Role of various natural, synthetic and semi-synthetic polymers on drug release kinetics of losartan potassium oral controlled release tablets

Abstract

Objective:The objective of the present work was to formulate and to characterize controlled release matrix tablets of losartan potassium in order to improve bioavailability and to minimize the frequency of administration and increase the patient compliance.Materials and Methods:Losartan potassium controlled release matrix tablets were prepared by direct compression technique by the use of different natural, synthetic and semisynthetic polymers such as gum copal, gum acacia, hydroxypropyl methyl cellulose K100 (HPMC K100), eudragit RL 100 and carboxy methyl ethyl cellulose (CMEC) individually and also in combination. Studies were carried out to study the influence of type of polymer on drug release rate. All the formulations were subjected to physiochemical characterization such as weight variation, hardness, thickness, friability, drug content, and swelling index. In vitro dissolution studies were carried out simulated gastric fluid (pH 1.2) for first 2 h and followed by simulated intestinal fluid (pH 6.8) up to 24 h, and obtained dissolution data were fitted to in vitro release kinetic equations in order to know the order of kinetics and mechanism of drug release.Results and Discussion:Results of physiochemical characterization of losartan potassium matrix tablets were within acceptable limits. Formulation containing HPMC K100 and CMEC achieved the desired drug release profile up to 24 h followed zero order kinetics, release pattern dominated by Korsmeyer — Peppas model and mechanism of drug release by nonfickian diffusion. The good correlation obtained from Hixson-Crowell model indicates that changes in surface area of the tablet also influences the drug release.Conclusion:Based on the results, losartan potassium controlled release matrix tablets prepared by employing HPMC K100 and CMEC can attain the desired drug release up to 24 h, which results in maintaining steady state concentration and improving bioavailability.

<p>Promising Swellable Floating Bupropion Tablets: Formulation, in vitro/in vivo Evaluation and Comparative Pharmacokinetic Study in Human Volunteers</p>

“…Additionally, the interaction between xanthan and HPMC K15M (AD) had a potent antagonistic effect on (Y 5 ) with a coefficient of (−78.79) which is attributed to the intermolecular hydrogen-bonding between them could occur. 42 Consistently, Equation (7) demonstrates the effect of xanthan gum and HPMC K15M on the drug release % after 8 h (Y 6 ) as they had the large significant negative coefficient values (−136.21, and −119.55), respectively. This is attributed to the rigid matrix layer of floating tablets containing a higher amount of xanthan and HPMC K15M, in addition to the slow erosion rate of the gel layer from these tablet matrices.…”

“…Polysaccharide gums are the most widely used materials because of naturally abundant, biocompatible/degradable, and nonimmunogenic properties. 7 Apart from successful dosage form preparation and optimization of the novel drug delivery systems with few experiments, design of experiment (DoE) was tailored as an economical approach. This is achieved by optimizing the composition of pharmaceutical formulations using the statistical experimental designs and desirability function as an efficient way to select the optimized formulation.…”

<p>Modulation of Drug Release from Natural Polymer Matrices by Response Surface Methodology: in vitro and in vivo Evaluation</p>

“…18 The polymeric matrices are generally made up of synthetic, semi-synthetic or natural polymers. [19][20][21] Among them, polymers of natural origin, which are commonly utilized in the cosmetic and food industry, are extensively adopted in pharmaceutical research and are currently used in matrix tablet technology. 17,22,23 Polysaccharide gums, including karaya gum and locust bean gum, are one of the natural polymers, which are biodegradable, non-toxic, biocompatible, non-immunogenic and naturally abundant.…”

3D printing of cellulose derivatives based-biogel matrices as the drug delivery system and support structure

“…(Debotton & Dahan, 2016;Marques-Marinho & Vianna-Soares, 2013;Ogaji et al, 2012). The HPMC-based hydrophilic matrices have been widely applied in pharmaceuticals as an excipient in controlled release drug delivery systems (Jayasree et al, 2014). The HPMC matrices prevent the diffusion or erosion of the dissolution medium through hydrated layers to dissolve solid pharmaceutical dosages (Bhatia, 2016;.…”

“…Those polymers that were naturally derived but chemically modified were semi-synthetic excipients, such as MC, HPMC, and carboxymethyl ethylcellulose (CMEC). Examples of synthetic excipient included the organic chemicals which were derived from oil or rock, such as poly (vinyl pyrrolidone) and poly (acrylic acid) Jayasree et al, 2014;Ogaji et al, 2012).…”