使用模糊法测定粉末混合物中活性药物成分的压片速度依赖性变形特性的表征

本研究研究了用于确定压片速度对药物粉末压缩性能的量化评价方法。西洛司唑和布洛芬用作活性药物成分（API）和混合乳糖一水合物和microcrystalline cellulose。检查粘弹性以评估原料，并进行应力松弛试验以确定安慰剂和两个API的表观粘度和弹性系数。

使用压实模拟器和旋转压片机以从实验室到商业的压片速度来制备平板电脑。模芯或ud-ud-udutry应变速率灵敏度（SRS）指数被确定为可压缩性和压缩性的量度。结果表明，模具外部SRS的敏感性高于模芯SRS的灵敏度。布洛芬20％粉末的模具外，显示出高弹性和低粘度的粉末为13.3-47.9％，而安慰剂和西洛他唑20％（w / w）粉末为<7.5％。

A peripheral speed difference of more than 300 mm/s during the out-of-die SRS was sensitive enough to detect the capping tendency. Cilostazol, which has lower elasticity and higher viscosity than ibuprofen, was tested using powder mixtures with the API concentrations of 5–40%; the compressibility SRS was <5% for all API concentrations. In contrast, the compressibility SRS of ibuprofen increased from 4.8 to 81% depending on the API concentration. Using the compressibility SRS as an index, it was possible to extract the tableting speed-dependent compressibility characteristics of API from the powder mixtures containing API.

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实验 - 材料
Cilostazol (Otsuka Pharmaceutical, Tokyo, Japan), an antiplatelet agent, and ibuprofen (Hachidai Pharmaceutical, Osaka, Japan), a nonsteroidal anti-inflammatory analgesic, were used as model APIs. Lactose monohydrate (Dilactose S; Freund, Tokyo, Japan), microcrystalline cellulose (亮度UF-711; Asahi Kasei, Tokyo, Japan), and vegetable-derived magnesium stearate (Taihei Chemical, Osaka, Japan) were used as excipients. A mixture of lactose monohydrate and microcrystalline cellulose (7 : 3) with 1% (w/w) magnesium stearate was used as the placebo mixture. Cilostazol and ibuprofen were added to the placebo mixture at a concentration of 5, 10, 20, and 40% (w/w) powder.

关于this article:使用模糊法测定粉末混合物中活性药物成分的压片速度变形特性的表征 - Daisuke Mizunaga，Mika Koseki，Naoki Kamemoto，Satoru Watano -化学。Pharm。公牛。69,1184-1194（2021） - https://doi.org/10.1248/cpb.c21-00665