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目的:建立线性探针测定阿魏酸皮下浓度方法,考察温度、灌流液流速、浓度对线性探针回收率的影响,研究阿魏酸溶液经皮给药后体内药动学。方法:采用减量法测定阿魏酸线性探针的体内外回收率的稳定性,采用增量法测定体外回收率的影响因素,选择CD-1裸鼠作为实验动物,采用经皮微透析法进行体内药动学研究,HPLC测定透析液中阿魏酸的浓度。结果:温度对阿魏酸体外回收率有显著性影响,随着温度的升高,阿魏酸的体外回收率显著提高,随着流速的增加阿魏酸的体外回收率呈指数下降,在测定范围内,浓度对阿魏酸的体内外回收率无影响,在测定时间内阿魏酸体内外回收率稳定性、重复性良好,体外平均回收率为(24.82±1.01)%;体内平均回收率为(16.50±1.92)%;经皮给药后,阿魏酸86 min达到峰值,平均滞留时间为291 min。结论:线性探针可用于阿魏酸经皮给药的研究;阿魏酸可迅速透过角质层,适宜制成经皮给药制剂。
OBJECTIVE: To establish a method for determining the subcutaneous concentration of ferulic acid by linear probe, investigate the effects of temperature, perfusate flow rate and concentration on the recovery of linear probe, and study the pharmacokinetics of ferulic acid solution after transdermal administration. Methods: The stability of the linear probe of ferulic acid in vitro and in vivo was determined by subtractive method. The factors influencing the rate of recovery in vitro were determined by incremental method. CD-1 nude mice were selected as experimental animals and the percutaneous microdialysis Pharmacokinetic studies were performed in vivo and the concentration of ferulic acid in the dialysate was determined by HPLC. Results: The temperature had a significant effect on the recovery of ferulic acid in vitro. The recovery of ferulic acid was significantly increased with the increase of temperature. The recovery of ferulic acid decreased exponentially with the increase of flow rate. Within the range, the concentration of ferulic acid in vitro and in vivo recovery has no effect on the determination of ferulic acid recovery in vitro and in vivo stability and repeatability, the average recovery was (24.82 ± 1.01)%; average recovery rate (16.50 ± 1.92)%. After transdermal administration, ferulic acid peaked at 86 min with an average retention time of 291 min. Conclusion: The linear probe can be used for the study of transdermal administration of ferulic acid. Ferulic acid can rapidly penetrate the stratum corneum and is suitable for transdermal drug delivery.