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 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.
Nacsa
A
A
Department of Pharmaceutical Technology, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
Ambrus
R
R
Berkesi
O
O
Szabó-Révész
P
P
Aigner
Z
Z
D002152:Calorimetry, Differential Scanning / Q000379:methods; D004339:Drug Compounding; D039563:Histamine H1 Antagonists, Non-Sedating / Q000032:analysis* / Q000737:chemistry; D006860:Hydrogen Bonding; D007700:Kinetics; D017336:Loratadine / Q000032:analysis* / Q000737:chemistry; D008872:Microwaves; D015394:Molecular Structure; D011208:Powders; D011827:Radiation; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D013818:Thermogravimetry / Q000379:methods; D014867:Water / Q000737:chemistry
D039563:Histamine H1 Antagonists, Non-Sedating; D011208:Powders; D014867:Water; D017336:Loratadine