Springer, Private Bag 65901, Mairangi Bay 0754, Auckland, New Zealand.
Drugs. 2016 Aug;76(12):1213-20. doi: 10.1007/s40265-016-0619-7.
An intravenous bolus formulation of the non-steroidal anti-inflammatory drug diclofenac sodium has been developed using hydroxypropyl-β-cyclodextrin (HPβCD) as a solubility enhancer. HPβCD diclofenac (Dyloject(TM)) is available for use in adults in the USA for the management of mild to moderate pain, and as monotherapy or in combination with opioid analgesics for the management of moderate to severe pain. In two multicentre, phase III studies in adults with acute moderate to severe postoperative pain, HPβCD diclofenac significantly reduced pain intensity and the need for rescue medication compared with placebo. In these studies, the tolerability profile of HPβCD diclofenac was generally similar to that of placebo and adverse events were mostly mild to moderate in severity. Constipation, infusion-site pain and dizziness were the most frequently reported adverse reactions occurring numerically more frequently with HPβCD diclofenac than placebo. Therapy with HPβCD diclofenac does not appear to be associated with an increased risk of cardiovascular, renal or bleeding-related adverse events versus placebo. Thus, HPβCD diclofenac extends the treatment options currently available for the management of moderate to severe postoperative pain in adults.
一种非甾体抗炎药双氯芬酸钠的静脉推注制剂已经开发出来，使用羟丙基-β-环糊精（HPβCD）作为增溶剂。HPβCD 双氯芬酸钠（Dyloject（TM））已在美国获准用于成人轻度至中度疼痛的治疗，以及作为单药治疗或与阿片类镇痛药联合用于治疗中度至重度疼痛。在两项针对成人急性中重度术后疼痛的多中心、III 期研究中，与安慰剂相比，HPβCD 双氯芬酸钠显著降低了疼痛强度和需要抢救药物的需求。在这些研究中，HPβCD 双氯芬酸钠的耐受性与安慰剂相似，大多数不良反应的严重程度为轻度至中度。便秘、输注部位疼痛和头晕是最常报告的不良反应，与安慰剂相比，HPβCD 双氯芬酸钠发生的频率更高。与安慰剂相比，HPβCD 双氯芬酸钠治疗似乎不会增加心血管、肾脏或出血相关不良事件的风险。因此，HPβCD 双氯芬酸钠扩展了目前可用于治疗成人中重度术后疼痛的治疗选择。
