ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF NEBIVOLOL BY SOLID DISPERSION TECHNIQUE

Authors

  • Isha Shah Maharishi Arvind Institute of Pharmacy, Mansarovar, Jaipur, India-302020.
  • Shailendra Bhatt Maharishi Arvind Institute of Pharmacy, Mansarovar, Jaipur, India-302020.
  • Alpesh Yadav Maharishi Arvind Institute of Pharmacy, Mansarovar, Jaipur, India-302020.

Keywords:

Nebivolol, Solid dispersion, Fusion method, Solvent evaporation method

Abstract

Objective: Solubility is greater challenges for formulation which can be explain by different technological approaches during the pharmaceutical product development and to improve water solubility and drug release respectively.

Methods: The solid dispersions of nebivolol were prepared in ratio 1:1, 1:3, 1:5 and 1:7 by fusion and solvent evaporation method using PEG 6000 and PVP K30 as carriers to enhance solubility of compound.

Results: All the solid dispersions were evaluated for drug content, phase solubility, in vitro dissolution study. Deferential Scanning Calorimetric (DSC) and Fourier Transformer Infra Red (FTIR) showed no chemical interaction between the drug and its carriers. Solubility of PEG 6000 and PVP K30 indicates a linear relationship (AL type of curve) in the investigated polymer concentration range. The Gibb's free energy showed declined trend with increase in the carrier concentrations. The uniformly of drug content was found in all solid dispersions. The drug release obtained from different drug-carrier concentration level fitted to different kinetic model and it was found that solid dispersions exhibited fickian diffusional characteristics and best fitted to higuchi model. A PVP K30 solid dispersion (1:7 ratio) prepared by solvent evaporation method showed faster dissolution rate (94.38 %) in 30 min among studied solid dispersions..

Conclusion: The overall results showed that process of nebivolol transfer from water to carrier solution is more favorable at higher level of PVP K30. The solid dispersion of drug: PVP K 30 (1:7 ratio) prepared by solvent evaporation method was found to be optimum in term of solubility and dissolution rate. Hence, we can concluded that solubility of nebivolol can be enhanced using this carrier ratio.

Downloads

Download data is not yet available.

References

Pankajkumar SY, Udaya PS, Hans RB, Vikas K, A. characterization and in vitro dissolution studies of solid dispersions of ketoprofen with PVP K30 and D-mannitol. Saudi Pharmaceutical Journal 2013;21:77-84.

Choudhary A, Rana AC, Aggarwal G, Kumar V, Zakir F, Sinica B. Development and characterization of an atorvastatin solid dispersion formulation using skimmed milk for improved oral bioavailability. Acta Pharmceutica 2012;2(4):421-8.

Aguiar AJ, Zelmer JE, Kinkel AW. Deaggregation behavior of a relatively insoluble substituted benzoic acid and its sodium salt. J Pharm Sci 1967;56(10):1243-52.

Swain S, Patra CN, Jammula S, Rao MEB. Design and evaluation of sustained release solid dispersions of verapamil hydrochloride. International Journal of Pharmceutical Science and Nanotechnology 2011;3(4):1252-62.

Leuner C, Dressman J. Improving drug solubility for oral delivery using solid dispersions. European journal of pharmaceutics and biopharmaceutics:official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik eV 2000;50(1):47-60.

Sugimoto M, Okagaki T, Narisawa S, Koida Y, Nakajima K. Improvement of dissolution characteristics and bioavailability of poorly water-soluble drugs by novel cogrinding method using water-soluble polymer. International Jornal of Pharmaceutics 1998;160:11-9.

Sheen PC, Khetarpal VK, Cariola CM, Rowlings CE. Formulation studies of a poorly water-soluble drug in solid dispersions to improve bioavailability. Int J Pharm 1995;118:221-7.

Higuchi T, Connors KA. Adv. Anal. Chem. Instrum. Eur J Haematol 1965;4:117-212.

Mahmoud EB, Gihan F, Mohamed F. Improvement of solubility and dissolution rate of indomethacin by solid dispersions in Gelucire 50/13 and PEG4000 Saudi Pharmaceutical Journal. Eur J Haematol 2009;17:217-25.

Tariqueiquebal Md. Enhancement of solubility for risperidone fast dissolving tablets International journal of universal pharmacy and life sciences MayJune 2012;2(3):394-408.

Habib MJ, Technomic T. Pharmaceutical Solid Dispersion Lancaster, Pennysylvania,. pp2001. 7-36.

Higuchi T. Mechanism of sustained-action medication:theoretical analysis of rate of release of solid drugs dispersed in solid matrices, J. Pharm. Sci. Eur J Haematol 1963;52:1145-9.

Korsemeyer RW, Peppas NA, Gurney R, Doelker E, Buri P. Mechanisms of solute release from porous hydrophilic polymers, Int. J. Pharm. Eur J Haematol 1983;15:25-35.

Ritschel WA. Biopharmaceutic and pharmacokinetic aspects in the design of controlled release peroral drug delivery systems, Drug Dev. Ind Pharm 1989;15:1073-103.

Singh K, Fong YF, Kuperan P. A comparison between intravenous iron polymaltose complex (Ferrum Hausmann) and oral ferrous fumarate in the treatment of iron deficiency anaemia in pregnancy. Eur J Haematol 1998;60(2):119-24.

Kadria AE, Maha AH, Samar AA. Formulation and optimization of orodispersible tablets of flutamide. Saudi Pharmaceutical Journal 2013:1-9.

Published

01-07-2014

How to Cite

Shah, I., S. Bhatt, and A. Yadav. “ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF NEBIVOLOL BY SOLID DISPERSION TECHNIQUE”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 6, no. 7, July 2014, pp. 566-71, https://www.innovareacademics.in/journals/index.php/ijpps/article/view/1762.

Issue

Section

Original Article(s)