氟比洛芬酯脂微球载体注射液治疗骨性关节炎临床观察

目的观察氟比洛芬酯脂微球载体注射液治疗骨性关节炎(OA)的临床效果。方法80例OA患者随机分为治疗组和对照组,各40例。治疗组应用氟比洛芬酯脂微球载体注射液,对照组应用塞来昔布,观察治疗前、后的疗效及安全性。结果氟比洛芬酯脂微球载体注射液可明显缓解OA的临床症状。结论应用氟比洛芬酯脂微球载体注射液治疗OA疗效明显,无严重不良反应。     

氟比洛芬酯用于乳腺手术患者术后镇痛的临床研究

目的氟比洛芬酯脂微球载体注射液(商品名:凯纷)是一种消炎镇痛作用强、毒副作用小的新一代非甾体抗炎药,用于乳腺手术后镇痛。方法选择ASAI～II级乳腺患者60例,随机双盲分为试验组和对照组,每组30例。试验组患者手术开始时缓慢静脉注射凯纷50 mg;对照组用安慰剂做术后镇痛。术后1 h、3 h、6 h观察并记录SBP、DBP、HR,SpO2、术后疼痛程度的评估采用0～10级线性视觉模拟评分法进行评估,分为无痛(0级),剧烈疼痛(无法控制10级)及药物的不良反应。结果使用凯纷做超前镇痛试验组与对照组各时间术后疼痛VAS评分均有显著性差异(P<0.05)。结论氟比洛芬酯脂微球载体注射液用于乳腺手术的术后镇痛,能有效预防/减轻患者疼痛且不良反应少。     

氟比洛芬酯脂微球注射液对老年癌痛镇痛作用的临床分析

目的观察氟比洛芬酯脂微球载体注射液(商品名凯纷)治疗老年癌痛的疗效和副作用。方法 47例不能耐受阿片类药物或阿片类药物效果不佳的癌性疼痛患在2周的时间内者每天静脉注射50～100 mg氟比洛芬酯脂微球载体注射液,分别就其疗效、生活质量改善情况以及不良反应等方面进行全面评价。结果氟比洛芬酯脂微球载体注射液治疗老年癌痛的有效率为87.23%(PR+CR),生活质量改善情况治疗前后差异有统计学意义(P<0.05)。但未见一般非甾体类药物常见腹痛、消化道出血等副作用;也未见便秘、恶心、呕吐、嗜睡、血压下降等阿片类药物常见不良反应。结论氟比洛芬酩脂微球载体注射液治疗老年癌痛疗效可靠,生活质量可得到改善,氟比洛芬酯脂微球载体注射液不良反应发生率较低,为临床止痛药物的选择提供了一个新途径。     

氟比洛芬酯脂微球注射液的配伍稳定性考察

摘 要 目的：考察氟比洛芬酯脂微球注射液与0.9%氯化钠注射液、5%葡萄糖注射液的配伍稳定性,为临床应用提供理论依据。方法: 测定在25℃避光条件下5 h内氟比洛芬酯脂微球注射液与0.9%氯化钠注射液或5%葡萄糖注射液配伍液的外观、氟比洛芬酯脂微球的粒径及氟比洛芬酯的含量变化;测定氟比洛芬酯脂微球注射液冻融前后与0.9%氯化钠注射液配伍液的外观及氟比洛芬酯脂微球的粒径变化。结果: 在25℃避光条件下放置5 h,各配伍液的外观、粒径和含量无明显变化;氟比洛芬酯脂微球注射液冻融前后的配伍液外观和粒径亦无明显变化。结论:氟比洛芬酯脂微球注射液在0.9%氯化钠注射液、5%葡萄糖注射液中配伍后,5 h内于避光条件下可稳定共存。     

氟比洛芬酯注射液的药理作用及临床应用

氟比洛芬酯注射液是氟比洛芬的脂微球制剂,能有效缓解术后疼痛和癌症疼痛,并且能避免口服制剂的不良反应.概述氟比洛芬酯注射液的药理作用和临床应用.     

氟比洛芬酯注射液对老年癌性疼痛的疗效分析

目的观察氟比洛芬酯脂微球注射液对老年癌性疼痛的疗效和毒副反应。方法对20例未用阿片类药物的老年患者出现癌性疼痛给予氟比洛芬酯脂微球注射液50～100mg/d静脉推注,应用1周以上,评价其疗效以及不良反应。结果氟比洛芬酯脂微球注射液治疗癌性疼痛的有效率（CR＋PR）为70%,生活舒适感得到不同程度的改善,不良反应发生率低,程度轻,未见消化道出血、便秘、尿潴留、嗜睡、返酸、恶心呕吐及呼吸抑制等。结论氟比洛芬酯脂微球注射液治疗老年癌性疼痛效果较理想,不良反应少。     

氟比洛芬酯脂微球注射液的制备及质量研究

目的:制备氟比洛芬酯脂微球注射液。方法:通过正交实验优化筛选得到氟比洛芬酯脂微球的最佳处方和工艺,并研究所得制剂的粒径、p H值、有关物质及含量等性质。结果:确定氟比洛芬酯脂微球注射液的处方组成及工艺为:10%的注射用大豆油、1.2%精制蛋黄卵磷脂、0.5%油酸、2.3%甘油、0.032%磷酸氢二钠、0.03%枸橼酸和95%的注射用水。均质8次,121℃灭菌15 min,灭菌后仍能保持良好的稳定性,制得脂微球注射液氟比洛芬酯的含量为99.45%,最大单一杂质0.085%,其他杂质总和0.23%。结论:该处方工艺可行,制得的脂微球质量可控。     

右酮洛芬胶囊用于镇痛的随机双盲对照临床试验

目的:评价右酮洛芬(dexketoprofen)胶囊的临床镇痛效果和不良反应。方法:采用多中心随机双盲平行对照的方法,以酮洛芬(ketoprofen)胶囊为对照药,用于治疗轻、中度疼痛;1d给药用于治疗痛经,一周给药用于治疗骨科慢性疼痛。以疼痛强度差(PID)、疼痛缓解率(PAR)、有效率等作为镇痛效果判定指标。结果:治疗痛经时,试验组与对照组PID值的差异无统计学意义。用于骨科慢性疼痛时,用药后PID增加,用药4d后PID值基本稳定,试验组与对照组PID值的差异无统计学意义。1d给药和一周给药试验组与对照组的完全缓解率、明显缓解率组间差异均无统计学意义。1d给药和一周给药的试验组与对照组的总有效率都在90%以上;两组总有效率差值的95%置信区间在(-15.0%,15%)等效界值内,表明试验药与对照药等效。不良反应主要有胃不适、恶心等。结论:右酮洛芬为治疗轻、中度疼痛的镇痛药。其不良反应较轻。25mg的右酮洛芬与50mg酮洛芬镇痛效果等效。     

氟比洛芬酯用于小儿唇腭裂修补术镇痛效果观察

术后疼痛是机体受到手术伤害刺激后的生理、心理和行为上的一系列反应,小儿唇腭裂患者术后疼痛可引起应激反应导致小儿生理和心理发生变化,对心身、家庭及社会带来负面影响[1].传统的术后镇痛治疗常以阿片类药物为主,如杜冷丁、吗啡及芬太尼等,但大量使用阿片类药物会引起许多围术期副作用.氟比洛芬酯(Flurbiprofen)是临床上广泛使用的非甾体抗炎药,具有抗炎、止痛及解热作用.氟比洛芬酯微球载体注射液,采用微球载体技术,使药物具有靶向性,起效时间短,持续时间长,静脉注药可以避免消化道局部刺激、呼吸抑制等副作用[2,3].本研究观察了氟比洛芬酯微球载体注射液用于小儿唇腭裂手术患者术后镇痛的效果及安全性.     

临床药师介入氟比洛芬酯超前镇痛对胸腔镜手术患者术后镇痛的疗效分析

<正>氟比洛芬酯注射液(商品名凯纷)是一种以脂微球为载体的具有靶向镇痛作用的非甾体抗炎药NSAIDs,将酯化氟比洛芬封固于脂肪微球,靶向聚集在手术切口,局部高浓度聚集直接抑制前列腺素合成[1];同时升高痛阈,降低神经末梢痛觉传导,减轻中枢敏化[2],在国外多作为手术后的单次镇痛和     

氟比洛芬酯脂微球载体制剂与注射用酮洛芬对照治疗术后及癌性疼痛

目的:观察氟比洛芬酯与酮洛芬对照治疗术后及癌性疼痛患者的有效性.方法:日本36家医院共入选腹部术后患者224例,癌性疼痛患者163例,随机分为氟比洛芬酯组192例与酮洛芬组195例,分别用氟比洛芬酯与酮洛芬安慰剂和酮洛芬与氟比洛芬酯安慰剂.氟比洛芬酯及其安慰剂5mL静脉内注射,酮洛芬及其安慰剂每瓶用2.5mL溶液溶解臀部肌内注射.结果:可评价病例氟比洛芬酯组对术后疼痛111例患者改善率为73.9%,高于酮洛芬组(n=109)的66.1%,但2组差异无显著性(P>0.05);药效持续时间氟比洛芬酯组比酮洛芬组延长(P<0.05).氟比洛芬酯组癌性疼痛(n=77)改善率为77%,高于酮洛芬组(n=81)的59.3% (P>0.05),药效持续时间氟比洛芬酯组比酮洛芬组延长(P<0.05).结论:在治疗术后疼痛和癌性疼痛时,氟比洛芬酯的疗效与酮洛芬相近,但镇痛时间明显延长.     

Analgesic efficacy of acetaminophen 1000 mg, acetaminophen 2000 mg, and the combination of acetaminophen 1000 mg and codeine phosphate 60 mg versus placebo in acute postoperative pain.

Acetaminophen (APAP) 1000 mg, APAP 2000 mg, the combination of APAP 1000 mg plus codeine phosphate 60 mg (APAPCOD), and placebo (PBO) were compared in a 6-hour, randomized, single-dose, double-blind, parallel-group analgesic trial. All active treatments were statistically superior (p less than 0.05) to placebo for 4 hours after medication with respect to pain intensity (PI) and pain intensity difference (PID), and up to 3 hours regarding pain relief (PAR). The combination scored better than all other treatments on the summary analgesic efficacy measures sum PI (SUMPI), sum PID (SPID), and total PAR (TOTPAR). The combination was statistically superior to APAP 1000 mg on SUMPI, TOTPAR and maximum PAR (MAXPAR). Acetaminophen 2000 mg showed marginal numerical superiority over 1000 mg for SUMPI, but was not statistically superior for any summary efficacy measure. The 2000-mg dose was numerically inferior to APAPCOD for every summary efficacy measure and statistically inferior regarding SPID and MAXPAR. We concluded that codeine 60 mg added to acetaminophen 1000 mg offers analgesic advantages, and acetaminophen reaches an analgesic ceiling effect at 1000 mg using the dental pain model.     

Lumiracoxib in the treatment of osteoarthritis, rheumatoid arthritis and acute postoperative dental pain: results of three dose-response studies

OBJECTIVES: Overview of three dose-response studies demonstrating the efficacy of lumiracoxib, a novel COX-2 selective inhibitor, for chronic pain associated with osteoarthritis (0A), or rheumatoid arthritis (RA) and acute pain following dental extraction. METHODS: OA and RA: 4-week, randomized, placebo- and active-controlled studies of similar design. Patients (OA, n = 583; RA, n = 571) received lumiracoxib 50 mg, 100 mg or 200 mg twice daily (bid), lumiracoxib 400 mg once daily (od), diclofenac 75 mg bid or placebo. Dental: 12-h, single-center, randomized, placebo- and active-controlled study. Patients (n = 202) received single oral doses of lumiracoxib 100 mg or 400 mg, ibuprofen 400 mg or placebo. Main outcome measures: OA: pain intensity (PI) in the target joint (visual analogue scale [VAS]) and WOMAC score at Week 4; RA: overall PI (VAS) and ACR20 response at Week 4; Dental: difference (PID, categorical and VAS) score over 12h post dose, time to onset of analgesia. RESULTS: Throughout the OA study, all lumiracoxib doses provided superior reductions in PI versus placebo and at Week 4, all lumiracoxib doses provided efficacy similar to each other and to diclofenac. In the RA study, lumiracoxib 100 mg bid, 200 mg bid and 400mg od were significantly better than placebo in PI at Weeks 1 and 2 (all p < 0.05) but demonstrated borderline significance at Week 4 (lumiracoxib 400 mg od, p = 0.06). In pain following dental surgery, PID scores for both lumiracoxib doses were superior to placebo from 1.5 h onwards and always comparable, or superior, to ibuprofen. Lumiracoxib 400 mg had the fastest onset of analgesia, measured as median time to confirmed first perceptible pain relief using the two-stopwatch method (37.4 min, superiority versus placebo, p < 0.001). Lumiracoxib was well tolerated in all studies. CONCLUSIONS: These studies provide initial evidence that lumiracoxib is an effective, well-tolerated agent for the treatment of chronic and acute pain.     

Dental impaction pain model as a potential tool to evaluate drugs with efficacy in neuropathic pain

Intravenous lidocaine, a nonspecific Na-channel blocker, was used to assess the dental impaction model for evaluation of neuropathic pain drugs. Sixty patients, experiencing moderate or severe pain after removal of > or = 2 third molars, were randomized (2:2:1:1) to lidocaine (4 mg/kg; maximal dose 300 mg), oxycodone/acetaminophen (10/650 mg), placebo, and active placebo (diphenhydramine, 50 mg). Lidocaine provided a modest degree of pain relief. Predefined endpoints of total pain relief and sum of pain intensity at 2, 4, and 6 hours showed numerically, not statistically significantly, greater pain relief versus placebo. A significantly greater effect over placebo was observed in peak effect and at shorter time points (30 minutes and 1 hour), consistent with the pharmacokinetic profile (plasma concentration of approximately 2 mug/mL). Oxycodone/acetaminophen provided significantly greater analgesia versus placebo, validating study conduct, and significantly greater pain relief was observed versus lidocaine, which is consistent with a smaller portion of dental extraction pain being of neuropathic origin.     

氟比洛芬酯在手外科手术镇痛中的应用

目的研究氟比洛芬酯用于手外科手术时超前镇痛的作用效果。方法 80例ASAⅠ～Ⅱ级行手外科手术的患者,随机分为两组,每组40例。Ⅰ组于手术前20min静脉缓慢推注氟比洛芬酯150mg;Ⅱ组于手术前20min静脉缓慢推注生理盐水20mL。分别记录术后1、2、4、6、8h的视觉模拟评分(VAS)。并在治疗结束后统计患者对镇痛疗效的满意度。结果术后1、2、4、6、8hVASⅠ组均低于Ⅱ组(P<0.05),患者对镇痛疗效满意度Ⅰ组和Ⅱ组比较Ⅱ级和Ⅳ级有显着意义(P<0.05)。结论氟比洛芬酯用于手外科手术超前应用,能减少术后的疼痛。     

Diclofenac sodium injection (Dyloject): in postoperative pain

*A new formulation of the nonselective NSAID diclofenac sodium suitable for intravenous bolus injection has been developed using hydroxypropyl beta-cyclodextrin as a solubility enhancer (HPbetaCD diclofenac). * HPbetaCD diclofenac intravenous bolus injection was shown to be bioequivalent to the existing parenteral formulation of diclofenac containing propylene glycol and benzyl alcohol as solubilizers (PG-BA diclofenac), which is relatively insoluble and requires slow intravenous infusion over 30 minutes. * Single-dose HPbetaCD diclofenac 3.75, 9.4, 18.75, 25, 37.5, 50 and 75 mg administered by intravenous bolus injection produced significantly greater responses than placebo for total pain relief (TOTPAR) over 6 hours or pain intensity at 4 hours in the treatment of moderate or severe postoperative dental pain in randomized, double-blind trials. HPbetaCD diclofenac 37.5 and 75 mg were similar in efficacy to intravenous bolus ketorolac 30 mg. * In a well controlled trial, single-dose HPbetaCD diclofenac 75 mg intravenous bolus injection was shown to be superior to PG-BA diclofenac 75 mg intravenous infusion with respect to TOTPAR over 4 hours, indicating faster onset of analgesia in the treatment of moderate or severe postoperative dental pain. Both HPbetaCD diclofenac and PG-BA diclofenac were superior to placebo. * HPbetaCD diclofenac was generally well tolerated during single-dose treatment of postoperative pain. The tolerability profile was similar to that of PG-BA diclofenac, but with a lower incidence of thrombophlebitis.     

An evaluation of flurbiprofen, aspirin, and placebo in postoperative oral surgery pain

One hundred sixty-four outpatients with postoperative pain after the removal of impacted third molars were randomly assigned on a double-blind basis, to receive oral doses of flurbiprofen 25, 50, or 100 mg; aspirin 600 mg; or placebo. Using a self-rating record, subjects rated their pain and its relief hourly for 8 hours after medicating. Estimates of sum of pain differences (SPID), peak pain intensity difference (PID), total relief, peak relief, and hours of 50% relief were derived from these subjective reports. All active medications were significantly superior to placebo. Analgesia was similar for flurbiprofen 25 mg and aspirin 600 mg. Flurbiprofen 50 and 100 mg were significantly superior to aspirin for every measure of analgesia except peak PID. There was a significant dose-response regression between flurbiprofen 25 mg and both of the higher dosages. Flurbiprofen 50 and 100 mg did not differ significantly, suggesting a plateau in flurbiprofen's analgesia. The analgesic effect of flurbiprofen was significant by hour 1 and persisted for 8 hours. The frequency of adverse effects was similar for the active medications.     

酮咯酸氨丁三醇联合盐酸哌替啶治疗肾绞痛的临床观察

目的:观察酮咯酸氨丁三醇联合盐酸哌替啶治疗肾绞痛的临床疗效。方法:将我院2008年5月-2010年5月收治的中、重度疼痛的肾绞痛患者120例随机均分为3组,均采取肌肉注射药物进行镇痛治疗。其中,Ⅰ组应用酮咯酸氨丁三醇60mg;Ⅱ组应用盐酸哌替啶100mg;Ⅲ组应用酮咯酸氨丁三醇30mg+盐酸哌替啶50mg。记录用药前以及用药后3h内(0、0.5、1、1.5、2、2.5、3h)的疼痛强度、疼痛强度差、疼痛缓解度以判断镇痛效果,并观察各组治疗中的不良反应情况。结果:用药后,3组均在0.5h起效,在中度疼痛的镇痛方面,Ⅲ组在用药3h内的所有观察点均优于Ⅰ、Ⅱ组(P<0.05),在2h时差异最为显著(P<0.01);在重度疼痛的镇痛方面,Ⅲ组在用药1.5、2、2.5、3h时效果优于Ⅰ、Ⅱ组(P<0.05);Ⅲ组的中度以上疼痛缓解程度除0.5h外,其余各点与Ⅰ、Ⅱ组比较,差异均有统计学意义(P<0.05)。Ⅲ组不良反应的发生率小于其他2组(P<0.05)。结论:酮咯酸氨丁三醇联合盐酸哌替啶治疗肾绞痛效果显著,同时可减少盐酸哌替啶的使用量,并可延长镇痛时间,且安全性较好。     

口服氨酚待因2号片镇痛效果的临床评价

氨酚待因2号片(PC-2)每片含磷酸可待因15 mg和扑热息痛300 mg,是国内新开发的复方镇痛药。本文采用多中心、随机双盲双模拟平行对照试验设计,对中度疼痛患者进行临床验证,以氨酚待因1号片(PC-1,每片含磷酸可待因8.4 mg和扑热息痛500 mg)作为阳性对照药,阴性对照药用安慰剂(PB)。患者总数338例(206例用PC-2,32例用PC-1,100例用PB)。临床验证结果表明:(1)PC-2组对中等程度的手术后疼痛、中晚期癌痛和某些神经痛均有满意的镇痛效果,其疼痛强度差、疼痛缓解度以及2度以上疼痛缓解率等各项检查指标均明显优于PB组(P<0.01)。PC-2组在服药后2 h的疼痛强度差及服药1 h后的镇痛总有效率均比PC-1组高(P<0.05),对癌症的镇痛效果优于PC-1组;(2)PC-2对术后痛、癌痛和神经痛的总有效率分别为82.5%、76.7%和60.0%,它对鼻咽癌和其它癌症的镇痛效果无明显差别;(3)PC-2 po后吸收迅速,1 h后出现镇痛效应,2 h达峰值,镇痛效应可持续3h;(4)PC-2的不良反应较轻,在进行不良反应观察的50例中,11例出现思睡(占22%),5例胃部不适(占10%),3例头晕(占6%),恶心1例(占2%),上述不良反应大多在1 d内消失,1例在服药第7 d出现便秘,本品对呼吸、心率、血压无影响,对肝、肾、血液系统无损害。     

Ibuprofen and acetaminophen in the relief of postpartum episiotomy pain

A single-dose, double-blind, randomized clinical trial was conducted to examine the relative analgesic efficacy of ibuprofen 400 mg (n = 36), acetaminophen 1000 mg (n = 37), and placebo (n = 38) in postpartum patients who had moderate to severe pain after episiotomy. At regular intervals over 4 hours, patients evaluated pain severity and relief on categorical scales and completed a categorical overall evaluation at the end of the trial. Both active agents were effective compared with placebo (P less than .05). Ibuprofen 400 mg was more effective than acetaminophen 1000 mg for the sum of pain intensity difference, total pain relief, and reduction of pain by more than 50% (P less than .05), suggesting a more rapid onset of action and a more prolonged effect by ibuprofen 400 mg. No adverse effects were reported. Based on the results of this conventional postpartum episiotomy pain model, both agents are considered efficacious and ibuprofen 400 mg is a more effective analgesic for the relief of acute pain than acetaminophen 1000 mg.