Evolution of the interaction of a new chemical entity, eflucimibe, with gamma-cyclodextrin during kneading process

Abstract : The aim of this study was to enhance the low solubility of eflucimibe, a new chemical entity which can be used as medicine to treat dyslipidemiae, by complexation with gamma-cyclodextrin. The complex was prepared using kneading method. The interaction evolution was studied during process by comparison of the semi-solid and physico-chemical states of the product. The evolution of the semi-solid state was followed by torque measurement when the evolution of physico-chemical state was studied by differential scanning calorimetry, infrared spectroscopy and by determination of the drug solubilisation profile. The interaction, which occurs during the process, is characterised by a modification of the product consistency and by a disappearance of the drug endothermic peaks, a disappearance of a drug spectral band and a widely improvement of the drug solubilisation profile. Indeed, after complete interaction, the drug quantity solubilised in specific conditions increased about 44-fold compared to those of untreated drug. Moreover, the comparison of the physico-chemical and semi-solid states during kneading process clearly shows that when the interaction takes place, a solidification of the paste occurs. The results of these works suggested that the formation of new solid phase allows an enhancement of the solubility of eflucimibe.
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A Gil, Alain Chamayou, E Leverd, J Bougaret, Michel Baron, et al.. Evolution of the interaction of a new chemical entity, eflucimibe, with gamma-cyclodextrin during kneading process. European Journal of Pharmaceutical Sciences, Elsevier, 2004, 23 (2), p.123-129. ⟨10.1016/j.ejps.2004.06.002⟩. ⟨hal-01632796⟩

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