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,T1/2 延长至(6.37±4.46)h,MRT0～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.
Abstract
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 T1/2 being extended to(6.37±4.46)h and MRT0～t increased by 17-folds.Conclusion Tandospirone transdermal patches show sustained release effects and become a new drug delivery formulation for tandospirone.
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