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.
Highlights
The focus of today’s pharmaceutical industry is to better drug delivery concepts and makes the simple standard formulations as economical as possible to produce
In the thermogram of the agglomerates showed a broad endothermic peak at the 178 °C which corresponds to a loss of water and shifting peak indicating hygroscopic nature of agglomerates. These findings indicated that raw crystals of LNZ have changed for agglomerates during recrystallization Differential scanning calorimetry (DSC) results were well supported with X-ray powder diffraction analysis (XRPD) indicating the polymorphic transition of LNZ during recrystallization
The time required for drug release over a period of 60 min, is as LA1>LA2>LA3
Summary
The focus of today’s pharmaceutical industry is to better drug delivery concepts and makes the simple standard formulations as economical as possible to produce. There is an interest in examining the potential of direct compression tabletting in recent years over traditional granulation process. Compressing a drug directly requires good micromeritic properties, such as flowability, good reproducible compression behaviour as it affects in vitro and in vivo performance of pharmaceuticals [2, 3], 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 [4, 5]. By this technique manufacturing process highly improved a high degree of particle functionality is achieved [6]
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