for sustained delivery, such as delivery following zero order kinetics.

Abstract translation: 本文公开了包含用于持续递送药物活性物质的羧基烷基纤维素酯的药物组合物。 所述组合物包含：至少一种药学活性剂和至少一种含有具有结构（I）的脱水葡萄糖重复单元的羧基烷基纤维素酯，其中：R 1 -R 6 各自独立地选自-OH，-OC（O）（烷基）和-O（CH 2）2 C（O）OH，和其药学上可接受的盐 其中x为1-3，-OH的每个脱水葡萄糖的取代度为0.1-0.7，-C（O）（烷基）的每个脱水葡萄糖的取代度为0.1- 2.7， -O（CH 2）2 C（O）OH的每个脱水葡萄糖的取代范围为0.2至0.75，并且其中在药学上可接受的介质中，所述组合物显示持续释放 至少一种药物活性剂。 还公开了施用用于持续递送的组合物的方法，例如在零级动力学之后的递送。

公开(公告)号：WO2007056205A2

公开(公告)日：2007-05-18

申请号：PCT/US2006043077

申请日：2006-11-03

Applicant: EASTMAN CHEM CO

Inventor： SHELTON MICHAEL CHARLES ,  POSEY-DOWTY JESSICA DEE ,  EDGAR KEVIN JOSEPH ,  LINGERFELT LARRY RONNIE JR ,  KLEIN SANDRA ,  KIRK SHANE KIPLEY ,  DRESSMAN JENNIFER JOY

IPC: A61K9/14 ,  A61K47/38

CPC classification number: A61K9/141 ,  A61K9/10 ,  A61K31/717 ,  A61K47/38

Abstract: Disclosed herein are pharmaceutical compositions comprising carboxyalkylcellulose esters for delivery of pharmaceutically active substances having low solubility in a medium such as water, an acidic aqueous buffer, a neutral aqueous buffer, or a basic aqueous buffer. Also disclosed are methods for making pharmaceutical compositions and methods of administering the compositions.

Abstract translation: 本文公开了包含羧基烷基纤维素酯的药物组合物，用于递送在诸如水，酸性水性缓冲液，中性水性缓冲液或碱性水性缓冲液的介质中具有低溶解度的药学活性物质。 还公开了制备药物组合物的方法和施用组合物的方法。