DESIGN AND DEVELOPMENT OF FLOATING PULSATILE DRUG DELIVERY OF LOSARTAN POTASSIUM

  • ANIL KUMAR J. SHINDE Department of Pharmaceutics, Bharati Vidyapeeth College of Pharmacy, Near Chitranagari, Kolhapur (M. S), India http://orcid.org/0000-0003-1857-3133
  • NIDHI S. PATIL Department of Pharmaceutics, Bharati Vidyapeeth College of Pharmacy, Near Chitranagari, Kolhapur (M. S), India
  • TRUPTI S. JADHAV Department of Pharmaceutics, Bharati Vidyapeeth College of Pharmacy, Near Chitranagari, Kolhapur (M. S), India
  • HARINATH N. MORE Department of Pharmaceutics, Bharati Vidyapeeth College of Pharmacy, Near Chitranagari, Kolhapur (M. S), India

Abstract

Objective: The objective of the present investigation was to the development of floating pulsatile drug delivery system of Losartan potassium (LP) tablets for obtaining no drug release during floating followed by pulsed, rapid drug release to achieve chronotherapeutic release. In hypertension, the risk of getting heart attacks early in the morning is high and therefore, there was need to develop drug delivery, which will release drugs at morning hours and provide efficacious therapy. LP is a short biological half-life (1.5-2.5h) and readily absorbed from the stomach and upper gastrointestinal tract.


Methods: Tablet formulation was prepared by press coating of rapid release core tablets and core tablets were further top coated with a buoyant layer of HPMC K4M and sodium bicarbonate. Various grades of HPMC polymer (E5/E15/E50) were used for the pulsatile coating layer. The developed formulations were characterized for physical characteristics, floating lag time, floating time, release lag time, drug content, swelling index, in vitro dissolution studies, DSC and XRD.


Results: The FTIR and DSC studies predicted that there was no chemical interaction between drug and excipients. The core tablet coated with HPMC E50 showed a high swelling index and release the drug 97.60±1.2% at 6h. Buoyant layer with 80 mg HPMC K4M and 25 mg sodium bicarbonate gave satisfactory floating lag time.


Conclusion: The system showed an excellent lag phase followed by burst release in the distal small intestine, which gives site and time-specific delivery of LP acting as per chronotherapy for treatment of hypertension.

Keywords: Losartan potassium, Floating, Pulsatile, Circadian rhythm, Press coating

References

1. Dalvadi H, Patel JK. Chronopharmaceutics, pulsatile drug delivery system as current trend. Asian J Pharma Sci 2010;5:204-30.
2. Kakade TB, Shelar DB, Tikole SS, Bamane GS, Ubale AT. Floating pulsatile drug delivery system: an overview. Int Res J Invent Pharma Sci 2014;2:151-62.
3. Parmar RD, Parikh RK, Vidyasagar G, Patel DV. Pulsatile drug delivery system: an overview. Int J Pharma Sci Nanotech 2009;2:605-14.
4. Rajput M, Sharma R, Kumar S, Jamil F, Sharma S. Pulsatile drug delivery system: a review. Int J Res Pharm Bio Sci 2012;3:118-24.
5. Survase S, Kumar N. Pulsatile drug delivery. Curr Scenario Crips 2007;8:27-33.
6. Sahitya G, Krishnamoorthy B, Muthukumaran M. Importance of preformulation studies in designing formulations for sustained release dosage forms. Int J Pharm Tech 2013;4:2311-31.
7. Latha K, Uhumwangho MU, Sunil SA, Srikanth MV, Ramanmurthy KV. In vitro evaluation of oral timed-release tablet of losartan potassium using natural gum and it’s solid characterization. Int J Pharm Pharma Sci 2012;4:89-95.
8. Subbarao J, Venkateswara Rao P, Vidyadhara S, Venkateswara Rao B, Sasidhar R. L. C, UV spectrophotometric validation for identification and determination of losartan potassium in tablets. Int J Pharm Tech 2012;4:4137-43.
9. Dhakar VK, Chaurasia B, Kar A. Development and evaluation of floating pulsatile multiparticulate drug delivery system using aceclofenac as a model drug. Int J Pharm Life Sci 2012;3:1787-96.
10. Avulapati S, Roy AK, Shashidhar KR. Formulation and evaluation of taste-masked and fast disintegrating Losartan potassium tablets. Int J Drug Dev Res 2011;3:45-51.
11. Rathnanand M, Pannala S. Formulation and in vitro evaluation of floating pulsatile tablets of nizatidine for chronotherapy of ulcers. J Pharm Res 2011;4:1338-90.
12. Reddy BV, Navaneetha K, Ramana Reddy KV. Process development and optimization for moisture activated dry granulation method for losartan potassium tablets. Int J Pharm Pharma Sci 2011;6:312-7.
13. Sokar MS, Hanafy AS, Kamel AH. Pulsatile core-in-cup valsartan tablet formulations: in vitro evaluation. Asian J Pharma Sci 2013;8:234-43.
14. Krogel I, Bodmeier R. Floating or pulsatile drug delivery systems based on coated effervescent cores. Int J Pharma 1999;187:175-84.
15. Zou H, Jiang X, Kong L, Gao S. Design and evaluation of a dry coated drug delivery system with the floating-pulsatile release. J Pharma Sci 2008;97:263-73.
16. Naik JB, Zine SP. Development of single unit floating pulsatile site-specific drug delivery system for the chronotherapeutic release of aceclofenac. Int J Appl Bio Pharma Tech 2011;2:339-48.
17. Patel S, Modasia MK, Patel VM, Patel AK. Design and development of floating pulsatile drug delivery system using meloxicam. Int J Pharma Res Bio-Sci 2012;1:215-35.
18. Naik CS, Rao Basaveswara. Design and formulation development of fast-dissolving tablets of ibuprofen using novel natural superdisintegrant. Asian J Pharma Clin Res 2019;12:34-41.
19. Jagdale SC, Suryawanshi VM, Pandya SV, Kuchekar BS, Chabukswar AR. Development of press-coated, floating-pulsatile drug delivery of lisinopril. Sci Pharm 2014;82:423-40.
20. Badve SS, Sher P, Korde A, Pawar AP. Development of hollow/porous calcium pectinate beads for floating-pulsatile drug delivery. Eur J Pharma Biopharma 2007;65:85-93.
21. Shaji J, Patole V. Novel floating pulsatile approach for chronotherapeutic release of Indomethacin. J Pharma Sci 2007;6:37-41.
22. Ganesh NS, Deecaraman. Chromodulated drug delivery system of lornoxicam using natural polymers. J Pharma Res 2011;4:825-28.
23. Patel KT, Mahajan AN, Shah DA. Studies in formulation development of chronotherapeutics dosage of model drug. Der Pharm Lett 2011;3:227-40.
24. Bajpai M, Singh DC, Bhattacharya A. Design and in vitro evaluation of compression-coated pulsatile release tablets of losartan potassium. Indian J Pharm Sci 2012;74:101-6.
25. Shivhare UD. Formulation and evaluation of pulsatile drug delivery system of Losartan potassium by using factorial design. Int J Pharma Sci Nanotech 2013;5:1895-901.
26. Raghavendra K, Marina K. An investigation on formulation and evaluation of specialized chronotherapeutical drug delivery system of losartan and hydrochlorothiazide for the treatment of hypertension. Sudi J Med Pharm Sci 2017;3:310-7.
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SHINDE, A. K. J., PATIL, N. S., JADHAV, T. S., & MORE, H. N. (2020). DESIGN AND DEVELOPMENT OF FLOATING PULSATILE DRUG DELIVERY OF LOSARTAN POTASSIUM. International Journal of Applied Pharmaceutics, 12(4), 218-227. https://doi.org/10.22159/ijap.2020v12i4.37607
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