Preparation and characterization of glassy celecoxib

被引：33

作者：

Paradkar, AR ^{[1
]}

Chauhan, B

Yamamura, S

Pawar, AP

机构：

[1] Bharati Vidyapeeth Deemed Univ, Poona Coll Pharm, Dept Pharmaceut, Pune 411038, Maharashtra, India

[2] Toho Univ, Sch Pharmaceut Sci, Chiba 2748510, Japan

来源：

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY | 2003年 / 29卷 / 07期

关键词：

celecoxib; glassy state; crystallization; degree of crystallinity; compressibility; X-ray powder diffraction;

D O I：

10.1081/DDC-120021773

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Celecoxib, a poorly water-soluble drug, was converted into a glassy state by melt quenching. The properties of glassy celecoxib were studied using infrared (IR) spectroscopy, differential scanning calorimetry (DSC, X-ray powder diffraction (XRPD), intrinsic dissolution rate (IDR), and thin-layer-chromatography (TLC). Glass transition occurred at 51.8degreesC. Infrared spectrum of glass has revealed significant changes due to H-bonding. Celecoxib glass shows around 15 times faster dissolution as compared with the crystalline state. Heckel plot analysis has shown better compressibility in glassy state. Unpulverized glass remained stable for 3 months, whereas after pulverization about 70% crystallinity was gained in 100 hours. Further attempts may be carried out to stabilize the glass.

引用

页码：739 / 744

页数：6

共 18 条

[1] The characterization of some silylcellulose derivatives by XRD measurements [J].