Formulation and evaluation of a bilayer tablet comprising of diclofenac potassium as orodispersible layer and diclofenac sodium as sustained release core

Abstract

Diclofenac a phenylacetic acid derivative has long been used

as an anti-inflammatory and analgesic drug to treat certain

conditions however its sustained release formulation with

immediate release loading dose is desirable. The rationale

of the current work was to develop and evaluate bilayer

tablets with diclofenac potassium as orodispersible layer and

diclofenac sodium as sustained release core. The diclofenac

sodium core was prepared by wet granulation method while the

orodispersible outer layer was prepared by direct compression

method using super disintegrant sodium starch glycolate. The

powder blends were then evaluated for both pre- compressional

and post compressional properties. The physical parameters

of both powders and tablets were in accordance with the

compendial standards. The orodispersible portion disintegrated

in less than 30sec releasing diclofenac potassium as the loading

dose while the core was able to sustain the release of diclofenac

sodium up to 10hrs in simulated intestinal fluid (pH 6.8). The

kinetic data revealed that the release pattern was best fitted into

Korsmeyer-Peppas model with non-fickian release. The outer

orodispersible layer of diclofenac potassium and sustained

release inner core of diclofenac sodium in a single tablet was

successfully formulated while sodium starch glycolate showed

to have good super disintegrant properties.

Keywords

• Orodispersible,Sustained release,Diclofenac,Direct Compression,Bilayer tablet

Ağızda dağılan tabaka olarak diklofenak potasyum, geciktirilmiş salım çekirdeği olarak diklofenak sodyum içeren iki tabakalı tabletin formülasyonu ve değerlendirilmesi

Abstract

Diklofenak, bir fenilasetik asit türevi olup uzun yıllardan beri

antienfamatuvar ve analjezik bir ilaç olarak kullanılmaktadır

ancak bu etken maddeden hareketle hemen salım için yükleme

dozu içeren geciktirilmiş salım formülasyonunun hazırlanması

istenmektedir. Bu çalışmanın amacı, ağızda dağılan tabaka

olarak diklofenak potasyum, geciktirilmiş salım çekirdeği

olarak diklofenak sodyum içeren iki tabakalı tabletlerin

formülasyonu ve değerlendirilmesidir. Diklofenak sodyum

içeren çekirdek yaş granülasyon yöntemi ile hazırlanırken

ağızda dağılan dış tabaka direct basım yöntemiyle ve süper

dağıtıcı olarak sodyum nişasta glikolat varlığında hazırlandı.

Toz karışımı hem basım öncesi hem de basım sonrası özellikleri

açısından değerlendirildi. Toz karışımının ve tabletlerin fiziksel

özelliklerinin zorunlu standartlarla uyumlu olduğu görüldü.

Ağızda dağılan kısmın 30 saniyeden kısa bir sürede dağılarak

yükleme dozu olan diklofenak potasyumu saldığı, çekirdek

kısmının ise simule bağırsak sıvısında (pH 6.8), 10 saate kadar

diklofenak sodyum salınımı sağladığı tespit edildi. Kinetik ile

ilgili veriler incelendiğinde, tabletin non-fickian salım gösterdiği

ve Korsmeyer-Peppas modeline uygun olduğu tespit edildi. Tek

bir tablet içeriğinde, ağızda dağılan tabaka olarak diklofenak

potasyum, geciktirilmiş salım çekirdeği olarak diklofenak

sodyum içeren ve süper dağıtıcı olarak sodyum nişasta glikolat

içeren tabletlerin formülasyonu başarıyla yapıldı.

Keywords

• Ağızda dağılan tablet,geciktirilmiş salım,diklofenak,direkt basım,iki tabakalı tableT

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