恩他卡朋是儿茶酚-O-甲基转移酶(COMT)的新型抑制剂,可作为左旋多巴疗法的辅助治疗帕金森氏病。但是,口服他卡朋的生物利用度相对较低(29-46%)。在这项研究中,我们制备了更多的恩他卡朋的亲脂性酰基酯和酰氧基酰基酯,酰氧基烷基醚和烷氧基羰基酯,我们将它们评估为增强恩他卡朋口服生物利用度的潜在前药。所有衍生物均符合前药标准,并在人血清中体外释放他卡酮。在大鼠中进一步研究了entacapone的单新戊酰基(1a)和二新戊酰基(1b)酯的口服生物利用度。1b的亲脂性较高(在pH 7.4时,log Papp 4.0),但口服生物利用度较低(F = 0.6%),最可能是由于其低水溶性。在pH 7.4时,entacapone(1a)的单新戊酰基酯的亲脂性(log Papp 0.80)比entacapone(log Papp 0.18)高,同时保持水溶性等于entacapone。但是,与母体药物恩他
HYDROCARBOXYLATION OF FORMALDEHYDE IN THE PRESENCE OF A HIGHER ORDER CARBOXYLIC ACID AND HETEROGENEOUS CATALYST
申请人:Barnicki Scott Donald
公开号:US20130261333A1
公开(公告)日:2013-10-03
Disclosed is a process for the production and purification of glycolic acid or glycolic acid derivatives by the carbonylation of formaldehyde in the presence of a solid acid catalyst and a carboxylic acid. This invention discloses hydrocarboxylations and corresponding glycolic acid separations wherein the glycolic acid stream is readily removed from the carboxylic acid and the carboxylic acid is recycled.
HYDROCARBOXYLATION OF METHYLENE DIPROPIONATE IN THE PRESENCE OF PROPIONIC ACID AND A HETEROGENEOUS CATALYST
申请人:Barnicki Scott Donald
公开号:US20130261337A1
公开(公告)日:2013-10-03
Disclosed is a process for the production and purification of glycolic acid or glycolic acid derivatives by the carbonylation of methylene dipropionate in the presence of a solid acid catalyst and propionic acid. This invention discloses hydrocarboxylations and corresponding glycolic acid separations wherein the propionic acid stream is readily removed from the glycolic acid and the propionic acid is recycled.
HYDROCARBOXYLATION OF METHYLENE DIPROPIONATE IN THE PRESENCE OF A PROPIONIC ACID AND A HOMOGENEOUS CATALYST
申请人:Barnicki Scott Donald
公开号:US20130261329A1
公开(公告)日:2013-10-03
Disclosed is a process for the production and purification of glycolic acid or glycolic acid derivatives by the carbonylation of methylene dipropionate in the presence of a homogeneous acid catalyst and propionic acid. This invention discloses hydrocarboxylations and corresponding homogeneous acid catalyst and glycolic acid separations. The homogeneous acid catalyst is readily separated from the hydrocarboxylation reaction effluent and recycled and the propionic acid is readily removed from the glycolic acid and the propionic acid is recycled
申请人:State of Oregon acting by and through the State Board of Higher Education on behalf of the Univers
公开号:US20150023643A1
公开(公告)日:2015-01-22
Gradient index optical materials are formed by drop by drop dispensing of nanoparticle/monomer suspensions. Refractive index variations are defined by nanoparticle concentrations that can vary in three dimensions. Droplets of differing compositions can be mixed, and droplets or layers or droplets are partially cross-linked by exposure to ultraviolet radiation prior to dispensing additional droplets. Gradient index optical elements such as lenses, prisms, and waveguides can be formed in flexible polymer layers.
Implantation device, method for producing and for applying the same
申请人:Stryker Trauma GmbH
公开号:EP1972352A1
公开(公告)日:2008-09-24
An implantation device for fixating a bone comprises a main body, wherein the main body has a peripheral region, wherein the main body comprises a polymeric material, and wherein the peripheral region comprises the polymeric material and a plasticizer. In particular, the peripheral region may be adapted to be fixed to a bone.A method for producing an implantation device comprises the steps of forming an implantation device using polymer material, and dipping at least a portion of the implantation device into a plasticizer in such a way that a peripheral region of the implantation device is plastified.