Tringali Giuseppe, Navarra Pierluigi
Institute of Pharmacology, Catholic University Medical School, Rome, Italy.
Evid Based Complement Alternat Med. 2017;2017:8321325. doi: 10.1155/2017/8321325. Epub 2017 Apr 10.
Because of low injection volume, the recently marketed injectable solution of diclofenac in complex with -cyclodextrin (Akis®, IBSA Farmaceutici Italia) is an ideal candidate for mesotherapy applications. In this study, we investigated the solubility of Akis, 25 and 50 mg/kg, in combination with various local anaesthetics (lidocaine, mepivacaine, bupivacaine, levobupivacaine, and ropivacaine) at different concentrations in aqueous vehicles (normal saline, sterile water, or bicarbonate). Final injection mixtures were classified as limpid, turbid, or milky at visual analysis under standardized conditions. We found that (i) the use of sterile water for injections or normal saline as vehicles to dilute Akis in combination with whatever local anaesthetic normally results in milky solutions and therefore is not recommended; (ii) using bicarbonate, optimal solubility was obtained combining Akis with lidocaine, both 1 and 2%, or mepivacaine, both 1 and 2%, whereas solutions were turbid in combination with bupivacaine, levobupivacaine, or ropivacaine. Thus, we recommend that Akis is used in combination with lidocaine or mepivacaine in a bicarbonate vehicle.
由于注射体积小，近期上市的双氯芬酸与β-环糊精的复方注射溶液（Akis®，意大利IBSA制药公司）是中胚层疗法应用的理想选择。在本研究中，我们研究了Akis在25和50mg/kg剂量下，与不同浓度的各种局部麻醉剂（利多卡因、甲哌卡因、布比卡因、左旋布比卡因和罗哌卡因）在水性载体（生理盐水、无菌水或碳酸氢盐）中的溶解度。在标准化条件下进行目视分析时，最终注射混合物分为澄清、浑浊或乳状。我们发现：（i）使用注射用无菌水或生理盐水作为载体来稀释Akis与任何局部麻醉剂的组合，通常会产生乳状溶液，因此不建议使用；（ii）使用碳酸氢盐时，将Akis与1%和2%的利多卡因或1%和2%的甲哌卡因组合可获得最佳溶解度，而与布比卡因、左旋布比卡因或罗哌卡因组合时溶液会浑浊。因此，我们建议在碳酸氢盐载体中，将Akis与利多卡因或甲哌卡因联合使用。
