右旋酮洛芬氨丁三醇和酮洛芬双盲对照治疗类风湿关节炎

目的：比较右族酮洛芬氨丁三醇和酮洛芬治疗类风湿关节炎的疗效和安全性。方法：采用随机、双盲、平行对照的方法治疗类风湿关节炎120例。试验组61例予右旋酮洛芬氨丁三醇25mg，po，tid；对照组59例予酮洛芬50mg，po，tid，疗程均为4周。结果：右旋酮洛芬氨丁三醇能明显改善患者的临床症状和体征，治疗有效率63．9％，与对照组(55．9％)相比无显著差异。右旋酮洛芬氨丁三醇的不良反应少量轻微，其中胃不适症状发生率两药相比有显著差异(分别为4．9％和18．6％)。结论：右旋酮洛芬治疗类风湿关节炎疗效与酮洛芬相近，耐受性优于酮洛芬。     

右酮洛芬氨丁三醇对佐剂性关节炎大鼠的治疗作用及胃肠道损伤作用的研究

目的　研究右酮洛芬氨丁三醇 (D KPT)对佐剂性关节炎大鼠的治疗作用及胃肠道损伤作用。方法　采用大鼠佐剂性关节炎模型 ,观察D KPT对佐剂性关节炎大鼠原发和继发性症状的作用以及对前列腺素E2 和胃、十二指肠的影响。结果　D KPT(2 5、5、10mg·kg-1)不仅能抑制佐剂性关节炎大鼠的原发性炎症 ,而且对继发性炎症和多发性关节炎有抑制作用。D KPT(10 -8、10 -7、10 -6 、10 -5、10 -4 mol·L-1)体外对佐剂性关节炎大鼠腹腔巨噬细胞产生过高的PGE2 有抑制作用。D KPT(10mg·kg-1)对胃、十二指肠黏膜有损伤作用 ,但损伤程度小于酮洛芬 (KP) (10mg·kg-1)。结论　D KPT对佐剂性关节炎大鼠有治疗作用 ,同时对胃、十二指肠损伤小于KP。     

右酮洛芬氨丁三醇注射液的人体药动学研究

目的:研究进口右酮洛芬氨丁三醇注射液在中国健康志愿者的人体药动学。方法:采用随机、开放、单剂量和多剂量口服给药的单中心试验方案。12位健康受试者单剂量和多剂量(50mg)静脉滴注右酮洛芬氨丁三醇注射液,采用液-质联用(LC-MS)法测定右酮洛芬氨的血药浓度,利用WinNonLin6.2计算药动学参数。结果:单剂量和多剂量静脉滴注右酮洛芬氨丁三醇的药动学参数为:c_(max)(6.698±1.058)、(5.088±0.525)μg·mL~(-1),t_(1/2)(2.2±0.3)、(2.4±0.7)h,t_(max)(0.5±0.1)、(0.5±0.1)h,AUC(8.043±0.907)、(6.120±0.796)μg·h·mL~(-1)。结论:右酮洛芬氨丁三醇注射液单剂量和多剂量给药的主要药动学参数的差异无统计学意义;右酮洛芬在人体内无明显蓄积。     

右旋酮洛芬氨丁三醇口服致消化道出血1例

患者,男,74岁。因摔伤致腰背部疼痛伴活动受限1周于2015年9月19日14∶28住院治疗。入院诊断:1.胸12椎体压缩性骨折;2.腰椎退行性改变;3.骨质疏松症;4.脑出血术后。既往高血压病史10年余,血压最高160/100mm Hg,间断口服珍菊降压片1片/次,2次/d,目前血压控制尚可。2007年因脑出血住院行手术治疗,术后右侧肢体偏瘫及失语,否认既往有     

右旋酮洛芬氨丁三醇片致过敏性休克1例

<正>1病例介绍患者男,27岁,因包皮完全遮盖龟头27年,于2018年7月30日收入本院泌尿外科。患者出生后即被发现其包皮完全遮盖龟头,因排尿顺畅,一直未予治疗。入院体格检查:体温36.2℃,脉搏76次·min~(-1),呼吸20次·min~(-1),血压110/70 mmHg(1 mmHg=0.133 kPa)。专科情况:阴茎发育正常,包皮过长,     

酮洛芬凝胶配合手法治疗膝骨关节炎的临床研究

目的观察酮洛芬凝胶配合手法治疗膝关节骨关节炎的临床疗效。方法 98例膝关节骨关节炎患者随机分为手法加酮洛芬凝胶组和手法加扶他林组进行治疗,疗程20d。观察治疗前后两组患者病情指标变化、临床疗效。结果两组患者治疗后均获得满意的临床疗效,治疗组显效率为81.63%,有效率为87.76%;对照组显效率为75.51%,有效率为79.59%。2组对比(P<0.05)有统计学意义。结论酮洛芬凝胶配合手法治疗膝骨关节炎疗效确切,不良反应少。     

高效液相色谱法测定右旋酮洛芬氨丁三醇及其对映体的含量

目的建立右旋酮洛芬氨丁三醇及其对映体的含量测定方法。方法采用高效液相色谱(HPLC)法测定,以KR100-5CHI-TBB手性柱(250mm×4.6mm,5μm)为色谱柱,流动相为正己烷-叔丁基甲醚-冰醋酸,流速为1.0mL/min,检测波长为254nm。结果两对映体分离良好,分离度>2.5;方法重现性好,RSD为0.5%。结论所建立的方法快速简便、准确可靠,可用于右旋酮洛芬氨丁三醇及其对映体的含量测定。     

右旋酮洛芬氨丁三醇水凝胶贴剂的制备及体外透皮研究

摘 要 目的：制备右旋酮洛芬氨丁三醇水凝胶贴剂,优化其处方并评价其体外透皮性能。方法: 选择NP 800为水凝胶骨架材料,甘羟铝为交联剂,EDTA为交联剂调节剂,甘油为保湿剂,制备右旋酮洛芬氨丁三醇水凝胶贴剂,以初黏力、持黏力、剥离强度和12 h累积透皮量为评价指标,进行正交优化试验,筛选出最佳处方。用改良的Franz扩散池进行透皮吸收试验,比较氮酮、油酸及薄荷脑对贴剂中右旋酮洛芬氨丁三醇的促渗作用。结果: 优选的最佳处方为：NP 800、甘羟铝、甘油、EDTA的质量百分含量分别为5%、0.3%、25%、0.15%。透皮促进剂对右旋酮洛芬氨丁三醇有透皮作用,其中以3%氮酮的作用最显著,其促渗倍数达3.26倍。结论: 制备的右旋酮洛芬氨丁三醇水凝胶贴剂处方工艺稳定,合理可行。     

鹿川活络胶囊联合酮洛芬治疗膝骨关节炎的临床研究

目的探讨鹿川活络胶囊联合酮洛芬缓释片治疗膝骨关节炎的临床疗效。方法回顾性分析2020年2月—2021年2月在天津市宝坻区人民医院治疗的106例膝骨关节炎患者临床资料,根据用药差别分为对照组和治疗组,每组各53例。对照组患者口服酮洛芬缓释片,75 mg/次,2次/d;治疗组患者在对照组基础上口服鹿川活络胶囊,1.35 g/次,3次/d。两组均经4周治疗进行效果比较。观察两组的临床疗效,比较两组治疗前后相关评分、血清学指标、超声指标的变化情况。结果经治疗,治疗组患者总有效率是98.11%,显著高于对照组的81.13%(P0.05)。经治疗,两组患者Lysholms评分显著升高,但VAS评分、WOMAC评分、ISOA评分及临床症状评分均显著降低(P0.05),治疗后,治疗组相关评分改善优于对照组(P0.05)。经治疗,两组患者髌上囊积液深度、腘窝囊肿范围、滑膜厚度均显著降低,但股骨内外侧髁软骨厚度均显著增加(P0.05);治疗后,治疗组软骨病变情况及滑膜组织改善优于对照组(P0.05)。经治疗,两组血清金属蛋白酶组织抑制因子1(TIMP-1)显著升高,但白细胞介素-1β(IL-1β)、血管内皮生长因子(VEGF)、基质金属蛋白酶-9(MMP-9)、白细胞介素-6(IL-6)均显著降低(P0.05);且治疗后,治疗组炎症介质水平改善优于对照组(P0.05)。结论鹿川活络胶囊联合酮洛芬缓释片治疗膝骨关节炎具有较好的临床疗效,可有效改善患者症状和关节功能,降低炎症介质水平和滑膜组织损伤,有着良好的临床应用价值。     

比较卡前列素氨丁三醇和米索前列醇治疗顽固性产后出血的疗效

目的比较卡前列素氨丁三醇(欣母沛)和米索前列醇治疗顽固性产后出血的疗效。方法选择2008年6月至2010年6月期间84例因顽固性产后出血需要治疗的患者,将其随机分成治疗组和对照组各42例,对照组采用米索前列醇治疗,治疗组采用欣母沛治疗。结果对照组采用米索前列醇治疗后有27例患者顽固性产后出血得到有效控制,治疗组采用欣母沛治疗后有40例患者出血得到有效控制,总有效率分别为64.28%和95.23%。两组比较差异有统计学意义(P<0.05)。结论卡前列素氨丁三醇治疗顽固性产后出血疗效显著。     

A review of dexketoprofen trometamol in acute pain

Objective: Dexketoprofen trometamol is a modified non-selective COX inhibitor with a rapid onset of action that is available as both oral and parenteral formulations. The aim of this narrative review was to assess the efficacy and tolerability/safety of dexketoprofen trometamol in acute pain states using the best available published scientific evidence (randomized controlled clinical trials and systematic reviews/meta-analyses).

Methods: Literature retrieval was performed via Medline, Embase and the Cochrane Library (from inception up to March 2017) using combinations of the terms “randomized controlled trials”, “dexketoprofen”, “celecoxib”, “etoricoxib”, “parecoxib” and “acute pain”.

Results: Single-dose dexketoprofen trometamol provides effective analgesia in the treatment of acute pain, such as postoperative pain (dental and non-dental surgery), renal colic, acute musculoskeletal disorders and dysmenorrhea, and reduces opioid consumption in the postoperative setting. It has a rapid onset of action (within 30?minutes) and is well tolerated during short-term treatment. Direct comparisons with COX-2 inhibitors are lacking; however, the efficacy and tolerability of single-dose dexketoprofen trometamol appears to be consistent with that seen with celecoxib, etoricoxib and parecoxib in the acute pain setting.

Conclusion: In conclusion, dexketoprofen trometamol appears to provide similar analgesic efficacy to COX-2 inhibitors when used to treat acute pain, has a rapid onset of action, is well tolerated, and has an opioid-sparing effect when used as part of a multimodal regimen in the acute pain setting.     

Comparative study of analgesic efficacy and morphine-sparing effect of intramuscular dexketoprofen trometamol with ketoprofen or placebo after major orthopaedic surgery

AIMS: Multimodal analgesia is thought to produce balanced and effective postoperative pain control. A combined therapy with nonsteroidal anti-inflammatory drugs (NSAIDs) and opiates could result in synergistic analgesia by acting through different mechanisms. Currently there are very few parenterally administered NSAIDs suitable for the immediate postoperative period. Therefore, this study was undertaken to assess the analgesic efficacy, relative potency, and safety of parenteral dexketoprofen trometamol following major orthopaedic surgery. METHODS: One hundred and seventy-two patients elected for prosthetic surgery, were randomized to receive two intramuscular injections (12 hourly) of either dexketoprofen 50 mg, ketoprofen 100 mg or placebo in a double-blind fashion. Postoperatively, the patient's pain was stabilized, then they were connected to a patient- controlled analgesia system (PCA) of morphine for 24 h (1 mg with 5 min lockout). RESULTS: The mean cumulative amount of morphine (CAM) used was of 39 mg in the dexketoprofen group and 45 mg in the ketoprofen group vs 64 mg in the placebo group. (Reduction in morphine use was approximately one-third between the active compounds compared with placebo (adjusted mean difference of -25 mg between dexketoprofen and placebo and -23 mg between ketoprofen and placebo. These differences were statistically significant: P 相似文献   

右旋酮洛芬氨丁三醇速释缓释双层片在Beagle犬体内的药物动力学及生物等效性

目的考察右旋酮洛芬氨丁三醇速释缓释双层片与普通制剂在Beagle犬体内的药物动力学特征和生物等效性。方法以自制的右旋酮洛芬氨丁三醇速释缓释双层片作为受试制剂,上市制剂"葵拉兰"作为参比制剂,采用UPLC-MS/MS联用技术,测定受试制剂与参比制剂在Beagle犬体内的血药浓度经时过程,数据经DAS2.0软件处理分析获得药物动力学参数,对AUC0-t、AUC0-∞、ρmax及tmax的对数值进行方差分析、双单侧t检验、非参数检验等统计学处理,评价双层片与普通制剂的生物等效性,利用Loo-Rigelman法评价其体内外相关性。结果与参比制剂相比,受试制剂的ρmax降低,tmax有所延长,体内外相关性中r=0.986 6。结论右旋酮洛芬氨丁三醇速释缓释双层片较参比制剂具有速释和缓释特征,体内吸收与体外释放具有良好的相关性。     

Subeffective doses of dexketoprofen trometamol enhance the potency and duration of fentanyl antinociception

The combination of classic non-steroidal antiinflammatory drugs (NSAIDs) with opiates induces more analgesia than the summed effect of each drug given separately. No studies have been performed using new generation NSAIDs and fentanyl nor on the duration of this effect. We have studied the analgesic effect of fentanyl alone and after the administration of subeffective doses of dexketoprofen trometamol in rat nociceptive responses. The responses were evoked by noxious mechanical stimulation and were recorded as single motor units in male Wistar rats anaesthetized with alpha-chloralose. The effective dose 50 (ED(50)) observed with fentanyl was 22.4 +/- 1.5 microg kg(-1) and full recovery was apparent 20 min later. The administration of a total dose of 40 microg kg(-1) of dexketoprofen trometamol did not induce any significant effect on the nociceptive responses. In the presence of dexketoprofen trometamol, the ED(50) for fentanyl was 5 fold lower than before: 3.8 +/- 1.1 microg kg(-1) and no significant recovery was observed 45 min later. The opioid antagonist naloxone (200 microg kg(-1)) did not reverse the effect, although in control experiments the same dose was able to prevent any action of fentanyl given alone. We conclude that the combination of fentanyl and subeffective doses of dexketoprofen trometamol induces a more potent and longer lasting analgesic effect than that observed with fentanyl alone, and that this is not an opioid mediated action.     

右旋酮洛芬氨丁三醇温敏水凝胶的释放度、稳定性及组织相容性研究

目的 建立右旋酮洛芬氨丁三醇（DKPF）温敏水凝胶的含量测定方法，考察其稳定性和组织相容性。方法 建立紫外分光光度法测定DKPF温敏水凝胶中DKPF含量，并考察方法的专属性、线性关系、定量限、精密度、回收率；应用建立的紫外分光光度法、恒温振荡法测定DKPF温敏水凝胶的释放度，检测高湿、光照、低温条件下的DKPF温敏水凝胶稳定性。随机选取80只昆明小鼠，分别sc 0.2 mL DKPF温敏水凝胶、空白水凝胶、DKPF生理盐水溶液（DKPF浓度同DKPF温敏水凝胶），于给药后1、3、6、9、12 d，每组各取5只脱颈处死，剖开注射部位皮肤观察水凝胶状态，并取皮下组织样本HE染色后光镜下观察，评价DKPF温敏水凝胶组织相容性。结果 DKPF在260 nm处有最大紫外吸收，DKPF质量浓度在1.70~25.56 μg/mL范围内呈良好的线性关系（r=0.999 9），方法学的日间、日内精密度，加样回收率均良好；DKPF温敏水凝胶主要以扩散为主，释放度符合规定，且工艺重现性好；水凝胶在低温、湿度75%条件下稳定性良好，不耐光照，需避光保存。sc给予小鼠水凝胶后，各组小鼠均成活，且水凝胶在皮下逐渐减小直至消失；病理切片结果提示，温敏水凝胶引起轻微炎症反应，随着时间延长逐渐消失，组织相容性良好。结论 本研究所建立的紫外分光光度法方法准确率高，重复性好，可应用于DKPF温敏水凝胶中DKPF含量测定；DKPF温敏水凝胶符合生物材料的安全标准。     

Low doses of nitroparacetamol or dexketoprofen trometamol enhance fentanyl antinociceptive activity

We have reported that subeffective doses of the nonsteroidal anti-inflammatory drug (NSAID) dexketoprofen trometamol enhances micro-opioid receptor agonist fentanyl antinociception. The aim of this study was to assess if this effect can also be observed with other new cyclooxygenase-inhibitors such as nitroparacetamol, and in responses to high intensity electrical stimulation (wind-up). Single motor units were recorded in male Wistar rats under alpha-chloralose anaesthesia. The antinociceptive effect of fentanyl was studied alone and in the presence of subeffective doses of dexketoprofen trometamol or nitroparacetamol. In responses to noxious mechanical stimulation, the potency of fentanyl was enhanced by more than threefold in the presence of the NSAIDs and no significant recovery was observed after 45 min. The opioid antagonist naloxone and the alpha(2)-adrenoceptor antagonist atipamezol did not reverse the effect. The enhancement of the effect of fentanyl in wind-up was lower though significant. We conclude that the co-administration of subeffective doses of new cyclooxygenase-inhibitors and the micro-opioid receptor agonist fentanyl should be considered as a potential pain therapy.