Improved Dissolution Properties of Co-amorphous Probucol with Atorvastatin Calcium Trihydrate Prepared by Spray-Drying

被引：0

作者：

Oyama, Shinji ^{[1
]}

Ogawa, Noriko ^{[1
]}

Kawai, Kaori ^{[1
]}

Iwai, Kanako ^{[1
]}

Yasunaga, Toshiya ^{[1
]}

Yamamoto, Hiromitsu ^{[1
]}

机构：

[1] Aichi Gakuin Univ, Dept Pharmaceut Engn, Sch Pharm, 1-100 Kusumoto cho,Chikusa ku, Nagoya 4648650, Japan

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2024年 / 72卷 / 02期

基金：

日本学术振兴会;

关键词：

atorvastatin calcium trihydrate salt; co-amorphous; dissolution test; probucol; spray-drying; stability test; SOLID DISPERSION-SYSTEMS; PHYSICAL STABILITY; PHYSICOCHEMICAL PROPERTIES; IN-VITRO; BIOAVAILABILITY; CRYSTALLINE; SOLUBILITY; CLASSIFICATION; NANOPARTICLES; TECHNOLOGIES;

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A co-amorphous model drug was prepared by the spray-drying (SD) of probucol (PC) and atorvastatin calcium trihydrate salt (ATO) as low water solubility and co-former components, respectively. The physicochemical properties of the prepared samples were characterized by powder X-ray diffraction (PXRD) analysis, thermal analysis, Fourier transform infrared spectroscopy (FTIR), and dissolution tests. Stability tests were also conducted under a stress environment of 40 degrees C and 75% relative humidity. The results of PXRD measurements and thermal analysis suggested that PC and ATO form a co-amorphous system by SD. Thermal analysis also indicated an endothermic peak that followed an exotherm in amorphous PC and a physical mixture ( PM) of amorphous PC and ATO; however, no endothermic peak was detected in the co-amorphous system. The dissolution profiles for PC in the co-amorphous sample composed of PC and ATO were improved compared to those for raw PC crystals or the PM. Stability tests indicated that the co-amorphous material formed by PC and ATO can be stored for 35 d without crystallization, whereas amorphous PC became crystallized within a day. Therefore, co-amorphization of PC and ATO prepared by SD is considered to be a useful method to improve the solubility of PC in water.

引用

页码：190 / 199

页数：10

共 49 条

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