Formulation optimization and evaluation of aceclofenac sustained release dosage form based on Kollidon sustained release

Habeeb Panikkarakayil, Madhavan Nampoothiri, Gladis Kachappilly, Mohammed Shameem, Raghunath Pariyani, Y Anitha

Abstract


Sustained release aceclofenac matrix tablets constituting Kollidon sustained release (KSR) (polyvinyl acetate and povidone‐based matrix retarding polymer) were developed in this study in an attempt to design a dosage form that
manifests desirable release profile and thorough adherence to official monographs. Nine matrix tablet formulations were prepared by dry blending and direct compression method by varying the proportion of KSR and compression load with fixed percentage of aceclofenac. Among this, by comparing response variables of the prepared formulations with that of the marketed product, two formulations (KSR5 and KSR7) were chosen as the optimized formulations. The formulation showed close resemblance to commercial products and compliance with United States Pharmacopoeia USP specification.The exponential model was applied to characterize the drug release behavior from polymeric systems. It was found that non‐Fickian release is predominant in tablets containing KSR with a trend toward zero‐order kinetics.The study also involves in vivo evaluation of the optimized formulations to find out relevant pharmacokinetic parameters. Correlation of in vitro drug release with that of amount of drug absorbed in vivo has also been performed.


Full Text:

PDF

References


Collet J, Moreton C. Modified‐release peroral dosage forms. In:

Aulton ME, editor. Pharmaceutics the Science of Dosage Form Design.

nd ed. London: Churchill Livingstone; 2002. p. 289‐305.

Helfand WH, Cowen DL. Evolution of pharmaceutical oral dosage forms.

Pharm Hist 1983;25:3‐18.

Ruchatz F, Kolter K, Wittemer S, Fraunhofer W. Kollidon SR. A new

excipient for sustained release matrices. Proc Int Symp Contr Rel Bioact

Mater 1999;26:869‐76.

Kolter K, Fraunhofer W, Ruchatz F. Properties of Kollidon SR as a new

excipient for sustained release dosage forms. AAPS PharmSci. 1999

AAPS Annual Meeting Suppl 1999;1 (1).

Draganoiu E, Andheria M, Sakr A. Evaluation of the new polyvinylacetate/

povidone excipient for matrix sustained release dosage forms. Pharm

Ind 2001;63:624‐9.

Reza MS, Quadir MA, Haider SS. Development of theophylline

sustained release dosage form based on Kollidon SR. Pak J Pharm Sci

;15:63‐70.

BASF, Technical Information, ME 397e, June 1999.

Solanki AB, Parikh JR, Parikh RH. Formulation and optimization of

piroxicamproniosomes by 3‐factor, 3‐level Box‐Behnken design. AAPS

PharmSciTech 2007;8:E1‐E7.

Schwartz JB. Optimization techniques in pharmaceutical formulation and

processing. In: Banker GS, Rhodes CT, editors. Modern Pharmaceutics.

nd ed, Ch. 20. New York: Marcel Dekker Inc; 1900. p. 803‐7.

Armstrong NA, James KC. Pharmaceutical Experimental Design and

Interpretation, United Kingdom: Taylor and Francis; 1996. p. 131‐6.

Merchant HA, Shoaib HM, Tazeen J, Yousuf R. Once‐daily tablet

formulation and in vitro release evaluation of cefpodoxime using

hydroxypropyl methylcellulose: A technical note. AAPS Pharm Sci Tech

;7:78.

Boza A, Caraballo I, Alvarez‐Fuentes J, Rabasco AM. Evaluation of

Eudragit RS‐PO and Ethocel 100 matrices for the controlled release of

lobenzarit disodium. Drug DevInd Pharm 1999;25:229‐33.

Kuksal A, Tiwary AK, Jain NK, Jain S. Formulation and in vitro, in vivo

evaluation of extended‐release matrix tablet of zidovudine: Influence

of combination of hydrophilic and hydrophobic matrix formers. AAPS

PharmSciTech 2006; Article 1:1‐9E1.

Zhang YE, Tchao R, Schwartz JB. Effect of processing methods and heat

treatment on the formation of wax matrix tablets for sustained drug

release. Pharm Dev Technol 2001;6:131‐44.

Iqbal Z, Babar A, Ashraf M. Controlled‐release naproxen using

micronized ethyl cellulose by wet‐granulation and solid‐dispersion

method. Drug Dev Ind Pharm 2002;28:129‐34.

Gohel MC, Panchal MK, Jogani VV. Novel mathematical method for

quantitative expression of deviation from the higuchi model. AAPS

PharmSciTech 2000;1:45‐50.E31.

Perioli L, Ambrogi V, Angelici F, Ricci M, Giovagnoli S, Capuccella M,

et al. Development of mucoadhesive patches for buccal administration

of ibuprofen. J Control Release 2004;99:73‐82.

Sinha Roy D, Rohera BD. Comparative evaluation of rate of hydration

and matrix erosion of HEC and HPC and study of drug release from

their matrices. Eur J Pharm Sci 2002;16:193‐9.

Musmade P, Subramanian G, Srinivasan KK. High‐performance liquid

chromatography and pharmacokinetics of aceclofenac in rats. Anal

Chim Acta 2007;585:103‐9.

Althaker AY, Alkharfy KM, Khan RM. Pharmacokinetics of diclofenacin

sheep following intravenous and intramuscular administration. Saudi

Pharm J 2005;13:106‐10.

Huang YB, Tsai YH, Yang WC, Chang JS, Wu PC, Takayama K. Once‐daily

propranolol extended‐release tablet dosage form: Formulation design

and in vitro/in vivo investigation. Eur J Pharm Biopharm 2004;58:607‐14.




DOI: http://dx.doi.org/10.22377/ajp.v7i1.34

Refbacks

  • There are currently no refbacks.