Screening paediatric rectal forms of azithromycin as an alternative to oral or injectable treatment

Abstract

Graphical abstract

Pharmaceutical development and optimization of azithromycin suppository for paediatric use

“…Work conducted in our laboratory (Kauss et al, 2012) had investigated options for a paediatric rectal formulation of azithromycin (AZ). The rectal route is acceptable in the targeted countries (Simba et al, 2009; Thera et al, 2007), and can be used in both uncomplicated and complicated (“non-per-os” cases); there is evidence, for instance, that rectal artesunate can save lives in case of malaria (Gomes et al, 2009).…”

“…In order to improve AZ bioavailability (Kauss et al, 2012) we tried: (i) enhancing viscosity and muco-adhesiveness to prolong the residence time with rectal gels, (ii) dry form formulated as rectal capsule, and (iii) enhancing solubility with solid dispersion suppositories. Fatty-base suppositories were excluded because their low melting point makes them incompatible with tropical conditions.…”

“…Fatty-base suppositories were excluded because their low melting point makes them incompatible with tropical conditions. The most promising prototype was the suspended AZ PEG suppositories based on solid dispersion approach, which attained 28% bioavailability (Kauss et al, 2012). In a solid dispersion, active ingredients are dispersed in an inert carrier or matrix of solid state, prepared by melting, solvent or melting-solvent method (Chiou and Riegelman, 1971).…”

Preliminary pharmaceutical development of antimalarial–antibiotic cotherapy as a pre-referral paediatric treatment of fever in malaria endemic areas

“…Compared to previously described AZ monotherapies (Kauss et al, 2013, 2012), HGC parameters were comparable (107% and 105% of relative bioavailability for AZ HGC in monotherapy and cotherapy respectively), but AZ HGC absorption was lower than the one obtained with AZ suppository (232% of relative bioavailability after 24 h) (Kauss et al, 2012). In conclusion, AZAM HGC provided AZ absorption comparable to the one obtained with rectal oily suspension, but did not enhance it.…”

Quantification of three macrolide antibiotics in pharmaceutical lots by HPLC: Development, validation and application to a simultaneous separation

“…Several HPLC methods for the individual analysis of macrolides in a variety of matrices including raw material, pharmaceutical dosage forms, biological fluids and various tissues have been reported (Kanfer et al, 1998;Nasr and Tscchappler, 1996; Research Article Kauss et al, 2012;Cao et al, 2013), merely for erythromycin and occasionally for the other macrolides. Unfortunately, most official methods for the analysis of macrolides are mainly antimicrobial assays (Mahmoudi et al, 2015;British Pharmacopoeia, 1998;Official Methods for Residual Substances in Livestock Products, 1994), which they suffer from many disadvantages as the long incubation periods and the lack of sensitivity.…”