Todo Hiroaki, Sato Kazuki, Takayama Kozo, Sugibayashi Kenji
Department of Pharmaceutical Sciences, Faculty of Pharmacy and Pharmaceutical Sciences, Josai University.
Chem Pharm Bull (Tokyo). 2018 Jul 1;66(7):748-756. doi: 10.1248/cpb.c18-00213. Epub 2018 May 8.
Direct compression is a popular choice as it provides the simplest way to prepare the tablet. It can be easily adopted when the active pharmaceutical ingredient (API) is unstable in water or to thermal drying. An optimal formulation of preliminary mixed powders (premix powders) is beneficial if prepared in advance for tableting use. The aim of this study was to find the optimal formulation of the premix powders composed of lactose (LAC), cornstarch (CS), and microcrystalline cellulose (MCC) by using statistical techniques. Based on the "Quality by Design" concept, a (3,3)-simplex lattice design consisting of three components, LAC, CS, and MCC was employed to prepare the model premix powders. Response surface method incorporating a thin-plate spline interpolation (RSM-S) was applied for estimation of the optimum premix powders for tableting use. The effect of tablet shape identified by the surface curvature on the optimization was investigated. The optimum premix powder was effective when the premix was applied to a small quantity of API, although the function of premix was limited in the case of the formulation of large amount of API. Statistical techniques are valuable to exploit new functions of well-known materials such as LAC, CS, and MCC.
直接压片是一种常用的选择，因为它提供了制备片剂最简单的方法。当活性药物成分（API）在水中不稳定或对热干燥不稳定时，它可以很容易地被采用。如果预先制备用于压片的预混粉末的最佳配方是有益的。本研究的目的是通过使用统计技术来找到由乳糖（LAC）、玉米淀粉（CS）和微晶纤维素（MCC）组成的预混粉末的最佳配方。基于“质量源于设计”的理念，采用由LAC、CS和MCC三种成分组成的（3,3）-单纯形格子设计来制备模型预混粉末。应用结合薄板样条插值的响应面法（RSM-S）来估计用于压片的最佳预混粉末。研究了由表面曲率确定的片剂形状对优化的影响。当预混物应用于少量API时，最佳预混粉末是有效的，尽管在大量API制剂的情况下预混物的功能有限。统计技术对于开发诸如LAC、CS和MCC等知名材料的新功能很有价值。
