Cocrystals have gained a lot of consideration regarding its superior role in
enhancement of solubility and dissolution of the included API. Cocrystals could be converted
to coamorphous systems via different techniques like milling and quench cooling; however,
the use of spray-drying technique has not been investigated before. So, the aim of this study
was to explore the effect of spray drying on the amorphization of indomethacin/nicotinamide,
INDNIC, as model cocrystals. Spray-drying operating parameters were optimized using the
Taguchi design of experiment for maximum powder yield and low moisture content. The
obtained INDNIC spray-dried cocrystals were characterized for their degree of crystallinity,
morphology, moisture content, and dissolution performance. In addition, stability study was
performed at different temperature and humidity conditions. Experimental design results
delineate that spray-drying inlet temperature and cocrystal concentrations as the most
influential factors for maximum powder yield and low moisture content. Powder X-ray
diffraction and differential scanning calorimetry studies revealed the conversion of INDNIC
cocrystals to a partial coamorphous or coamorphous structure without dissociation of
INDNIC molecular structure. INDNIC coamorphous powders showed a significantly higher
release of IND compared with cocrystals and remain physically stable for 2 months when
stored in the refrigerator.
قسم البحث
مجلة البحث
AAPSPharmSciTech
الناشر
Springer
تصنيف البحث
1
عدد البحث
21:181
موقع البحث
DOI: 10.1208/s12249-020-01732-x
سنة البحث
2020
المشارك في البحث
ملخص البحث