Chen Liang, He Zizhou, Kunnath Kuriakose, Zheng Kai, Kim Sangah, Davé Rajesh N
New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Newark, NJ 07102, USA.
New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Newark, NJ 07102, USA.
Eur J Pharm Sci. 2020 Aug 1;151:105408. doi: 10.1016/j.ejps.2020.105408. Epub 2020 Jun 3.
Recent work showed that contrary to conventional wisdom, fine surface engineered excipients outperform their larger counterparts in blends of highly loaded blends of cohesive drug powders in terms of their packing, flowability and tablet tensile strength. Here, two continuous devices, fluid-energy mill (FEM) and conical mill (Comil), are compared with LabRAM, a batch device used in previous work, for nano-silica dry coating of microcrystalline cellulose (MCC) excipients, 20 and 30 μm. Coated MCCs from all three devices had higher bulk densities and flow function coefficients (FFCs) compared with Avicel PH-102. Silica coating quality was best with LabRAM, but also good with FEM and Comil, although Comil was less effective for the finer MCC. However, the better coating quality of LabRAM had a downside of having poorer compaction properties. The most surprising outcome was that multi-component blends of 17 wt% coated MCC with 60 wt % Ibuprofen 50 had higher bulk density, higher or similar flowability, higher tablet tensile strength, and comparable Ibuprofen dissolution from tablets, compared to those with Prosolv 50, a silicified excipient. The FEM dry coated MCC blends, having only 0.17 wt% silica, performed the best, having desirable bulk density, FFC, and tensile strength that could facilitate high-speed direct compression tableting. In summary, considering that achieving best coating quality need not be the primary objective, FEM may be the best option for producing desired sized dry coated fine excipients.
最近的研究表明，与传统观念相反，在高负载粘性药物粉末混合物中，经过精细表面工程处理的辅料在堆积、流动性和片剂抗张强度方面优于其较大的同类产品。在此，将两种连续设备，即流体能量磨（FEM）和锥形磨（Comil），与之前工作中使用的间歇式设备LabRAM进行比较，用于对20和30μm的微晶纤维素（MCC）辅料进行纳米二氧化硅干法包衣。与Avicel PH - 102相比，来自所有三种设备的包衣MCC具有更高的堆积密度和流动功能系数（FFC）。LabRAM的二氧化硅包衣质量最佳，但FEM和Comil的包衣质量也很好，不过Comil对较细的MCC效果较差。然而，LabRAM较好的包衣质量存在压实性能较差的缺点。最令人惊讶的结果是，与含有硅化辅料Prosolv 50的混合物相比，17 wt%包衣MCC与60 wt%布洛芬50的多组分混合物具有更高的堆积密度、更高或相似的流动性、更高的片剂抗张强度以及相当的布洛芬片剂溶出度。仅含有0.17 wt%二氧化硅的FEM干法包衣MCC混合物表现最佳，具有理想的堆积密度、FFC和抗张强度，有利于高速直接压片。总之，考虑到获得最佳包衣质量不一定是主要目标，FEM可能是生产所需尺寸的干法包衣精细辅料的最佳选择。
