Development of a Biphasic-Release Multiple-Unit Pellet System with Diclofenac Sodium Using Novel Calcium Phosphate-Based Starter Pellets.

Daniel Zakowiecki,Krzysztof Cal,Grzegorz Garbacz,Maja Frankiewicz,Dorota Haznar-Garbacz,Justyna Dabrowska,Maciej Gajda,Bartlomiej Kubiak,Marcela Wiater,Tobias Hess,Dagmara Hoc,Jadwiga Paszkowska

doi:10.3390/pharmaceutics13060805

Daniel Zakowiecki, Krzysztof Cal + Show 10 more

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https://doi.org/10.3390/pharmaceutics13060805

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Abstract

Novel calcium phosphate-based starter pellets were used to develop a biphasic-release multiple-unit pellet system (MUPS) with diclofenac sodium as a model drug in the form of hard gelatin capsules. For comparative purposes, corresponding formulations based on the inert cores made of microcrystalline cellulose, sucrose and isomalt were prepared. The developed system consisted of two types of drug-layered pellets attaining different release patterns: delayed-release (enteric-coated) and extended-release. Dissolution characteristics were examined using both compendial and biorelevant methods, which reflected fed and fasting conditions. The results were collated with an equivalent commercial product but prepared with the direct pelletization technique.

Highlights

Pharmaceutical pellets, sometimes referred to as microparticulates, are free-flowing spherical particulates/beads ranging typically from 0.2–1.5 mm in size; other sizes are frequently used [1,2,3]
The beads are used for manufacturing various multiple-unit pellet systems (MUPS), which are a kind of multiparticulate dosage form, where one or more drugs are split into numerous small independent subunits
The release ofthe the drug substance stance from the pellets with water-soluble cores practically stopped after h of the test, the pellets with water-soluble cores practically stopped after 6 h of the test, while gradual while gradual was for stillthe observed for the other pellets

Summary

Introduction

Pharmaceutical pellets, sometimes referred to as microparticulates, are free-flowing spherical particulates/beads ranging typically from 0.2–1.5 mm in size; other sizes are frequently used [1,2,3]. The beads are used for manufacturing various multiple-unit pellet systems (MUPS), which are a kind of multiparticulate dosage form, where one or more drugs are split into numerous small independent subunits. MUPSs consist of drug-loaded pellets, which are either compressed into tablets or filled into hard capsules [5,6,7,8,9]. In recent years, such multiparticulate dosage forms have gained considerable popularity, and more pharmaceutical preparations of such kind are increasingly present on the market.

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