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Optimisation of Alfuzosin Hydrochloride Organogels for Transdermal Delivery

机译:盐酸阿夫唑嗪透皮给药的优化

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Introduction: The purpose of present research was to prepare and optimise alfuzosin hydrochloride (AH) organogels for transdermal delivery using box-behnken design. Methods: Organogels were prepared by fluid filled fiber mechanism. In box-behnken design, the effect of gelling agent, concentration of gelling agent, apolar solvent and permeation enhancer on flux and Q24 was studied. The prepared organogels were evaluated for physicochemical properties and in vitro diffusion studies, ex vivo permeation, skin irritation and stability studies. Results: All the formulations have shown better physicochemical properties. Ex-vivo skin permeation studies reveals that, Tween80 based organogel formulated using 70% w/w of Tween80, IPM as apolar solvent and Tween20 as permeation enhancer has shown maximum drug release of 89.53% for 24 hrs with flux of 33.03±0.19 μg/cm2/hr and Q24 of 914.05±1.42 μg/cm2. Modified backward model was the best fit model in box-behnken design. Permeability coefficient, lag time and skin content were found to be 3.303±0.02 cm/hr, 0.45±0.30 hr and 240.66±9.89 μg/g respectively. The transdemal flux was enhanced by 8.34 times over pure drug solution. Skin irritation studies showed irritation potential of ‘0’, thus proving to be non-irritant. The formulations were stable at room temperature for 1 month. Conclusion: Results suggested that Tween80 based organogels are better carriers for transdermal delivery of AH when compared with soyalecithin and Span80: Tween80 based organogels.
机译:简介:本研究的目的是使用Box-Behnken设计来制备和优化盐酸阿夫唑嗪(AH)有机凝胶,以便透皮递送。方法:采用流体填充纤维机理制备有机胶。在盒式设计中,研究了胶凝剂,胶凝剂浓度,非极性溶剂和渗透促进剂对通量和Q 24 的影响。对制备的有机凝胶进行了理化性质和体外扩散研究,离体渗透,皮肤刺激性和稳定性研究。结果:所有制剂均表现出更好的理化性质。离体皮肤渗透研究表明,使用70%w / w的Tween80,IPM作为非极性溶剂和Tween20作为渗透促进剂配制的基于Tween80的有机凝胶显示24小时的最大药物释放率为89.53%,通量为33.03±0.19μg/ cm 2 / hr和Q 24 为914.05±1.42μg/ cm 2 。修正后向模型是Box-Behnken设计中的最佳拟合模型。发现渗透系数,滞后时间和皮肤含量分别为3.303±0.02cm / hr,0.45±0.30hr和240.66±9.89μg/ g。与纯药物溶液相比,透皮通量提高了8.34倍。皮肤刺激性研究显示刺激性为“ 0”,因此被证明是无刺激性的。该制剂在室温下稳定1个月。结论:结果表明,与大豆卵磷脂和Span80:基于Tween80的有机凝胶相比,基于Tween80的有机凝胶是AH透皮递送的更好载体。

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