Development of Co-Amorphous Loratadine–Citric Acid Orodispersible Drug Formulations

This study aimed at the preparation and characterization of co-amorphous loratadine–citric acid orally disintegrating dosage forms (ODx). A co-amorphous loratadine–citric acid was prepared by solvent evaporation method in three different molecular ratios. DSC, FTIR, and dissolution studies have been...

Full description

Saved in:
Bibliographic Details
Published inProcesses Vol. 10; no. 12; p. 2722
Main Authors Rédai, Emőke Margit, Sipos, Emese, Vlad, Robert Alexandru, Antonoaea, Paula, Todoran, Nicoleta, Ciurba, Adriana
Format Journal Article
LanguageEnglish
Published Basel MDPI AG 01.12.2022
Subjects
Amino acids
Binary systems
Bioavailability
Buffer solutions
Cellulose
Citric acid
Compression
Data analysis
Diameters
Disintegration
Dissolution
Dosage
Evaporation
Friability
Humidity
Lactose
Loratadine
Mechanical properties
Patient compliance
Pharmaceuticals
Software
Spectrum analysis
China
Germany
United States > US
Online AccessGet full text

Cover

More Information
Summary:This study aimed at the preparation and characterization of co-amorphous loratadine–citric acid orally disintegrating dosage forms (ODx). A co-amorphous loratadine–citric acid was prepared by solvent evaporation method in three different molecular ratios. DSC, FTIR, and dissolution studies have been conducted for the binary system. The co-amorphous system was used to obtain oral lyophilizates and orally disintegrating tablets by direct compression. Diameter, thickness, hardness, disintegration time, uniformity of mass, and dissolution was determined for the dosage forms. DSC curves showed a lack of sharp endothermic peaks for the binary systems. FTIR spectra presented a hypsochromic modification of the characteristic peaks. Dissolution studies indicated a five-fold increase in the dissolved amount compared to pure loratadine in water. Disintegration times of direct compression ODx varied in the range of 34–41 s and for freeze-dried ODx in the range of 8–9 s. Friability was under 1% in all cases. The dissolution of loratadine in buffer solution at pH = 1 was almost complete. In conclusion binary systems of loratadine and citric acid enhance solubility and combined with the orally disintegrating pharmaceutical form also increase patient compliance.
ISSN:2227-9717
2227-9717
DOI:10.3390/pr10122722