Singh Inderbir, Kumar Pradeep
Chitkara College of Pharmacy, Chitkara University, Patiala, Punjab, India.
Pak J Pharm Sci. 2012 Oct;25(4):741-9.
Tramadol loaded alginate beads were formulated by ionic cross-linking technique employing calcium chloride as cross-linking agent. Several parameters like bead size, swelling index, incorporation efficiency, in vitro release and in vivo drug activity studies were investigated. Tramadol loading and concentration of calcium chloride were found to have a significant effect on the selected parameters. Tramadol release decreased with decreasing drug loading and increasing concentration of cross-linking agent. Kinetic modeling indicates the involvement of both swelling and erosion on the release characteristics of the drug from the beads. A 2 factors-3 levels central composite design (CCD) was employed to evaluate the effect of critical formulation variables, namely drug loading (X1) and concentration of calcium chloride (X2) on various responses. Multiple linear regression analysis generated polynomial mathematical models for various response variables and the corresponding response surface and contour plots were drawn. X1 was found to have more significant effect than X2 on the dependent variables. In vivo drug activity studies of the alginate beads demonstrated significant antinociceptive effect of tramadol.
采用氯化钙作为交联剂，通过离子交联技术制备了载曲马多的海藻酸钠珠。研究了几个参数，如珠粒大小、溶胀指数、包封效率、体外释放和体内药物活性研究。发现曲马多载药量和氯化钙浓度对所选参数有显著影响。曲马多释放量随药物载药量降低和交联剂浓度增加而减少。动力学模型表明溶胀和侵蚀都参与了药物从珠粒中的释放特性。采用二因素三水平中心复合设计（CCD）来评估关键制剂变量，即药物载药量（X1）和氯化钙浓度（X2）对各种响应的影响。多元线性回归分析生成了各种响应变量的多项式数学模型，并绘制了相应的响应面和等高线图。发现X1对因变量的影响比X2更显著。海藻酸钠珠的体内药物活性研究表明曲马多具有显著的镇痛作用。
