We describe strategies in drug development to reduce the gastrointestinal (GI) toxicity of nonsteroidal anti-inflammatory drugs (NSAIDs). We then provide an overview of the experiments that led to the development of PC-NSAIDs, a novel family of NSAIDs associated with phosphatidylcholine (PC) that have reduced GI toxicity and full therapeutic activity. Furthermore, we describe the evidence showing: that the stomach possesses hydrophobic properties that are attributable to phospholipids lining the mucus gel layer; and that NSAIDs chemically associate with intrinsic PC, thereby attenuating the tissue's hydrophobic properties. Further, pre-associating NSAIDs with PC reduces the GI toxicity of these drugs, both in rodent ulcer models and in human subjects, without affecting the drugs' therapeutic activity. Finally, we discuss the commercialization and launch of Aspirin-PC, an over-the-counter (OTC) drug with the brand name Vazalore®.

2022-04-22·ChemSusChem2区 · 化学

Versatile Chemical Recycling Strategies: Value‐Added Chemicals from Polyester and Polycarbonate Waste

2区 · 化学

Article

作者: Davidson, Matthew G. ; Jones, Matthew D. ; Kamran, Muhammad ; Payne, Jack M.

AbstractZnII‐complexes bearing half‐salan ligands were exploited in the mild and selective chemical upcycling of various commercial polyesters and polycarbonates. Remarkably, we report the first example of discrete metal‐mediated poly(bisphenol A carbonate) (BPA‐PC) methanolysis being appreciably active at room temperature. Indeed, Zn(2)2 and Zn(2)Et achieved complete BPA‐PC consumption within 12–18 mins in 2‐Me‐THF, noting high bisphenol A (BPA) yields (SBPA=85–91 %) within 2–4 h. Further kinetic analysis found such catalysts to possess kapp values of 0.28±0.040 and 0.47±0.049 min−1 respectively at 4 wt%, the highest reported to date. A completely circular upcycling approach to plastic waste was demonstrated through the production of several renewable poly(ester‐amide)s (PEAs), based on a terephthalamide monomer derived from bottle‐grade poly(ethylene terephthalate) (PET), which exhibited excellent thermal properties.

2021-03-15·Angewandte Chemie International Edition1区 · 化学

Selective Chemical Upcycling of Mixed Plastics Guided by a Thermally Stable Organocatalyst

1区 · 化学

Article

作者: Mantione, Daniele ; Sardon, Haritz ; Jehanno, Coralie ; Arno, Maria C. ; Demarteau, Jeremy ; Ruipérez, Fernando ; Dove, Andrew P. ; Hedrick, James L.

AbstractChemical recycling of plastic waste represents a greener alternative to landfill and incineration, and potentially offers a solution to the environmental consequences of increased plastic waste. Most plastics that are widely used today are designed for durability, hence currently available depolymerisation methods typically require harsh conditions and when applied to blended and mixed plastic feeds generate a mixture of products. Herein, we demonstrate that the energetic differences for the glycolysis of BPA‐PC and PET in the presence of a protic ionic salt TBD:MSA catalyst enables the selective and sequential depolymerisation of these two commonly employed polymers. Employing the same procedure, functionalised cyclic carbonates can be obtained from both mixed plastic wastes and industrial polymer blend. This methodology demonstrates that the concept of catalytic depolymerisation offers great potential for selective polymer recycling and also presents plastic waste as a “greener” alternative feedstock for the synthesis of high added value molecules.

100 项与阿司匹林/卵磷脂相关的药物交易

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适应症	最高研发状态	国家/地区	公司	日期
发热	临床1期	美国	PLx Pharma, Inc.	-
心肌梗塞	临床1期	美国	PLx Pharma, Inc.	-
疼痛	临床1期	美国	PLx Pharma, Inc.	-
脑卒中	临床1期	美国	PLx Pharma, Inc.	-

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


AUA2017	N/A	-	199	PCNL with perioperative aspirin use	構選構壓簾範網遞鬱鬱(醖壓襯範顧憲繭築鹹網) = There were no Clavien-Dindo grade III or higher complications in the course of our review 獵繭繭繭淵衊糧選齋鏇 (齋蓋淵鹽築製獵鹽壓願 )	-	2017-04-01