公开(公告)号：WO03080079B1

公开(公告)日：2004-07-15

申请号：PCT/US0308348

申请日：2003-03-19

Applicant: CYDEX INC ,  MOSHER GEROLD L ,  PIPKIN JAMES D ,  ZIMMERER RUPERT O ,  FULK CHRISTINA M ,  THOMPSON DIANE O

Inventor： MOSHER GEROLD L ,  PIPKIN JAMES D ,  ZIMMERER RUPERT O ,  FULK CHRISTINA M ,  THOMPSON DIANE O

IPC: A61K9/00 ,  A61K31/05 ,  A61K31/724 ,  A61K47/32 ,  A61K47/34 ,  A61K47/40 ,  A61K47/46 ,  A61K47/48

CPC classification number: B82Y5/00 ,  A61K9/0019 ,  A61K31/05 ,  A61K31/724 ,  A61K47/40 ,  A61K47/6951 ,  A61K2300/00

Abstract: A method of preserving formulations is provided. The method includes the step of including a derivatized cyclodextrin in a formulation capable of sustaining microbial growth. One embodiment of the formulation employs a sulfoalkyl ether cyclodextrin as a preservative and optionally as a solubilizing and complexing agent. A suitable cyclodextrin is the CAPTISOL" brand cyclodextrin (sulfobutyl ether R-cyclodextrin). Whether or not the formulation includes a conventional preservative, the formulation will remain preserved for at least a minimum predetermined period. Specific embodiments of the invention include a carrier, a derivatized cyclodextrin and optionally one or more active agents, one or more water activity-reducing agents, and/or one or more complexation-enhancing agents. The derivatized cyclodextrin reduces the water activity of the formulation. A liquid formulation can be lyophilized or otherwise dried to yield a solid formulation that is optionally reconstitutable.

Abstract translation: 提供了一种保存制剂的方法。 该方法包括将衍生化的环糊精包含在能够维持微生物生长的制剂中的步骤。 制剂的一个实施方案采用磺基烷基醚环糊精作为防腐剂，任选地作为增溶剂和络合剂。 合适的环糊精是CAPTISOL“品牌的环糊精（磺丁基醚R-环糊精），无论制剂是否含有常规的防腐剂，制剂将保持至少保持至少最小的预定时间。本发明的具体实施方案包括载体， 衍生化的环糊精和任选的一种或多种活性剂，一种或多种水活性降低剂和/或一种或多种络合增强剂。衍生化的环糊精降低制剂的水活性。液体制剂可以冻干或以其它方式干燥 以产生任选可重构的固体制剂。

公开(公告)号：WO2003080079A1

公开(公告)日：2003-10-02

申请号：PCT/US2003/008348

申请日：2003-03-19

Applicant: CYDEX, INC. ,  MOSHER, Gerold, L. ,  PIPKIN, James, D. ,  ZIMMERER, Rupert, O. ,  FULK, CHristina, M. ,  THOMPSON, Diane, O.

Inventor： MOSHER, Gerold, L. ,  PIPKIN, James, D. ,  ZIMMERER, Rupert, O. ,  FULK, CHristina, M. ,  THOMPSON, Diane, O.

IPC: A61K31/724

CPC classification number: B82Y5/00 ,  A61K9/0019 ,  A61K31/05 ,  A61K31/724 ,  A61K47/40 ,  A61K47/6951 ,  Y02A50/473 ,  A61K2300/00

Abstract: A method of preserving formulations is provided. The method includes the step of including a derivatized cyclodextrin in a formulation capable of sustaining microbial growth. One embodiment of the formulation employs a sulfoalkyl ether cyclodextrin as a preservative and optionally as a solubilizing and complexing agent. A suitable cyclodextrin is the CAPTISOL" brand cyclodextrin (sulfobutyl ether R-cyclodextrin). Whether or not the formulation includes a conventional preservative, the formulation will remain preserved for at least a minimum predetermined period. Specific embodiments of the invention include a carrier, a derivatized cyclodextrin and optionally one or more active agents, one or more water activity-reducing agents, and/or one or more complexation-enhancing agents. The derivatized cyclodextrin reduces the water activity of the formulation. A liquid formulation can be lyophilized or otherwise dried to yield a solid formulation that is optionally reconstitutable.

Abstract translation: 提供了一种保存制剂的方法。 该方法包括将衍生化的环糊精包含在能够维持微生物生长的制剂中的步骤。 制剂的一个实施方案采用磺基烷基醚环糊精作为防腐剂，任选地作为增溶剂和络合剂。 合适的环糊精是CAPTISOL“品牌的环糊精（磺丁基醚R-环糊精），无论制剂是否含有常规的防腐剂，制剂将保持至少保持至少最小的预定时间。本发明的具体实施方案包括载体， 衍生化的环糊精和任选的一种或多种活性剂，一种或多种水活性降低剂和/或一种或多种络合增强剂。衍生化的环糊精降低制剂的水活性。液体制剂可以冻干或以其它方式干燥 以产生任选可重构的固体制剂。