Development and Validation of a Stability-Indicating Assay of Etofenamate by RP-HPLC and Characterization of Degradation Products

A validated stability-indicating RP-HPLC method for etofenamate (ETF) was developed by separating its degradation products on a C18 (250 mm × 4.6 mm 5 μm) Qualisil BDS column using a phosphate buffer (pH-adjusted to 6.0 with orthophosphoric acid) and methanol in the ratio of 20:80 % v/v as the mobile phase at a flow rate of 1.0 mL/min. The column effluents were monitored by a photodiode array detector set at 286 nm. The method was validated in terms of specificity, linearity, accuracy, precision, detection limit, quantification limit, and robustness. Forced degradation of etofenamate was carried out under acidic, basic, thermal, photo, and peroxide conditions and the major degradation products of acidic and basic degradation were isolated and characterized by ¹H-NMR, ¹³C-NMR, and mass spectral studies. The mass balance of the method varied between 92–99%.     

依托芬那酯凝胶治疗运动系统慢性软组织损伤的临床疗效分析

目的分析依托芬那酯凝胶治疗运动系统慢性软组织损伤的有效性。方法将2011年9月-2012年3月收治的120例慢性运动系统软组织损伤患者随机分为两组，每组各60例。治疗组采用依托芬那酯凝胶予以治疗，对照组应用双氯芬酸钠乳胶剂治疗，疗程均为2周。结果治疗2周后，两组患者疼痛视觉模拟评分（VAS）≤3分者明显增加，临床疗效明显；尽管治疗组VAS评分≤3分的例数多于对照组，但两组治疗总体疗效比较，差异无统计学意义（P〉0．05），提示两种药物对运动系统慢性损伤的疗效相当。治疗组发生不良反应2例，对照组发生不良反应3例，均较轻微，无严重不良事件发生。结论依托芬那酯凝胶治疗运动系统慢性损伤有效，元严重不良反应，特别适合有胃肠系统疾病的门诊患者。     

依托芬那酯凝胶对比双氯芬酸二乙胺乳胶治疗髌股关节骨关节炎的临床观察

目的:观察依托芬那酯凝胶对比双氯芬酸二乙胺乳胶治疗髌股关节骨关节炎的临床疗效和安全性。方法:94例髌股关节骨关节炎患者按随机数字表法均分为试验组和对照组。试验组患者给予10%依托芬那酯凝胶,根据疼痛部位大小,每次涂3 cm药物在局部并用手轻按摩,tid;对照组患者给予1%双氯芬酸二乙胺乳胶,根据疼痛部位大小,每次涂3 cm药物在局部并用手轻按摩,tid。两组患者患处不覆盖敷料或绷带,疗程均为7 d。观察两组患者的临床疗效、20 m步行痛评分、西方安大略和麦克马斯特大学骨关节炎指数(WOMAC)评分、关节触痛评分及不良反应发生情况。结果:治疗后试验组患者总有效率显著高于对照组,两组比较差异有统计学意义(P<0.05)。治疗前两组患者20 m步行痛评分、WOMAC评分、关节触痛评分比较,差异无统计学意义(P>0.05);治疗后两组患者20 m步行痛评分、WOMAC评分、关节触痛评分均显著低于同组治疗前,且试验组低于对照组,差异有统计学意义(P<0.05)。两组患者不良反应发生率比较,差异无统计学意义(P>0.05)。结论:依托芬那酯凝胶治疗髌股关节骨关节炎疗效优于双氯芬酸二乙胺乳胶,安全性相当。     

Topical gels of etofenamate: in vitro and in vivo evaluation

Abstract

Non-steroid anti-inflammatory drugs (NSAIDs), such as etofenamate, are among the most prescribed drugs used for their analgesic, anti-rheumatic, antipyretic and anti-inflammatory properties. Topical formulations have the main advantage of targeted delivery. However, drugs must overcome the skin due to its role as a physical and chemical barrier against the penetration of chemicals and microorganisms. This barrier must be altered to allow the permeation of drugs at a suitable rate to the desired site of activity. Permeation modulators can intercalate the skin outer layers causing structure disruption, opening an energetically favourable route for the drug to diffuse through. The aim of this work was the development of hydroalcoholic gels containing 5.0% (w/w) of etofenamate for topical administration with anti-inflammatory activity and enhanced drug delivery. The physical and chemical characterization, in vitro release and permeation studies and in vivo anti-inflammatory activity were assessed. The gel with 30% ethanol showed in vivo anti-inflammatory activity with suitable physical chemical and microbiologic characteristics. In vitro release and permeation studies revealed that the different amounts of ethanol used influenced the release profiles of etofenamate. Moreover, it was demonstrated that this formulation is an adequate vehicle for the etofenamate skin permeation.     

Repetitive Endoscopy and Continuous Alkaline Gastric Irrigation in a Case of Arsenic Poisoning

Background: The poor prognosis of patients with persistent gastrointestinal radio-opacities after oral arsenic poisoning supports efficient gastrointestinal decontamination as critical for survival. In a case of massive arsenic ingestion, we performed repetitive gastric endoscopy and a continuous alkaline irrigation of the stomach over several days.Case Report: A 41-year-old woman was admitted 4 hours after intentional ingestion of trivalent arsenic powder 5 g. The admission abdominal X-ray confirmed the presence of multiple gastric opacities. Initial treatment was gastric lavage with normal saline, dimercaprol chelation, and supportive therapy. Since gastric opacities persisted on the abdominal X-ray at 34 hours despite repeated gastric lavage, a gastroscopy was performed showing nonremovable agglomerates. In an attempt to achieve further gastric decontamination, we performed a continuous gastric alkaline irrigation. After 3 days of alkaline irrigation, the abdomen was normal on X-ray but the gastroscopy still showed arsenic concretions. Alkaline irrigation was continued for another 3 days until total disappearance of arsenic agglomerates at the gastroscopy. Admission urinary arsenic was 3663 μgmg/L. A total of 46.2-mg of inorganic arsenic, or less than 1% the ingested dose, was extracted from the stomach by this technique. The patient was discharged from the intensive care unit 20 days after admission without sequelae.     

综合疗法治疗膝关节骨性关节炎的疗效观察

目的 观察综合疗法治疗膝关节骨性关节炎的疗效.方法 120例膝关节骨性关节炎患者,随机分为口服盐酸氨基葡萄糖组（A组）和综合采用依托芬那酯凝胶膝部外用、微波理疗、运动疗法配合口服氨基葡萄糖等方法 治疗组（B组）.A组口服盐酸氨基葡萄糖,0.75g/次,2次/d,疗程6周;B组口服盐酸氨基葡萄糖,0.75g/次,2次/d,疗程6周,同时用依托芬那酯凝胶膝部外用,3次,d,疗程10d、膝部微波理疗,2次/d,疗程10d、运动疗法,2次/d,疗程2个月.结果 治疗2周后A组优0例,良16例,优良率26.7%;B组60例优6例,良27例,优良率55.0%.随访3个月后A组优2例,良23例,优良率41.7%;B组优9例.良31例,优良率66.7%.结论 综合疗法治疗膝关节骨性关节炎安全有效,疗效明显优于单纯口服盐酸氨基葡萄糖.     

依托芬那酯凝胶治疗腱鞘炎超声引导下微创术后临床观察

目的评价依托芬那酯凝胶治疗腱鞘炎在超声引导下微创术后肿痛的有效性和安全性。方法采用随机、对照的设计,将2011年5月-2012年7月,在四川省人民医院门诊接受腱鞘炎超声引导微创术后的患者157例,分为两组,治疗组（n=81）采用依托芬那酯凝胶外用,对照组（n=76）不使用外用药物。结果两组治疗后24h及3d的疼痛评分、压痛及关节功能缓解率与治疗前自身比较及组间比较,差别均有统计学意义（P〈0．05）,7d时治疗组临床总有效率为90．12％,对照组为89．47％,组间比较无统计学意义（P〉0．05）,治疗组在使用应急药物上明显优于对照组。两组安全性评价比较差异无统计学意义（P〉0．05）。结论依托芬那酯凝胶能快速、有效、安全地缓解腱鞘炎超声引导微创术后局部肿胀疼痛的症状。     

超短波、超声依托芬那酯药物透入治疗颞下颌关节紊乱病疗效观察68例

目的探讨超短波、超声依托芬那酯药物透入治疗颞下颌关节紊乱病(TMD)的疗效。方法将68例TMD患者分为治疗组和对照组,对照组给予吲哚美辛25mg3次/d,治疗组在此基础上加用超短波与超声依托芬那酯药物透入。结果经过1个疗程的治疗后,治疗组的痊愈率为47.06%,显效率为91.18%;对照组痊愈率为11.76%,显效率为44.12%。结论超短波、超声依托芬那酯药物透入对治疗颞下颌关节紊乱病有良好疗效。     

依托芬那酯凝胶治疗双膝骨性关节炎疗效观察

目的：评价依托芬那酯凝胶治疗膝骨性关节炎患者的疗效和安全性。方法80例符合美国风湿病学院（ACR）膝骨性关节炎标准的患者纳入随机、塞来昔布对照组、双模拟研究,塞来昔布组200mg/d,局部依托芬那酯凝胶外用3次/d,治疗4周。结果经4周治疗后,治疗组的疗效指标[骨关节炎指数（62.4±13.9）、10米步行时间（9.1±0.9）、起立-行走计时测试（10.9±0.7）]均较治疗前明显改善（P<0.05）。结论应用依托芬那酯凝胶治疗膝骨性关节炎疗效与塞来昔布基本相当,而且依托芬那酯凝胶的作用更安全,无严重不良发生,安全性好。