Trisopon Karnkamol, Kittipongpatana Nisit, Wattanaarsakit Phanphen, Kittipongpatana Ornanong Suwannapakul
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.
Research Center for Development of Local Lanna Rice and Rice Products, Chiang Mai University, Chiang Mai 50200, Thailand.
Pharmaceuticals (Basel). 2021 Oct 14;14(10):1047. doi: 10.3390/ph14101047.
A co-processed, rice starch-based excipient (CS), previously developed and shown to exhibit good pharmaceutical properties, is investigated as an all-in-one excipient for direct compression (DC). An SeDeM-ODT expert system is applied to evaluate the formulation containing CS, in comparison with those containing the physical mixture and the commercial DC excipients. The results revealed that CS showed acceptable values in all six incidence factors of the SeDeM-ODT diagram. In addition, the comprehensive indices (IGC and IGCB) were higher than 5.0, which indicated that CS could be compressed with DC technique without additional blending with a disintegrant in tablet formulation. The formulation study suggested that CS can be diluted up to 60% in the formulation to compensate for unsatisfactory properties of paracetamol. At this percentage, CS-containing tablets exhibited narrow weight variation (1.5%), low friability (0.43%), acceptable drug content (98%), and rapid disintegration (10 s). The dissolution profile of CS displayed that more than 80% of the drug content was released within 2 min. The functionality of CS was comparable to that of high functionality excipient composite (HFEC), whereas other excipients were unsuccessful in formulating the tablets. These results indicated that CS was a suitable all-in-one excipient for application in DC of tablets.
一种先前开发并已证明具有良好药学性质的共处理大米淀粉基辅料（CS），被作为直接压片（DC）的一体化辅料进行研究。应用SeDeM-ODT专家系统对含CS的制剂进行评估，并与含物理混合物和市售DC辅料的制剂进行比较。结果显示，CS在SeDeM-ODT图的所有六个发生率因素中均显示出可接受的值。此外，综合指数（IGC和IGCB）高于5.0，这表明CS在片剂制剂中可采用DC技术进行压片，无需额外与崩解剂混合。制剂研究表明，在制剂中CS可稀释至60%，以弥补对乙酰氨基酚不理想的性质。在此百分比下，含CS的片剂表现出窄的重量差异（1.5%）、低的脆碎度（0.43%）、可接受的药物含量（98%）和快速崩解（10秒）。CS的溶出曲线显示，超过80%的药物含量在2分钟内释放。CS的功能与高功能辅料复合物（HFEC）相当，而其他辅料在片剂制剂中未成功。这些结果表明，CS是适用于片剂DC的一体化辅料。
