Development of enteric coated sustained release minitablets containing mesalamine

Dayse Fernanda De Souza,Itamar Francisco Andreazza,Karin Goebel

doi:10.1590/s1984-82502013000300014

Dayse Fernanda De Souza, Itamar Francisco Andreazza + Show 1 more

Open Access

https://doi.org/10.1590/s1984-82502013000300014

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Abstract

The aim of this study was to develop and evaluate a multiparticulate modified release system, composed of minitablets with a sustained release matrix system coated with a pH-dependent release polymer, using mesalamine as a model drug. Polyox® WSR 1105 was the polymer used in the matrix system and Eudragit® L30D55 was used as a pH-dependent polymer. The minitablets (with 20%, 30% or 40% Polyox® concentration) were prepared by dry granulation, which led to good quality minitablets. The developed minitablets were coated in a fluidized bed at 8% of the coating level. Dissolution studies were performed in media that simulated the gastrointestinal tract (pH 1.4, 6.0 and 7.2) and showed that formulations with higher Polyox® concentrations were capable of retaining the drug release in pH 1.4. All formulations prolonged the drug release and presented zero-order kinetic behaviour. The Korsmeyer-Peppas model demonstrated that formulations with 20% or 30% of polymer exhibited anomalous transport behaviour, whilst the 40% sample exhibited super case II model transportation. Dissolution efficiency showed that only the formulations containing 20% and 40% polymer could be considered statistically different.

Highlights

IntroductionSolid dosage forms are the most frequently used for oral administration, and tablets represent the mostMultiparticulate dosage forms present multiple advantages over single unit dosage forms, demonstrated as flexibility during formulation development andD
Solid dosage forms are the most frequently used for oral administration, and tablets represent the mostMultiparticulate dosage forms present multiple advantages over single unit dosage forms, demonstrated as flexibility during formulation development andD
The powder flow evaluation is one of the most important parameters in the development of a solid dosage form, because commercial production requires a continuous flow of powder mixes during the manufacturing process (Yang, Venkateshi, Fassihi, 1996)

Summary

Introduction

Solid dosage forms are the most frequently used for oral administration, and tablets represent the mostMultiparticulate dosage forms present multiple advantages over single unit dosage forms, demonstrated as flexibility during formulation development andD. Solid dosage forms are the most frequently used for oral administration, and tablets represent the most. Multiparticulate dosage forms present multiple advantages over single unit dosage forms, demonstrated as flexibility during formulation development and. F. Andreazza therapeutic benefits for the patients, including increased bioavailability, reduced risk of systemic toxicity due to dose dumping and reduced risk of local irritation, besides predictable gastric emptying (Kramar, Turk, Vrecer, 2003)

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