Volume : 11, Issue : 02, February – 2024

Title:

FORMULATION AND EVALUATION OF SUSTAINED RELEASE FORMULATIONS OF LOSARTAN POTASSIUM BY MELT GRANULATION TECHNIQUE

Authors :

Sasikanth Kothamasu*, Inturi Syamala, B. Thangabalan

Abstract :

Losartan potassium is an anti hypertensive. It is used in the treatment of hypertension. However oral bioavailability is poor (about 38%) which is due to first-pass hepatic metabolism. After oral administration, the terminal half-life is between 1.5 -2 h, and it is hygroscopic and light sensitive. Hence, it is considered as a suitable candidate for the Sustained release formulations by melt granulation method. Melt granulation can protect the drug from moisture and light and at the same time, it may also impart sustained release properties to the granulation. Thus reducing the frequency of administration and enhancing the patient compliance and maximizing the drug utility with minimum dose. To prepare the sustained release granules of Losartan potassium using different hydrophobic waxes like stearic acid, glyceryl monostearate and hydrogenated castor oil in different drug-wax ratios (1:1, 1:2, 1:3) and also in varying combinations (1:1:1), by melt granulation method and to evaluate the effect of concentration of hydrophobic polymer on the release rate of the water soluble drug, Losartan potassium. To evaluate the prepared granules for various pre-compression parameters such as angle of repose, bulk density, tapped density, compressibility index, particle size distribution, moisture absorbance and Hausner’s ratio etc. To evaluate the sustained release capsules for weight variation, drug content uniformity, in vitro drug release, and drug-excipient interactions (IR spectroscopy).
Keywords: Losartan potassium, Melt granulation method, Sustained release formulations.

Cite This Article:

Please cite this article in press Sasikanth Kothamasu et al., Formulation And Evaluation Of Sustained Release Formulations Of Losartan Potassium By Melt Granulation Technique, Indo Am. J. P. Sci, 2024; 11 (02).

Number of Downloads : 10

References:

1) Jantez GM, Robinson JR. Sustained- and Controlled- release drug delivery systems. In: Banker GS, Rhodes CT, editors. Modern pharmaceutics. 3rd edition,New York: Marcel Dekker Inc; 1996.
2) Popli H, Sharma SN. Trends in oral sustained-release formulations-I. The Eastern Pharmacist 1989; 32: p.99-103.
3) Hui HW, Robinson JR, Lee VHL. Design and fabrication of oral controlled release drug delivery systems. In: Robinson JR, Lee V, editors. Controlled drug delivery fundamentals and applications. 2nd ed. New York: Marcel Dekker Inc; 1987.
4) Chien YW. Novel drug delivery systems. 2nd ed. New York: MarcelDekker Inc; 1992.
5) Lachman L, Lieberman HA, Kanig JL, editors. The theory and practice of industrial pharmacy. 3rd ed. Bombay: Varghese Publishing House; 1987.
6) Lee TWY, Robinson JR. Controlled-release drug-delivery systems. In:Gennaro AR,editor. Remington: the science and practice of pharmacy. 20th ed. Easton, Pennsylvania: Mac Publishing Company; 2001.
7) Pandey VP, Manawalan R, Rajan TS, Ganesh KS. Formulation and release characteristics of sustained release Diltiazem hydrochloride tablets. Ind. J. pharm. Sci. 2003; 65(1): p. 44-48.
8) Gudsoorkar VR, Rambhau D. sustained release of drugs. The Eastern Pharmacist 1993; 36 (429): p. 17-22.
9) Gudsoorkar VR, Rambhau D. sustained release of drugs. The Eastern Pharmacist 1994; 37(433): p. 87-90.
10) D. M. Brahmankar & Sunil B. Jaishwal, “Controlled release medication” chapter 15th in “Biopharmaceutics and Pharmacokinetics – A Treatise, 1st edition, Vallabh Prakashan: 347- 353pp.
11. Brahmaiah.B, Madhu Gudipati, GP Bhagath, Formulation and Evaluation of Gastro retentive Floating Drug Delivery System of Metoprolol Tartarate, International Journal of Life Sciences Biotechnology and Pharma Research, ISSN:2250-3137, Vol-2(1), 184-201, January 2013.
12 .Brahmaiah.B, Sasikanth Kothamasu, Sreekanth Nama, Formulation and evaluation of extended release mucoadhesive microspheres of Rosuvastatin, International Journal of Biological & Pharmaceutical Research, e-ISSN NO-0976-3651, Print ISSN NO-2229-7480, 2013; 4(4): 271-281.
13. Brahmaiah Bonthagarala, Sreekanth Nama, Leela Madhuri Pola, Enhancement of Dissolution Rate of Ciprofloxacin by Using Various Solid Dispersion Techniques, International Journal of Pharmaceutical Sciences and Research, ISSN: 0975-8232, IJPSR, 2013; Vol.4(11): 4376-4383.
14.Brahmaiah Bonthagarala, G.Poornima, Sreekanth Nama, N.Suresh, Formulation and Evaluation of Pulsatile Drug Delivery System of Atenolol, American Journal of Biological and Pharmaceutical Research, Print ISSN-2228-6435, 2014; Vol-1(1): 28-33.
15.Brahmaiah Bonthagarala, G.Poornima, Sreekanth Nama, N.Suresh, Formulation and evaluation of Sublingual tablets of Sumatriptan, Indian Journal of Pharmaceutical Science and Research, e-ISSN No-2248-9126, Print ISSN NO-2248-9118, 2013; Vol-3(2):69-73.
16. Brahmaiah Bonthagarala, Sreekanth Nama, Sudarshan Donthiboina, Formulation and Evaluation of Sustained Release Matrix Tablets of Ozacarbazepine by Using Various Polymers, Singapore Journal of Pharmaceutical Research, e-ISSN No-1456-9126, Print ISSN NO-1278-9118, 2014; Vol-1(1): 1-7.
17.Brahmaiah Bonthagarala, Sreekanth Nama, Prasanna Kumar Desu*, Formulation and Evaluation of Fast Dissolving Films of Rizatriptan, International Journal of Pharmaceutical Research and Bio-Science, ISSN: 2277-8713, 2013; Volume 2(3)-298-305.
18.Brahmaiah.B, Chandu Babu Rao, Sreekanth Nama, Sreenivaulu.K, Enhancement of Dissolution Rate of Cefixime Trihydrate by Using Various Solid Dispersion Techniques, International Journal of Pharmacy & Therapeutics, e-ISSN-0976-0342, Print ISSN-2229-7456, 4(3), 2013, 140-147.
19. Brahmaiah.B, Prasanna Kumar Desu, Sreekanth Nama, S.Satish Babu, Formulation and evaluation of extended release mucoadhesive microspheres of simvastatin, International Journal of Pharmaceutical and biomedical Research, ISSN No. 0976-0350, March 2013, V0l 4(1), 57-64. www.pharmscidirect journal.
20.Brahmaiah Bonthagarala, Prasanth Pasumarthi, Katta Vamshi Kiran, Sathram Nataraja, Sudarshan Donthiboina, Formulation and evaluation of orodispersable Atenolol Maleate Tablets: A comparative Study on Natural Super disintegrents and Synthetic Super disintegrents, International Journal of Research in Ayrveda and Pharmacy, ISSN(Online)-2299-3566, ISSN (Print)-2277-4343, 5(2), Mar-Apr 2014, 185-192.
21.Bhagwat DA, Kawtikwar PS, Sakarkar DM. Sustained release matrices of verapamil HCl using glyceryl monostearate and stearic acid. Res J Pharm Tech 2008; 1(4): 405-9.
22. Senthilkumar B, Premanand DC, Senthilkumar KL, Saravanakumar M, Thirumurthy R. Formulation and evaluation of diltiazem HCl extended release tablet by melt granulation technique. Int J Pharm Ind Res 2011; 01: 36-42.