Catalytic functionalization of polymers: a novel approach to site-specific delivery of misoprostol to the stomach
摘要:
The application of functionalized polymers to site-directed delivery of the antiulcer prostaglandin, misoprostol, is described. By use of homogeneous catalysis, the simple polymer, polybutadiene, was modified to incorporate the specialized requirements for controlled delivery of misoprostol to the stomach. An acid labile silyl ether bond to the C-11 hydroxyl of misoprostol was installed as the primary rate determining step for drug release, and a series of analogs, in which the steric hindrance about the silicon atom was varied, was prepared and evaluated for in vitro release rates, efficacy against indomethacin induced gastric damage and diarrheagenic activity. The diisopropylsilyl analog, the slowest releasing system studied, showed efficacy equal to misoprostol against indomethacin-induced gastric damage and no diarrhea at the highest dose tested.
FLAVANTHRENE DERIVATIVES AND THEIR USE AS ORGANIC SEMICONDUCTORS
申请人:Wang Changsheng
公开号:US20130306914A1
公开(公告)日:2013-11-21
The invention relates to benzo[h]benz[5,6]acridino[2,1,9,8-klmna]acridines, methods of their preparation, their use as semiconductors in organic electronic (OE) devices, and to OE devices comprising them.
Foss, V. L.; Veits, Yu. A.; Leksunkin, V. A., Journal of general chemistry of the USSR, 1985, vol. 55, # 7, p. 1458 - 1459
作者:Foss, V. L.、Veits, Yu. A.、Leksunkin, V. A.、Gurov, M. V.
DOI:——
日期:——
FOSS, V. L.;VEJTS, YU. A.;LEKSUNKIN, V. A.;GUROV, M. V., ZH. OBSHCH. XIMII, 1985, 55, N 7, 1639-1640
作者:FOSS, V. L.、VEJTS, YU. A.、LEKSUNKIN, V. A.、GUROV, M. V.
DOI:——
日期:——
Catalytic functionalization of polymers: a novel approach to site-specific delivery of misoprostol to the stomach
作者:Samuel J. Tremont、Paul W. Collins、William E. Perkins、Rick L. Fenton、Denis Forster、Martin P. McGrath、Grace M. Wagner、Alan F. Gasiecki、Robert G. Bianchi
DOI:10.1021/jm00073a007
日期:1993.10
The application of functionalized polymers to site-directed delivery of the antiulcer prostaglandin, misoprostol, is described. By use of homogeneous catalysis, the simple polymer, polybutadiene, was modified to incorporate the specialized requirements for controlled delivery of misoprostol to the stomach. An acid labile silyl ether bond to the C-11 hydroxyl of misoprostol was installed as the primary rate determining step for drug release, and a series of analogs, in which the steric hindrance about the silicon atom was varied, was prepared and evaluated for in vitro release rates, efficacy against indomethacin induced gastric damage and diarrheagenic activity. The diisopropylsilyl analog, the slowest releasing system studied, showed efficacy equal to misoprostol against indomethacin-induced gastric damage and no diarrhea at the highest dose tested.
Flavanthrene derivatives and their use as organic semiconductors
申请人:Wang Changsheng
公开号:US09373801B2
公开(公告)日:2016-06-21
The invention relates to benzo[h]benz[5,6]acridino[2,1,9,8-klmna]acridines, methods of their preparation, their use as semiconductors in organic electronic (OE) devices, and to OE devices comprising them.