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Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

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Solid-state characterization of nevirapine.

Mahua Sarkar¹, O P Perumal, R Panchagnula

¹Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER) Sector 67, S. A. S Nagar-160 062, India.

Indian Journal of Pharmaceutical Sciences

|March 12, 2011

Summary

This study characterized nevirapine solid-state properties. Recrystallization yielded different crystal habits but not new polymorphs, with compression influencing crystal form and desolvation.

Keywords:

Desolvation nevirapine powder dissolution solid state solvates

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Area of Science:

Pharmaceutical Sciences
Solid-State Chemistry

Background:

Nevirapine is a crucial antiretroviral medication.
Understanding its solid-state properties is vital for formulation and bioavailability.

Purpose of the Study:

To characterize nevirapine from commercial and recrystallized samples.
To investigate the impact of crystallization conditions and compression on its solid-state behavior.

Main Methods:

Solid-state characterization using microscopy, DSC, TGA, FTIR, and PXRD.
Dissolution studies at varying pH and particle sizes.
Analysis of recrystallized samples from different solvent systems.

Main Results:

Commercial nevirapine exhibited a consistent polymorphic form and anhedral habit.
Recrystallization yielded varied crystal habits and weak solvates, but no new polymorphs.
Dissolution rates were pH-dependent and affected by crystallization and compression.

Conclusions:

Nevirapine's solid-state properties are sensitive to crystallization and compression.
Compression can induce desolvation and polymorphic conversion.
Amorphous nevirapine shows slightly enhanced aqueous solubility compared to the crystalline form.