Blair Hannah A, Plosker Greg L
Springer, Private Bag 65901, Mairangi Bay 0754, Auckland, New Zealand,
Clin Drug Investig. 2015 Jun;35(6):397-404. doi: 10.1007/s40261-015-0294-6.
A novel formulation of diclofenac sodium suitable for subcutaneous or intramuscular injection (Akis(®), Dicloin(®)) has been developed using the complexing agent hydroxypropyl-β-cyclodextrin (HPβCD) as a solubility enhancer. Diclofenac HPβCD is available in several European countries, where it is indicated for use in adults with acute forms of pain, including postoperative pain. Clinical trials have demonstrated the analgesic efficacy of diclofenac HPβCD in terms of relieving moderate to severe postoperative pain in patients undergoing dental surgery or minor orthopaedic surgery. Subcutaneous diclofenac HPβCD also effectively relieved moderate to severe neuropathic pain, related to cancer or not. Diclofenac HPβCD was generally well tolerated in clinical trials, with injection-site reactions among the most commonly reported adverse events. The local tolerability of diclofenac HPβCD was consistently rated as 'good' or 'excellent' across all studies. Subcutaneous administration of diclofenac is a valid alternative to intramuscular delivery, with the advantages of easier administration, the availability of additional body sites suitable for injection and the potential for self-administration. Thus, diclofenac HPβCD 25, 50 or 75 mg/mL solution for subcutaneous or intramuscular injection extends the treatment options available for use in the management of pain in adults.
已研发出一种适用于皮下或肌肉注射的双氯芬酸钠新型制剂（Akis(®)、Dicloin(®)），使用络合剂羟丙基-β-环糊精（HPβCD）作为溶解度增强剂。双氯芬酸HPβCD在几个欧洲国家有售，适用于患有急性疼痛（包括术后疼痛）的成人。临床试验已证明双氯芬酸HPβCD在缓解接受牙科手术或小型骨科手术患者的中度至重度术后疼痛方面具有镇痛效果。皮下注射双氯芬酸HPβCD还能有效缓解与癌症相关或无关的中度至重度神经性疼痛。在临床试验中，双氯芬酸HPβCD总体耐受性良好，注射部位反应是最常报告的不良事件之一。在所有研究中，双氯芬酸HPβCD的局部耐受性一直被评为“良好”或“优秀”。皮下注射双氯芬酸是肌肉注射的有效替代方法，具有给药更简便、有更多适合注射的身体部位以及可自我给药的优点。因此，用于皮下或肌肉注射的25、50或75mg/mL双氯芬酸HPβCD溶液扩展了可用于治疗成人疼痛的选择。
