坦度螺酮透皮贴剂的制备及评价  

Preparation and evaluation of tandospirone transdermal patches

作　　者：符渝昕 杜卓芳 程泽能 FU Yu-xin;DU Zhuo-fang;CHENG Ze-neng(Xiangya School of Pharmaceutical Sciences,Central South University,Changsha 410000;Hunan Huize Bio-pharmaceutical Co.,Ltd.,Changsha 410000)

机构地区：[1]中南大学湘雅药学院,长沙410000 [2]湖南慧泽生物医药科技有限公司,长沙410000

出　　处：《中南药学》2024年第6期1491-1497,共7页Central South Pharmacy

摘　　要：目的 制备坦度螺酮透皮贴剂并进行体内外评价。方法 合成胆碱-油酸离子液体作为联合促渗剂;通过单因素实验,以外观、累计透过量等为评价指标,筛选优化处方,通过SD大鼠实验研究贴剂药动学特征。结果 坦度螺酮透皮贴剂处方:10%坦度螺酮,7.5%胆碱-油酸,7.5%肉豆蔻酸异丙酯,75%DURO-TAK 4098。24 h单位面积累计渗透量为(309.33±45.98)μg·cm^(-2),稳态透皮速率为(13.43±1.93)μg·cm^(-2)·h^(-1)。SD大鼠实验表明,与坦度螺酮混悬液相比,透皮贴剂具有缓释特征,T_(1/2)延长至(6.37±4.46)h,MRT_(0~t)约提高17倍。结论 坦度螺酮透皮贴剂具有缓释效果,有望成为坦度螺酮新型给药制剂。Objective To prepare tandospirone transdermal patches and evaluate their quality.Methods Synthesized of choline-oleic acid ionic liquid was used as a combined osmotic promoter.The prescriptions were screened and optimized by a one-way test with appearance and cumulative transmittance as the evaluation indexes.Pharmacokinetic characteristics of the patches were determined by SD rat test.Results Tandospirone transdermal patches included:10%tandospirone,7.5%choline-oleic acid,7.5%isopropyl myristate,and 75%DURO-TAK 4098.The 24-hour cumulative permeation was(309.33±45.98)μg·cm^(-2),and the transdermal steady-state flux was(13.43±1.93)μg·cm^(-2)·h^(-1).SD rats experiments showed that tandospirone transdermal patches held slow-release characteristics compared with tandospirone suspension,with T_(1/2) being extended to(6.37±4.46)h and MRT_(0~t) increased by 17-folds.Conclusion Tandospirone transdermal patches show sustained release effects and become a new drug delivery formulation for tandospirone.

关 键 词：坦度螺酮 透皮贴剂 离子液体 促渗剂 

分 类 号：R944[医药卫生—药剂学]