betadex and maropitant

Sulfobuthylether-beta-cyclodextrin (SBECD) is a substituted derivative of a cyclic oligosaccharide containing seven glucopyranose units, which bear pH-independent negative charges because of sulfonate groups. This derivative has better solubility and toxicological characteristics than the unsubstituted beta-cyclodextrin, and the presence of sulfobuthyl groups opens new dimensions in the interactions acting the part of the complex formation. These create opportunities for the pharmaceutical applications of this compound. Currently six pharmaceutical preparations circulate--moiety of these circulates in Hungary also--which have a composition containing SBECD as pharmaceutical excipient. Out of the main effects of the complex-forming agent the solubility enhancement is utilized in these compositions to achieve the solution of a therapeutic dose in the case of intravascular administration. Available experimental evidences and published patents are indicative of broadening the circle of the applications in point of both technological advantages and dosage forms.

Topics: Amiodarone; Animals; Anti-Arrhythmia Agents; Antiemetics; Antifungal Agents; Antipsychotic Agents; Aripiprazole; beta-Cyclodextrins; Chemistry, Pharmaceutical; Dosage Forms; Drug Stability; Humans; Hungary; Multiple Myeloma; Oligopeptides; Piperazines; Pyrimidines; Quinolones; Quinuclidines; Solubility; Thiazoles; Triazoles; Voriconazole

Injection pain has been associated with veterinary use of the antiemetic maropitant (Cerenia, Pfizer Animal Health). Cerenia is formulated using sulphobutylether-beta-cyclodextrin to bind maropitant and mitigate injection pain. The objective of this study was to determine whether the temperature of Cerenia alters binding between maropitant and sulphobutylether-beta-cyclodextrin and affects injection pain. Binding decreased as temperature increased, and Cerenia-elicited injection pain increased at warmer drug temperatures. These data suggest that the amount of free unbound maropitant increases with temperature and that injection pain increases with temperature in a similar fashion. Clinically, these studies suggest that injection of refrigerated Cerenia may significantly reduce or eliminate pain associated with SC injection of Cerenia.

Topics: Animals; Antiemetics; beta-Cyclodextrins; Dog Diseases; Dogs; Excipients; Pain; Quinuclidines; Refrigeration