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Published on: March 17, 2023
Vapor-induced phase transformations in docetaxel
Lakshmi Kumar Tatini1, K V S R Krishna Reddy, N Someswara Rao
1Analytical Development, Aptuit Laurus Pvt. Ltd., ICICI Knowledge Park, Turkapally, Shameerpet, Hyderabad, 500 078, India. kumarltatini@gmail.com
AAPS Pharmscitech
|April 6, 2012
Summary
Vapor-induced transformations of docetaxel anhydrous yielded new solid forms, including solvates and hydrates. These novel docetaxel forms were fully characterized using advanced analytical techniques.
Area of Science:
- Solid-state chemistry
- Pharmaceutical science
- Materials science
Background:
- Docetaxel anhydrous (form D(A)) is a crucial pharmaceutical agent.
- Understanding its solid-state transformations is vital for drug formulation and stability.
- Previous studies may not have fully explored vapor-induced transformations under ambient conditions.
Purpose of the Study:
- To investigate the vapor-induced transformations of docetaxel anhydrous (form D(A)) using different solvent vapors.
- To identify and characterize any new solid forms generated during these transformations.
- To elucidate the structural and thermodynamic properties of the newly formed docetaxel entities.
Main Methods:
- Powder X-ray diffractometry (PXRD) for online monitoring and structural analysis.
- Differential Scanning Calorimetry (DSC) for thermal property assessment.
- Thermogravimetric Analysis (TGA) for evaluating thermal stability and solvent content.
- Spectroscopic techniques including solid-state NMR ((13)C SSNMR), solution NMR ((1)H NMR), and FTIR for structural elucidation.
Main Results:
- Docetaxel anhydrous (form D(A)) underwent transformations when exposed to methanol, ethanol, and water vapors.
- New solid forms were successfully obtained in defined stoichiometric ratios.
- Identified new forms include methanol solvate (D(M)), ethanol solvate (D(E)), monohydrate (D(MH)), trihydrate (D(TH)), and two new anhydrous forms (D(AN-I) and D(AN-II)).
- Comprehensive characterization confirmed the distinct structural and thermal properties of these novel forms.
Conclusions:
- Vapor-induced transformations offer a viable route to generate novel solid forms of docetaxel.
- The identified solvates, hydrates, and anhydrous forms possess unique characteristics.
- This research expands the understanding of docetaxel's solid-state behavior, impacting its pharmaceutical development.
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