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Title: Development of rectal self-emulsifying suspension of a moisture-labile water-soluble drug
Authors: Tina Kauss
Alexandra Gaubert
Luc Tabaran
Giovanni Tonelli
Thida Phoeung
Marie Hélène Langlois
Nick White
Anthony Cartwright
Melba Gomes
Karen Gaudin
Université de Bordeaux
Organisation Mondiale de la Santé
University of Oxford
Mahidol University
Global Regulatory Solutions
Keywords: Pharmacology, Toxicology and Pharmaceutics
Issue Date: 30-Jan-2018
Citation: International Journal of Pharmaceutics. Vol.536, No.1 (2018), 283-291
Abstract: © 2017 Self-emulsifying drug delivery systems, commonly used for oral delivery of poorly soluble compounds, were used to formulate water soluble but moisture labile compounds for rectal application. The objective was to use the oily phase of the system to formulate a liquid, non-aqueous product while obtaining the advantages of self-emulsification, rapid contact with the rectal mucosa and rapid absorption post-administration. Ceftriaxone was used as a model drug and the human bile salt sodium chenodeoxycholate was used as an absorption enhancer. After preliminary screening of 23 excipients, based on their emulsification ability and emulsion fineness in binary and ternary mixtures, a full factorial design was used to screen different formulations of three preselected excipients. The optimal formulation contained 60% of excipients, namely Capryol 90, Kolliphor EL and Kolliphor PS20 in 4: 6: 6 ratio and 40% of a powder blend that included 500 mg of ceftriaxone. Characterization of the system showed that it complied with the requirements for rectal administration, in particular rapid emulsification in a small quantity of liquid. Rabbit bioavailability showed rapid absorption of ceftriaxone, achieving 128% bioavailability compared to powder control formulation. These results demonstrated the potential of self-emulsifying formulations for rectal administration of Class 3 BCS drugs.
ISSN: 18733476
Appears in Collections:Scopus 2018

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