Dual-release capsule of pseudoephedrine and cetirizine for reduced dosing frequency and improved therapy

Vollständiger Abstract

Worum geht es in dieser Arbeit?

Pseudoephedrine hydrochloride is a sympathomimetic agent acting on α‑ and β‑adrenergic receptors with a half‑life of 5–8 h, requiring multiple daily doses. Sustained‑release formulations are desirable to maintain therapeutic plasma concentrations, reduce dosing frequency, and minimize fluctuations. Cetirizine dihydrochloride, a long‑acting non‑sedating antihistamine with a half‑life of ~10 h, is suitable for immediate‑release dosage forms. This study aimed to develop a dual‑release capsule containing pseudoephedrine hydrochloride sustained‑release granules and cetirizine dihydrochloride immediate‑release granules. Ethyl cellulose N100 was employed as a coating agent, while starch served as a disintegrant. The granule mixture exhibited acceptable physicochemical properties, with moisture content of 4.185–4.513%, flow rate of 10.63–12.30 g/s, and angle of repose between 23.78°–27.53°. Capsule content uniformity ranged from 97.15–98.45% for pseudoephedrine hydrochloride and 99.33–104.61% for cetirizine dihydrochloride. Dissolution testing revealed two distinct release profiles. Cetirizine dihydrochloride showed dissolution behavior comparable to the reference product, whereas pseudoephedrine hydrochloride exhibited significant differences. In conclusion, combining sustained‑release pseudoephedrine hydrochloride with immediate‑release cetirizine dihydrochloride in a single capsule is feasible. Further optimization is required to align pseudoephedrine hydrochloride release with the reference product.