![]() ![]() Our preliminary results, supported by the literature reports (2), showed that cetirizine does not degrade under acidic or basic conditions. However, cetirizine formulated in PEG-containing solution for Softgels was found to degrade during manufacture and storage. In order to develop this highly water soluble and sensitive compound in soft gelatin dosage form, cetirizine was formulated in PEG-containing matrix. Softgel dosage forms are perceived by customers as easier to swallow, help to mask the taste of the medicine and provide faster onset of action (1). Many problems associated with tableting, including poor compaction and lack of content or weight uniformity, can be eliminated if drug is incorporated into this dosage form. A softgel can therefore contain the active ingredient in solution, suspension or emulsion, which may inherently lead to better absorption of the active ingredient compared to the delivery in a tablet or powder. Soft gelatin capsules (Softgels) offer the possibility of delivering a liquid in a solid oral dosage form. INTRODUCTION Cetirizine hydrochloride (cetirizine), the active component of ZYRTEC® tablets and syrup, is an orally active and selective H1-receptor antagonist used for the treatment of allergy symptoms. Fatmi Banner Pharmacaps, 4125 Premier Drive, High Point, North Carolina 27265, USA e-mail: ![]() ![]() Selective oxidation of cetirizine and isolation/characterization of the oxidation product allowed the identification of the oxidation product as cetirizine N-oxide. Conclusions Degradation of cetirizine in polyethylene glycol arose from the reaction between the drug and the reactive peroxide intermediates such as peroxyl radicals formed through oxidation of PEG. The finding was verified by spiking of cetirizine degradation sample with cetirizine N-oxide reference standard. ![]() Site of oxidation is proposed based on correlation of the results of forced degradation with ionization scheme of cetirizine. Results Oxidation process was investigated in order to model the degradation of cetirizine in PEG-containing formulation. The reaction mixture was purified, and the isolated material was analyzed by 1H NMR. Additionally, pure cetirizine was subjected to selective oxidization by hydrogen peroxide and sodium percarbonate. Methods Cetirizine, formulated in PEG-containing matrix, was subjected to forced degradation conditions in the pH range from 3 to 10, and the product was analyzed by HPLC and LC-MS/MS. Received: / Accepted: 24 November 2009 / Published online: 31 March 2010 # Springer Science+Business Media, LLC 2010ĪBSTRACT Purpose The goal of the study was to isolate and analyze a cetirizine degradation product, formed within a PEG-containing formulation and to elucidate the mechanism of oxidation of cetirizine. Isolation and Characterization of Cetirizine Degradation Product: Mechanism of Cetirizine Oxidation Tatyana Dyakonov & April Muir & Hassen Nasri & Dana Toops & Aqeel Fatmi ![]()
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