Donoso M, Kildsig D O, Ghaly Evone S
School of Pharmacy, Medical Sciences Campus, University of Puerto Rico, San Juan, Puerto Rico 00936-5067, USA.
Pharm Dev Technol. 2003;8(4):357-66. doi: 10.1081/pdt-120024689.
The main objective of this research is to use the near-infrared diffuse reflectance method to evaluate and quantify the effects of hardness and porosity on the near-infrared spectras of tablets. To develop a model equation, validate the model and test the model predictive ability. Seven theophylline tablet formulations of the same composition but with seven different hardness values (3, 6, 8, 10, 12, 15, and 17 kp) were prepared. Another seven theophylline tablets formulation with seven different porosity values (57.4, 50.3, 41.9, 40.3, 39.9, 37.3, and 35.1%) were prepared. Five placebo tablets formulation with different hardness and porosity values were also prepared. Laboratory hardness and porosity values were compared to near-infrared diffuse reflectance data. Linear regression, quadratic, cubic and partial least square techniques were used to determine the relationship between hardness, porosity and the near-infrared spectras. The results demonstrated that an increase in tablet hardness and a decrease in tablets porosity produced an increase in near-infrared absorbance. Series of model equations depending on the mathematical technique used for regression were developed from the calibration of hardness and porosity data using laboratory equipment vs. the near-infrared diffuse reflectance for each formulations. The results of near-infrared hardness and porosity predictions were very similar to laboratory hardness and porosity tests. The near-infrared diffuse reflectance spectroscopy method is an alternative nondestructive method for measurement of hardness and porosity of tablets.
本研究的主要目的是使用近红外漫反射法评估并量化硬度和孔隙率对片剂近红外光谱的影响。建立一个模型方程，验证该模型并测试其预测能力。制备了七种相同组成但硬度值不同（3、6、8、10、12、15和17 kp）的茶碱片剂配方。还制备了另外七种孔隙率值不同（57.4%、50.3%、41.9%、40.3%、39.9%、37.3%和35.1%）的茶碱片剂配方。还制备了五种具有不同硬度和孔隙率值的安慰剂片剂配方。将实验室硬度和孔隙率值与近红外漫反射数据进行比较。使用线性回归、二次、三次和偏最小二乘技术来确定硬度、孔隙率与近红外光谱之间的关系。结果表明，片剂硬度增加和片剂孔隙率降低会导致近红外吸光度增加。根据用于回归的数学技术，通过使用实验室设备对硬度和孔隙率数据与每种配方的近红外漫反射进行校准，建立了一系列模型方程。近红外硬度和孔隙率预测结果与实验室硬度和孔隙率测试结果非常相似。近红外漫反射光谱法是一种用于测量片剂硬度和孔隙率的替代性无损方法。
