Investigation of the compatibility between kaempferol and excipients by thermal, spectroscopic and chemometric methods
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Investigation of the compatibility between kaempferol and excipients by thermal, spectroscopic and chemometric methods Gabriela de Lima Melchiades1 · Valéria Weiss Angeli2 · Mariana Colombo1 · Letícia Scherer Koester1 Received: 28 May 2019 / Accepted: 23 November 2019 © Akadémiai Kiadó, Budapest, Hungary 2019
Abstract Compatibility is an important step in pre-formulation studies during the development of solid dosage forms. In the present study, we used thermal analysis (differential scanning calorimetry and thermogravimetry), isothermal stress testing followed by high-performance liquid chromatography and Fourier transform infrared spectroscopy complemented by two multivariate techniques (hierarchical cluster analysis and principal component analysis) to detect potential incompatibilities between kaempferol and commonly used solid dosage form excipients in binary mixtures. The excipients that were studied were starch, microcrystalline cellulose, magnesium stearate, hydroxypropylmethylcellulose, lactose, sodium lauryl sulfate and polyvinylpyrrolidone. The thermal analyses results indicated interactions occurred between kaempferol and all excipients studied except microcrystalline cellulose. However, infrared spectroscopy complemented by multivariate analysis indicated compatibility between kaempferol and all excipients. Isothermal stress testing confirmed the absence of significant change in the content of kaempferol in the binary mixtures. Our study demonstrates the importance of combining different techniques and multivariate data analysis for pre-formulation drug-excipient analysis. Keywords Kaempferol · Excipients · Compatibility · Thermal analysis · Cluster analysis · Principal component analysis
Introduction The quality of a pharmaceutical formulation depends not only on the choice of active substance and the production process, but also on the appropriate selection of excipients [1–3]. In the pre-formulation stage of development, the study of drug-excipient compatibility is one of the most important steps as it enhances the understanding of drug-excipient interactions and highlights changes in the physical or chemical properties of the drug and/or therapeutic response [3–5]. Compatibility screening involves the analysis of mixtures of the drug with one or more excipients.
* Letícia Scherer Koester [email protected] 1
Laboratório de Desenvolvimento Galênico, Programa de Pós‑Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752/607, Porto Alegre, RS 90.610‑000, Brazil
Programa de Pós‑Graduação em Engenharia de Processos e Tecnologias, Universidade de Caxias do Sul - Campus-Sede, Caxias do Sul, RS, Brazil
2
Thermoanalytical techniques such as differential scanning calorimetry (DSC) and thermogravimetry (TG) are used for a quick screening due to their ease of use [6, 7]. Although spectroscopic techniques such as Fourier transform infrared spectroscopy (FTIR) are also easily conducted, the volumes of data that are generated
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