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Updated: Jan 11, 2026
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Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS
Published on: November 8, 2015
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Design expert analysis of tacrolimus compatibility with common excipients
Sara Sajjadi1,2, Ali Shayanfar3, Mohammadreza Siahi-Shadbad2
1Student Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran.
Drug Development and Industrial Pharmacy
|November 10, 2025
Summary
Tacrolimus degradation is accelerated by humidity, temperature, and excipient ratios. Magnesium stearate showed unique interactions, necessitating careful formulation considerations for tacrolimus stability.
Area of Science:
- Pharmaceutical Sciences
- Drug Formulation
- Chemical Engineering
Background:
- Tacrolimus is a vital immunosuppressant for organ transplantation and autoimmune diseases.
- Excipient compatibility is crucial for stable drug formulations.
- Limited data exists on tacrolimus compatibility with common pharmaceutical excipients.
Purpose of the Study:
- To evaluate the compatibility of tacrolimus with sodium croscarmellose, hydroxypropyl methylcellulose (HPMC), magnesium stearate, and lactose monohydrate.
- To determine the impact of temperature, relative humidity (RH), and drug-to-excipient ratio on tacrolimus stability.
- To assess physicochemical interactions using DSC and FT-IR.
Main Methods:
- Design of Experiments (DOE) approach with 14 runs.
- Tacrolimus blended with excipients at varying ratios.
- Storage under controlled temperature and RH, followed by HPLC analysis for residual tacrolimus.
- Differential Scanning Calorimetry (DSC) and Fourier-Transform Infrared (FT-IR) spectroscopy for interaction analysis.
Main Results:
- Increased RH significantly accelerated tacrolimus degradation across all excipients.
- Higher temperature and drug-to-excipient ratios generally decreased residual tacrolimus, except with magnesium stearate.
- DSC showed no significant changes, but FT-IR indicated specific interactions between tacrolimus and magnesium stearate.
Conclusions:
- Tacrolimus stability is sensitive to humidity, temperature, and excipient ratios.
- Magnesium stearate exhibits unique physicochemical interactions with tacrolimus.
- Careful selection of excipients, particularly magnesium stearate, is essential for developing stable tacrolimus formulations.
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