Zhang Lijing, Xie Jiao, Liu Cheng, Sun Yinghua, Zhang Peng
Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang, China.
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China.
Chirality. 2022 Jun;34(6):894-900. doi: 10.1002/chir.23441. Epub 2022 Apr 12.
Flurbiprofen is clinically effective for the treatment of acute or long-term rheumatoid arthritis and osteoarthritis. Studies showed that S-flurbiprofen had better anti-inflammatory effect than R-flurbiprofen. As flurbiprofen racemates are usually used in the form of transdermal preparations, such as Flurbiprofen Cataplasms (Zepolas), it is of great significance to investigate the percutaneous permeation profiles of flurbiprofen enantiomers for considering whether it is necessary to develop the transdermal preparation with single optical enantiomer. Taking the economy into consideration, the flurbiprofen enantiomers as the mode drug and the CHIRALPAKAAGP column we had as instrument were used to perform the following experiments. On the basis of experiences provided by predecessors, we made some improvements to the analytical conditions, and method validation was developed to verify the feasibility of the method. The results showed that the established method could be used to analyze the percutaneous permeation profiles of flurbiprofen enantiomers in the flurbiprofen cataplasms accurately and effectively, and the percutaneous permeation profiles of flurbiprofen enantiomers had no significantly difference no matter under what conditions (P > 0.05).
氟比洛芬在临床上对治疗急性或长期类风湿性关节炎和骨关节炎有效。研究表明，S-氟比洛芬的抗炎效果优于R-氟比洛芬。由于氟比洛芬外消旋体通常以透皮制剂的形式使用，如氟比洛芬巴布膏（泽普思），研究氟比洛芬对映体的经皮渗透情况对于考虑是否有必要开发单一光学对映体的透皮制剂具有重要意义。考虑到经济性，以氟比洛芬对映体为模型药物，以我们拥有的CHIRALPAK AAGP柱为仪器进行以下实验。在前人提供的经验基础上，我们对分析条件进行了一些改进，并开展了方法验证以验证该方法的可行性。结果表明，所建立的方法能够准确、有效地分析氟比洛芬巴布膏中氟比洛芬对映体的经皮渗透情况，且无论在何种条件下氟比洛芬对映体的经皮渗透情况均无显著差异（P＞0.05）。
