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首页> 外文期刊>International Journal of Pharmaceutical Sciences and Research >FORMULATION AND EVALUATION OF NON EFFERVESCENT FLOATING TABLETS OF CEFUROXIME AXETIL
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FORMULATION AND EVALUATION OF NON EFFERVESCENT FLOATING TABLETS OF CEFUROXIME AXETIL

机译:头孢呋辛酯非泡腾片的配方与评价

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The objective of this work was to develop non effervescent floating tablets by Melt granulation technique. Cefuroxime axetil is having shorter half life of 80 min and hydrolyzed by intestinal esterase to the non absorbable cefuroxime in the gut lumen and is, therefore, suspected as a possible cause of incomplete bioavailability. So there is a need to increase the gastric residence time of the drug. These tablets were prepared by different meltable binders such as paraffin wax, bees wax and carnauba wax as release retardants. Various formulations have been developed by varying concentration of waxes, buoyancing agent and disintegrating agent. The FTIR spectrum indicated the stability and compatability of drug and excipients. All the formulations (F1 to F9) were evaluated for weight variation, hardness, friability, buoyancy studies and In-vitro drug release studies. Among all the formulations, dissolution studies data indicated that F9 formulation exhibited good drug release 0f 91.67% and has shown floating time more than 24hrs with a lag time of 30 min. The mechanism of drug release of NEF tablets of Cefuroxime Axetil was determined by the application of Korsmeyer-Peppas model, Higuchi’s model, Zero order and first order kinetics. From the drug release plots it was observed that the drug release was following zero order kinetics and non – fickian diffusion (n value 0.5 to 1) fitting in to Korsmeyer -Peppas equation. This indicates that drug release depends on erosion of waxes.
机译:这项工作的目的是通过熔体造粒技术开发非泡腾的漂浮片剂。头孢呋辛酯的半衰期较短,为80分钟,并且被肠道酯酶水解为肠腔中不可吸收的头孢呋辛酯,因此被怀疑是生物利用度不完全的可能原因。因此需要增加药物在胃中的停留时间。这些片剂是由不同的可熔性粘合剂(如石蜡,蜂蜡和巴西棕榈蜡)制成的,作为释放抑制剂。通过改变蜡,浮力剂和崩解剂的浓度已经开发出各种配方。 FTIR光谱表明药物和赋形剂的稳定性和相容性。评价所有制剂(F1-F9)的重量变化,硬度,脆性,浮力研究和体外药物释放研究。在所有制剂中,溶出度研究数据表明F9制剂显示出良好的药物释放0f 91.67%,并显示超过24小时的漂浮时间和30分​​钟的滞后时间。通过应用Korsmeyer-Peppas模型,Higuchi模型,零级和一级动力学确定了头孢呋辛酯NEF片剂的药物释放机制。从药物释放曲线可以看出,药物释放遵循零阶动力学和非菲克扩散(n值为0.5到1),符合Korsmeyer -Peppas方程。这表明药物释放取决于蜡的侵蚀。

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