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Characterization of olanzapine-solid dispersions.

Venkateskumar Krishnamoorthy, Arunkumar Nagalingam, Verma Priya Ranjan Prasad

Iranian Journal of Pharmaceutical Research : IJPR

|December 24, 2013

Summary

Solid dispersion technique significantly enhances olanzapine

Keywords:

Differential scanning calorimetry Fourier transform infrared spectroscopy.Near infra red spectroscopy Pregelatinised starch Sodium starch glycollate X ray diffraction

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Area of Science:

Pharmaceutical Technology
Drug Delivery Systems

Background:

Olanzapine exhibits poor aqueous solubility, limiting its therapeutic efficacy.
The solid dispersion technique offers a promising approach to improve the solubility of poorly soluble drugs.

Purpose of the Study:

To enhance the aqueous solubility and dissolution rate of olanzapine.
To evaluate the effectiveness of pregelatinised starch (PGS) and sodium starch glycollate (SSG) as carriers for olanzapine solid dispersions.

Main Methods:

Solid dispersions of olanzapine were prepared using PGS and SSG at various drug-carrier ratios (1:1 to 1:10) via the dispersion method.
Characterization involved phase solubility, in-vitro release, saturation solubility, permeation, wettability, X-ray diffraction (XRD), and Fourier-transform infrared (FTIR) spectroscopy.

Main Results:

Solid dispersions demonstrated significantly higher solubility and improved in-vitro drug release compared to pure olanzapine.
The optimal drug-polymer ratio of 1:10 (olanzapine:carrier) yielded the best release profile.
XRD and FTIR analyses confirmed reduced crystallinity and carrier inertness, respectively.

Conclusions:

Pregelatinised starch (PGS) and sodium starch glycollate (SSG) are effective carriers for improving the aqueous solubility of olanzapine.
The solid dispersion technique is a viable strategy for enhancing the dissolution and bioavailability of poorly soluble drugs like olanzapine.