The effect of amorphous and crystal sodium warfarin and its content uniformity on bioequivalence of tablets

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081731%3A_____%2F18%3A00495859" target="_blank" >RIV/68081731:_____/18:00495859 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/62157124:16370/18:43876653 RIV/00216305:26310/18:PU129764

Výsledek na webu

<a href="http://dx.doi.org/10.1016/j.ejps.2018.09.022" target="_blank" >http://dx.doi.org/10.1016/j.ejps.2018.09.022</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.ejps.2018.09.022" target="_blank" >10.1016/j.ejps.2018.09.022</a>

Jazyk výsledku

angličtina

Název v původním jazyce

The effect of amorphous and crystal sodium warfarin and its content uniformity on bioequivalence of tablets

Popis výsledku v původním jazyce

Warfarin is intensively discussed in terms of generic substitution due to particular cases of bleeding, which are attributable to fluctuations in API content or the substitution of crystalline (WSC) for amorphous (WSA) warfarin. The aim of this study was to assess to what extent the in vitro release was affected by the form of API depending on the composition and technology. Bioequivalent tablets containing 5 mg of WSA or WSC prepared by we granulation or direct compression were used. Furthermore, tablets of the same composition with WSC or WSA prepared by direct compression were evaluated. Raman spectroscopy was used to confirm the presence of WSA or WSC. The dissolution was more influenced by the technology than by the form of API but even tablets with dissimilar profiles were bioequivalent. This is probably due to the precipitation of WSA and WSC in the stomach on a poorly soluble acidic form, which subsequently dissolves in the neutral environment of the small intestine. Recrystallization was demonstrated in the in vitro assay a a pH of 1.2 and 4.5 using Raman spectroscopy and X-ray diffraction. In summary, the content uniformity appears to be the main factor affecting the safety of the treatment.

Název v anglickém jazyce

The effect of amorphous and crystal sodium warfarin and its content uniformity on bioequivalence of tablets

Popis výsledku anglicky

Warfarin is intensively discussed in terms of generic substitution due to particular cases of bleeding, which are attributable to fluctuations in API content or the substitution of crystalline (WSC) for amorphous (WSA) warfarin. The aim of this study was to assess to what extent the in vitro release was affected by the form of API depending on the composition and technology. Bioequivalent tablets containing 5 mg of WSA or WSC prepared by we granulation or direct compression were used. Furthermore, tablets of the same composition with WSC or WSA prepared by direct compression were evaluated. Raman spectroscopy was used to confirm the presence of WSA or WSC. The dissolution was more influenced by the technology than by the form of API but even tablets with dissimilar profiles were bioequivalent. This is probably due to the precipitation of WSA and WSC in the stomach on a poorly soluble acidic form, which subsequently dissolves in the neutral environment of the small intestine. Recrystallization was demonstrated in the in vitro assay a a pH of 1.2 and 4.5 using Raman spectroscopy and X-ray diffraction. In summary, the content uniformity appears to be the main factor affecting the safety of the treatment.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

20602 - Medical laboratory technology (including laboratory samples analysis; diagnostic technologies) (Biomaterials to be 2.9 [physical characteristics of living material as related to medical implants, devices, sensors])

Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2018

Kód důvěrnosti údajů

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

Název periodika

European Journal of Pharmaceutical Sciences

ISSN

0928-0987

e-ISSN

—

Svazek periodika

125

Číslo periodika v rámci svazku

DEC

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

10

Strana od-do

120-129

Kód UT WoS článku

000448169800013

EID výsledku v databázi Scopus

2-s2.0-85054244270