布洛芬混悬液治疗小儿发热的疗效和安全性研究

发热症状是儿科最为常见的一种症状之一,它能很大程度上影响小儿的正常身心健康,严重者会对小儿中枢神经系统造成较大的危害[1]。因此,引起普遍关注,对其及时进行科学、合理地治疗,有利于病情的缓解以及尽快使患儿恢复至健康的状况。目前,临床上使用较多的是布洛芬混悬液治疗小儿发热症状[2],能够有效地缓解小儿发热症状。本文将我院200例具有发热症状患儿临床资料进行回顾性分析,报告如下。     

布洛芬控释片的药理作用及临床应用

布洛芬控释片(芬尼康)是将非甾体解热抗炎镇痛药布洛芬制成的控释片。本文就其药理作用及临床应用作一概述。 1 药效学 该药抗炎、镇痛作用机制是通过与体内的环氧化酶催化部位以疏水键形式结合从而抑制环氧化酶,阻止其与花生四烯酸作用产生与炎症有关的前列腺素,从而达到抗炎止痛作用。适用于消除或减轻骨骼-肌肉系统疾病引起的疼痛或炎症等。     

布洛芬控释片的药理作用及临床应用

布洛芬控释片(芬尼康)是将非甾体解热抗炎镇痛药布洛芬制成的控释片.本文就其药理作用及临床应用作一概述.1 药效学该药抗炎、镇痛作用机制是通过与体内的环氧化酶催化部位以疏水键形式结合从而抑制环氧化酶,阻止其与花生四烯酸作用产生与炎症有关的前列腺素,从而达到抗炎止痛作用.适用于消除或减轻骨骼-肌肉系统疾病引起的疼痛或炎症等.     

布洛芬静脉注射制剂的开发与临床应用

非甾体类解热镇痛药大多为口服制剂,在口服困难的患者中存在很大的缺陷,2009年美国FDA首次批准上市了首个治疗疼痛和发热的布洛芬静脉注射制剂。本文介绍了布洛芬注射液的制剂开发、药理学、药动学、临床应用、不良反应以及与其他药物的相互作用等,供临床参考,以促进临床安全合理用药。     

布洛芬不同给药途径治疗小儿发热的疗效观察

目的探讨布洛芬不同的给药途径对小儿发热进行治疗的临床疗效。方法选取我院在2012年6月至2013年6月期间收治的128例发热患儿,其体温均高于38．5℃,伴有急性呼吸道感染,并随机将患者分为三组,分别为灌肠组、口服组以及肛塞组,然后观察和对比三组患者的降温效果。结果三组患者的降温有效率以及显效率之间没有显著的差异（P〉0．05）,三组患者在0．5h、1h、2h的降温效果没有显著的差异（P〉0．05）,在4h时,三组降温效果之间的差异具有统计学意义（P〈0．05）。结论在实际的治疗过程中,应该根据患几的情况选择适宜的给药途径,布洛芬进行肛塞的降温效果较好,临床疗效比较满意,而且给药方便,没有明显的不良反应,值得在临床上进行推广。     

布洛芬-壳聚糖缓释微囊药代动力学研究

目的研究自制布洛芬壳-聚糖微囊的药代动力学。方法以市售布洛芬普通片剂为参比通过高效液相色谱测定模型动物家兔药时曲线。结果相对于普通片剂,兔口服布洛芬-壳聚糖微囊后,达峰时间明显推迟,且达峰浓度降低（P〈0.05）;同时药物在兔体内平均驻留时间明显长于普通片（P〈0.05）;但两制剂的AUC无差异（P〉0.05）。结论研制的布洛芬-壳聚糖微囊具有较好的缓释效果,且吸收程度与普通布洛芬片剂等效。     

布洛芬精氨酸注射及口服给药在大鼠体内的立体选择性药代动力学

利用手性高效液相色谱法研究大鼠注射及口服布洛芬精氨酸之后布洛芬对映体的药代动力学。布洛芬精氨酸注射及口服给药后, 布洛芬对映体的药代动力学呈现立体选择性, 且口服给药后立体选择性程度更高。与系统前转化相比, R-布洛芬至S-布洛芬的系统转化在口服给药后立体选择性药代动力学中起更重要的作用。布洛芬精氨酸口服给药后, 优势对映体S-布洛芬迅速吸收, S-布洛芬与R-布洛芬的绝对生物利用度分别为100% 和80%。基于研究发现的S-布洛芬体内系统性暴露, 可以推断布洛芬精氨酸注射及口服给药后的药理作用相似, 仅在作用的起始阶段存在差异。     

Osteoarthritis of the knee and hip. Part II: therapy with ibuprofen and a review of clinical trials

Objectives We review the pharmacological properties and clinical evidence pertaining to the efficacy of ibuprofen as a first‐line treatment in hip and knee osteoarthritis (OA). In the context of our previous paper's exploration of the aetiology and pathogenesis of OA as a basis for pharmacotherapy, we discuss the pharmacokinetics (PK) and clinical pharmacodynamics (PD) of ibuprofen relevant to OA. Key findings Although widely used, the benefits and risks of ibuprofen, especially compared with other non‐steroidal anti‐inflammatory drugs (NSAIDs) and placebo, have only recently been evaluated in OA of the hip and knee in randomized‐controlled clinical trials (RCT). The efficacy and occurrence of adverse reactions from ibuprofen was compared with placebo in a structural review of the literature and systematic review of RCTs in large‐scale clinical trials. Ibuprofen has been found to result in approximately 50–60% improvement over placebo in WOMAC scores, including those reflecting inflammatory joint pain in knee and hip OA or other indices of pain, disability and impaired function. Mega‐trials performed in comparison with the newer NSAIDs, the coxibs, have shown that ibuprofen has comparable therapeutic benefits and although serious gastrointestinal conditions are sometimes more frequent after short‐term treatment, longer‐term (several months) therapy in OA reduces the advantages of the coxibs over other NSAIDs including ibuprofen. Cardiovascular risk, though present with coxibs and some NSAIDs in OA, is lower or slightly so with ibuprofen compared with coxibs. Summary Ibuprofen is effective and relatively safe (especially at low over‐the‐counter doses and in the short term) for mild‐to‐moderate OA of the knee and hip. The PK properties of ibuprofen in OA (short plasma t½) confer advantages of this drug for OA, while evidence for clinically relevant PD benefits in joints of patients with OA, though limited, is suggestive of local anti‐inflammatory activity.     

RP-HPLC法同时测定血浆中布洛芬丁香酚酯和布洛芬的含量

目的建立测定血浆中布洛芬丁香酚酯及布洛芬含量的HPLC方法,并应用于药物动力学研究。方法采用RP-HPLC法。色谱柱:ODS色谱柱;流动相:乙腈-甲醇-体积分数为0.2%的三氟乙酸-四氢呋喃(体积比为50∶10∶15∶2);流速:1.0 mL.min-1;检测波长:230 nm;室温测定。布洛芬、内标甘草次酸、布洛芬丁香酚酯的保留时间分别为5.62、15.981、8.05 min。结果布洛芬和布洛芬丁香酚酯的的线性范围分别为0.64~64μg.L-1和0.8~80μg.L-1;最低检测限分别为0.64 mg.L-1和0.16 mg.L-1,日内和日间变异系数小于10%,精密度大于90%。结论该方法灵敏、快速、准确,操作简便、线性范围宽,可适用于同时测定血浆中布洛芬丁香酚酯和布洛芬的含量。     

PR-HPLC法同时测定血浆中布洛芬丁香酚酯和 布洛芬的含量

目的 建立测定血浆中布洛芬丁香酚酯及布洛芬含量的HPLC方法，并应用于药物动力学研究。 方法 采用RP-HPLC法。色谱柱:ODS色谱柱；流动相：乙腈-甲醇-体积分数为0.2%的三氟乙酸-四氢呋喃(体积比为50∶10∶15∶2)；流速：1.0 mL•min-1；检测波长：230 nm；室温测定。布洛芬、内标甘草次酸、布洛芬丁香酚酯的保留时间分别为5.62、15.98、18.05 min。结果 布洛芬和布洛芬丁香酚酯的的线性范围分别为0.64～64 μg•L-1和0.8～80 μg•L-1；最低检测限分别为0.64 mg•L-1和0.16 mg•L-1，日内和日间变异系数小于10%，精密度大于90%。结论 该方法灵敏、快速、准确，操作简便、线性范围宽，可适用于同时测定血浆中布洛芬丁香酚酯和布洛芬的含量。     

精氨酸布洛芬糖浆与布洛芬片剂人体药动学及生物等效性比较

目的:比较精氨酸布洛芬糖浆与布洛芬片在健康人体中的药动学及生物等效性。方法:采用液相色谱法测定18位健康男性受试者交叉服用精氨酸布洛芬糖浆和布洛芬片后的血浆中布洛芬浓度。结果:糖浆剂的药动学参数为:AUC_(0-10)=(150±s 17)mg·h·L~(-1),C_(max)=(47±9)mg·L~(-1),t_(max)=(0．6±0．3)h;布洛芬片剂的药动学参数为:AUC_(0-10)=(136±13)mg·L~(-1),c_(max)=(28±4)mg·L~(-1),t_(max)=(2．7±1．0)h,相对生物利用度为 (98±7)％。结论:精氨酸布洛芬糖浆和布洛芬片生物等效。     

心血管疾病新药阿齐沙坦酯的药理与临床评价

阿齐沙坦酯(azilsartan medoxomil)是一种血管紧张素II受体拮抗剂,用于治疗高血压,可与其他抗高血压药物联用。本文参照美国FDA有关该药的申报资料,对其药理作用、药代动力学、临床评价、安全性评价及药物相互作用等进行综述。     

抗惊厥新药依佐加滨的药理与临床评价

依佐加滨是首个治疗癫痫的神经元钾离子通道开放剂,已于2011年6月13日被美国FDA批准用于成人惊厥部分发作的治疗。其作用机制并未完全阐明,可能是通过稳定神经元钾离子通道使其保持"开放"状态,降低其兴奋性而产生抗惊厥作用。其常见的不良反应有眩晕、嗜睡、乏力、意识错乱等。本文对依佐加滨的药理作用、药代动力学、药物相互作用、临床评价和安全性等进行介绍。     

Pharmacokinetics of intravenous ibuprofen: implications of time of infusion in the treatment of pain and fever

Intravenous NSAIDs are playing an increasingly large role in analgesia, anti-inflammation and antipyresis in the hospitalized setting. For many years, ketorolac was the only intravenous NSAID available in the US, but in 2009 intravenous ibuprofen was approved by the US FDA for the treatment of pain and fever in adults. In developing intravenous ibuprofen, a range of times of infusion and dosing levels have been utilized and compared with the oral route of administration. The earliest studies utilized a 60-minute infusion, and later a 30-minute infusion was used for the pivotal/registration studies demonstrating efficacy and safety. Another recent trial in healthy volunteers demonstrated a safe and tolerable rapid infusion (5-7 minute) of intravenous ibuprofen. The pharmacokinetic data from all of the clinical trials on 400 and 800?mg doses of intravenous ibuprofen were compiled, and pharmacokinetic modelling was utilized to simulate any data not acquired in the clinical studies. The pharmacokinetic profile of the following doses was modelled: 30-minute infusion of 800?mg intravenous ibuprofen, 5- to 7-minute infusion of 400?mg intravenous ibuprofen and 400?mg ibuprofen oral tablet. These pharmacokinetic analyses revealed that, in general, maximum plasma concentration (C(max)) decreases considerably as the length of the infusion increases and that an oral dose is not able to achieve the C(max) level of any intravenous dose. For the rapid infusion, C(max) was twice that of the oral dose and, as expected, time to C(max) (t(max)) was much more rapid than with the oral dose. However, the oral dose still maintained virtually 100% oral bioavailability. The efficacy of intravenous ibuprofen in terms of pain and fever has also been studied and this review found the drug to be efficacious for both indications. Future areas of study should include assessment of the analgesic and antipyretic efficacy of a rapid (5- to 10-minute) infusion and further assessment of pre-emptive administration of intravenous ibuprofen as part of a multimodal analgesic approach in the surgical setting.