Advancing In Antihistamine Delivery Systems: A Preclinical Evaluation of Levocetrizine Dihydrochloride Oral Spray
Year: 2025
Type: article
Abstract: Objective: Levocetirizine dihydrochloride is also known as “Xyzol.” Levocetirizine dihydrochloride is a second-generation piperazine derivative, potent H1 selective agent. Levocetirizine dihydrochloride is the active R (-) enantiomer of cetirizine dihydrochloride. In the case of an allergic or histaminic reaction, the medication must respond rapidly. Many older patients, infants, and dysphagia patients have trouble swallowing traditional tablets or capsules. Hence, a need exists for a relatively fast-acting oral spray form. Methods: The oral spray were prepared by direct dissolving drug component into water with added buffering agents, sweetening agent, preservative and flavors. The oral spray was evaluated for general parameters like Appearance, Odor, pH and solution clarity. Then, the spray was filled in suitable plastic container having the spray device. Oral spray was evaluated for comparative pre clinical and bioequivalence against common tablet form. Results: The oral spray Results demonstrated comparable systemic drug exposure for both formulations, with AUC values of 2731.25 ppm·hr and 2704.25 ppm·hr for the tablet and oral spray, respectively. The oral spray achieved a slightly higher Cmax (199 ppm) compared to the tablet (189 ppm), withboth formulations reaching Tmax at 1 hour. The elimination half-life was 15.83 hours for the tablet and 14.56 hours for the oral spray. Relative bioavailability of the oral spray was 99.01%, indicating bioequivalence within the accepted range. Conclusion: Study concluded that oral spray system has several advantages like rapid drug availability in blood plasma allow drug for faster action. The rapid availability could enhance the onset of action, making it a favorable option for achieving faster therapeutic effects. The results show that Levocetirizine oral spray exhibited comparable pharmacokinetic parameters to the tablet formulation, including Cmax, Tmax, and elimination half-life. The faster absorption in the oral spray suggests it may provide quicker symptom relief in allergic reactions. Both formulations followed a similar elimination profile, with concentrations reaching near zero by 48 hours. This study supports the oral spray as a viable alternative to the tablet, particularly for patients with swallowing difficulties or those seeking more convenient administration. However, human studies are needed to confirm these findings and evaluate patient preferences.
Author: Laxmikant Harsola
Institution: Indus University
Language: English
Subfield: Pharmaceutical Science
Domain: Life Sciences
Open Access status: hybrid
OpenAlex ID: W4410410256