Physicochemical properties of tamoxifen hemicitrate sesquihydrate.

Abstract:

:A novel modification of tamoxifen [(Z)-2-[4-(1,2-diphenyl-1-butenyl) phenoxy]-N,N-dimethylethylamine] citrate, tamoxifen hemicitrate hydrate was prepared. The crystalline form was identified and characterized by powder and single crystal X-ray diffractometries, differential scanning calorimetry (DSC), thermal gravimetric analysis (TGA), and hot-stage microscopy, and its physicochemical stability was also evaluated. The results of an elemental analysis, a single crystal X-ray analysis, and the TGA suggested that the molar ratio of tamoxifen:citric acid:water was 2:1:3 indicating it to be tamoxifen hemicitrate sesquihydrate. Simultaneous XRD-DSC measurements also indicated that two hydrates, sesquihydrate and hemihydrate, and an anhydrous form would exist during heating. The physicochemical stability of tamoxifen citrate forms A and B suspended in water and of form A during kneading and drying suggested that tamoxifen citrate was transformed into tamoxifen hemicitrate hydrate in water within 24 h, whereas tamoxifen citrate in a mixture with microcrystalline cellulose was quite stable during kneading. These results suggested that water and a mixture of water and organic solvent should be used for the manufacturing process with special attention paid to the transformation to tamoxifen hemicitrate sesquihydrate, because it showed a different stoichiometry from the active ingredient, tamoxifen citrate.

journal_name

Int J Pharm

authors

Kojima T,Katoh F,Matsuda Y,Teraoka R,Kitagawa S

doi

10.1016/j.ijpharm.2007.10.021

subject

Has Abstract

pub_date

2008-03-20 00:00:00

pages

146-51

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(07)00849-6

journal_volume

352

pub_type

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