TY  - JOUR
AU  - Szabados-Nacsa, Ágnes
AU  - Sipos, Péter
AU  - Martinek, Tamás
AU  - Mándity, István
AU  - Blazsó, Gábor
AU  - Balogh, A
AU  - Révész, Piroska
AU  - Aigner, Zoltán
TI  - Physico-chemical characterization and in vitro/in vivo evaluation of loratadine: dimethyl-β-cyclodextrin inclusion complexes
JF  - JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
J2  - J PHARMACEUT BIOMED ANAL
VL  - 55
PY  - 2011
IS  - 2
SP  - 294
EP  - 300
PG  - 7
SN  - 0731-7085
DO  - 10.1016/j.jpba.2011.01.024
UR  - https://m2.mtmt.hu/api/publication/1696527
ID  - 1696527
N1  - Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720, Szeged, Hungary            
            Institute of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Szeged, H-6720, Szeged, Hungary            
            Department of Pharmacodynamics and Biopharmacy, Faculty of Pharmacy, University of Szeged, H-6720, Szeged, Hungary            
            Cited By :16            
            Export Date: 18 November 2022            
            CODEN: JPBAD            
            Correspondence Address: Aigner, Z.; Department of Pharmaceutical Technology, Eötvös u. 6, H-6720, Szeged, Hungary; email: aigner@pharm.u-szeged.hu
AB  - A tricyclic, piperidine derivative of antihistamines, loratadine, which belongs in class II of the Biopharmaceutical Classification System, was investigated. It is an ionizable drug, whose solubility depends on the gastrointestinal pH, and the bioavailability is therefore very variable. Inclusion complexes were prepared by kneading method, containing loratadine (LOR) and dimethyl-beta-cyclodextrin (DIMEB) in two different molar ratios in an attempt to achieve better dissolution and therefore the better bioavailability of loratadine. The formation and physicochemical properties of the inclusion complexes were investigated by means of dissolution tests, pH-dependent solubility studies, electrospray ionization mass spectrometry and diffusion-ordered (1)H NMR spectroscopy. The in vivo efficiency of the complexes was examined in rat animal experiments to confirm the better in vitro dissolution. The instrumental examinations proved the presence of total complexes in 1:1 ratio in both compositions. However, the in vitro pH-dependent solubility results, the in vivo blood levels and the greater pharmacological effect prove that excess DIMEB is needed to achieve the pH-independent and complete solubility of LOR, and therefore better and more consistent bioavailability. (C) 2011 Elsevier B.V. All rights reserved.
LA  - English
DB  - MTMT
ER  -