Immediate Release Tablets of Valsartan and Efavirenz: Role of Concentration of Superdisintegrants

Authors

  • K KESAVAN Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi – 221 005, India
  • UV RAO SP (Hong Kong) Limited, Rajbhavan Road, Somajiguda, Hyderabad – 500 082, India
  • K BINDU SP (Hong Kong) Limited, Rajbhavan Road, Somajiguda, Hyderabad – 500 082, India
  • PS RAJINIKANTH Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi – 221 005, India
  • M WANI SP (Hong Kong) Limited, Rajbhavan Road, Somajiguda, Hyderabad – 500 082, India
  • J BALASUBRAMANIAM SP (Hong Kong) Limited, Rajbhavan Road, Somajiguda, Hyderabad – 500 082, India

Keywords:

Valsartan, Efavirenz, In-vitro dissolution, Superdisintegrants, Immediate release tablets

Abstract

The objective of this study was to formulate directly compressible fast disintegrating tablets of poorly water solubledrugs with different extent of drug solubilities, like valsartan and efavirenz, as model drugs. Effect of varying concentrationsof different superdisintegrants such as crospovidone, croscarmellose sodium, and sodium starch glycolate ondisintegration time and in vitro drug dissolution was studied. The disintegration time of the best immediate release tabletformulation among those tested was observed to be 21.5±1.26 sec and 20.16±0.85 sec for valsartan and efavirenz tabletscontaining 20% of Crospovidone, respectively. Drug release (from both valsartan and Efavirenz tablets) was faster fromformulations containing crospovidone compared to the other formulation. The effect was more apparent in Efavirenz,which has lesser aqueous solubility than valsartan. It was observed that 20% crospovidone was required to achieve80% drug release from efavirenz tablets. Differential scanning calorimetric studies did not indicate any drug-excipientincompatibility. In conclusion, directly compressible fast disintegrating tablets of valsartan and efavirenz with shorterdisintegration times and high dissolution rate were obtained and crospovidone seemed to be a better disintegrant forboth valsartan and efavirenz, based on disintegration time and T80% values obtained.

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References

Brown C.K, Chokshi H.P., Nickerson B., Reed R.A., Rohrs B.R. and Shah P.A. Acceptable analytical practices for dissolution testing of poorly soluble compounds. Pharm.Technol. 2005; 28(12): 56-65.

Zhang Y, Law Y, Chakrabarti S. Physical Properties and Compact Analysis of Commonly used Direct Compression Binder. AAPS Pharm.Sci.Tech. 2003; 4(4): 62.

Katakuse Y, Kohlmeyer M, Taike T, Wagner R.F, and Yamato F. Solid oral dosage forms of valsartan. US patent 6,858,228. Feb 2005.

Huang H.H. and Huang C. Preparation of solid coprecipitates of amorphous valsartan. US patent 20070166372. July 2007.

Veldkamp A.I, Heeswijk R.P.G, Meenhorst P.L et al., Quantitative determination of efavirenz (DMP 266), a novel non-nucleoside reverse transcriptase inhibitor, in human plasma using isocratic reversed-phase high-performance liquid chromatography with ultraviolet detection” Journal of Chromatography B., 1999, 734: 55–61.

International Specialty Products (ISP). Crospovidone Website: http://www.ispcorp.com/products/pharma/content/brochure/

polycros/. Accessed August 16, 2006.

Gorman E.A., Rhodes C.T., and Rudnic E.M. An evaluation of croscarmellose as a tablet disintegrant in direct compression

systems. Drug Dev. Ind. Pharm. 1982; 8(3):397–410.

Wan L.S.C., Prasad K.P.P. Uptake of water by excipients in tablets. Int. J. Pharm. 1989; 50:147–153.

Yen S.Y., Chen C.R., Lee M.T., and Chen L.C. Investigation of dissolution enhancement of nifedipine by deposition on superdisintegrants. Drug Dev. Ind. Pharm, 1997; 23(3): 313–317.

Balasubramaniam J., Bindu K., Rao U. V., Ray D., Haldar R., and Brzeczko A. Effect of superdisintegrants on dissolution of cationic drugs. Disso. Technol. 2008; 15 (2): 18-23.

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Published

2008-09-20

How to Cite

1.
KESAVAN K, RAO U, BINDU K, RAJINIKANTH P, WANI M, BALASUBRAMANIAM J. Immediate Release Tablets of Valsartan and Efavirenz: Role of Concentration of Superdisintegrants. Ars Pharm [Internet]. 2008 Sep. 20 [cited 2024 Jul. 22];49(3):229-43. Available from: https://revistaseug.ugr.es/index.php/ars/article/view/4952

Issue

Vol. 49 No. 3 (2008)

Section

Original Articles

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