Formulation Development, Optimization and Evaluation of Flurbiprofen Microsponge Tablet for the Treatment of Rheumatoid Arthritis (RA) by using Box- Behnken Design.

Q4 Medicine
Muthadi Radhika Reddy, Madhavi Latha Samala, Narahari Kv, J K Shyamala, Parag Kulkarni, Bhargav Gunnepalli, Prasanthi Boddu, T Naga Aparna
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引用次数: 0

Abstract

Introduction: Rheumatoid arthritis (RA) is a chronic, autoimmune and inflammatory disease that mostly impacts the joints. Chronotherapeutics refers to a treatment method in which in-vivo drug availability is timed to match rhythms of disease in order to optimize therapeutic outcomes and minimize side effects. Flurbiprofen is a non-steroidal anti-inflammatory drug, indicated for the relief of inflammation.

Objectives: The aim of the present study was to develop & optimize the microsponges based of Flurbiprofen tablet for Chronotherapeutics for enhanced therapeutic effect.

Methods: Microsponges were developed by Quasi Emulsion solvent diffusion method. Prepared microsponges were optimized in order to analyze the effects of independent variables like concentration of PVA (X1), Volume of Dichloromethane (X2) & stirring speed (X3) on the Entrapment Efficiency (Y1), Mean particle size (Y2) and Drug release at 8 hr (Y3) using box Behnken design. The optimized formulation was subjected to in vitro study and Comparison with marketed formulation. With release kinetics study.

Result: The optimized formulation Batch (F-18) Show particle size of 49.12µm, entrapment efficiency of 87.46%, and drug release at 8 h 70.49%, which is under the acceptance criteria, which is more effective compared with Marketed tablet.

Conclusion: The results showed that, as stirring speed increases, the particle size decreases and entrapment efficiency increases. While volume of dichloromethane increases, particle size decreases. Morphology was found to be porous and spherical. Optimized batch of Flurbiprofen microsponge was further formulated in future for invivo study and clinical trials.

采用方框贝肯设计开发、优化和评估用于治疗类风湿性关节炎(RA)的氟比洛芬微海绵片的配方
导言类风湿性关节炎(RA)是一种主要影响关节的慢性自身免疫性炎症疾病。慢性治疗学是指一种治疗方法,根据疾病的节律调整体内药物的供应时间,以优化治疗效果并减少副作用。氟比洛芬是一种非甾体抗炎药,适用于缓解炎症:本研究旨在开发和优化用于慢性治疗的氟比洛芬片的微海绵,以提高治疗效果:方法:采用准乳液溶剂扩散法研制微海绵。方法:采用准乳液溶剂扩散法制备微海绵,并利用盒式贝肯设计对制备的微海绵进行优化,以分析 PVA 浓度(X1)、二氯甲烷体积(X2)和搅拌速度(X3)等自变量对包封效率(Y1)、平均粒径(Y2)和 8 小时药物释放量(Y3)的影响。对优化后的制剂进行了体外研究,并与市场上销售的制剂进行了比较。结果:结果:优化配方批次(F-18)的粒度为 49.12µm,夹带效率为 87.46%,8 小时药物释放率为 70.49%,均在接受标准范围内,与市售片剂相比更有效:结果表明,随着搅拌速度的增加,粒度减小,夹带效率增加。随着二氯甲烷体积的增加,粒径减小。形态为多孔球形。优化后的氟比洛芬微海绵将进一步用于体内研究和临床试验。
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CiteScore
0.70
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53
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