生物活性 | |||
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描述 | Loxoprofen (LOX) is a non-selective cyclooxygenase inhibitor that is widely used for the treatment of pain and inflammation caused by chronic and transitory conditions. In addition, LOX can also be converted into an inactive hydroxylated metabolite (OH-LOXs) by cytochrome P450 (CYP) [3]. Loxoprofen (Loxonin(®), Loxonin(®) Pap, Loxonin(®) Tape) is a prodrug-type NSAID that is available in several formulations, including 60 mg tablets, 100 mg hydrogel patches and 50 or 100 mg tape. Loxoprofen is a useful analgesic option for patients with pain and inflammation, with topical loxoprofen potentially reducing the risk of gastrointestinal, cardiovascular and renal complications associated with oral NSAID use[4]. The uptake of loxoprofen into Caco-2 cells was pH- and concentration-dependent, and was described by a Michaelis-Menten equation with passive diffusion (Km : 4.8 mm, Vmax : 142 nmol/mg protein/30 s, and Kd : 2.2 μl/mg protein/30 s). Transport of loxoprofen in Caco-2 cells is, at least in part, mediated by a proton-dependent transport system[5]. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02384928 | Sciatica Inte... 展开 >>rvertebral Disc Displacement 收起 << | Not Applicable | Completed | - | Korea, Republic of ... 展开 >> Jaseng Hospital of Korean Medicine Seoul, Gangnam-Gu, Korea, Republic of, 135-896 收起 << |
NCT03386149 | Lumbar Disc Herniation | Phase 3 | Recruiting | September 30, 2018 | Korea, Republic of ... 展开 >> Dongguk University Bundang Oriental Hospital Recruiting Seongnam, Gyeonggi, Korea, Republic of, 13601 Contact: Eun-Jung Kim, PhD., KMD +82317103751 hanijjung@naver.com Daegu Korean Medicine Hospital of Daegu Haany University Recruiting Daegu, Korea, Republic of, 42158 Contact: I-Rang Choi, B.S +82537702324 soongood88@dhu.ac.kr Kyunghee University Medical Center Recruiting Seoul, Korea, Republic of, 02447 Contact: Sae-Rom Jeon, B.S. +821050478756 sr9213@naver.com Kyung Hee University Hospital at Gangdong Recruiting Seoul, Korea, Republic of, 05278 Contact: Bonhyuk Goo, M.S., KMD +8224406099 goobh99@naver.com 收起 << |
NCT02467504 | Rheumatoid Arthritis | Phase 2 | Unknown | June 2017 | China, Beijing ... 展开 >> Department of Rheumatology and Immunology, Peking University People's Hospital Recruiting Beijing, Beijing, China, 100044 Contact: Xiaoying Zhang, MD +8613810001444 xiaoying19880307@163.com 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.06mL 0.81mL 0.41mL |
20.30mL 4.06mL 2.03mL |
40.60mL 8.12mL 4.06mL |
参考文献 |
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