Structural changes of sodium warfarin in tablets affecting the dissolution profiles and potential safety of generic substitution

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389013%3A_____%2F21%3A00545620" target="_blank" >RIV/61389013:_____/21:00545620 - isvavai.cz</a>

Alternative codes found

RIV/00216305:26310/21:PU141616 RIV/00216224:14160/21:00122723

Result on the web

<a href="https://www.mdpi.com/1999-4923/13/9/1364" target="_blank" >https://www.mdpi.com/1999-4923/13/9/1364</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/pharmaceutics13091364" target="_blank" >10.3390/pharmaceutics13091364</a>

Result language

angličtina

Original language name

Structural changes of sodium warfarin in tablets affecting the dissolution profiles and potential safety of generic substitution

Original language description

At present, the risk of generic substitutions in warfarin tablets is still being discussed. The aim of this study was to assess whether API interactions with commonly used excipients may affect the safety of generic replacement of warfarin sodium tablets. These interactions were observed during an accelerated stability study, and the effect of the warfarin solid phase (crystalline/amorphous form) as well as the API particle size distribution was studied. Commercial tablets and prepared tablets containing crystalline warfarin or amorphous warfarin were used. In addition, binary mixtures of warfarin with various excipients were prepared. The structural changes before and after the stability study were monitored by dissolution test in different media, solid-state NMR spectroscopy and Raman microscopy. During the stability study, the conversion of the sodium in warfarin to its acid form was demonstrated by some excipients (e.g., calcium phosphate). This change in the solid phase of warfarin leads to significant changes in dissolution, especially with the different particle sizes of the APIs in the tablet. Thus, the choice of suitable excipients and particle sizes are critical factors influencing the safety of generic warfarin sodium tablets.

Czech name

—

Czech description

—

Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

OECD FORD branch

10403 - Physical chemistry

Project

<a href="/en/project/LTAUSA18011" target="_blank" >LTAUSA18011: Ab Initio Investigation of Polymorphism of Active Pharmaceutical Ingredients Supported by State of the Art NMR Crystallographic and Calorimetric Experiments.</a><br>

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2021

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Pharmaceutics

ISSN

1999-4923

e-ISSN

1999-4923

Volume of the periodical

13

Issue of the periodical within the volume

9

Country of publishing house

CH - SWITZERLAND

Number of pages

19

Pages from-to

1364

UT code for WoS article

000701490900001

EID of the result in the Scopus database

2-s2.0-85114262641