Development and in-vitro Evaluation of Once Daily Tablet Dosage Form of Loxoprofen Sodium

Purpose: To formulate and characterize once daily controlled release tablet of loxoprofen sodium. Methods : Eudragit RS-100, hydroxylpropyl methylcellulose (HPMC) and pectin were used as release retarding polymers. All the formulations were prepared by direct compression method. Various precompression studies were carried out to determine Hausner’s ratio, Carr’s index, angle of repose, bulk density and tapped density Differential scanning calorimetry (DSC) studies and also post-compression studies to evaluate hardness, friability, weight variation, drug content, in-vitro drug release were conducted on the tablets. The drug release data were subjected to kinetic models, including zero order, first order, Hixon Crowell, Higuchi and Korsmeyer-Peppas. Results : Compressibility index (7.6 ± 1.32 - 12.5 ± 1.43%), Hausner’s ratio (1.08 ± 0.04 - 1.14 ± 0.03), angle of repose (27.78 ± 0.47 - 30.49 ± 0.46°), hardness (6.25 ± 0.27 - 7.21±0.21 kg/cm2), friability (0.14 ± 0.06 - 0.28 ± 0.0 %), weight variation (249.5 ± 2.09 - 251.35 ± 2.41 mg) and drug content  (97.30 ± 0.28 - 103.70 ± 0.31 %) were within generally accepted limits for the pre-and post-compression formulations, respectively. The tablets having the maximum amount of among the three polymers tested as matrix materials, HPMC, represented by F3 tablets, exerted better sustained release properties after 12 h. Release pattern was more of Fickian diffusion followed by Higuchi mechanism. Conclusion : The release of the loxoprofen sodium was optimized up to 12 h. Keywords : Loxoprofen, Sustained release, hydroxypropyl methylcelluose, Pectin, Eudragit, Matrix tablets

[1]  M. Shoaib,et al.  Formulation development of intermediate release Nimesulide tablets by CCRD for IVIVC studies. , 2014, Pakistan journal of pharmaceutical sciences.

[2]  Sanjay K. Jain,et al.  Development and in vitro characterization of floating microspheres bearing tramadol HC1. , 2011, Acta Poloniae Pharmaceutica - Drug Research.

[3]  R. Manavalan,et al.  Preparation and evaluation of sustained release loxoprofen loaded microspheres , 2011, Journal of basic and clinical pharmacy.

[4]  G. Murtaza,et al.  Formulation and characterization of modified release tablets containing isoniazid using swellable polymers. , 2011, African journal of traditional, complementary, and alternative medicines : AJTCAM.

[5]  S. Naseem,et al.  Encapsulation and characterization of controlled release flurbiprofen loaded microspheres using beeswax as an encapsulating agent , 2010, Journal of materials science. Materials in medicine.

[6]  N. K. Jain,et al.  Formulation and in vitro, in vivo evaluation of extended- release matrix tablet of Zidovudine: Influence of combination of hydrophilic and hydrophobic matrix formers , 2006, AAPS PharmSciTech.

[7]  J. Gierse,et al.  Enzymologic and pharmacologic profile of loxoprofen sodium and its metabolites. , 2005, Biological & pharmaceutical bulletin.

[8]  Santi,et al.  Swellable matrices for controlled drug delivery: gel-layer behaviour, mechanisms and optimal performance. , 2000, Pharmaceutical science & technology today.

[9]  Ravi Kumar M.N.V. Nano and microparticles as controlled drug delivery devices. , 2000 .

[10]  N. Peppas,et al.  Mechanisms of solute release from porous hydrophilic polymers , 1983 .

[11]  H. Khan,et al.  Formulation and Evaluation of Mouth Disintegrating Tablets of Atenolol and Atorvastatin , 2015, Indian journal of pharmaceutical sciences.

[12]  Manimaran,et al.  Formulation and In-Vitro Evaluation of Sustained Release Matrix Tablets Of Losartan Potassium , 2014 .

[13]  M. Shoaib,et al.  Formulation development and optimization of nimesulide tablets by central composit design and effect of surfactants on dissolution studies , 2011 .

[14]  Kale,et al.  A NEW BINARY POLYMERIC MATRIX SYSTEM FOR SUSTAINEDRESEASE DRUG DELIVERY OF HIGHLY SOLUBLE DRUG: DILTIAZEM HYDROCHLORIDE , 2011 .

[15]  R. RadhikaP.,et al.  FABRICAT ION OF SUSTAINED RELEASE MATRIX TABLETS OF VE NLAFAXINE HYDROCHLORIDE USING EUDRAGITS , 2011 .

[16]  R. Gollapudi,et al.  FORMULATION AND INVITRO EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF LOSARTAN POTASSIUM , 2011 .