Department of Pharmaceutics, Gupta College of Technological Sciences, Asansol-713301, India.
Acta Pharm. 2011 Mar;61(1):25-36. doi: 10.2478/v10007-011-0002-x.
The present study deals with the development of hydroxyapatite (HAp)-ciprofloxacin bone-implants using the »Quality by design« approach. The effect of various synthesis parameters like drug amount added in the process, stirring speed and addition rate of orthophosphoric acid in the synthesis on drug concentration in the HAp-ciprofloxacin system synthesized by the precipitation technique using 23 factorial design was analyzed. Optimization methodology utillizing the first-order polynomial equation was used to search for optimal drug concentration in the HAp-ciprofloxacin implant system. The observed responses coincided well with the predicted values from the optimization technique. New implants were manufactured using various HAp-ciprofloxacin composites and 1.5 % (m/V) guar gum as a binder. Characterization of the delivery system was done by XRPD, FTIR spectroscopy and SEM. Even at highest drug concentration (76.6 ± 0.5 %, m/m), ciprofloxacin was present in noncrystalline state. The in vitro ciprofloxacin release from various bone-implants was sustained for several weeks and the drug release pattern correlated well with the Korsmeyer- Peppas model.
本研究采用“质量源于设计”方法开发了载羟磷灰石（HAp）-环丙沙星骨植入物。通过 23 因子设计，利用沉淀技术合成 HAp-环丙沙星体系时，分析了各种合成参数（如加入过程中的药物量、搅拌速度和正磷酸的加入速率）对药物浓度的影响。利用一阶多项式方程的优化方法，搜索 HAp-环丙沙星植入物系统中药物的最佳浓度。观察到的响应与优化技术的预测值吻合良好。使用各种 HAp-环丙沙星复合材料和 1.5%（m/V）瓜尔胶作为粘合剂制造了新的植入物。通过 X 射线衍射（XRPD）、傅里叶变换红外光谱（FTIR）和扫描电子显微镜（SEM）对输送系统进行了表征。即使在最高药物浓度（76.6±0.5%，m/m）下，环丙沙星也呈非晶态存在。各种骨植入物中，环丙沙星的体外释放可持续数周，药物释放模式与 Korsmeyer-Peppas 模型很好地相关。
