Morisseau K M, Rhodes C T
Applied Pharmaceutical Sciences, University of Rhode Island, Kingston 02881, USA.
Pharm Res. 1997 Jan;14(1):108-11. doi: 10.1023/a:1012071904673.
Near-infrared reflectance spectroscopy (NIRS) was used to evaluate and quantify the effect of compression force on the NIR spectra of tablets.
Flat, white tablets with no orientation (scoring, etc.) were manufactured on a Stokes Rotary Tablet Press. NIRS was used to predict tablet hardness on the following four formulations and one placebo matrix: hydrochlorothiazide (HCTZ) 15% and 20% in a placebo matrix (microcrystalline cellulose and magnesium stearate), and chlorpheniramine maleate (CTM) 2% and 6% in a placebo matrix. Five or six levels of tablet hardness from 2 to 12 kg were used for each formulation. Laboratory hardness data was compared to NIR reflectance data using a NIRSystems Rapid Content Analyzer. Multiple linear regression and partial least squares regression techniques were used to determine the relationship between tablet hardness and NIRS spectra.
An increase in tablet hardness produced an upward shift (increase in absorbance) in the NIRS spectra. A series of equations was developed by calibrating tablet hardness data against NIR reflectance response for each formulation. The results of NIRS hardness prediction were at least as precise as the laboratory hardness test (SE = 0.32).
A NIRS method is presented which has the potential as an alternative to conventional hardness testing of tablets.
采用近红外反射光谱法（NIRS）评估并量化压力对片剂近红外光谱的影响。
在斯托克斯旋转压片机上制备无定向（无刻痕等）的扁平白色片剂。使用NIRS对以下四种制剂和一种安慰剂基质预测片剂硬度：安慰剂基质（微晶纤维素和硬脂酸镁）中含15%和20%的氢氯噻嗪（HCTZ），以及安慰剂基质中含2%和6%的马来酸氯苯那敏（CTM）。每种制剂使用五或六个硬度水平，范围为2至12千克。使用NIRSystems快速含量分析仪将实验室硬度数据与近红外反射数据进行比较。采用多元线性回归和偏最小二乘回归技术确定片剂硬度与NIRS光谱之间的关系。
片剂硬度增加使NIRS光谱向上偏移（吸光度增加）。通过针对每种制剂将片剂硬度数据与近红外反射响应进行校准，建立了一系列方程。NIRS硬度预测结果至少与实验室硬度测试一样精确（标准误差 = 0.32）。
提出了一种NIRS方法，它有潜力作为片剂传统硬度测试的替代方法。
