CHRONOTHERAPEUTIC DELIVERY OF DICLOFENACSODIUM USING ALMOND GUM AS CARRIER FOR THE TREATEMENT OF RHEUMATOID ARTHRITIS
Abstract
Â
 Objective: The objective of the present work was to develop and evaluate a matrix system for chronotherapeutic delivery of diclofenac sodium using almond gum as a carrier for the treatment rheumatoid arthritis.
Methods: Matrix tablets of diclofenac sodium were prepared using 30, 40, 50, 60, and 70% w/w of tablet using almond gum as a carrier by wet granulation technique. These tablets were compression coated with Eudragit S100 to prevent drug release in the stomach. All formulations were evaluated for hardness, friability, weight variation, drug content, in vitro and in vivo studies. The release kinetics were studied. The almond gum was characterized by viscosity measurements and Fourier transform infrared spectroscopy (FTIR) analysis. The coated (FC1 to FC5) and uncoated tablets (F1 to F5) were evaluated for in vitro release of diclofenac sodium after sequential exposure to pH 1.2, pH 7.4, and pH 6.8, respectively, for 2 hr, 3 hr, and 19 hr in the absence as well as presence of rat cecal content. The selected formulation was subjected to in vivo targeting efficacy studies by roentgenography technique.
Results: In vitro release studies indicated that the matrix tablets (F1 to F5) failed to control the drug release in the physiological environment of the stomach and small intestine. On the other hand, compression-coated formulations were able to protect the tablet cores from premature drug release. In the presence of rat cecal contents, FC5 formulation has shown highest release for longer period when compared to that of FC5 in the absence of cecal contents. The values of the correlation coefficient indicated that the drug release followed zero order drug release kinetics with Peppas drug release mechanism. FTIR studies confirmed that there was no interaction between the drug and the carrier. X-ray studies confirmed that the tablet successfully reached colon without getting disintegrated in upper gastrointestinal tract.
Conclusion: Based on the results, selective delivery of diclofenac sodium to the colon could be achieved using 70% w/w (FC5) of almond gum matrix tablets compression coated with Eudragit S100 as a carrier.
Keywords: Diclofenac sodium, Gum almond, Eudragit S100, Roentgenography, Rat cecal content.
Downloads
References
Salunkhe KS, Kulakarni MV. Colon specific drug delivery. J Pharm Res 2007;6(4):248-50.
Biswal PK, Kumar A, Bhadouriya AS. Design and evolution of colon specific drug delivery system. Int J Pharm Chem Biol Sci 2013;3(1):150 67.
Lemmer B. Chronopharmacokinetics: Implications for drug treatment. J Pharm Pharmacol 1999;51:887-90.
Subba Rao G, Murthy TE. Formulation and evaluation of diltiazem HCl colon targeted tablets. IJRPC 2013;3(4):819-27.
Mallikarjuna Gouda M, Shyale S, Kumar PR, Shanta Kumar SM. Design and evaluation studies on colon specific ciprofloxacin matrix tablets for inflammatory bowel disease treatment. Der Pharm Lettre2011;3(2):383-95.
U.S. Pharmacopoeia. Pharmaceutical Dosage Forms-Powders. USP29-NF24. United States: U.S. Pharmacopoeia; 2008-10.
Aulton ME. The Design and Manufacture of Medicine. 3rd ed. Spain: Churchill Livingstone, Elsevier; 2009. p. 172-5.
Lachman L, Lieberman HA, Kanig JL. The Theory and Practice of Industrial Pharmacy. 3rd ed. Bombay: Varghese Publishing House; 1987. p. 297.
Krishnaiah YS, Satyanarayana V, Dinesh Kumar B, Karthikeyan RS. In vitro drug release studies on guar gum-based colon targeted oral drug delivery systems of 5-fluorouracil. Eur J Pharm Sci 2002;16(3):185-92.
Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm 2010;67(3):217-23.
Han M, Fang QL, Zhan HW, Luo T, Liang WQ, Gao JQ. In vitro and in vivo evaluation of a novel capsule for colon-specific drug delivery. J Pharm Sci 2009;98(8):2626-35.
Van den Mooter G, Samyn C, Kinget R. In vivo evaluation of a colon-specific drug delivery system: An absorption study of theophylline from capsules coated with azo polymers in rats. Pharm Res 1995;12(2):244 7.
Published
How to Cite
Issue
Section
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.