Preparation and Evaluation of Hot-Melt Extruded Patient-Centric Ketoprofen Mini-Tablets

Author(s): Abdullah S. Alshetaili, Bjad K. Almutairy, Roshan V. Tiwari, Joseph T. Morott, Sultan M. Alshehri, Xin Feng, Bader B. Alsulays, Jun-Bom Park, Feng Zhang, Michael A. Repka

Journal Name: Current Drug Delivery

Volume 13 , Issue 5 , 2016


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Abstract:

Background: Bitter tasting drugs represent a large portion of active pharmaceutical ingredients. Mini-tablets are specifically designed for patients with difficulty in swallowing particular in young children up to 10 years of age, geriatric patients and patients with esophagitis.

Objective: The present study was aimed to prepare, taste-masked mini-tablets, which are easily swallowed dosage forms, primarily to be used by pediatric and geriatric patients.

Methods: Ketoprofen (10%-50% w/w) and Eudragit® EPO were blended and extruded with a 5-mm strand die and cut into consistent mini-tablets by using an adapted downstream pelletizer.

Results: Differential scanning calorimetry and polarized light microscopy-hot stage microscopy studies confirmed that the binary mixtures were miscible under the employed extrusion temperatures. In-vitro release studies showed that drug release was less than 0.5% within the first 2 min in simulated salivary fluid (pH 6.8) and more than 90% in the first 20 min in gastric media (pH 1.0). The results of the electronic tongue analysis were well correlated with the drug release profile of the mini-tablets in the artificial saliva. Scanning electron microscopy revealed no cracks on the surface of the minitablets, confirming that the mini-tablets were compact solids. Chemical imaging confirmed the uniform distribution of ketoprofen inside the polymer matrices.

Conclusion: Eudragit® EPO containing ketoprofen at various drug loads were successfully melt extruded into tastedmasked mini-tablets. The reduced drug release at salivary pH correlated well with Astree e-Tongue studies for taste masking efficiency.

Keywords: Eudragit® E PO, FTIR chemical imaging, Hot-melt extrusion, Ketoprofen, Mini-tablets, Taste masking.

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Article Details

VOLUME: 13
ISSUE: 5
Year: 2016
Published on: 24 June, 2016
Page: [730 - 741]
Pages: 12
DOI: 10.2174/1567201812666151012113806
Price: $65

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