IMPROVEMENT OF MICROMERITIC, COMPRESSIBILITY AND SOLUBILITY CHARACTERISTICS OF LINEZOLID BY CRYSTALLO-CO-AGGLOMERATION TECHNIQUE
DOI:
https://doi.org/10.22159/ijap.2017v9i4.18915Keywords:
Crystallo-co-agglomeration, Good solvent, Micrometrics, Linezolid, Direct compressionAbstract
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.
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References
Shangraw RF. Compressed tablets by direct compression. In: Lieberman HA, Lachman L, Schwartz JB. editors. Pharmaceutical dosage forms: tablets. Vol. I. 2nd ed. New York: Marcel Dekker; 1989. p. 195–246.
Ali N, Maryam M, Davood H, Mohammad BJ. Preparation of agglomerated crystals for improving flowability and compactibility of poorly flowable and compatible drugs and excipients. Powder Technol 2007;175:73–81.
Paradkar A, York P. Crystal engineering and particle design for the powder compaction process In Celik M. editors. Pharmaceutical powder compaction technology. 2nd ed. London: Informa healthcare; 2011. p. 235-52.
Hassanpour A, Ghadiri M. Distinct element analysis and experimental evaluation of heckle analysis of bulk powder compression. Powder Technol 2004;141:251–61.
Denny PJ. Compaction equations: a comparison of the Heckel and Kawakita equations. Powder Technol 2002;127:162–72.
Kawashima Y. Spherical crystallization as a novel particle design technique for oral drug delivery system. Chin Pharm J 1989;41:163-72.
Yadav VB, Yadav AV. Comparative tabletting behavior of carbamazepine granules with spherically agglomerated crystals prepared by spherical crystallisation technique. Int J ChemTech Res 2009;1:476-82.
Kadam SS, Mahadik KR, Paradkar AR. Inventors a process for making agglomerates for use as or in a drug delivery system. Indian Patent 183036; 1997.
Kadam SS, Mahadik KR, Paradkar AR. Inventors a process for making agglomerates for use as or in a drug delivery system. Indian Patent 183481; 1997.
Pawar AP, Paradkar AR, Kadam SS, Mahadik KR. Crystallo-co-agglomeration: a novel technique to obtain ibuprofen-paracetamol agglomerates. AAPS PharmSciTech 2004;5:44.
Sarfaraz MD, Arshad K, Doddayya H, Reddy SR, Udupi RH. Particle design of aceclofenac-disintegrant agglomerates for direct compression by crystallo-CoAgglomeration technique. Asian J Pharm Tech 2011;1:40-8.
Nokhodchi A, Maghsoodi M. Preparation of spherical crystal agglomerates of naproxen-containing disintegrant for direct tablet making by spherical crystallization technique. AAPS PharmSciTech 2008;9:54-9.
Keshwani B, Jaimini M, Sharma D. Spherical crystallization: a revolution in the field of particle engineering. Int J Curr Pharm Res 2015;7:19-25.
Chaturvedi A, Sharma P, Bansal M. A review on recent advancement in crystallo-co-agglomeration. Adv Biol Res 2011;5:273-81.
Yadav AV, Yadav VB. Designing of pharmaceuticals to improve physiochemical properties by spherical crystallization technique. J Pharm Res 2008;1:105-12.
Higuchi T, Connors KA. Phase-solubility techniques. Adv Anal Chem Inst 1965;4:117–212.
Shendge RS, Sayyad FJ. Formulation development and evaluation of colonic drug delivery system of budesonide microspheres by using spray drying technique. J Pharm Res 2013;6:456-61.
Ganeshan V, Ethiraj T. Preparation and characterization of crystals of prulifloxacin. Int J Pharm Pharm Sci 2015;7:307-10.
Heckel RW. Density-pressure relationships in powder compaction. Trans Metall Soc AIME 1961;221:671-5.
Heckel RW. An analysis of powder compaction phenomena. Trans Metall Soc AIME 1961;221:1001-8.
Rubinstein MH, Musikabhumma P. A universal friability test for tablet granules. Pharm Acta Helv 1978;53:125-9.
Yadav AA, Yadav DS, Karekar PS, Pore YV, Gajare PS. Enhanced solubility and dissolution rate of Olmesartan medoxomil using the crystallo-co-agglomeration technique. Pharm Sinica 2012;3:160-9.
Patil S, Pawar A, Shahoo SK. Effect of additives on the physicochemical and drug release properties of pioglitazone hydrochloride spherical agglomerates. Trop J Pharm Res 2012;11:18-27.
Kawashima Y. Crystal modification of phenytoin with polyethylene glycol for improving mechanical strength, dissolution rate and bioavailability by spherical crystallization technique. Chem Pharm Bull 1986;34:3376-83.
Jadhav NR, Pawar AP, Paradkar AR. Design and evaluation of deformable talc agglomerates prepared by crystallo-co-agglomeration technique for generating the heterogeneous matrix. AAPS PharmSciTech 2007;8:1-7.
Lalla JK, Bhat SU. A look at process costing and cost-effectiveness of a pharmaceutical formulation. Indian Drugs 1995;32:551-60.
Sanghavi NM, Sivanand R, Kotwaney HN. Dissolution pattern of miniscular sulfisoxazole. Indian J Pharm Sci 1979;41:116-7.
Alsaidan SM, Abdulhakeem AA, Eshra AG. The improved dissolution rate of indomethacin by adsorbents. Drug Dev Ind Pharm 1998;24:389-94.
Pawar AP, Paradkar AR, Kadam SS, Mahadik KR. Agglomeration of ibuprofen with talc by novel crystallo-co-agglomeration technique. AAPS PharmSciTech 2004;5:30-5.
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