公开(公告)号：WO1998030208A1

公开(公告)日：1998-07-16

申请号：PCT/US1997023358

申请日：1997-12-18

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  QIU, Yihong ,  TRIVEDI, Jay, S. ,  GRAHAM, Sharon, L. ,  FLOOD, Kolette, M. ,  KRILL, Steven, L.

IPC: A61K09/20

CPC classification number: A61K9/2086

Abstract: The present invention provides a tablet for the controlled release of an active agent comprising (a) a core layer comprising an active agent embedded in a non-swelling, non-erodible hydrophobic matrix; (b) a first barrier layer applied to and coating a single face of the core layer; and (c) an optional second barrier layer applied to and coating the opposite face of the core layer and oppositely disposed to the first barrier layer; wherein the core comprises up to about 80 % active agent and from about 5 % to about 80 % by weight of nonswellable waxes or polymeric material insoluble in aqueous medium, and the first and second barrier layers independently comprise (1) polymeric material exhibiting a high degree of swelling and gelling in aqueous medium, or (2) nonswellable wax or polymeric material insoluble in aqueous medium.

Abstract translation: 本发明提供了一种用于控制释放活性剂的片剂，其包含（a）核心层，其包含嵌入非溶胀，不可侵蚀的疏水基质中的活性剂; （b）施加到芯层的单面上并涂覆其上的第一阻挡层; 和（c）可选的第二阻挡层，其施加到芯层的相对面并涂覆在第一阻挡层的相对面上; 其中所述核心包含至多约80％的活性剂和约5％至约80％重量的不溶于水性介质的不可渗透的蜡或聚合物，并且所述第一和第二阻隔层独立地包含（1）表现出高的 在水性介质中膨胀和凝胶化程度，或（2）不溶于水的介质中不可渗透的蜡或聚合物。

公开(公告)号：EP0951279A1

公开(公告)日：1999-10-27

申请号：EP97952511.0

申请日：1997-12-18

Applicant: Abbott Laboratories

Inventor： QIU, Yihong ,  TRIVEDI, Jay, S. ,  GRAHAM, Sharon, L. ,  FLOOD, Kolette, M. ,  KRILL, Steven, L.

IPC: A61K9 ,  A61K31 ,  A61P11

CPC classification number: A61K9/2086

Abstract: The present invention provides a tablet for the controlled release of an active agent comprising (a) a core layer comprising an active agent embedded in a non-swelling, non-erodible hydrophobic matrix; (b) a first barrier layer applied to and coating a single face of the core layer; and (c) an optional second barrier layer applied to and coating the opposite face of the core layer and oppositely disposed to the first barrier layer; wherein the core comprises up to about 80 % active agent and from about 5 % to about 80 % by weight of nonswellable waxes or polymeric material insoluble in aqueous medium, and the first and second barrier layers independently comprise (1) polymeric material exhibiting a high degree of swelling and gelling in aqueous medium, or (2) nonswellable wax or polymeric material insoluble in aqueous medium.

公开(公告)号：EP0975330A1

公开(公告)日：2000-02-02

申请号：EP98903718.9

申请日：1998-01-26

Applicant: Abbott Laboratories

Inventor： LIU, Rong ,  PECK, Kendall, D. ,  FLOOD, Kolette, M. ,  ZHENG, Jack

IPC: A61K9/127 ,  A61K31/70

CPC classification number: A61K31/7048 ,  A61K9/127

Abstract: Disclosed is an invention directed towards pain-reducing parenteral formulations comprising a macrolide drug entrapped in a liposome vesicle. The macrolide drug is selected from the group consisting of derivatives of erythromycins A, B, C and D; clarithromycin; azithromycin; dirithromycin; josamycin; midecamycin; kitasamycin; roxithromycin; rokitamycin; oleandomycin; miocamycin; flurithromycin; rosaramicin; 8,9-anhydro-4''-deoxy-3'-N-desmethyl-3'-N-ethylerythromycin B 6,9-hemiacetal; 8,9-anhydro-4''-deoxy-3'-N-desmethyl-3'-N-ethylerythromycin A 6,9-hemiacetal; and 11-amino-11-deoxy-3-oxo-5-O-desosaminyl-6-O-[1'-3'-quinolyl-2'-propenyl]-erythronolide A 11,12-cyclic carbamate. The formulations of the invention are effective in substantially reducing the pain at the injection site typically associated with the injection of macrolide antibiotics.