Drug Discov Ther. 2011;5(6):311-318. (DOI: 10.5582/ddt.2011.v5.6.311)

Preparation and evaluation of fenoterol hydrobromide suppositories.

Ghorab D, Refai H, Tag R

Fenoterol HBr is a bronchodilator known to be subject to first pass effect after oral administration. The aim of this study was to prepare and evaluate fenoterol HBr suppositories. Suppositories were prepared by a fusion method using different fatty bases, viz. Witepsol H15, Witepsol E75, Suppocire AP, and Suppocire BM, as well as different hydrophilic bases, viz. polyethylene glycol and poloxamer bases. In vitro release studies revealed a greater release of the drug from hydrophilic bases than from fatty bases. The effect of incorporating different types and concentrations of non-ionic surfactants (Tween 60 and Span 20) on the release rate of the drug from Witepsol H15, as a model fatty base, was investigated. Results showed an enhanced release at low surfactant concentrations. A very fast 100% drug release was achieved when the drug was incorporated as an aqueous solution in Witepsol H15 (F17). This formula was selected to test the effect of fenoterol HBr suppositories on histamine-induced bronchospasms in Guinea pigs. No dyspnea of the animals was recorded for up to 30 min. In addition, thermogel liquid suppositories of different poloxamer 188 and poloxamer 407 proportions in the presence of sodium alginate as a mucoadhesive polymer were prepared. The different formulations behaved similarly concerning sustainment of drug release, however, only the formula containing 15% poloxamer 188 and 25% poloxamer 407 (F20) showed optimal gelation at body temperature. In conclusion, among the studied suppository bases there are bases suitable for fast release of the drug like F17 and hydrophilic bases especially polyethylene glycol, as well as other bases for sustained release applications of fenoterol HBr like fatty and thermogel bases.

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