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KMID : 1146920230530030417
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Journal of Pharmaceutical Investigation
2023 Volume.53 No. 3 p.417 ~ p.426
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Orodispersible film incorporating nanoparticulate loratadine for an enhanced oral bioavailability
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Khanh Van Nguyen
Thu Kim Dang
Linh Thi Dieu Vu
Nhan Thi Ha
Hieu Duy Truong
Tuan Hiep Tran
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Abstract
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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 single-factor 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 (AUC0-24 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 water-soluble drugs and promote compliance in pediatric and geriatric patients.
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KEYWORD
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Loratadine, Orodispersible film, Nanoparticles, Enhancement of bioavailability, Pharmacokinetics
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