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Vaporization01:18

Vaporization

The physical form of a substance changes by changing its temperature. For example, raising the temperature of a liquid causes the liquid to vaporize (convert into vapor). The process is called vaporization—a surface phenomenon. For vaporization to occur, kinetic energy must be greater than the intermolecular forces that keep molecules bonded. The amount of energy needed to vaporize a quantity of liquid at a given pressure and a constant temperature is called the heat of vaporization. When...
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Formulation and Characterization of Bioactive Agent Containing Nanodisks
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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
PubMed
Summary
This summary is machine-generated.

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.

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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.