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采用 Box-Behnken 设计研制、优化并评价治疗类风湿关节炎(RA)的氟比洛芬微球片。

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

机构信息

Associate Professor, Gurunanak Institution of Technical campus- School of Pharmacy, Hyderabad, India.

Associate Professor, Aditya College of Pharmacy, Aditya nagar, ADB road, Surampalem, kakinada district, Andhra Pradesh 533437.

出版信息

Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2024 Jul 24;40:e20240016. doi: 10.62958/j.cjap.2024.016.

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.

摘要

简介

类风湿性关节炎(RA)是一种慢性、自身免疫性和炎症性疾病,主要影响关节。时间治疗学是指一种治疗方法,即将体内药物的可用性与疾病的节律相匹配,以优化治疗效果并最小化副作用。氟比洛芬是非甾体抗炎药,用于缓解炎症。

目的

本研究旨在开发和优化基于氟比洛芬的微海绵片的时间治疗学,以增强治疗效果。

方法

采用准乳液溶剂扩散法制备微海绵。采用 Box-Behnken 设计,以聚乙烯醇(X1)浓度、二氯甲烷(X2)体积和搅拌速度(X3)为自变量,对载药量(Y1)、平均粒径(Y2)和 8 小时药物释放(Y3)进行优化。将优化后的配方进行体外研究,并与市售配方进行比较。通过释放动力学研究。

结果

优化后的配方(F-18)粒径为 49.12µm,包封率为 87.46%,8 小时药物释放 70.49%,符合接受标准,与市售片剂相比更有效。

结论

结果表明,搅拌速度增加时,粒径减小,包封效率增加。而二氯甲烷体积增加时,粒径减小。形态被发现是多孔和球形的。优化的氟比洛芬微海绵批将进一步用于未来的体内研究和临床试验。

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