用实验设计法对阿瑞吡坦速溶膜配方进行优化及评价

Rajni Bala , Shailesh Sharma , IKGPTU
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引用次数: 42

摘要

快速溶解剂型作为一种新型给药系统,已成为一种流行的给药方式。通过减少给药频率,该系统将提供最大的治疗效果,提高生物利用度和最大的稳定性。它还可以避免药物的第一次代谢。该系统提供更快的药物吸收从胃前区域,这可能提供快速起效。本研究旨在制备阿瑞吡坦快速溶解膜(FDF),用于预防和治疗化疗引起的恶心和呕吐。采用溶剂铸造法制备FDF,并考虑成膜聚合物(普鲁兰)和peg400两个自变量,采用中心复合设计对FDF进行优化。以崩解时间、润湿时间、药物释放和折叠时间为因变量。优化后的配方崩解时间最短(20 s),溶出率最高(88.87%),理化性质满意。从上述结果可以明显看出,所开发的制剂可以是一种创新剂型,以改善药物输送、起效以及改善患者依从性。
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Formulation optimization and evaluation of fast dissolving film of aprepitant by using design of experiment

The concept of fast dissolving dosage form has become popular as new delivery system. This system will provide maximum therapeutic efficacy, increased bioavailability and maximum stability by reducing the frequency of dosage. It will also avoid first pass metabolism of the drugs. This system provides more rapid drug absorption from the pre gastric area which may provide quick onset of action. The present research aimed to prepare fast dissolving films (FDF) of aprepitant used in the prevention and treatment of chemotherapy-induced nausea and vomiting. The FDF was prepared using solvent casting method and optimized employing central composite design considering two independent variables film forming polymer (pullulan) and PEG 400. Disintegration time, wetting time, drug release and folding endurance were taken as dependent variables. The prepared optimized formulation showed minimum disintegration time (20 s), highest dissolution rate (88.87%) and satisfactory physicochemical properties. It is evident from the above results that the developed formulation can be an innovative dosage form to improve the drug delivery, onset of action as well as improve patient compliance.

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