Water-soluble loratadine inclusion complex

Analytical control of the preparation by microwave irradiation

Á Nacsa, R. Ambrus, O. Berkesi, P. Szabó-Révész, Z. Aigner

Research output: Contribution to journalArticle

29 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1020-1023
Number of pages4
JournalJournal of Pharmaceutical and Biomedical Analysis
Volume48
Issue number3
DOIs
Publication statusPublished - Nov 4 2008

Fingerprint

Loratadine
Microwave irradiation
Microwaves
Dissolution
Solubility
Water
Cyclodextrins
Fourier Analysis
Hydrogen Bonding
Complexation
Pharmaceutical Preparations
Thermoanalysis
Biological Availability
Fourier transforms
Hydrogen bonds
Hot Temperature
Infrared radiation
Crystals
Molecules

Keywords

  • Co-crystals
  • Cyclodextrin
  • Loratadine
  • Microwave irradiation
  • Structural analysis

ASJC Scopus subject areas

  • Analytical Chemistry
  • Drug Discovery
  • Pharmaceutical Science
  • Spectroscopy
  • Clinical Biochemistry

Cite this

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abstract = "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.",
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T2 - Analytical control of the preparation by microwave irradiation

AU - Nacsa, Á

AU - Ambrus, R.

AU - Berkesi, O.

AU - Szabó-Révész, P.

AU - Aigner, Z.

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N2 - 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.

AB - 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.

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KW - Microwave irradiation

KW - Structural analysis

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