Effect of Particle Size of Drug on Conversion of Crystals to an Amorphous State in a Solid Dispersion with Crospovidone

被引：8

作者：

Sugamura, Yuka ^{[1
]}

Fujii, Makiko ^{[1
,2
]}

Nakanishi, Sayaka ^{[1
]}

Suzuki, Ayako ^{[1
]}

Shibata, Yusuke ^{[1
,3
]}

Koizumi, Naoya ^{[1
]}

Watanabe, Yoshiteru ^{[1
,2
]}

机构：

[1] Showa Pharmaceut Univ, Dept Pharmaceut & Biopharmaceut, Tokyo 1948543, Japan

[2] Showa Pharmaceut Univ, High Technol Res Ctr, Tokyo 1948543, Japan

[3] Kissei Pharmceut Co Ltd, Pharmaceut Res Labs, Nagano 3998304, Japan

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2011年 / 59卷 / 02期

关键词：

solid dispersion; crospovidone; amorphous; particle size; solid-solid interaction; PHYSICAL STABILITY; INDOMETHACIN; PHASE;

D O I：

10.1248/cpb.59.235

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The effect of particle size on amorphization of drugs in a solid dispersion (SD) was investigated for two drugs, indomethacin (IM) and nifedipine (NP). The SD of drugs were prepared in a mixture with crospovidone by a variety of mechanical methods, and their properties investigated by particle sizing, thermal analysis, and powder X-ray diffraction. IM, which had an initial particle size of 1 AM and tends to aggregate, was forced through a sieve to break up the particles. NP, which had a large initial particle size, was jet-milled. In both cases, reduction of the particle size of the drugs enabled transition to an amorphous state below the melting point of the drug. The reduction in particle size is considered to enable increased contact between the crospovidone and drug particles, increasing interactions between the two compounds.

引用

页码：235 / 238

页数：4

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