Development of carvedilol‐cyclodextrin inclusion complexes using fluid‐bed granulation: a novel solid‐state complexation alternative with technological advantages. (27th July 2016)

• Record Type: Journal Article
• Authors: Alonso, Ellen C. P.; Riccomini, Karina; Silva, Luis Antônio D.; Galter, Daniela; Lima, Eliana M.; Durig, Thomas; Taveira, Stephania F.; Martins, Felipe Terra; Cunha‐Filho, Marcílio S. S.; Marreto, Ricardo N.
• Is Part Of: Journal of pharmacy and pharmacology. Volume 68:Number 10(2016:Oct.)
• Page Start: 1299
• Page End: 1309
• Publication Date: 2016-07-27
• Subjects: carvedilol -- hydroxypropyl‐β‐cyclodextrin -- hydroxypropyl‐γ‐cyclodextrin -- solid‐state inclusion complex; Pharmacy -- Periodicals; Pharmacology -- Periodicals; 615.1
• DOI: 10.1111/jphp.12601
• Languages: English
• ISSNs: 0022-3573

Abstract

Abstract: Objectives: This study sought to evaluate the achievement of carvedilol (CARV) inclusion complexes with modified cyclodextrins (HPβCD and HPγCD) using fluid‐bed granulation (FB). Methods: The solid complexes were produced using FB and spray drying (SD) and were characterised by differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), powder X‐ray diffraction, SEM, flowability and particle size analyses and in vitro dissolution. Key findings: The DSC, FTIR and powder X‐ray diffraction findings suggested successful CARV inclusion in the modified β‐ and γ‐cyclodextrins, which was more evident in acidic media. The CARV dissolution rate was ~7‐fold higher for complexes with both cyclodextrins prepared using SD than for raw CARV. Complexes prepared with HPβCD using FB also resulted in a significant improvement in dissolution rate (~5‐fold) and presented superior flowability and larger particle size. Conclusions: The findings suggested that FB is the best alternative for large‐scale production of solid dosage forms containing CARV. Additionally, the results suggest that HPγCD could be considered as another option for CARV complexation because of its excellent performance in inclusion complex formation in the solid state.