OPTIMIZED DELIVERY OF DICLOFENAC SODIUM FORMULATED IN A SUSTAINED RELEASE RAPHIA AFRICANA HYDROCOLLOID MATRIX
Objective: The aim of this research work was to comparatively study various proportions of a natural hydrocolloid-Raphia africana, and polyvinylpyrrolidone (PVP) as release sustaining agents in diclofenac sodium tablet formulation.
Methods: The purified hydrocolloid (R. africana) was characterized by evaluating its organoleptic, physicochemical and flow properties. Diclofenac-polymer ratios of 1:0, 1:0.2, 1:0.4, 1:0.6, and 1:0.8 were employed to produce different granule batches using wet granulation method (that is, the drug was formulated with 0, 5, 10, 15 and 20 % w/w of either R. africana hydrocolloid or PVP, and coded DWB-00, DRA-05, DRA-10, DRA-15, DRA-20, DPP-05, DPP-10, DPP-15 and DPP-20, respectively). Flow properties of granules were studied by determining bulk density, tapped density, Carrâ€™s index, and Hausnerâ€™s ratio for all the formulations. Compressed tablets were evaluated using various parameters as weight variation, friability, hardness, tablet thickness and diameter, content uniformity and in vitro dissolution evaluated in phosphate buffer (pH 7.3).
Results: Flowability, mechanical and release parameters determined were within pharmacopoeial limits. Generally, the values of bulk and tapped densities increase as binder concentrations increase for both PVP and R. africana hydrocolloid. The values were significantly different across the batches (p<0.05). Hardness values obtained varied significantly (p<0.05) and were between 5 and 12 KgF which imply that most of the tablet batches are harder than normal depending on the proportion of the polymer used. All the batches exhibited friability within the standard limit without significant difference in values (p>0.05), indicating that tablet formulated with the experimental binders would not undergo surface abrasion. All the formulations exhibited zero order kinetics except batches DPP-10 and DPP-15 which showed Higuchi mechanism. Formulation batches DRA-05 and DRA-10 showed maximum drug release of 98% and 95% respectively after 6 h. A prolonged drug release was observed on increasing polymer ratio. Significantly higher release rates (p<0.05) were observed in the tablets formulated with PVP than those containing R. africana gum. All the batches followed non-fickian diffusion release mechanism.
Conclusion: From the study, purified R. africana hydrocolloid generally appeared to perform better than PVP as sustained release agent.
2. Salsa T, Veiga F, Pinna ME. Oral controlled release dosage forms. I. Cellulose ether polymers in hydrophilic matrices. Drug Dev Ind Pharm 1997;23:929-38.
3. Burcea Dragomiroiu GTA, Miron DS, Baloescu C, Barca M, Mitu MA, Popa DE, et al. Comparative in vitro study of immediate and modified released oral dosage forms of cefaclor. Farmacia 2012;60:334-41.
4. Tungaraza TE, Talapan-Manikoth P, Jenkins R. Curse of the ghost pills: the role of oral controlled-release formulations in the passage of empty intact shells in faeces. Two case reports and a literature review relevant to psychiatry. Ther Adv Drug Saf 2013;4:63-71.
5. Rathbone MJ, Hadgraft J, Robert MS. editors. Modified release drug delivery technology, New York: Marcell Dekker Inc; 2003.
6. Reddy MR, Manjunath K. Pharmaceutical applications of natural gums, mucilage and pectins. Chem Sci 2013;2:1233-9.
7. Baveja SK, Rao KVR, Arora J. Examination of natural gums and muclages as sustaining materials in tablet dosage form. Indian J Pharm Sci 1988;50:89-92.
8. Sujitha B, Krishnamoorthy B, Muthukumaran M. A role of natural polymers used in the formulation of pharmaceutical dosage forms. Int J Pharm Technol 2012;4:2247-62.
9. Obahiagbon FI. A review of the origin, morphology, cultivation, economic products, health and physiological implications of raphia palm. Afr J Food Sci 2009;3:447-53.
10. Adedokun MO, Olorunsola EO, Anselem EL. Comparative evaluation of metronidazole suspensions formulated with Raphia africana hydrocolloid and other natural polymers. J Appl Pharm Sci 2017;7:83-92.
11. Fitz Gerald GA, Patrono C. The coxibs selective inhibitors of cyclooxygenase-2. New Eng J Med 2001;345:433-42.
12. Solomon DH, Avorn J, Sturmer T. Cardiovascular outcomes in new users of coxibs and non-steroidal anti-inflammatory drugs: High-risk subgroups and time course of risk. Arthritis Rheum 2006;54:1378-89.
13. Dutta NK, Mazumdar K, Dastidar SG, Park JH. The activity of diclofenac used alone and in combination with streptomycin against mycobacterium tuberculosis in mice. Int J Antimicrobial Agent 2007;30:336-40.
14. Majekodunmi SO, Itiola OA. Physicochemical and binding properties of Raphia africana gum in paracetamol tablet formulations. Aca J Biotechnol 2016;4:177-85.
15. Adedokun MO, Ayorinde JO, Odeniyi MA. Compressional, mechanical and release properties of a novel gum in paracetamol tablet formulations. Curr Issues Pharm Med Sci 2014;27:187-94.
16. Bhosale RR, Riyaz AM, Osmani PC, Moin A. Formulation and evaluation of sustained release dosage form using modified cashew gum. Int J Pharm Pharm Sci 2015;7:141-50.
17. Okhamafe AO, Igboechi A, Obaseki TO. Celluloses extracted from groundnut shell and rice husk 1: preliminary physicochemical characterization. Pharm World J 1991;8: 120-30.
18. Ohwoavworhua FO, Adelakun TA. Some physical characteristics of microcrystalline cellulose obtained from raw cotton of Cochiospermum planchonii Trop J Pharm Res 2005;4:501-7.
19. Solsulski FW. The centrifuge method for determining flour absorptivity in hard red spring wheat. Cereal Chem 1962;39:344â€“50.
20. Momoh MA, Brown SA, Onunkwo GC, Chime SA, Adedokun M, Akpabio EI. Effect of hydrophilic and hydrophobic binders on the physicochemical properties of sodium salicylate tablet formulation. J Pharm Res 2012;5:2045-8.
21. Adedokun M, Essien E, Uwah T, Umoh R, Josiah J, Jackson C. Evaluation of the release properties of microcrystalline cellulose derived from Saccharum officinarum L. in paracetamol tablet formulation. J Pharm Sci Res 2014;6:342-6.
22. Deshpande AH, Wasule D. Design and evaluation of food grade wax matrix sustained release mini-tablets of montelukast sodium. Asian J Pharm Clin Res 2017;10:317-21.
23. Chukka S, Shaik S. Development and characterization of gastro-retentive drug delivery system for ritonavir tablets using natural polymers. Asian J Pharm Clin Res 2017;10:318-22.
24. Roy SKR, Naskar S, Kundu S, Koutsu K. Formulation and evaluation of sustained release bi-layer tablets of propranolol hydrochloride. Int J Pharm Pharm Sci 2014;7:264-9.
25. Adedokun MO, Itiola OA. Material properties and compaction characteristics of natural and pregelatinized forms of four starches. Carbohydr Polym 2010;79:818â€“24.
26. The United States Pharmacopoeia/National Formulary, USP 37/NF 32. Vol. I. The United States Pharmacopoeial Convention, Timbrook Parkway, Rockville; 2014. p. 344-6, 487, 491-4, 1145-7.
27. Jackson C, Akpabio E, Umoh R, Adedokun M, Ubulom P, Ekpe G. Evaluation of Sesamum indicum gum as a binder in the formulation of paracetamol granules and tablets. Res Pharm Biotechnol 2012;4:1-5.
28. Mohite PB, Khanage SG, Harish Chandra VS, Shirsath Y. Recent advances in microsponges drug delivery system. J Crit Rev 2016;3:9-16.
29. Bhosale RR, Riyaz AM, Osmani PC, Moin A. Formulation and evaluation of sustained release dosage form using modified cashew gum. Int J Pharm Pharm Sci 2015;7:141-50.
30. British Pharmacopoeia. Her Majestyâ€™s Stationary Office, London. Vol. I; 2002.