RATIONAL DESIGNING OF SUSTAINED RELEASE MATRIX FORMULATION OF ETODOLAC EMPLOYING HYPROMELLOSE, CARBOMER, EUDRAGIT AND POVIDONE

Nilesh N Mahajan,Pooja Wadhavane,Debarshi Kar Mahapatra

doi:10.22159/ijpps.2017v9i12.19702

Nilesh N Mahajan, Pooja Wadhavane + Show 1 more

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https://doi.org/10.22159/ijpps.2017v9i12.19702

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Abstract

Objective: The existing investigation represents a challenge in formulating etodolac oral controlled release tablets employing five most prominent hydrophilic release rate retardant polymers like HPMC K100M, HPMC K4M, Carbopol 934P, Eudragit RS100, and Polyvinyl pyrrolidone K90 which are USFDA approved non-toxic substances, cost-effective, and easily available.Methods: The tablets were manufactured by wet granulation method along with talc, anhydrous lactose, and magnesium stearate. The pre-compression attributes of the produced granules and the post-compression characteristics were assessed according to the specified protocols. The formulations were accessed for their ability to release the drug in the simulated gastric media and the obtained results were fitted into various kinetic models to determine the probable drug release mechanism(s). A short-term stability study (for 90 days duration) was also performed.Results: The prepared granules demonstrated superior flow properties and packing ability, whereas the fabricated sustained release matrix batches showed excellent mechanical characteristics. The in vitro drug release profile of the hypromellose, carbomer, eudragit and povidone based sustained release matrix tablet formulations expressed drug release for the period of 12 hr following the diffusion cum erosion mechanism(s) (termed as anomalous diffusion) and illustrated comparable drug release with that of marketed formulation (Etogesic®-ER 600 mg). The produced formulations revealed splendid reproducibility and stability under accelerated conditions.Conclusion: The judiciously planned fabrication of the matrix formulations possess the ability to decrease the frequency of drug administration to twice-daily along with minimizing the blood level fluctuations, which ultimately leads to enhanced patient compliance and better therapeutic regimens.

Highlights

Etodolac (ETO) is a biopharmaceutics classification system (BCS) Class-II drug used primarily as non-steroidal anti-inflammatory (NSAID) drugs for treating pain related to arthritis
The existing investigation represents a challenge in formulating etodolac oral controlled-release tablets employing five most prominent hydrophilic release rate retardant polymers like hydroxypropyl methylcellulose (HPMC) K100M, HPMC K4M, carbopol 934P, eudragit RS100, and polyvinylpyrrolidone K90 which are non-toxic substances, costeffective, and available
The judiciously planned fabrication of the matrix formulations possesses the ability to decrease the frequency of drug administration to twice-daily along with minimizing the blood level fluctuations, which leads to enhanced patient compliance and better therapeutic regimens

Summary

Introduction

Etodolac (ETO) is a biopharmaceutics classification system (BCS) Class-II drug used primarily as non-steroidal anti-inflammatory (NSAID) drugs for treating pain related to arthritis. ETO decreases the synthesis of peripheral prostaglandins which are involved in mediating inflammation. It binds to the upper portion of the cyclooxygenase (COX) enzyme active site and prevents its substrate, arachidonic acid, from entering the active site. It is 5–50 times more selective for COX-2 than COX-1, which makes it therapeutically more efficient in managing arthritis-related pain [1,2]. Fecal excretion accounts for 16% of its elimination. It is not known whether ETO is excreted in human milk; based on its physical-chemical properties, excretion into breast milk is expected [3,4]

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