Development and optimization of ketoconazole oral strips by means of continuous hot-melt extrusion processing

Abstract

Abstract:Objectives The aim of this study was to develop mucoadhesive oral strips using hot-melt extrusion as a continuous manufacturing process. Methods Powder blends of ketoconazole, a water insoluble drug; either hydroxypropyl methylcellulose (HPMC) or soluplus (SOL), sorbitol (SRB) and magnesium aluminometasilicate (MAS) were extruded to manufacture thin strips with 0.5 mm thickness. The presence of the inorganic metasilicate facilitated smooth processing of the extruded strips as it worked as an absorbent directly impacting on the extensive mixing of the drug/excipients inside the extruder barrel. Key findings The use of MAS also favoured the rapid hydration, swelling and eventual disintegration of the strips. Differential scanning calorimetry (DSC) and transmission X-ray diffraction (TXRD) analysis revealed the existence of the amorphous drug within the extruded strips. Scanning electron microscopy (SEM) and energy dispersive X-Ray (EDS) undertaken on the formulations showed a homogeneous drug distribution within the extruded strips. Conclusion The strips produced via continuous HME processing showed significantly faster release of KTZ compared to the bulk drug substance. Journal of Pharmacy and Key findingsThe use of MAS also favoured the rapid hydration, swelling and eventual disintegration of the strips. Differential scanning calorimetry (DSC) and transmission X-ray diffraction (TXRD) analysis revealed the existence of the amorphous drug within the extruded strips. Scanning electron microscopy (SEM) and energy dispersive X-Ray (EDS) undertaken on the formulations showed a homogeneous drug distribution within the extruded strips. ConclusionThe strips produced via continuous HME processing showed significantly faster release of KTZ compared to the bulk drug substance.

RETRACTED: Development and characterisation of semi-crystalline composite granules: The effect of particle chemistry and the electrostatic charging

“…Similar results were found in one of our previously reported study [20]. Moreover, EDS analysis was performed to map the distribution of IBU and homogeneity of the composite granules [24,25]. Both the drug and polymeric career used in this study mainly contain C and O atoms likewise most of the polymers.…”

Oral Thin Films As a Remedy for Noncompliance in Pediatric and Geriatric Patients

“…Manirruzaman and co-workers designed oral thin films of ketoconazole produced by HME which showed more rapid drug dissolution compared to the pure drug [30].…”

Continuous manufacturing via hot-melt extrusion and scale up: regulatory matters

“…It is the knowledge gained and submitted to the authorities, and not the volume of data collected, that forms the basis for science-and risk-based submissions and regulatory evaluations'. There is a clear indication that all of the above-mentioned guidelines and the recently emphasized QbD framework could have a significant impact on the development, optimization, and implementation of HME processing [88] as a CM process.…”