Preparation and characterization of aceclofenac microspheres

Parul Trivedi, A M L Verma, N Garud


The objective of the present study was to microencapsulate the anti-inflammatory drug (aceclofenac) to provide controlled release and minimizing or eliminating local side effect by avoiding the drug release in the upper gastrointestinal track.
The drug was targeted to the colon and their aligned area for their local effect. Aceclofenac was microencapsulated with Eudragit (S 100, RL 100, and RS 100), using an O/W emulsion-solvent evaporation technique. Aceclofenac microspheres
were subjected to micromeritic properties including angle of repose, bulk density, tapped density, Carr’s index, Hausner’s ratio, and particle size determination. Microspheres were subjected to drug loading, in vitro drug release as well as for
scanning electron microscopy.The prepared microspheres were white, free-flowing, and almost spherical in shape.The drug- loaded microspheres show 60-82% drug entrapment, angle of repose was in the range of 16.13 ± 0.621-24 ± 0.590, bulk
and tapped densities respectively were in the range of 0.311 ± 0.006-0.562 ± 0.012 and 0.373 ± 0.01-0.735 ± 0.02, Carr’s index ranges from 14.04 ± 0.026 to 27.25 ± 1.405, Hausner’s ratio was 1.14 ± 0.026-1.37 ± 0.03, and particle size was in the range of 79.7016-144.840 μm. In vitro drug release studies were carried out up to 24 h in three different pH media, i.e., 0.1 N HCl (pH 1.2), phosphate buffer (pH 6.8), and phosphate buffer (pH 7.4). The drug-polymer concentration of dispersed phase influences the particle size and drug release properties. All the formulations at higher pH were followed
by the Matrix-Higuchi model.

Full Text:



An article on Aceclofenac 100 mg tables: High in efficacy, Higher in

safety by Intas Pharmaceutical ltd.

Lay Summary of Aceclofenac 100 mg tablets by MHRA - PAR-PL


Parfitt K. Analgesic Anti inflammatory and antipyretic. In: Reynolds JE,

editor. Martindale: The complete drug reference. 32nd ed. Massachusetts:

p. 2-12.

Mutalik S, Naha A, Usha AN, Ranjith AK, Musmade P, Manoj K, et al.

Preparations: In-vitro, Preclinical and clinical evaluation of once daily

sustained release tablets of Aceclofenac. Arch Pharm Res 2007;30:


Yamazaki R, Kawai S, Mizushima Y, Matsuzaki T, Hashimoto S,

Yokokura T, et al. A major metabolites of Aceclofenac, 4’-hydroxy

Aceclofenac Suppress the production of interstitial pro-collagenase -

pro MMP-1 and Pro-stromelysin-1 - Pro MMP-3 by human rheumatoid

synovial cells. Inflamm Res 2000;49:133-8.

Bolourtchian N, Karimi K, Aboofazel R. Preparation and characterization

of Ibuprofen microsphere. J Microencap 2005;22:529-38.

Obeidat WM, Price JC. Preparations and evaluation of eudragit S

microspheres as pH Sensitive release preparation for Piroxicam

and Theophylline using the emulsion-solvent evaporation method.

J Microencap 2006;23:195-202.

Perumal D, Dangor CM, Alcock RS, Hurbons N, Moopanar KR. Effect

of formulation variables on in-vitro drug release and Micromeritic

properties of modified release Ibuprofen microspheres. J Microencap


Jain SK, Rai G, Saraf DK, Agrawal GP. The preparation and evaluation

of Albendazole microspheres for colonic delivery. Pharma Tech 2004;:


Sahoo SK, Mallick AA, Barik BB, Senapati PC. Formulation and in-vitro

evaluation of eudragit microsphere of stavudine. Trop J Pharm Res


Ziyaur R, Kanchan K, Khar RK, Mushir A, Charoo NA, Shamsher AA.

Characterization of 5-fluorouracil microsphere for colonic delivery.

AAPS Pharm Sci Tech 2006;7:2.

Tamilvanan S. BSA effect of production variable on the physical

characteristics of Ibuprofen loaded polystyrene microparticles.

J Microencap 1999;16:411-8.

P formulate excipents - Aspartame Methacrylate - Based coating by

Rohm. America, 1-2.

Jain D, Panda DK, Majumdar DK, Eudragit S. 100 entrapped insulin

microspheres for oral delivery. AAPs Pharm Sci Tech 2005;6:E100-7.

Amal H, Kamel EL, AL-Shora DH, El Sayed YM. Formulation and

pharmacodynamic evaluation of captopril sustain release microparticles.

J Microencap 2006;23:389-404.

Patel JK, Patel RP, Amin AF, Patel MM. Formulation and evaluation

of Mucoadhesive glipizide microsphere. AAPs Pharm Sci Tech


Milling EL. The theory and practice of industrial pharmacy. In:

Lachman L, Liberman HA, editors. 3rd ed. Mumbai India: Varghese

Publishing House; 1991. p. 26-7.

Banker G, Anderson R. Tablet. In: Lachman L, Liberman H, Kanig J,

editors. The theory and practice of industrial pharmacy. Philadelphia:

Lea and Febiger; 1987. p. 317.

Liberman HA, Lachman L, Schwartz JB. Pharmaceutical dosage forms:

Tablet, 2, New York: Marcel Dekker; 1990. p. 201-43.



  • There are currently no refbacks.