FORMULATION AND IN-VITRO EVALUATION OF FLOATING DRUG DELIVERY SYSTEM OF LOSARTAN POTASSIUM

FORMULATION AND IN-VITRO EVALUATION OF FLOATING DRUG DELIVERY SYSTEM OF LOSARTAN POTASSIUM.

Authors:  Sagar K Khokale*, Dr. Laxmikant B Borse , Prof. Mitesh Sonawane

^1,2,  Sandip Institute of Pharmaceutical Sciences, Mahiravani, Nashik, Maharashtra 422213.

³     LN. Dr. J. D. Pawar, College of Pharmacy, Manur, Kalwan, Nashik, Maharashtra 423501.

Corresponding author: Sagar K Khokale

Sandip Institute of Pharmaceutical Sciences,

Mahiravani, Nashik,

Maharashtra 422213

Abstract

Objective In the present study, Gastro Retentive Floating Drug Delivery systems (GRDDS) of Losartan potassium, an antihypertensive drug, with an oral bioavailability of only 33% (because of its poor absorption from lower gastrointestinal tract) have been designed to increase the therapeutic efficacy & gastric residence time and to reduce frequency of administration. Losartan potassium having a short biological half-life of 1.5 -2 h is eliminated quickly from the body leading to low therapeutic efficacy¹.

Method The tablets were prepared by direct compression method, by employing semi-synthetic and natural polymers like HPMCK100M, HPMC K4M, and Guar gum respectively in various concentrations. Carbopol 934 and sodium bicarbonate as gas generating agent to reduce floating lag time¹.

Result Precompression parameters are evaluated including bulk density, tapped density, Carr’s index, Hausner’s ratio, angle of repose for powder material. Prepared tablets were evaluated for hardness, thickness, friability, weight variation, drug content, swelling index.. In-vitro drug release was tested in phosphate buffer pH 2.1 in time upto 12 hrs.²

Conclusion Among all these formulations F3 shows maximum drug release up to 96.02% Optimized tablet formulation was subjected Accelerated stability studies (AST) was carried for optimized formulation F3 by exposing it to 40°C/75% RH for one month and analyzed the sample at the interval of 7,14,21,28 days. Kinetics of formulation purely follows the Anomolous transport mechanism

Keywords Losartan potassium, HPMCK100M, HPMCK4, Carbopol 934.