IMPROVEMENT OF MICROMERITIC, COMPRESSIBILITY AND SOLUBILITY CHARACTERISTICS OF LINEZOLID BY CRYSTALLO-CO-AGGLOMERATION TECHNIQUE


Atul M. Kadam, Shitalkumar S. Patil

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.


Keywords


Crystallo-co-agglomeration, Good solvent, Micrometrics, Linezolid, Direct compression

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About this article

Title

IMPROVEMENT OF MICROMERITIC, COMPRESSIBILITY AND SOLUBILITY CHARACTERISTICS OF LINEZOLID BY CRYSTALLO-CO-AGGLOMERATION TECHNIQUE

Keywords

Crystallo-co-agglomeration, Good solvent, Micrometrics, Linezolid, Direct compression

DOI

10.22159/ijap.2017v9i4.18915

Date

13-07-2017

Additional Links

Manuscript Submission

Journal

International Journal of Applied Pharmaceutics
Vol 9, Issue 4, 2017 Page: 47-53

Online ISSN

0975-7058

Statistics

9 Views | 42 Downloads

Authors & Affiliations

Atul M. Kadam
Department of Pharmaceutics, Ashokrao Mane College of Pharmacy, Peth-Vadgaon, Shivaji University, Kolhapur, Maharashtra, India
India

Shitalkumar S. Patil
Department of Pharmaceutics, Ashokrao Mane College of Pharmacy, Peth-Vadgaon, Shivaji University, Kolhapur, Maharashtra, India
India


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