Dogrul Ahmet, Arslan Seyda Akkus, Tirnaksiz Figen
Department of Medical Pharmacology, Gülhane Military Academy of Medicine (GATA) , Ankara , Turkey and.
J Microencapsul. 2014;31(5):448-60. doi: 10.3109/02652048.2013.879926. Epub 2014 Apr 3.
The purpose of this study was to develop a water/oil microemulsion containing lidocaine hydrochloride (4%) and to compare its local anaesthetic efficacy with commercial products. A pseudoternary diagram (Km:1/1 or 1/2) was constructed using lecithin/ethanol/oil/water. The droplet size, viscosity and release of the microemulsions were evaluated. Tail flick tests were conducted for in vivo effectiveness; the initiation time of effect, maximum effect, time to reach maximum effect, and relative efficacy were evaluated. The drug caused a significant increase in droplet size. The use of olive oil resulted in a decrease in the solubilisation parameter, as well as a reduction in the release. The droplet size and viscosity of the microemulsion composed of Miglyol/lecithin/ethanol/water/drug (Km:1/2) was lower than other microemulsions (8.38 nm, 6.9 mPa), and its release rate (1.61 mg/h) was higher. This system had a faster and more efficient anaesthetic effect than the other microemulsions and commercial products. Results indicate that a water/oil type microemulsion (Miglyol/lecithin/ethanol/water) has promising potential to increase the local anaesthetic effect.
本研究的目的是开发一种含有4%盐酸利多卡因的水/油微乳剂，并将其局部麻醉效果与市售产品进行比较。使用卵磷脂/乙醇/油/水构建了拟三元相图（Km:1/1或1/2）。对微乳剂的粒径、粘度和释放情况进行了评估。进行了甩尾试验以评估体内有效性；评估了起效时间、最大效应、达到最大效应的时间和相对疗效。药物导致粒径显著增加。使用橄榄油导致增溶参数降低，同时释放减少。由Miglyol/卵磷脂/乙醇/水/药物组成的微乳剂（Km:1/2）的粒径和粘度低于其他微乳剂（8.38 nm，6.9 mPa），其释放速率（1.61 mg/h）更高。该体系比其他微乳剂和市售产品具有更快、更有效的麻醉效果。结果表明，水/油型微乳剂（Miglyol/卵磷脂/乙醇/水）具有增强局部麻醉效果的潜在前景。
