Detail publikace

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

FRANC, A. MUSELÍK, J. ZEMAN, J. LUKÁŠOVÁ, I. KURHAJEC, S. BARTONÍČKOVÁ, E. GALVÁNKOVÁ, L. MIKA, F. MARTIN, D. VETCHÝ, D.

Originální název

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

Typ

článek v časopise ve Web of Science, Jimp

Jazyk

angličtina

Originální abstrakt

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

Klíčová slova

Warfarin sodium; Polymorphism; Dissolution; Raman spectroscopy; X-ray; Generic substitution

Autoři

FRANC, A.; MUSELÍK, J.; ZEMAN, J.; LUKÁŠOVÁ, I.; KURHAJEC, S.; BARTONÍČKOVÁ, E.; GALVÁNKOVÁ, L.; MIKA, F.; MARTIN, D.; VETCHÝ, D.

Vydáno

1. 12. 2018

Nakladatel

ELSEVIER SCIENCE BV,

Místo

AMSTERDAM, NETHERLANDS

ISSN

0928-0987

Periodikum

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Číslo

125

Stát

Nizozemsko

Strany od

120

Strany do

129

Strany počet

10

URL

http://apps.webofknowledge.com/full_record.do?product=WOS&search_mode=GeneralSearch&qid=1&SID=E1ef4BtSpJKfeCobRUR&page=1&doc=1

BibTex

@article{BUT151263,
  author="Aleš {Franc} and Jan {Muselík} and Jiří {Zeman} and Ivana {Lukášová} and Slavomír {Kurhajec} and Eva {Bartoníčková} and Lucie {Dlabajová} and Filip {Mika} and Dominik {Martin} and David {Vetchý}",
  title="The effect of amorphous and crystal sodium warfarin and its content uniformity on bioequivalence of tablets",
  journal="EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES",
  year="2018",
  number="125",
  pages="120--129",
  doi="10.1016/j.ejps.2018.09.022",
  issn="0928-0987",
  url="http://apps.webofknowledge.com/full_record.do?product=WOS&search_mode=GeneralSearch&qid=1&SID=E1ef4BtSpJKfeCobRUR&page=1&doc=1"
}