Effect of Lubricants on Properties of Conventional Tablets of Antihypertensive Drugs from Different Biopharmaceutical Classification System

Authors

  • Dindawar Kavita PES College of Pharmacy, Bengaluru, Karnataka 560050
  • B.M Supriya PES College of Pharmacy, Bengaluru, Karnataka.
  • Kolageri Shivanand BLDEA’s SSM College of Pharmacy and Research Centre, Vijayapur, Karnataka -India

DOI:

https://doi.org/10.22270/ajprd.v11i5.1303

Keywords:

Metoprolol Succinate, Nifedipine, Atenolol, Furosemide and Sodiumstearyl fumarate, Magnesium stearate.

Abstract

 

 

Background: Hypertension is a long-term medical condition in which blood pressure in the arteries is elevated. Hypertension causes coronary artery disease, stroke, heartfailure; kidney diseases etc.to over come hypertension, antihypertensive drugs are used.

Objectives: The aim of present work was to find out effectsof lubricants on properties of conventionaltablets containing antihypertensive drugs from different BCS class. Antihypertensive drugs suchas Metoprolol succinate, and Atenolol were selected which represented BCS class I, and II respectively.

Methods: Lubricants are the essential components of all solid dosage forms. Sodium stearyl fumarate, a hydrophilic lubricant was compared with Magnesium stearate,a conventional hydrophobic lubricant. Uncoatedtabletswereprepared either by direct compression or wet granulation technique employing sodium stearyl fumarate or magnesium stearate as a lubricant at 1% or 2%, mixing time of lubricants was varied as 3 and 6mins.

Results: Irrespective of class of drug, concentration, mixing time and processing method sodium stearyl fumarate turned out to be effective as tablet lubricant than Magnesium stearate. Both the Lubricants, when used at lower concentration and shorter mixing time resulted in superior tablets properties.Direc tcompression method gave better results than wet granulation technique. Both Sodium stearyl fumarate and Magnesium stearate (1%, 3min) were subjected to storage at400± 20C/ 75% RH for 90 days to check effect of aging and storage.

Conclusion: According to at the end of storage period up on investigating for different tablet properties there were no significan tchanges observed.

 

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Author Biographies

Dindawar Kavita, PES College of Pharmacy, Bengaluru, Karnataka 560050

PES College of Pharmacy, Bengaluru, Karnataka 560050

B.M Supriya, PES College of Pharmacy, Bengaluru, Karnataka.

PES College of Pharmacy, Bengaluru, Karnataka.

Kolageri Shivanand, BLDEA’s SSM College of Pharmacy and Research Centre, Vijayapur, Karnataka -India

BLDEA’s SSM College of Pharmacy and Research Centre, Vijayapur, Karnataka -India

References

1. Sandberg A, Ragnarsson G, Jonsson UE, Sjögren J. Design of a new multiple-unit controlled-release formulation of metoprolol-metoprolol CR. European journal of clinical pharmacology. 1988 Jan;33:S3-7.
2. Rahul M, Patil S, Shetkar M, Chavan D, Bhagwat P. A review on immediate release drug delivery systems. PharmaTutor. 2014 Aug 1;2(8):95-109.
3. Kunde SD, Bhilegaonkar S, Godbole AM, Gajr P. Biopharmaceutical classification system: A brief account. International Journal of Research Methodology. 2015;1(1):20-46.
4. Shah J, Tomar M, Singh AK, Sinha AR. Study of microcrystalline cellulose as a substitute of magnesium stearate towards functionality of lubricant in aspirin formulation. Int. J. of development research. 2017;7(10):15879-84.
5. Plosker GL, Clissold SP. Controlled release metoprolol formulations: a review of their pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension and ischaemic heart disease. Drugs. 1992 Mar;43(3):382-414.
6. Kendall MJ, Maxwell SR, Sandberg A, Westergren G. Controlled release metoprolol: clinical pharmacokinetic and therapeutic implications. Clinical pharmacokinetics. 1991 Nov;21:319-30.
7. Sonje A, Yadav A, Chandra A, Jain DA. Formulation and evaluation of immediate release tablet of antihypertensive drugs according to BCS system. Int J Therap Appl. 2012;7:18-24.
8. Sharma VJ, Amin PD. Design and optimization of metoprolol succinate formulation using melt granulation technique. Int J Pharm Pharm Sci. 2013;5(3).
9. Ajaykumar B, Babu R. Y., Sasikanth K., Laxmi Aswini G., Srinivas D. Study on Influence of Super Disintegrants and Lubricants on the Dissolution Rate of Atenolol Tablets. Res. J. Chem. Env. Sci. 2013;1(4):52-5.
10. Schwartz E, Fitchner V, Irlinger B, Haeusler O. Influence of lubricants on the tableting and disintegration time of tablets made up of coprecessed excipients vs. the physical blends. InProceedings of 5th world meeting on pharmaceutics, Biopharmaceutics and Pharmaceutical Technology, Geneva 2006 (pp. 27-30).
11. Bastos MD, Friedrich RB, Beck RC. Effects of filler-binders and lubricants on physicochemical properties of tablets obtained by direct compression: a 22 factorial design. Lat. Am. J. Pharm. 2008 Jul 1;27(4):578-83.
12. Uğurlu T, Turkoğlu M. Hexagonal boron nitride as a tablet lubricant and a comparison with conventional lubricants. International journal of pharmaceutics. 2008 Apr 2;353(1-2):45-51.
13. Aoshima H, Miyagisnima A, Nozawa Y, Sadzuka Y, Sonobe T. Glycerin fatty acid esters as a new lubricant of tablets. International journal of pharmaceutics. 2005 Apr 11;293(1-2):25-34.
14. Otsuka M, Yamane I, Matsuda Y. Effects of lubricant mixing on compression properties of various kinds of direct compression excipients and physical properties of the tablets. Advanced Powder Technology. 2004 Jan 1;15(4):477-93.
15. Kikuta JI, Kitamori N. Effect of mixing time on the lubricating properties of magnesium stearate and the final characteristics of the compressed tablets. Drug development and industrial pharmacy. 1994 Jan 1;20(3):343-55.
16. Portillo PM, Muzzio FJ, Ierapetritou MG. Using compartment modeling to investigate mixing behavior of a continuous mixer. Journal of Pharmaceutical Innovation. 2008 Sep;3:161-74.
17. Lennernäs H, Abrahamsson B. The use of biopharmaceutic classification of drugs in drug discovery and development: current status and future extension. Journal of pharmacy and pharmacology. 2005 Mar;57(3):273-85.
18. Jarosz PJ, Parrott EL. Effect of lubricants on tensile strengths of tablets. Drug development and industrial pharmacy. 1984 Jan 1;10(2):259-73.
19. Vaithianathan S, Haidar SH, Zhang X, Jiang W, Avon C, Dowling TC, Shao C, Kane M, Hoag SW, Flasar MH, Ting TY. Effect of common excipients on the oral drug absorption of biopharmaceutics classification system class 3 drugs cimetidine and acyclovir. Journal of pharmaceutical sciences. 2016 Feb 1;105(2):996-1005.
20. Rashid I, Daraghmeh N, Al-Remawi M, Leharne SA, Chowdhry BZ, Badwan A. Characterization of the impact of magnesium stearate lubrication on the tableting properties of chitin-Mg silicate as a superdisintegrating binder when compared to Avicel® 200. Powder Technology. 2010 Nov 25;203(3):609-19.
21. Parr A, Hidalgo IJ, Bode C, Brown W, Yazdanian M, Gonzalez MA, Sagawa K, Miller K, Jiang W, Stippler ES. The effect of excipients on the permeability of BCS Class III compounds and implications for biowaivers. Pharmaceutical research. 2016 Jan;33:167-76.
22. Jadhav SB, Mali AD, Rajeghadage SH, Bathe RS. Formulation and evaluation of immediate release tablets of Imipramine hydrochloride. Int. J. Biomed. Adv. Res. 2014;5(11):559-65.
23. Jamakandi VG. Formulation and evaluation of immediate release tablet of carvedilol using liquisolid compacts technique for solubility enhancement. Asian Journal of Pharmaceutics (AJP). 2016 Sep 10;10(03).
24. Deepak G, Rahul R, Senthil A, Shantesh UM. Formulation and evaluation of irbesartan immediate release tablets. Int Res J Pharm. 2012;3(4):410

Published

2023-11-24

How to Cite

Kavita, D., Supriya, B., & Shivanand, K. (2023). Effect of Lubricants on Properties of Conventional Tablets of Antihypertensive Drugs from Different Biopharmaceutical Classification System. Asian Journal of Pharmaceutical Research and Development, 11(5), 53–63. https://doi.org/10.22270/ajprd.v11i5.1303