Pharmaceutics 2013, 5(4), 570-590; doi:10.3390/pharmaceutics5040570

Design of Olanzapine/Lutrol Solid Dispersions of Improved Stability and Performances

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Received: 3 September 2013; in revised form: 11 October 2013 / Accepted: 14 October 2013 / Published: 25 October 2013
(This article belongs to the Special Issue Solid State Chemistry of Drugs)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: Eleven solid dispersions containing olanzapine, with carriers of different composition (Lutrol® F68, Lutrol® F127, Gelucire® 44/14), were prepared and examined by thermal (differential scanning calorimetry (DSC); thermomicroscopy (HSM)) and X-ray diffraction (XRD) analysis, both as fresh or aged (one year) samples. Drug and carriers were preliminarily selected in order to avoid problems related to the aging of the formulation, according to the solubility parameters of carriers and drug. These parameters make it possible to predict the low solubility of olanzapine in the carriers (alone or in mixtures). Systems containing only Lutrol (also in the presence of Transcutol®) contain the drug in the form of particles of reduced size and in a crystalline form. Gelucire® 44/14 apparently increases the amount of olanzapine dissolved in the solid carrier, but this is presumed to be a metastable state, probably related to the heterogeneous nature of the carrier that delays crystallization of the drug. The high hydrophilicity of the carriers proves suitable to an accelerated and quick release of the drug regardless of aging. Differences in the release profiles between Lutrol- and Gelucire-containing systems were interpreted in terms of the formation of polymer micelles by the Lutrols when in aqueous solution.
Keywords: olanzapine; solid dispersion; Lutrol® F68 and Lutrol® F127; Gelucire® 44/14; DSC; HSM; XRD; stability; accelerated release
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MDPI and ACS Style

Cavallari, C.; Fini, A.; Ceschel, G. Design of Olanzapine/Lutrol Solid Dispersions of Improved Stability and Performances. Pharmaceutics 2013, 5, 570-590.

AMA Style

Cavallari C, Fini A, Ceschel G. Design of Olanzapine/Lutrol Solid Dispersions of Improved Stability and Performances. Pharmaceutics. 2013; 5(4):570-590.

Chicago/Turabian Style

Cavallari, Cristina; Fini, Adamo; Ceschel, Giancarlo. 2013. "Design of Olanzapine/Lutrol Solid Dispersions of Improved Stability and Performances." Pharmaceutics 5, no. 4: 570-590.

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