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        Orodispersible film incorporating nanoparticulate loratadine for an enhanced oral bioavailability

        Van Nguyen Khanh,Dang Thu Kim,Vu Linh Thi Dieu,Ha Nhan Thi,Truong Hieu Duy,Tran Tuan Hiep 한국약제학회 2023 Journal of Pharmaceutical Investigation Vol.53 No.3

        Purpose Loratadine (LOR), a commonly prescribed antihistamine, has low water solubility but high permeability. In this study, an orodispersible film incorporating the nanoparticulate loratadine was prepared to enhance the oral bioavailability of a poorly water-soluble drug. Methods Nanoparticulate loratadine was formulated using the antisolvent precipitation method and optimized by a singlefactor design based on the particle size and polydispersity index. The optimal formulation was spray-dried and characterized by powder X-ray diffraction and differential scanning calorimetry. Nanoparticulate loratadine was loaded into an orodispersible film using a solvent casting method. Results In the dissolution tests, the nanoparticulate loratadine-loaded orodispersible film exhibited a 6.5-fold higher dissolution rate than the pure loratadine-loaded film and a similar dissolution rate compared to the commercialized orodispersible tablet, Loratadine SPM. In pharmacokinetic studies conducted on rats, the maximum concentration (Cmax) and area under the curve of the plasma concentration–time profile from 0 to 24 h (AUC 0-24 h) of the nanoparticulate loratadine-loaded orodispersible film significantly increased 1.8-fold and 5.8-fold, respectively. The elimination half-life (t1//2) increased 5.1-fold compared to the loratadine-loaded counterpart. Conclusion These results suggest the potential of orodispersible films to improve the oral bioavailability of poorly watersoluble drugs and promote compliance in pediatric and geriatric patients.

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