alexa Formulation, Characterization and Pharmacokinetic Evaluation of Telmisartan Solid Dispersions | OMICS International| Abstract

ISSN: 2329-9053

Journal of Molecular Pharmaceutics & Organic Process Research

  • Research Article   
  • J Mol Pharm Org Process Res 2016, Vol 4(1): 131
  • DOI: 10.4172/2329-9053.1000131

Formulation, Characterization and Pharmacokinetic Evaluation of Telmisartan Solid Dispersions

Arno A Enose1, Priya Dasan2, Hariharan Sivaramakrishanan3 and Vandita Kakkar4*
1Reckitt Benckiser Health Care India Pvt Limited, Village-sandholi, Distt Solan, Baddi, Himachal Pradesh, India
2Material Chemistry Division, VIT University, Vellore, India
3Piramal Enterprises Limited, Mumbai, India
4Department of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India
*Corresponding Author : Vandita Kakkar, Department of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh-160014, India, Tel: 0172-2541142, Email: [email protected]

Received Date: Mar 03, 2016 / Accepted Date: Jun 08, 2016 / Published Date: Jun 15, 2016

Abstract

Telmisartan (TEL), a BCS class II antihypertensive drug possesses poor aqueous solubility which results in poor bioavailability after oral administration. Solid dispersion approach has been widely and successfully used to improve the biopharmaceutical profiles of the poorly soluble drugs. Present study was an attempt to prepare and compare the solid dispersion (SD) of Telmisartan using a novel polymer soluplus® by employing spray drying and melt extrusion techniques. Results demonstrated an improvement in solubility of TEL by 44, 3.3, 11 and 99 times as compared to pure drug in water and buffers pH 1.2, 4.5 and 7.4 respectively, post preparation of solid dispersions. Further, similar improvement was observed in in vitro release studies highlighting the importance of formulating solid dispersion. DSC and PXRD study revealed the amorphous state of TEL in solid dispersion. The developed SD were found to be stable at 40°C/75% RH, 25°C/60% RH and 2-8°C in accordance to ICH guidelines. The pharmacokinetic study in rats revealed promising results which were correlated well with the in vitro dissolution and solubility study. Results indicated the usefulness of solid dispersions prepared using soluplus® by industrially viable techniques to improve not only the bioavailability of TEL but also their potential for commercialization.

Keywords: Telmisartan; Bioavailability; Melt extrusion; Spray drying; Commercialization

Citation: Enose AA, Dasan P, Sivaramakrishanan H, Kakkar V (2016) Formulation, Characterization and Pharmacokinetic Evaluation of Telmisartan Solid Dispersions. J Mol Pharm Org Process Res 4: 131. Doi: 10.4172/2329-9053.1000131

Copyright: ©2016 Enose AA, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Select your language of interest to view the total content in your interested language

Post Your Comment
Share This Article
Relevant Topics
Recommended Conferences
Article Usage
  • Total views: 10042
  • [From(publication date): 6-2016 - Apr 21, 2018]
  • Breakdown by view type
  • HTML page views: 9774
  • PDF downloads: 268