Abstract

This research was aimed atformulatingand evaluating time dependent delayed-release diclofenac tablets forchronopharmaceutical drug delivery using press-coating technology. Rapiddisintegrating diclofenac core tablets were initially formulated using the directcompression method. Coats of powdered tragacanth or xanthan gum alone, and incombination in variousmixing ratios of 25:75, 40:60, 50:50 and 75:25 were compressed around the coretablet to form 3- layered tablets. Thepress-coated tablets were evaluated for post compression parameters such asweight variation, crushing strength, friability as well as, swelling index, lagtime and in vitro release studies in three different simulated gastro-intestinalfluids. The result revealed that thecore and compression coated tablet formulations were within the officialspecified limits. The release profile of the press coated tabletsexhibited lag times depending upon the type, amount and polymer combinationratio in the tablet coat. Optimizationwas done using analysis of variance (ANOVA). The optimizedbatch F6 which consisted of 40% xanthan and 60% tragacanth gave a lag time of 6h followed with burst release and complete drug release of 98.51%. Thisresearch shows that press-coated diclofenac tablets with 40:60% xanthan andtragacanth gum coat can be exploited in chronopharmaceutical delivery ofdiclofenac sodium.

Highlights

  • The oral route remains the most frequently used route for drug administration because of the low cost of the therapy, ease of administration and high levels of patient compliance (Peter, 2013)

  • To achieve a chronopharmaceutical pattern of drug delivery, development of delayed release tablets is one of the promising time specific delivery systems that release the drug after a predetermined lag time, such that upon administration of the drug by 10 pm, the release is delayed by 6 h followed by a burst release of the drug between 4 and 6 am to coincide with the time of peak symptom manifestation of the disease

  • The characteristic peaks between 3257 cm1 – 1572 cm-1 indicate stretching frequency as a result of the carboxylic groups present. It serves as a diagnostic peak for carbonyl groups of organic acids and the major functional group of diclofenac sodium which belongs to the anthranilates group of nonsteroidal anti-inflammatory drugs

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Summary

Introduction

The oral route remains the most frequently used route for drug administration because of the low cost of the therapy, ease of administration and high levels of patient compliance (Peter, 2013). Some disadvantages still exist which include possible inactivation of the drug by the gastrointestinal tract enzymes, poor bioavailability with poorly soluble drugs e.g. griseofulvin and extensive metabolism (first-pass effect) of certain drugs like propranolol, may occur via this route (Verma et al, 2010). This has led to the development of the modified-release or nonconventional release systems. Press-coating is becoming a technique of great interest in the formulation of delayed release tablets due to its advantages over liquid coating and other solid dosage forms (Pawar et al, 2014)

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