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Design of Olanzapine/Lutrol Solid Dispersions of Improved Stability and Performances
Department FABIT, University of Bologna, Via San Donato 15, 40127 Bologna, Italy
Montefarmaco OTC S.p.A., Bollate-Milan 20021, Italy
* Author to whom correspondence should be addressed.
Received: 3 September 2013; in revised form: 11 October 2013 / Accepted: 14 October 2013 / Published: 25 October 2013
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.
Cavallari C, Fini A, Ceschel G. Design of Olanzapine/Lutrol Solid Dispersions of Improved Stability and Performances. Pharmaceutics. 2013; 5(4):570-590.
Cavallari, Cristina; Fini, Adamo; Ceschel, Giancarlo. 2013. "Design of Olanzapine/Lutrol Solid Dispersions of Improved Stability and Performances." Pharmaceutics 5, no. 4: 570-590.