Use of phyllosilicate clay mineral to increase solubility olanzapine

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• 作者：M. L. C. M. Gonçalves ; M. A. M. Lyra…
• 关键词：Phyllosilicate ; Olanzapine ; Increased solubility ; New excipient ; Drug delivery
• 刊名：Journal of Thermal Analysis and Calorimetry
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：127
• 期：2
• 页码：1743-1750
• 全文大小：
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Physical Chemistry; Analytical Chemistry; Polymer Sciences; Inorganic Chemistry; Measurement Science and Instrumentation;
• 出版者：Springer Netherlands
• ISSN：1588-2926
• 卷排序：127

文摘

Phyllosilicates have interesting properties, such as high capacity of ion exchange, adsorption, physicochemical stability and low/null toxicity, and thus, they are a promising material in pharmaceutical studies. Olanzapine (OLZ), used in the treatment of schizophrenia, is a drug of high cost and low water solubility, which are an obstacle to its use. In this work, an oral delivery system was developed using phyllosilicate (PHY-NT) and OLZ together to increase its solubility. PHY-NT was synthesized by sol–gel method, and then, OLZ was adsorbed creating the system called PHY-NT:OLZ. Thermal analysis was performed to investigate possible interactions between olanzapine and phyllosilicate. a sharp endothermic peak at 468 K was observed, which corresponds to the melting process of OLZ. When OLZ was added to PHY-NT, this peak was absent, suggesting an efficient denaturation of its crystal lattice. FTIR spectroscopy and X-ray powder diffraction were performed as complementary techniques to adequately support thermal analysis results. The created system caused a considerable increase in OLZ dissolution efficiency, and more than 80 % of the drug was released from PHY-NT:OLZ after 20 min. Drug release was evaluated in vitro and showed a Fickian diffusion-based pattern. Thus, results suggest that PHY-NT can be used as an alternative to increase drug dissolution rate of OLZ, expanding applications of these materials.