Water-soluble loratadine inclusion complex: Analytical control of the preparation by microwave irradiation

The majority of active pharmaceutical ingredients are poorly soluble in water. The rate-determining step of absorption is the dissolution of these drugs. Inclusion complexation with cyclodextrin derivatives can lead to improved aqueous solubility and bioavailability of pharmacons due to the formatio...

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Veröffentlicht in:Journal of pharmaceutical and biomedical analysis 2008-11, Vol.48 (3), p.1020-1023
Hauptverfasser: Nacsa, Á., Ambrus, R., Berkesi, O., Szabó-Révész, P., Aigner, Z.
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Sprache:eng
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Zusammenfassung:The majority of active pharmaceutical ingredients are poorly soluble in water. The rate-determining step of absorption is the dissolution of these drugs. Inclusion complexation with cyclodextrin derivatives can lead to improved aqueous solubility and bioavailability of pharmacons due to the formation of co-crystals through hydrogen-bonding between the components. Inclusion complexes of loratadine were prepared by a convenient new method involving microwave irradiation and the products were compared with those of a conventional preparation method. Dissolution studies demonstrated that the solubility and rate of dissolution of loratadine increased in both of the methods used. The interactions between the components were investigated by thermal analysis and Fourier Transform Infrared studies. The microwave treatment did not cause any chemical changes in the loratadine molecule.
ISSN:0731-7085
1873-264X
DOI:10.1016/j.jpba.2008.07.001