首页> 美国卫生研究院文献>Journal of Pharmaceutics >Combined Effect of Synthetic and Natural Polymers in Preparation of Cetirizine Hydrochloride Oral Disintegrating Tablets: Optimization by Central Composite Design
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Combined Effect of Synthetic and Natural Polymers in Preparation of Cetirizine Hydrochloride Oral Disintegrating Tablets: Optimization by Central Composite Design

机译:合成和天然聚合物在制备盐酸西替利嗪口服崩解片中的联合作用:中央复合设计优化

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摘要

Our aim was to employ experimental design to formulate and optimize cetirizine hydrochloride oral disintegrating tablets (ODTs) by direct compression technique, using the mutual effect of synthetic croscarmellose sodium (CCS) and natural Hibiscus rosa-sinensis mucilage (HRM) as disintegrants in the formulation. Central composite design (CCD) was applied to optimize the influence of three levels each of CCS (X 1) and HRM (X 2) concentrations (independent variables) for investigated responses: disintegration time (DT) (Y 1), % friability (F) (Y 2), and % cumulative drug release (DR) (Y 3) (dependent variables). This face-centered second-order model's reliability was verified by the probability and adequate precision values from the analysis of variance, while the significant factor effects influencing the studied responses were identified using multiple linear regression analysis. Perturbation and response surface plots were interpreted to evaluate the responses' sensitivity towards the variables. During optimization, the concentrations of the processed factors were evaluated, and the resulting values were in good agreement with predicted estimates endorsing the validity. Spectral study by Fourier Transform Infrared Spectroscopy (FTIR) and thermograms from Differential Scanning Calorimetry (DSC) demonstrated the drug-excipients compatibility of the optimized formulation. The optimized formulation has concentrations of 9.05 mg and 16.04 mg of CCS and HRM each, respectively, and the model predicted DT of 13.271 sec, F of 0.498, and DR of 99.768%.
机译:我们的目的是采用实验设计,通过直接压片技术,利用合成交联羧甲基纤维素钠(CCS)和天然芙蓉-粘液(HRM)作为制剂中的崩解剂,共同配制和优化盐酸西替利嗪口服崩解片(ODT)。 。应用中央复合设计(CCD)来优化三个水平的CCS(X 1)和HRM(X 2)浓度(独立变量)对调查响应的影响:崩解时间(DT)(Y 1),%脆碎度( F)(Y 2)和累积药物释放百分比(DR)(Y 3)(因变量)。通过方差分析的概率和足够的精度值验证了以面部为中心的二阶模型的可靠性,同时使用多元线性回归分析确定了影响研究响应的重要因素。解释了扰动和响应面图,以评估响应对变量的敏感性。在优化过程中,对加工因子的浓度进行了评估,得出的值与预测的估计值吻合,证明了其有效性。通过傅立叶变换红外光谱(FTIR)进行的光谱研究和差示扫描量热法(DSC)的热谱图表明,优化制剂的药物-辅料相容性。优化配方的CCS和HRM的浓度分别为9.05μg和16.04μmg,模型预测的DT为13.271 sec,F为0.498,DR为99.768%。

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