Abstract

Oral modified-release multiparticulate dosage forms, which are also referred to as oral multiple-unit particulate systems, are becoming increasingly popular for oral drug delivery applications. The compaction of polymer-coated multiparticulates into tablets to produce a sustained-release dosage form is preferred over hard gelatin capsules. Moreover, multiparticulate tablets are a promising solution to chronic conditions, patients’ adherence, and swallowing difficulties if incorporated into orodispersible matrices. Nonetheless, the compaction of multiparticulates often damages the functional polymer coat, which results in a rapid release of the drug substance and the subsequent loss of sustained-release properties. This review brings to the forefront key formulation variables that are likely to influence the compaction of coated multiparticulates into sustained-release tablets. It focusses on the tabletting of coated drug-loaded pellets, microparticles, and nanoparticles with a designated section on each. Furthermore, it explores the various approaches that are used to evaluate the compaction behaviour of particulate systems.

Highlights

  • Conventional immediate-release (IR) dosage forms fail to maintain stable plasma levels of drug over a prolonged period; they generally tend to have a short duration of action, which necessitates multiple daily dosing

  • It is not just a financial burden; patients who choose to ignore medical advice given to them or forget to take their medication risk worsening their condition or in some cases reducing their chances of survival

  • The results revealed a successful sustained release of tramadol hydrochloride from the palletised tablets, which was attributed to the intact polymer coat

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Summary

Introduction

Conventional immediate-release (IR) dosage forms fail to maintain stable plasma levels of drug over a prolonged period; they generally tend to have a short duration of action, which necessitates multiple daily dosing. For long-term chronic conditions where treatment may be for several months or even years, multiple daily dosing is undesirable and inconvenient for the patient, and can result in missed doses or made-up doses [1]. Hospitalisation costs as a result of patients being noncompliant with their medication are as high as $13.35 billion a year. It is not just a financial burden; patients who choose to ignore medical advice given to them or forget to take their medication (which is more common with geriatric patients) risk worsening their condition or in some cases reducing their chances of survival. Patient adherence to the thrice-daily schedule was 59% whereas for the once-daily regimen, around 84% of patients complied with the medication schedule [2]

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