<abstract xmlns="http://www.w3.org/1999/xhtml"><p>An ultra-high performance liquid chromatography method for simultaneous determination of tacrolimus impurities in pharmaceutical dosage forms has been developed. Appropriate chromatographic separation was achieved on a BEH C<sub>18</sub> column using gradient elution with a total run time of 14 min. The method was applied to analyses of commercial samples and was validated in terms of linearity, precision, accuracy, sensitivity and specificity. It was found to be linear, precise and accurate in the range of 0.05 to 0.6 % of the impurities level in pharmaceutical dosage forms. Stability indicating power of the method was demonstrated by the results of forced degradation studies. The forced degradation study in solution revealed tacrolimus instability under stress alkaline, thermal, light and photolytic conditions and in the presence of a radical initiator or metal ions. The drug was stable at pH 3–5. Solid-state degradation studies conducted on amorphous tacrolimus demonstrated its sensitivity to light, elevated temperature, humidity and oxidation.</p></abstract>

An ultra-high performance liquid chromatography method for simultaneous determination of tacrolimus impurities in pharmaceutical dosage forms has been developed. Appropriate chromatographic separation was achieved on a BEH C18 column using gradient elution with a total run time of 14 min. The method was applied to analyses of commercial samples and was validated in terms of linearity, precision, accuracy, sensitivity and specificity. It was found to be linear, precise and accurate in the range of 0.05 to 0.6 % of the impurities level in pharmaceutical dosage forms. Stability indicating power of the method was demonstrated by the results of forced degradation studies. The forced degradation study in solution revealed tacrolimus instability under stress alkaline, thermal, light and photolytic conditions and in the presence of a radical initiator or metal ions. The drug was stable at pH 3–5. Solid-state degradation studies conducted on amorphous tacrolimus demonstrated its sensitivity to light, elevated temperature, humidity and oxidation.

Forced degradation of tacrolimus and the development of a UHPLC method for impurities determination

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

An ultra-high performance liquid chromatography method for simultaneous determination of tacrolimus impurities in pharmaceutical dosage forms has been...

Forced degradation of tacrolimus and the development of a UHPLC method for impurities determination

Publié en ligne: 26 juin 2019

Pages: 363 - 380

Accepté: 29 déc. 2018

DOI: https://doi.org/10.2478/acph-2019-0025

Mots clés
tacrolimus, forced degradation, UHPLC, impurities, stability

© 2019 Tanja Rozman Peterka et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Forced degradation of tacrolimus and the development of a UHPLC method for impurities determination

Publié en ligne: 26 juin 2019

Pages: 363 - 380

Accepté: 29 déc. 2018

DOI: https://doi.org/10.2478/acph-2019-0025

Mots cléstacrolimus, forced degradation, UHPLC, impurities, stability

© 2019 Tanja Rozman Peterka et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Mots clés
tacrolimus, forced degradation, UHPLC, impurities, stability