Formulation and Evaluation of Floating Pulsatile Drug Delivery System of Ibuprofen and Ranitidine Combination

DOI:

https://doi.org/10.37285/ijpsn.2015.8.4.3

Authors

  • Behin Sundara Raj
  • I S R Punitha
  • M J Gifty

Abstract

Since rheumatoid arthritis patients experience severe pain, inflammation, and joint stiffness in the early morning hours a pulsatile drug delivery system of a suitable anti-inflammatory drug that is administered at bedtime but release the drug in the early morning would be a promising system. The objective of this work was to develop a pulsatile release tablet containing a combination of ibuprofen and ranitidine HCl from which ibuprofen gets released after a lag time of 6-7 hours. The methodology involves; analytical method development for simultaneous estimation of combination drugs, development of pulsatile release tablet and an in vivo study in rats. Lag time was controlled by coating the rapid release core tablet with different grades and concentrations of HPMC polymer. A floating gastroretentive layer was applied on top to prevent metabolism of ranitidine at the last part of the intestine. Six different formulations were prepared with three different concentrations of HPMCK4M and HPMCK100M. In vitro studies showed that the lag time increased with an increase in both concentration and viscosity of polymers. The formulation where the core tablet was coated with 100 mg of HPMCK100M had an optimum lag time of 6.3 hrs. In vivo study evaluated the ulcer protection of the formulation in four animal groups; first group remained as control, the second group received ibuprofen at a dose of 180 mg/kg, third and fourth groups received a combination of both the drugs but ranitidine in different doses. Based on this research, it can be concluded that pulsatile release of ibuprofen tablets can be successfully formulated by using HPMC polymers. The usage of ranitidine along with ibuprofen reduces the ulcerogenecity of the later.

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Keywords:

Circadian rhythm, Floating pulsatile system, Rheumatoid arthritis, Ibuprofen, Ranitidine

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Published

2015-11-30

How to Cite

1.
Raj BS, Punitha ISR, Gifty MJ. Formulation and Evaluation of Floating Pulsatile Drug Delivery System of Ibuprofen and Ranitidine Combination. Scopus Indexed [Internet]. 2015 Nov. 30 [cited 2024 Nov. 19];8(4):3009-17. Available from: https://ijpsnonline.com/index.php/ijpsn/article/view/805

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Section

Research Articles

References

Bechtold DA, Gibbs JE and Loudon AS (2010). Circadian dysfunction in disease. Trends Pharmacol Sci, 31(5):191-8.

Bhavesh S, Surendra G and Sanjay S (2008). Formulation and evaluation of bi-layer tablet of Metochlopramide Hydrochloride and Ibuprofen. AAPS Pharm Sci Tech, 9(3):818-27.

Bodmeier R and Rujivipat S (2010). Modified release from hydroxypropyl methylcellulose compression-coated tablets. Int J Pharm, 402(1-2):72-9.

Chaudary AB, Patel RK and Chaudary SA (2010). Estimation of Vasartan and Nebivolol in pharmaceutical dosage forms by absorption ratio method. Int J Res Pharm Sci, 1(2): 108-112.

Cutolo M, Seriolo B, Craviotto C, Pizzorni C and Sulli A (2003). Circadian rhythms in RA. Ann Rheum Dis, 62:593–6.

Cutolo M, Straub RH and Buttgereit F (2008). Circadian rhythms of nocturnal hormones in rheumatoid arthritis: translation from bench to bedside. Ann Rheum Dis, 67(7):905-8.

Dalavadi H and Patel PK (2010). Chronopharmaceutics pulsatile drug delivery system as a current trend. Asian J Pharma Sci, 5(5): 207-30.

Dashputre NL and Naikwade NS (2011). Evaluation of anti-ulcer activity of methanolic extract of Abutilon indicum Linn leaves in experimental rats. Int J Pharmaceu Sci Drug Res, 3(2): 97-100.

Efentakis M, Koligliati S and Vlachou M (2006). Design and evaluation of a dry coated drug delivery system with an impermeable cup, swellable top layer and pulsatile release. Int. J. Pharm, 311(1-2): 147-56.

Jain S, Sudhakar CK and Sanjay J (2012). Formulation and evaluation of floating pulsatile drug delivery system for chronotherapy of rheumatoid arthritis. Int J Pharm Pharm Sci, 1(5): 212 -5.

Janardhanan D, Lingam M, Mohan CK and Venkateswarlu V (2008). Formulation and in vitro evaluation of gastro retentive drug delivery system for ranitidine hydrochloride. Int J Pharm Sci Nono, (1): 227-32.

Jagdale SC, Sali MS, Barhate AL, Kuchekar BS and Chabukswar AR (2013). Formulation, development, and evaluation of floating pulsatile drug delivery system of atenolol. PDA J Pharm Sci Technol, 67(3): 214-28.

Jennifer M, Wicks JR and Audoly LP (2002). The role of prostaglandin E2 receptors in the pathogenesis of rheumatoid arthritis. J Clin Invest, 110(5): 651-58.

Kalantzi L, Karavas E, Koutris E and Bikiaris DN (2009). Recent advances in oral pulsatile drug delivery. Recent Pat Drug Deliv Formul, 3(1): 49-62.

Kay J and Calabrese L (2004). The role of interleukin-1 in the pathogenesis of rheumatoid arthritis. Rheumatology, 43(3): iii2–iii9.

Madhusudhan TR, Rangan A and Gregg PJ (2008). Gastric protection and gastrointestinal bleeding with aspirin thromboprophylaxis in hip and knee joint replacements. Ann R Coll Surg Engl, 90(4): 332-5.

Patel JD, Aneja K and Majumdar SH (2010). Pulsatile drug delivery system: an user friendly dosage form. J Pharmaceut Res Health Care, 2(2): 204-15.

Pawar V, Gohil V, Tamboli R, Giridhar R and Yadav MR (2012). Cartilage targeted chemical delivery of naproxen and ibuprofen for the treatment of arthritis. J Pharm Bioallied Sci, (Suppl 1): 10-1.

Praveen S, Ingavle G, Ponrathnam S, Benson JR, Li N and Pawar AP (2009). Novel/Conceptual Floating Pulsatile System Using High Internal Phase Emulsion Based Porous Material Intended for Chronotherapy. AAPS Pharm Sci Tech, 10(4): 1368–80.

Qureshi J, Ahuja A, Baboota S, Chutani K, Jain S and Ali J (2009). Development and evaluation of a time-specific pulsatile-release tablet of aceclofenac: a solution for morning pain in rheumatoid arthritis. Methods Find Exp Clin Pharmacol, 31(1):15-23.

Rainsford KD (2009). Ibuprofen: pharmacology, efficacy and safety. Inflammopharmacology, 17(6): 275-342.

Mogal RT, Galgatte UC and Chaudhari PD (2013). Floating pulsatile drug delivery of ranitidine Hydrochloride for nocturnal acid breakthrough: design, optimization, In-Vitro and In-Vivo evaluation. Int J Pharm Pharm Sci, 5(3): 722-7.

Rajput M, Sharma R, Kumar S, Jamil F, Sissodia N and Sharma S (2012). Pulsatile drug delivery system: a review. Int J Res Pharm Bio Sci, 3(1): 118-24.

Robinson M, Mills RJ and Euler AR (1991). Ranitidine prevents duodenal ulcers associated with non-steroidal anti-inflammatory drug therapy. Aliment Pharmacol Ther, 5(2): 143-50.

Salunkhe AK, Dias RJ, Mali KK, Mahajan NS and Ghorpade VS (2011). Formulation and evaluation of floating pulsatile drug delivery system of Metoprolol tartrate. Der Pharmacia Lettre, 3(3): 147-60.

Straub H R and Cutolo M (2007). Circadian rhythms in rheumatoid arthritis; implications for pathophysiology and therapeutic management. Arthritis Rheum, 56(2): 399-408.

Sukumaran S, Almon RR, DuBois D and Jusko JW (2010). Circadian rhythms in gene expression: Relationship to physiology, disease, drug disposition and drug action. Adv. Drug Delivery Rev, (62): 904-17.

The European Agency for the Evaluation of Medical Products, ICH Topic Q2B Note for Guidance on Validation of Analytical Procedures (1996): Methodology GPMP/ICH/281/95, IFPMA, Geneva, Switzerland: 1-8.

Vinothapooshan G and Sundar K (2010). Anti-ulcer activity of Mimosa pudica leaves against gastric ulcer in rats. Res J Pharmaceu Bio Che Sci, 1(4): 606-13.

Wiklund I (1999). Quality of life in arthritis patients using nonsteroidal anti-inflammatory drugs. Can J Gastroenterol, 13(2): 129-33.