FORMULATION AND OPTIMIZATION OF GASTRO-RETENTIVE FLOATING TABLETS OF ENALAPRIL MALEATE AND LOSARTAN FOR ENHANCED BIOAVAILABILITY AND THERAPEUTIC EFFICACY

Rohit Jaimini; Dr. Manish Jaimini

doi:10.61280/tjpls.v12i1.170

Rohit Jaimini Maharishi Arvind University, Mudiaramsar, Jaipur, Raj., Pin-302041
Dr. Manish Jaimini Maharishi Arvind University, Mudiaramsar, Jaipur, Raj., Pin-302041

10.61280/tjpls.v12i1.170

Keywords:

Floating tablets, Enalapril Maleate, Losartan, Bioavailability, GRDDS

Abstract

The objective of this study was to formulate and optimize gastro-retentive floating tablets of Enalapril Maleate and Losartan to enhance their bioavailability and therapeutic efficacy. These drugs, commonly used in the management of hypertension and heart failure, suffer from limited solubility and rapid gastric emptying, which reduce their effectiveness. Gastro-retentive floating tablets were developed using hydroxypropyl methylcellulose (HPMC K4M) and guar gum as release-controlling agents, with sodium bicarbonate and citric acid as effervescent agents to ensure buoyancy. Twenty formulations were prepared using the direct compression method and evaluated for critical parameters, including hardness, friability, swelling index, floating lag time, total floating time, and in-vitro drug release.
Preformulation studies confirmed the compatibility of the drugs with excipients, with no chemical interactions detected using FTIR spectroscopy. The micrometric properties of the powder blends demonstrated excellent flowability and compressibility, ensuring suitability for tablet manufacturing. All formulations showed acceptable weight variation, hardness, and friability. The floating lag time ranged from 4.3 to 5.1 minutes, and total floating times exceeded 8 hours for all batches. Drug content ranged from 96.79% to 99.57%, reflecting uniformity and accuracy in dosing.
In-vitro dissolution studies revealed sustained release profiles, with optimized formulations achieving over 90% cumulative drug release within 12 hours. Batch F7 demonstrated the best overall performance, with a high swelling index, minimal floating lag time, prolonged floating duration, and consistent drug release. These findings indicate that gastro-retentive floating tablets of Enalapril Maleate and Losartan can effectively address challenges associated with poor bioavailability and rapid gastric emptying, offering a promising approach for improved therapeutic outcomes and patient compliance.

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