Controlled-release antihistamines using supercritical antisolvent process

Antihistamines are widely used to treat allergic diseases; these drugs plasma concentration reaches a peak in a relatively short time, counteracting the allergy?s acute effects. Considering the chronicity of some symptoms, the effect of the antihistamine has to be prolonged over time; therefore, it is important to propose controlled-release systems. Supercritical Antisolvent coprecipitation is used to process cetirizine dihydrochloride and ketotifen, two antihistamines, using zein as the carrier to obtain controlled-release systems. The effect of temperature and polymer/drug ratio on the morphology and mean size of the powders is evaluated. From the UV?vis drug dissolution tests, it is possible to observe that the release of the active ingredient is significantly prolonged for both the antihistamines. Thanks to the presence of an initial burst effect, last generation formulations with bimodal releases are obtained, which allow to offer immediate relief from allergic symptoms followed by a prolonged release of the active ingredient.

Automated summary

The study used Supercritical Antisolvent coprecipitation to prepare controlled-release systems of antihistamines, showing significantly prolonged release of the active ingredients and achieving last generation formulations with bimodal releases.