Ishikawa Agata, Takasaki Hiroshi, Sakurai Atsushi, Katayama Takuma, Wada Koichi, Furuishi Takayuki, Fukuzawa Kaori, Obata Yasuko, Yonemochi Etsuo
School of Pharmacy and Pharmaceutical Sciences, Hoshi University.
Nippon Boehringer Ingelheim Co., Ltd.
Chem Pharm Bull (Tokyo). 2021;69(5):447-455. doi: 10.1248/cpb.c20-00970.
This study aimed to compare the manufacturability and granule and tablet properties of green fluidized bed granulation (GFBG) and of direct compression (DC). Acetaminophen was used as a low compactability model drug. The process time of GFBG to produce final mixtures was comparable to that of DC, and thus GFBG could be considered a simple process. DC could not produce 30% drug load tablets owing to poor granule flowability, whereas no problems were observed in the GFBG tableting process up to 80% of drug load. Tablets prepared with GFBG showed higher tensile strength than those prepared using DC. Compactability evaluation results show that the yield pressure of the granules prepared with GFBG was significantly lower than that of DC, suggesting that the granules prepared with GFBG were easily plastically deformed. Moreover, tablets prepared with GFBG showed fast disintegration, which was faster than that of DC. We conclude that GFBG produces granules with higher drug content and desired physicochemical properties at low cost.
本研究旨在比较绿色流化床制粒（GFBG）和直接压片（DC）的可制造性以及颗粒和片剂性质。对乙酰氨基酚用作低可压性模型药物。GFBG制备最终混合物的工艺时间与DC相当，因此GFBG可被视为一种简单工艺。由于颗粒流动性差，DC无法生产30%载药量的片剂，而在GFBG压片过程中，载药量高达80%时未观察到问题。用GFBG制备的片剂显示出比用DC制备的片剂更高的抗张强度。可压性评估结果表明，用GFBG制备的颗粒的屈服压力明显低于DC，这表明用GFBG制备的颗粒易于发生塑性变形。此外，用GFBG制备的片剂崩解迅速，比DC更快。我们得出结论，GFBG能以低成本生产具有更高药物含量和所需理化性质的颗粒。
