Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Rangsit University, Muang, Pathum Thani, 12000, Thailand.
Pharmaceutical Laboratory Service Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla, 90112, Thailand.
AAPS PharmSciTech. 2019 Oct 24;20(8):322. doi: 10.1208/s12249-019-1545-2.
The objectives of this work were to prepare a 5 wt% lidocaine-diclofenac ionic liquid drug-loaded gelatin/poly(vinyl alcohol) transdermal patch using a freeze/thaw method and to evaluate its physicochemical properties, in vitro release of lidocaine and diclofenac, and stability test. The lidocaine-diclofenac ionic liquid drug was produced by the ion pair reaction between the hydrochloride salts of lidocaine and the sodium salts of diclofenac. The thermal properties of the final drug product were significantly changed from the primary drugs. The ionic liquid drug could be dissolved in water and mixed in a polymer solution. The resulting transdermal patch was then exposed to 10 cycles of freezing and thawing preparation at - 20°C for 8 h and at 25°C for 4 h, respectively. As a result, it was found that the lidocaine-diclofenac ionic liquid drug-loaded transdermal patch showed good physicochemical properties and could feasibly be used in pharmaceutical applications. The lidocaine-diclofenac ionic liquid drug was not affected by the properties of the transdermal patch due to the lack of chemical interaction between polymer base and drug. The high drug release values of both lidocaine and diclofenac were controlled by the gelatin/poly(vinyl alcohol) transdermal patch. The patch showed good stability over the study period of 3 months when kept at 4°C or under ambient temperature.
本工作的目的是采用冻融法制备 5wt%盐酸利多卡因-双氯芬酸钠离子液体载药明胶/聚乙烯醇经皮贴剂，并对其理化性质、盐酸利多卡因和双氯芬酸钠的体外释放以及稳定性试验进行评价。盐酸利多卡因-双氯芬酸钠离子液体药物是由盐酸利多卡因和双氯芬酸钠的钠盐之间的离子对反应产生的。最终药物产品的热性能与原药相比有明显变化。离子液体药物可溶于水并混入聚合物溶液中。所得经皮贴剂随后在-20°C下分别经历 10 个冷冻和解冻循环（8 h）和在 25°C下经历 4 个冷冻和解冻循环（4 h）。结果表明，盐酸利多卡因-双氯芬酸钠离子液体载药经皮贴剂具有良好的理化性质，可实际用于药物应用。由于聚合物基质与药物之间缺乏化学相互作用，离子液体药物中的盐酸利多卡因和双氯芬酸钠不受经皮贴剂性质的影响。高药物释放值的盐酸利多卡因和双氯芬酸钠均由明胶/聚乙烯醇经皮贴剂控制。在 4°C 或室温下保存时，该贴剂在 3 个月的研究期间表现出良好的稳定性。
