Solubility and Physical Stability Enhancement of Loratadine by Preparation of Co-Amorphous Solid Dispersion with Chlorpheniramine and Polyvinylpyrrolidone

Loratadine (LRD), a non-sedating and slow-acting antihistamine, is often given in combination with short-onset chlorpheniramine maleate (CPM) to increase efficacy. However, LRD has poor water solubility resulting in low bioavailability. The aim of this study was to improve LRD solubility by preparin...

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Published inPharmaceutics Vol. 15; no. 11; p. 2558
Main Authors Suknuntha, Krit, Khumpirapang, Nattakanwadee, Tantishaiyakul, Vimon, Okonogi, Siriporn
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 31.10.2023
Subjects
Aluminum
amorphous
Bioavailability
Calorimetry
Chlorpheniramine
Diffraction
Drug dosages
Ethanol
Fourier transforms
Histamine
Infrared spectroscopy
Loratadine
Oral administration
Polymers
polyvinylpyrrolidone
Povidone
solid dispersion
solubility enhancement
Spectrum analysis
X-rays
Thailand
United States > US
amorphous
film casting
quench cooling
solid dispersion
polyvinylpyrrolidone
loratadine
solubility enhancement
chlorpheniramine
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Summary:Loratadine (LRD), a non-sedating and slow-acting antihistamine, is often given in combination with short-onset chlorpheniramine maleate (CPM) to increase efficacy. However, LRD has poor water solubility resulting in low bioavailability. The aim of this study was to improve LRD solubility by preparing co-amorphous LRD-CPM. However, the obtained co-amorphous LRD-CPM recrystallized rapidly, and the solubility of LRD returned to a poor state again. Therefore, co-amorphous LRD-CPM solid dispersions using polyvinylpyrrolidone (PVP) as a carrier were prepared. The obtained solid dispersions were characterized using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT-IR). The solubility, dissolution, and mechanism of drug release from the LRD-CPM/PVP co-amorphous solid dispersions were studied and compared with those of intact LRD, LRD/PVP solid dispersions, and co-amorphous LRD-CPM mixtures. The results from XRPD and DSC confirmed the amorphous form of LRD in the co-amorphous solid dispersions. The FTIR results indicated that there was no intermolecular interaction between LRD, CPM, and PVP. In conclusion, the obtained LRD-CPM/PVP co-amorphous solid dispersions can successfully increase the water solubility and dissolution of LRD and extend the amorphous state of LRD without recrystallization.
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ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics15112558