Ahmed Sofia, Sheraz Muhammad Ali, Ahmad Iqbal
Baqai Institute of Pharmaceutical Sciences, Baqai Medical University, Karachi, Pakistan.
Profiles Drug Subst Excip Relat Methodol. 2018;43:255-319. doi: 10.1016/bs.podrm.2018.01.001. Epub 2018 Mar 16.
Tolfenamic acid (TA) is a nonsteroidal antiinflammatory drug and belongs to the group of fenamates. It is used as a potent pain reliever in the treatment of acute migraine attacks, and disorders like dysmenorrhea, rheumatoid, and osteoarthritis. TA has shown excellent in vitro antibacterial activity against certain ATCC strains of bacteria when complexed with bismuth(III). It has also been reported to block pathological processes associated with Alzheimer's disease. In the recent past, TA has also been used as a novel anticancer agent for the treatment of various cancers. In view of the clinical importance of TA, a comprehensive review of the physical and pharmaceutical properties and details of the various analytical methods used for the assay of the drug in pharmaceutical and biological systems has been made. The methods reviewed include identification tests and titrimetric, spectrophotometric, chromatographic, electrochemical, thermal, microscopic, enzymatic, and solid-state techniques. Along with the analytical profile, the stability and degradation of TA, its pharmacology and pharmacokinetics, dosage forms and dose, adverse effects and toxicity, and interactions have been discussed.
托芬那酸(TA)是一种非甾体抗炎药,属于芬那酸盐类。它在治疗急性偏头痛发作以及痛经、类风湿性关节炎和骨关节炎等疾病时用作强效止痛剂。当与铋(III)络合时,TA对某些ATCC菌株显示出优异的体外抗菌活性。据报道,它还能阻断与阿尔茨海默病相关的病理过程。最近,TA也被用作治疗各种癌症的新型抗癌剂。鉴于TA的临床重要性,本文对其物理和药学性质以及用于药物和生物体系中该药物测定的各种分析方法的细节进行了全面综述。所综述的方法包括鉴别试验以及滴定法、分光光度法、色谱法、电化学法、热分析法、显微镜法、酶法和固态技术。除了分析概况外,还讨论了TA的稳定性和降解、药理学和药代动力学、剂型和剂量、不良反应和毒性以及相互作用。