用以檢測布洛芬之鏡像異構物的套組及方法

專利類型

發明

專利國別 (專利申請國家)

中華民國

專利申請案號

108113804

專利證號

I 715968

專利獲證名稱

用以檢測布洛芬之鏡像異構物的套組及方法

專利所屬機關 (申請機關)

高雄醫學大學

獲證日期

2021/01/11

技術說明

布洛芬是一種在全世界運用廣泛之非類固醇類抗發炎藥物，其在非處方藥常用於治療慢性疼痛與發炎。布洛芬結構上具有R form及S form異構物，S form是主要活性成分透過抑制環氧化酶 (cyclooxygenase) 來降低前列腺素 (prostaglandins) 及血栓素 (thromboxanes) 的合成進而抑制發炎反應。臨床上若病人使用消旋混合物(racemic mixture)之布洛芬來治療疼痛與發炎需要增加劑量，為了減少劑量，市售藥品亦有純化單一S form布洛芬如dexibuprofen。布洛芬在非處方藥市場取得相當容易，以致民眾容易忽略其危險性和副作用如消化道出血，皮疹，類天皰瘡，腎功能衰竭，凝血功能受損，高血壓和心肌梗塞等，根據衛福部公布的藥害救濟案件，布洛芬是引起不良反應的可疑藥品之一，因此，建立一套分析方法來監控R form及S form布洛芬是需要的。此研究以一段特殊胜肽搭配液相層析質譜儀來建立布洛芬異構物之快速偵測方法，結果顯示此分析方法有用於分離與偵測R form及S form布洛芬是可行的。 Ibuprofen, a non-steroidal anti-inflammatory drug, is widely used throughout the world. It is also a very popular over-the-counter (OTC) drug used for the treatment of chronic pain and inflammation. Ibuprofen contains S form and R form isomers in its structure, S form isomer is the active component to inhibit the activity of cyclooxygenase and synthesis of prostaglandins and thromboxanes. If patients use racemic mixture of ibuprofen to treat pain or inflammation, the clinical dose may increase. To decrease the clinical dose, commercial drug dexibuprofen (S form) has been purified and isolated. Ibuprofen is easily available in OTC market, hence, people are easy to ignore it side effects (such as gastrointestinal bleeding, rash, bullous pemphigoid, renal failure, impairment of coagulation, hypertension and myocardial infarction). According to reports published by the Ministry of Health and Welfare (MOHW), ibuprofen is a suspected drug that causes adverse reactions. Therefore, it is necessary to develop an analytical methods for monitoring the S form and R form isomer of ibuprofen. In this study, a sensitive and fast liquid chromatography combined with mass spectrometry (LC-MS) method was developed and validated for the determination of ibuprofen isomers after reacting with a special peptide. The results show that this proposed method is workable to separate and detect S form and R form isomer of ibuprofen.

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