Comparison of X-ray powder diffraction and solid-state nuclear magnetic resonance in estimating crystalline fraction of tacrolimus in sustained-release amorphous solid dispersion and development of discriminating dissolution method

Journal of Pharmaceutical Sciences
Ziyaur RahmanMansoor A Khan

Abstract

The focus of present investigation was to explore X-ray powder diffraction (XRPD) and solid-state nuclear magnetic resonance (ssNMR) techniques for amorphous and crystalline tacrolimus quantification in the sustained-release amorphous solid dispersion (ASD), and to propose discriminating dissolution method that can detect crystalline drug. The ASD and crystalline physical mixture was mixed in various proportions to make sample matrices containing 0%-100% crystalline-amorphous tacrolimus. Partial-least-square regression and principle component regression were applied to the spectral data. Dissolution of the ASD in the US FDA recommended dissolution medium with and without surfactant was performed. R(2) > 0.99 and slope was close to one for all the models. Root-mean-square of prediction, standard error of prediction, and bias were higher in ssNMR-based models when compared with XRPD data models. Dissolution of the ASD decreased with an increase in the crystalline tacrolimus in the formulations. Furthermore, detection of crystalline tacrolimus in the ASD was progressively masked with an increase in the surfactant level in the dissolution medium. XRPD and ssNMR can be used equally to quantitate the crystalline and amorphous fractio...Continue Reading

References

Oct 9, 1999·Journal of Pharmaceutical Sciences·T KristmundsdóttirH Thormar
Aug 1, 2000·International Journal of Pharmaceutics·M A Repka, J W McGinity
Nov 1, 2005·Journal of Pharmaceutical Sciences·Thomas J OfferdahlEric J Munson
Aug 5, 2006·Solid State Nuclear Magnetic Resonance·Dewey H BarichEric J Munson
Jun 26, 2007·Solid State Nuclear Magnetic Resonance·Jason R WickhamCharles V Rice
Jun 6, 2009·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Sandrien JanssensGuy Van den Mooter
Oct 26, 2011·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Jian X WuJukka Rantanen
Nov 1, 2011·International Journal of Pharmaceutics·Ziyaur RahmanMansoor A Khan
Nov 22, 2011·International Journal of Pharmaceutics·Ahmed S ZidanMansoor A Khan
Jan 4, 2012·Journal of Pharmaceutical Sciences·Ann NewmanGeorge Zografi

❮ Previous
Next ❯

Citations

Dec 30, 2015·Advanced Drug Delivery Reviews·Seema ThakralRaj Suryanarayanan
Oct 25, 2016·International Journal of Pharmaceutics·Dariusz Maciej PisklakŁukasz Szeleszczuk
May 5, 2020·Drug Development and Industrial Pharmacy·Naseem A CharooZiyaur Rahman

❮ Previous
Next ❯

Related Concepts

Related Feeds

Autism

Autism spectrum disorder is associated with challenges with social skills, repetitive behaviors, and often accompanied by sensory sensitivities and medical issues. Here is the latest research on autism.