Improvement of Micromeritic, Compressibility and Solubility Characteristics of Linezolid by Crystallo-Co-Agglomeration Technique

Abstract

Objective: The purpose of current study was to improve physicochemical properties such as micrometric, compressibility and solubility of linezolid (LNZ) by preparing crystallo-co-agglomerates (CCA) in the presence of polymer for the enhancement of overall physicochemical performance. Methods:The process of agglomeration involves the use of dichloromethane (DCM) as a good solvent and chloroform as bridging liquid were used to prepare agglomerates. Agglomerates were characterised in the solid state using several techniques such as Scanning electronic microscopy(SEM), Fourier transformation infrared spectroscopy (FTIR), X-ray powder diffraction analysis (XRPD) The agglomerates obtained were evaluated for micrometric, mechanical, deformation, compressibility and drug release properties.Results: It was found that micrometric properties and dissolution characteristics of agglomerates were significantly improved than that of pure linezolid. Solubility was found to be increased than pure linezolid. The solubility of crystallo co-agglomerates was found an increase in 5 fold 3 fold and 3.7 fold for PVPK30 (0.5%), PVPK30 (0.25%) and PVPK30 (0.75%) respectively. The angle of repose for all batches was found between 22 ° to 30 °Carrs index was between 12.27±0.6 to 18.73±0.4 and Hausners ratio Near to 1, indicated good flow ability of agglomerates. The time required for drug release over a period of 60 min, is as LA1>LA2>LA3. LA3 shows fast drug release than LA1 and LA2, due to solubilization of drug due to more concentration of PVPK30 and less concentration of talc.Conclusion: Based on the above results, it was revealed that CCA of linezolid prepared with DCM and HPMC (Hydroxypropyl methyl cellulose)/PEG (Polyethylene glycol)/PVP (Polyvinylpyrrolidone) K30 exhibited improved micrometric properties, compressibility and in addition to improving solubility and dissolution rate.

Preparation of Functionalized Sodium carboxymethyl cellulose/Sodium alginate-Based Tween (80) for Potential Allocation of Linezolid as Antimicrobial Agents

“…(11(a-d)). Figure (11(a)) veri es the scanned pure drug surface in crystal needlelike (Kadam et al ( 2017)) [29]. For all tested samples in Fig.…”

“…Generally, XRD analysis is a non-destructive technique utilized to scrutinize the crystallinity, amorphicity, and physical nature of the tested samples. Figure (2) depicts the XRD of the Linezolid drug alone which submitted sharp intense peaks at θ scattering angles at Table (2) con rming the nature crystallinity of the drug [13,14]. But when Linezolid was incorporated into the polymer blend/ (0.1 ml) Tween(80), the interaction between the high content of Linezolid drug especially 40, 60, and 80 mg/g, and the blend do not hinder crystal peaks of Linezolid drug Fig.…”

Identification of Chemical Compounds and Antibacterial Activity of 96% Ethanol Extract From Moringa Oleifera Lam. Leaves Against Mrsa (Methicillin Resistant Staphylococcus Aureus)

“…The results of the antibacterial activity test were summarized in [23]. In this research, the highest zones of inhibition were lower than positive control linezolid 30µg than known as the first oxazolidinones of antibacterial drugs [24]. It has inhibitory activity against a broad range of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) [25].…”

Crystallo-co-Agglomeration Technique for Improving Physicochemical Properties, Compressibility and Solubility Characteristics of Metronidazole

“…However, compressing a drug directly requires good micromeritic properties, such as flowability, good reproducible compression behaviour as it affects it's in vitro and in vivo performance (Paradkar and York, 2011), but it strongly depends upon the quality of the crystals used. To impart these properties the drugs are subjected to particle design techniques, spherical crystallization is one of the techniques of particle design (Kadam and Patil, 2017). By this technique manufacturing process are highly improved and a high degree of particle functionality is achieved.…”