莫西沙星的处方开发与评价。盐酸快溶片

R. Gunda, J. S. Kumar
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引用次数: 10

摘要

本研究的主要目的是研制莫西沙星。盐酸快溶片。莫西沙星。盐酸,一种合成氟喹诺酮类抗菌剂,用于治疗急性细菌性鼻窦炎、慢性支气管炎急性细菌性加重。莫西沙星快溶片的研制。采用32因子设计,采用直接压缩技术,以不同浓度的交叉维酮和交叉卡蜜糖钠作为超崩解剂,以不同的组合方式制备HCl。分别以交联维酮和交联棉糖钠的浓度X1和X2为自变量,以润湿时间、崩解时间、t50%和t90%为因变量。设计了9种制剂,并对其硬度、脆度、厚度、含量、润湿时间、崩解时间、体外释放度进行了评价。结果表明,各制剂均符合药典标准,并拟合各制剂的体外溶出度曲线符合不同的动力学模型,计算其截距(a)、斜率(b)和回归系数(r)等统计参数。建立了润湿时间、崩解时间、t50%、t90%的多项式方程。通过设计2个检查点公式(C1, C2)验证了所建立的多项式方程的有效性。根据SUPAC指南,含有7.5%交叉维酮和7.5%交叉卡蜜糖的配方(F5)与上市产品(AVELOX-400)最相似(相似因子f2=68.88,不同因子f1= 3.35,无显著差异,t= 0.00354)。所选制剂(F5)符合一级动力学,药物释放机制为非菲克扩散超级转运(n= 1.902)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation Development and Evaluation of Moxifloxacin.HCL Fast Dissolving Tablets
The main objective of present research investigation is to formulate the Moxifloxacin.HCl Fast Dissolving tablets. Moxifloxacin.HCl, a synthetic fluoroquinolone antibacterial agent, and used to treatacute bacterial sinusitis, acute bacterial exacerbation of chronic bronchitis. The Fast Dissolving tablets of Moxifloxacin.HCl were prepared employing different concentrations of Crospovidone and Croscarmellose sodium in different combinations as a Superdisintegrants by Direct Compression technique using 32 factorial design. The concentration of Crospovidone and Croscarmellose sodium was selected as independent variables, X1 and X2 respectively whereas, wetting time, Disintegration time, t50%, and t90%were selected as dependent variables. Totally nine formulations were designed and are evaluated for hardness, friability, thickness, Assay, Wetting time, Disintegration time, In-vitro drug release. From the Results concluded that all the formulation were found to be with in the Pharmacopoeial limits and the In-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for Wetting time, Disintegration time, t50%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations (C1, C2). According to SUPAC guidelines the formulation (F5) containing combination of 7.5% Crospovidone and 7.5% Croscarmellose, is the most similar formulation (similarity factor f2=68.88, dissimilarity factor f1= 3.35& No significant difference, t= 0.00354) to marketed product (AVELOX-400). The selected formulation (F5) follows First order, Higuchi’s kinetics, mechanism of drug release was found to be Non-Fickian Diffusion Super Case-II Transport (n= 1.902).
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