Journal of Pharmacy And Bioallied Sciences
Journal of Pharmacy And Bioallied Sciences Login  | Users Online: 706  Print this pageEmail this pageSmall font sizeDefault font sizeIncrease font size 
    Home | About us | Editorial board | Search | Ahead of print | Current Issue | Past Issues | Instructions | Online submission




 
 Table of Contents  
ORIGINAL/BRIEF
Year : 2012  |  Volume : 4  |  Issue : 5  |  Page : 40-41  

Enhancement of solubility of poorly water soluble anti hypertensive drug by nanosizing approach


Department of Pharmaceutics, B. S. Patel Pharmacy College, S.I.T. Campus, Linch, Mehsana, Gujarat, India

Date of Web Publication21-Mar-2012

Correspondence Address:
Divyesh Thakar
Department of Pharmaceutics, B. S. Patel Pharmacy College, S.I.T. Campus, Linch, Mehsana, Gujarat
India
Login to access the Email id

Source of Support: None, Conflict of Interest: None


DOI: 10.4103/0975-7406.94137

Rights and Permissions
   Abstract 

The objective of this research study was to optimize formulation and process variables affecting characteristic of nanosuspension in bead milling process. In this study, the practically water-insoluble telmisartan was nanoground by using top down method i.e. media milling method. Here the media used is ZnO 2 beads. A variety of surface active agents were tested for their stabilizing effects. Formulation factors evaluated were ratio of polymer to drug, whereas process parameters were milling time and concentration of ZnO 2 beads. Different concentration of stabilizers such as poloxamer 188, poloxamer 407, HPMC E 15, PVP K30 and combination of stabilizers were used for preparation of telmisartan nanosuspension. Responses measured in this study include particle size measurement, particle size distribution and zeta potential.

Keywords: Nanosuspension, solubility, zeta potential, lyophilised


How to cite this article:
Thakar D, Bharadia P, Pandya V. Enhancement of solubility of poorly water soluble anti hypertensive drug by nanosizing approach. J Pharm Bioall Sci 2012;4, Suppl S1:40-1

How to cite this URL:
Thakar D, Bharadia P, Pandya V. Enhancement of solubility of poorly water soluble anti hypertensive drug by nanosizing approach. J Pharm Bioall Sci [serial online] 2012 [cited 2019 May 21];4, Suppl S1:40-1. Available from: http://www.jpbsonline.org/text.asp?2012/4/5/40/94137

Water solubility has always been a key obstacle in pharmaceutical formulation, affecting formulation stability and drug bioavailability. Approaches for achieving complete dissolution often have disadvantages associated with the large quantities of required excipients. Nanosuspension, consisting essentially of pure anti hypertensive drug telmisartan with minimum amount of stabilizers was formulated for rapid dissolution, thus achieving pharmacokinetic properties similar to those of a solution. [1],[2] Telmisartan is practically insoluble in water, has a high melting point (261 - 263°c) and has a high log P value (7.7). Given these features, nanosuspension can be considered as an attractive formulation approach. Poloxamer 188, poloxamer 407, HPMC E 15, PVP K 30, poloxamer 188/poloxamer 407, poloxamer 188/HPMC E15 and poloxamer 188/HPMC E15-stabilized nanosuspension were produced on a laboratory scale using media milling. Zirconium oxide beads are used as milling media in research study. [3]


   Materials and Methods Top


Telmisartan was kindly provided by Sunij Pharama Pvt Ltd (Ahmedabad, Gujarat). Poloxamer 188 (Zydus Cadila Healthcare Ltd, Bavala, Gujarat) and Poloxamer 407 (Torrent Pharmaceuticals Ltd., Bhat, Gujarat) were commercially obtained. HPMC E15 and PVP K30 used were of laboratory grade. Zirconium oxide beads were kindly provided by Sun Pharma (Baroda, Gujarat). All other chemicals and solvents were of analytical reagent grade and deionized- distilled water was throughout the study.

Method

Nanosuspension was prepared using media milling. In 20 ml vial, solution of stabilizer was prepared in 10 ml water. 20 mg telmisartan was to prepare suspension. To this suspension, 15 gm of zirconium beads (Ø 0.8 mm) were added as a milling agent. Add a magnetic bead in to this vial and placed on the magnetic stirrer at 700 rpm for 18 hr. After milling, the vials were removed from the magnetic stirrer and the nanosuspension was separated from zirconium beads by decanting the suspension followed by washing of the beads with water.


   Results and Discussion Top


Prepared nanosuspension was evaluated for particle size measurement, zeta potential, dissolution study and morphological characterization. The milling process resulted in, particle size in the range of 200 nm-600 nm, polydispersity index in the range of 0.3 to 0.7 and zeta potential in the range of −6mV to 10mV. An observation shows higher dissolution rates in nanosized product compared to untreated physical mixture. For the nanosuspension, have excellent disintegration and high surface area of the telmisartan nanoparticles give rise to a dissolution profile showing complete dissolution within minutes.


   Conclusion Top


Media milling proved to be successful for the laboratory scale production of telmisartan nanosuspension. The process yielded nanosuspension with a mean particle size 450±35 nm, a mean polydispersity index 0.4±0.1 and zeta potential -6.0±0.5 mV. It is possible to transform the liquid nanosuspension formulation to solid powder. So the final product formulation should be the lyophilised nanopowder for getting the better stability during storage.[4]

 
   References Top

1.Verma S, Lanb Y, Gokhale R, Burgess DJ. Quality by design approach to understand the process of nanosuspension preparation. Int J Pharm. 2009; 377: 185-198.  Back to cited text no. 1
    
2.Merisko-Liversidge E, Liversidge GG, Cooper ER. Nanosizing: A formulation approach for poorly-water-soluble compounds. Eur. J. Pharm. Sci. 2003; 18: 113-120.  Back to cited text no. 2
    
3.Muller RH, Jacobs C, Kayser O. Nanosuspensions as particulate drug f ormulations in therapy rationale for development and what we can expect for the future. Adv. Drug Deliv. 2001; 47: 3-19.  Back to cited text no. 3
    
4.Konan YN, Gurny R, Alleman E. Preparation and characterization of sterile and freeze dried sub -200 nm nanoparticles. Int. J. Pharm. 2002; 233: 239-252  Back to cited text no. 4
    



This article has been cited by
1 Nanotechnology Based Approaches for Enhancing Oral Bioavailability of Poorly Water Soluble Antihypertensive Drugs
Mayank Sharma,Rajesh Sharma,Dinesh Kumar Jain
Scientifica. 2016; 2016: 1
[Pubmed] | [DOI]
2 In vitro/in silico investigation of the drug substance and telmisartan tablets [In vitro/in silico ispitivanje lekovite supstance i tableta telmisartana]
Homšek, I. and Cvetković, N. and Marie, L. and Spasić, A. and Ivić, B. and Erić, S.
Arhiv za Farmaciju. 2012; 62(6): 548-561
[Pubmed]



 

Top
 
 
  Search
 
    Similar in PUBMED
   Search Pubmed for
   Search in Google Scholar for
 Related articles
    Access Statistics
    Email Alert *
    Add to My List *
* Registration required (free)  

 
  In this article
    Abstract
    Materials and Me...
    Results and Disc...
   Conclusion
    References

 Article Access Statistics
    Viewed1810    
    Printed89    
    Emailed2    
    PDF Downloaded183    
    Comments [Add]    
    Cited by others 2    

Recommend this journal