Dissolution Modulating Mechanism of Flurbiprofen Solid Dispersions: Characterization, Physical Stability and in vivo Performance: Formulation Considerations and optimization study

R. Tiwari, G. Tiwari, Pranaywal, Ankitawal
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引用次数: 3

Abstract

Present work studied interaction between Surelease, Urea, and Eudragit RL100 (RL) polymers with nonsteroidal anti-inflammatory drug FLP. Solid dispersions at different weight ratios were prepared by fusion (Method A) and coprecipitation (Method B). Characterization of solid dispersions (SDs) included elemental analysis, Fourier transform (FTIR), Differential scanning calorimetry (DSC), Powder-x-ray diffractometry (XRD), Scanning electron microscopy (SEM) as well as wettability study, angle of repose, aqueous solubility determination, in vitro and in vivo drug release. FTIR studies showed the stability FLP. DSC and XRD studies confirmed the amorphous state of FLP in its SDs. SEM showed the formation of effective SDs of FLP with polymers. Pre-formulation studies showed increased hydrophilicity but a non-significant increase in lipophilicity of the SDs. IDR value is only 0.03±0.001 mg/cm2-min. whereas wettability of solid dispersions was found to be controlled. Angle of repose shows good flowability characteristics. The dissolution rate of FLPSDs prepared by method A was significantly greater than that from method B. Method A with urea and RL provides slower and more gradual increase in dissolution rate than those of FLP, when polymer ratios were increased. TF20 possess longer duration of action compared to FLP.
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氟比洛芬固体分散体的溶出调节机制:表征、物理稳定性和体内性能:处方考虑和优化研究
本工作研究了舒立、尿素和乌桕RL100 (RL)聚合物与非甾体抗炎药FLP的相互作用。采用熔合法(A)和共沉淀法(B)制备了不同重量比的固体分散体。固体分散体的表征包括元素分析、傅里叶变换(FTIR)、差示扫描量热法(DSC)、粉末x射线衍射法(XRD)、扫描电镜(SEM)以及润湿性研究、静止角、水溶性测定、体外和体内药物释放。FTIR研究表明其具有稳定的FLP。DSC和XRD研究证实了FLP在SDs中的非晶态。扫描电镜显示,聚合物与FLP形成了有效的SDs。制剂前研究显示SDs的亲水性增加,但亲脂性无显著增加。IDR值仅为0.03±0.001 mg/cm2-min。而固体分散体的润湿性是可控的。休止角表现出良好的流动性特性。方法A制备的flpsd的溶出率显著大于方法b制备的flpsd的溶出率。当聚合物比增加时,尿素和RL的方法A的溶出率比FLP的溶出率增加得更慢、更渐进。与FLP相比,TF20具有更长的作用时间。
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