The impact of crystallinity on Brequinar sodium hygroscopicity.

Abstract:

:The hygroscopicity of Brequinar sodium, an organ transplant immunosuppressant, at 75% relative humidity highly depends on the crystal form or crystallinity of the drug substance. Hygroscopicity and ease of water uptake of three lots of Brequinar sodium were investigated. Those lots contained different impurities at levels ranging from 0.26% to 0.5%. DSC thermograms of the hydrated samples suggest that unbound/loosely bound water was released around 90 degrees C and water of hydration was released at 175 degrees C. At equilibrium, 2% of the water was tightly bound. Stoichiometry suggests that this is a hemihydrate. Unbound/loosely bound water has no impact on the hemihydrate crystal structure as indicated by x-ray powder diffraction patterns. The results suggest that the less perfect crystals exhibited a faster water uptake and converted to a stable hemihydrate when stored at 75% relative humidity. Both the anhydrous and the hemihydrate forms of Brequinar sodium exhibited rapid dissolution rate and comparable water solubility.

journal_name

Pharm Dev Technol

authors

Wu LS,Pang J,Hussain MA

doi

10.3109/10837459609031417

subject

Has Abstract

pub_date

1996-04-01 00:00:00

pages

43-9

issue

1

eissn

1083-7450

issn

1097-9867

journal_volume

1

pub_type

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