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首页> 美国卫生研究院文献>AAPS PharmSciTech >Enhanced Bioavailability of Buspirone From Reservoir-Based Transdermal Therapeutic System Optimization of Formulation Employing Box–Behnken Statistical Design
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Enhanced Bioavailability of Buspirone From Reservoir-Based Transdermal Therapeutic System Optimization of Formulation Employing Box–Behnken Statistical Design

机译：基于储库的透皮治疗系统提高丁螺环酮的生物利用度采用Box-Behnken统计设计优化配方

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The purpose of the present study was to develop and optimize reservoir-based transdermal therapeutic system (TTS) for buspirone (BUSP), a low bioavailable drug. A three-factor, three-level Box–Behnken design was employed to optimize the TTS. Hydroxypropyl methylcellulose, d-limonene and propylene glycol were varied as independent variables; cumulative amount permeated across rat abdominal skin in 24 h, flux and lag time were selected as dependent variables. Mathematical equations and response surface plots were used to relate the dependent and independent variables. The statistical validity of polynomials was established, and optimized formulation factors were selected by feasibility and grid search. Validation of the optimization study with seven confirmatory runs indicated high degree of prognostic ability of response surface methodology. BUSP-OPT (optimized formulation) showed a flux 104.6 µg cm−2 h−1, which could meet target flux. The bioavailability studies in rabbits showed that about 2.65 times improvement (p < 0.05) in bioavailability, after transdermal administration of BUSP-OPT compared to oral solution. The ex vivo–in vivo correlation was found to have biphasic pattern and followed type A correlation. Reservoir-based TTS for BUSP was developed and optimized using Box–Behnken statistical design and could provide an effective treatment in the management of anxiety.
机译：本研究的目的是开发和优化低生物利用度的丁螺环酮（BUSP）的基于储库的透皮治疗系统（TTS）。采用三因素，三级Box-Behnken设计来优化TTS。羟丙基甲基纤维素，d-柠檬烯和丙二醇作为独立变量而变化；选择24小时内穿过大鼠腹部皮肤的累积量，通量和滞后时间作为因变量。数学方程和响应面图用于关联因变量和自变量。建立了多项式的统计有效性，并通过可行性和网格搜索选择了优化的配方因子。通过七次验证性运行对优化研究的验证表明，响应面方法的高度预后能力。 BUSP-OPT（优化配方）的通量为104.6 µg cm -2 h -1 ，可以满足目标通量。对兔子的生物利用度研究表明，与口服溶液相比，经皮给予BUSP-OPT后，生物利用度提高了约2.65倍（p <0.05）。发现离体-体内相关具有双相性，并遵循A型相关。使用Box–Behnken统计设计开发和优化了基于储层的BUSP TTS，可以为焦虑症的治疗提供有效的治疗方法。

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