Spironolactone Crystal Forms

Abstract

U n i v e r s i t y o f S t r a t h c l y d e , Glasgow, S c o t l a n d . ABSTRACT S p i r o n o l a c t o n e was o b t a i n e d i n t h r e e polymorphic and f i v e s o l v a t e d c r y s t a l l i n e forms which d i f f e r e d i n i n i t i a l d i s s o l u t i o n r a t e i n water by a b o u t a f a c t o r o f 1 2 , t h e most r a p i d l y d i s s o l v i n g form a c h i e v i n g c o n c e n t r a t i o n s a b o u t twice t h e e q u i l i b r i u m s o l u b i l i t y ; on p r o l o n g e d c o n t a c t w i t h water t r a n s f o r m a t i o n t o an h y d r a t e d phase o c c u r r e d . I t is s u g g e s t e d t h a

Characterization and Quantitation of Aprepitant Drug Substance Polymorphs by Attenuated Total Reflectance Fourier Transform Infrared Spectroscopy

“…This region in the XRPD pattern was chosen for quantification of form II. A set of calibration standards containing 2, 4, 6, 8, 10, 12,14,16,18,20 and 30 wt % of form II in the polymorph mixture was used in order to build a calibration model for the purpose of quantitation by XRPD. XRPD patterns were obtained for all the standards, and the maximum peak intensity was determined in the range of 21.08-21.17°.…”

“…The mixture was ground in a mortar and thoroughly agitated for 5 min to ensure mixing uniformity. The total weights were kept consistent for each set of samples at ∼100 mg. Calibration standards containing 2, 4, 5, 6, 8, 10, 12,14,15,16,18,20,30,35,40, 60 and 80 wt % of form II were prepared in this manner. A test group of polymorphic mixtures containing varying ratios of the two crystal forms was also prepared for polymorph analysis and comparison study.…”

Utility of Fourier Transform-Raman and Fourier Transform-Infrared Diffuse Reflectance Spectroscopy for Differentiation of Polymorphic Spironolactone Samples

“…3 Mesley and Johnson4 distinguished two crystalline forms of spironoladone in 1965 with IR spectrometry (with liquid parailin mulls) and X-ray diffradometry. Salole and Al-Sarraj, 8. Salole and Al-Sarraj, 8.…”

Pharmaceutical Cocrystals: An Overview

“…Solvates/hydrates are quite unstable, because they lose solvent/water at high temperature and low humidity during storage and the physiochemical properties will be different for hydrated/dehydrated forms [22][23][24] . Dissolution rate of the drug was enhanced by the solvated forms of spironolactone [25] . Different polymorphic cocrystals and solvates of caffeine and anthranilic acid were prepared by using different solvents via liquid assisted grinding [26] .…”