Definition of a Solvent System for Spherical Crystallization of Salbutamol Sulfate by Quasi-Emulsion Solvent Diffusion (QESD) Method

International audienceIn this paper we describe how the spherical crystallization process by QESD method can be applied to a water-soluble drug, salbutamol sulfate. The type of solvent, antisolvent, and emulsi®er and the concentration of emulsi®er to be used for the production of spherical particles with a size range 80±500 mm are determined. Furthermore, the solvent/antisolvent ratio and the temperature difference between them (DT) are studied. It was observed that, in the case of salbutamol sulfate, the DT value has no in¯uence on the formation of spherical particles. A very large metastable zone of salbutamol sulfate in water could explain this phenomenon. Finally, the in¯uence of emulsi®er concentration and of maturation time on the size of spherical particles is studied. The results show that these two parameters must be ®xed to control the size of the recovered particles

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

International audienceThe 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

Preliminary evaluation of primaquine activity on rodent malaria model after transdermal administration

The aim of this preliminary study was to investigate the potential use of the transdermal route for primaquine administration in the treatment of malaria. Thus the activity of this drug on asexual blood forms of two rodent malaria parasites (P. v. petteri and P. y. nigeriensis) was evaluated following a single TTS patch application. Sustained plasma concentration values wete observed for about 60 hours. The results obtained from a prepotency test showed that primaquine was more active towards P. v.petteri than P. y. nigeriensis. This preliminary study showed that the transdermal route for primaquine administration may be a promising strategy for improving the treatment of malaria in both causal prophylactic and prevention of relapses infection

Les substances alimentaires filmogènes

National audienc