Formulation and Optimization of Polyherbal Fast Dissolving Tablet of Curcumin, Quercetin and Rutin
Abstract
The current study was focused on the design, development, and evaluation of the fast-dissolving tablet of a polyherbal combination of curcumin, quercetin, and rutin. These herbal drugs are poorly water-soluble. The center of attention for this study is to provide quick onset of action, improved bioavailability, and increased patient compliance for administering a tablet. All parameters of Polyherbal Fast dissolving tablets were evaluated, and all were found within the official range. Drug content ranges between 90 to 105%. The formulation PHT24 containing a high concentration of Crosspovidone enhanced the drug release up to 94% within 5 minutes compared with the control. The optimized formula PHT24 showed favorable drug dissolve characteristics with better mouth feel and acceptable fast-dissolving properties. It was also observed that all formulations were acceptable with reasonable limits of the standard required for fast-dissolving tablets. The study also reveals that the Superdisintegrants used were effective in low or high concentrations. It was concluded that fast dissolving tablets with enhanced dissolution rates could be made using selected Superdisintegrants.
Keywords:
Curcumin, Quercetin, Rutin, crospovidone, polyherbal combination, direct compression method, polyherbal fast-dissolving tabletsDOI
https://doi.org/10.25004/IJPSDR.2021.130609References
Wadworth AN, Faulds D. Hydroxyethylrutosides. A review of its pharmacology, and therapeutic efficacy in venous insufficiency and related disorders. Drugs. 1992 Dec 1;44(6):1013-1032. Available from: DOI: 10.2165/00003495-199244060-00009
Ferrandiz ML, Alcaraz MJ. Anti-inflammatory activity and inhibition of arachidonic acid metabolism by flavonoids. Agents and actions. 1991 Mar;32(3):283-288.
Mascolo N, Pinto A, Capasso F. Flavonoids, leucocyte migration and eicosanoids. Journal of pharmacy and pharmacology. 1988 Apr;40(4):293-295. Available from: doi.org/10.1111/ j.2042- 7158.1988.tb05250.x
Middleton Jr E, Kandaswami C. Effects of flavonoids on immune and inflammatory cell functions. Biochemical pharmacology. 1992 Mar 17;43(6):1167-1179. Available from: doi.org/10.1016/0006- 2952(92)90489-90486
Bar-Sela G, Epelbaum R, Schaffer M. Curcumin as an anti-cancer agent: review of the gap between basic and clinical applications. Current medicinal chemistry. 2010 Jan 1;17(3):190-197. Available from: doi.org/10.2174/092986710790149738
Jurenka JS. Anti-inflammatory properties of curcumin, a major constituent of Curcuma longa: a review of preclinical and clinical research. Alternative medicine review. 2009 Jun 1;14(2).
Maheshwari RK, Singh AK, Gaddipati J, Srimal RC. Multiple biological activities of curcumin: a short review. Life sciences. 2006 Mar 27;78(18):2081-2087. Available from: doi.org/10.1016/j.lfs.2005. 12.007
Strimpakos AS, Sharma RA. Curcumin: preventive and therapeutic properties in laboratory studies and clinical trials. Antioxidants & redox signaling. 2008 Mar 1;10(3):511-546. Available from: doi. org/10.1089/ars.2007.1769
Sharma RA, Steward WP, Gescher AJ. Pharmacokinetics and pharmacodynamics of curcumin. The molecular targets and therapeutic uses of curcumin in health and disease. 2007:453-470.
Mauludin R, Müller RH, Keck CM. Development of an oral rutin nanocrystal formulation. International journal of pharmaceutics. 2009 Mar 31;370(1-2):202-209. Available from: doi.org/10.1016/j. ijpharm.2008.11.029
Yang J, Guo J, Yuan J. In vitro antioxidant properties of rutin. LWT-Food Science and Technology. 2008 Jul 1;41(6):1060-1066. Available from: doi.org/10.1016/j.lwt.2007.06.010
Boots AW, Haenen GR, Bast A. Health effects of quercetin: from antioxidant to nutraceutical. European journal of pharmacology. 2008 May 13;585(2-3):325-337. Available from: doi.org/10.1016/j. ejphar.2008.03.008
Laughton MJ, Halliwell B, Evans PJ, Robin J, Hoult S. Antioxidant and pro-oxidant actions of the plant phenolics quercetin, gossypol and myricetin: effects on lipid peroxidation, hydroxyl radical generation and bleomycin-dependent damage to DNA. Biochemical pharmacology. 1989 Sep 1;38(17):2859-2865. Available from: doi. org/10.1016/0006-2952(89)90442-5
Oršolić N, Knežević AH, Šver L, Terzić S, Bašić I. Immunomodulatory and antimetastatic action of propolis and related polyphenolic compounds. Journal of ethnopharmacology. 2004 Oct 1;94(2-3):307-315. Available from: doi.org/10.1016/j.jep.2004.06.006
Cushnie TT, Lamb AJ. Antimicrobial activity of flavonoids. International journal of antimicrobial agents. 2005 Nov 1;26(5):343-356. Available from: doi.org/10.1016/j.ijantimicag.2005.09.002
Bucki R, Pastore JJ, Giraud F, Sulpice JC, Janmey PA. Flavonoid inhibition of platelet procoagulant activity and phosphoinositide sy nthesis. Journal of Thrombosis and Haemost asis. 2003 Aug;1(8):1820-1828. Available from: doi.org/10.1046/j.1538- 7836.2003.00294.x
Duarte J, Pérez‐Palencia R, Vargas F, Angeles Ocete M, Pérez‐Vizcaino F, Zarzuelo A, Tamargo J. Antihypertensive effects of the flavonoid quercetin in spontaneously hypertensive rats. British journal of pharmacology. 2001 May;133(1):117-124. Available from: doi.org/10.1038/sj.bjp.0704064
Fincher JH. Particle size of drugs and its relationship to absorption and activity. Journal of pharmaceutical sciences. 1968 Nov 1; 57(11):1825-1835. Available from: doi.org/10.1002/jps.2600571102
Krasnyuk II, Koval’skii IV, Nikulina OI, Belyatskaya AV, Kharitonov Y Y, Grikh VV, Obidchenko YA, Vorob’ev AN. Preparation and investigation of tabletted medicinal formulations of a solid dispersion of rutin. Pharmaceutical Chemistry Journal. 2015 Oct 1;49(7):481-485. Available from: DOI 10.1007/s11094-015-1310-0
Bardakov AI, Litvin AA, Slivkin AI, Biopharmaceutical Approaches to the Development and Assessment of Ready pharmaceutical Formulations: a Textbook [in Russian], IPTs VGU, Voronezh.
Seager H. Drug-delivery products and the Zydis fast-dissolving dosage form. Journal of pharmacy and pharmacology. 1998 Apr;50(4): 375-382. Available from: doi.org/10.1111/j.2042-7158.1998. tb06876.x
Habib W, Khankari R, Hontz J. Fast-dissolve drug delivery systems. Critical Reviews™ in Therapeutic Drug Carrier Systems. 2000;17(1). Available from: DOI: 10.1615/CritRevTherDrugCarrierSyst.v17.i1.20
Indurwade NH, Rajyaguru TH, Nakhat PD. Novel approach- Fast dissolving tablets. Indian drugs. 2002; 39:405-409.
Swain RP, Nagamani R, Panda S. Formulation, in vitro characterization and stability studies of fast dispersing tablets of diclofenac sodium. J. Appl. Pharm. Sci. 2015 Jul;5:94-102. Available from: DOI: 10.7324/ JAPS.2015.50715
Sohi H, Sultana Y, Khar RK. Taste masking technologies in oral pharmaceuticals: recent developments and approaches. Drug development and industrial pharmacy. 2004 Jan 1;30(5):429-448. Available from: doi.org/10.1081/DDC-120037477
Kagalkar AA, Nitave SA. Development & evaluation of herbal fast dissolving tablet of Bauhenia veriagata Linn. Indian Journal of Drugs. 2014;2(4):169-173.
Pawar H, Varkhade C, Jadhav P, Mehra K. Development and evaluation of orodispersible tablets using a natural polysaccharide isolated from Cassia tora seeds. Integrative medicine research. 2014 Jun 1;3(2):91-98. Available from: doi.org/10.1016/j.imr.2014.03.002
Aulton ME. Pharmaceutics: The Science of Dosage Form Design. 2nd edition, Published by Churchill Livingstone, USA 1998; 223-253.
Martin A, Swarbrick J, Cammarata A. “Physical Pharmacy”, 3rd Ed, Varghese Publishing Company, Bombay 1991; 492-520.
Augshurger LL , Vuppla MK . Hand Book of Pharmaceutical Granulation Technology, Drugs and the Pharmaceutical Sciences, 7-23.
Encyclopedia of Pharmaceutical Technology, IIIrd Edition, Vol.-I, 4078.
Government of India, Ministry of health and family welfare, Indian Pharmacopoeia. The controller of Publications Ghaziabad, 2007; Vol- II, 423-424.
Subrahmanyam C.V.S. “Text Book of Physical Pharmaceutics”. 2nd edition. Delhi: Vallabh Prakashan. 2004; 210-228.
Shahi SR, Agrawal GR, Shinde NV, Shaikh SA, Shaikh SS, Somani VG, Shamkuvar PB, Kale MA. Formulation and in vitro evaluation of orodispersible tablets of etoricoxib with emphasis on comparative functionality evaluation of three classes of superdisintegrants. Rasayan J Chem. 2008;1(2):292-300.
Indian Pharmacopoeia the Controller Publication.Vol. II. Delhi; 1996; 256-257
British Pharmacopoeia- London, Vol-I and II, 2009; 1973-1977.
Furtado S, Deveswaran R, Bharath S, Basavaraj BV, Abraham S, Madhavan V. Development and characterization of orodispersible tablets of famotidine containing a subliming agent. Tropical journal of pharmaceutical research. 2008;7(4):1185-9. Available from: DOI: 10.4314/tjpr.v7i4.14705
Singh J, Singh R. Optimization and formulation of orodispersible tablets of meloxicam. Tropical Journal of Pharmaceutical Research. 2009;8(2). Available from: DOI: 10.4314/tjpr.v8i2.44524
Radke RS, Jadhav JK, Chajeed MR. Formulation and evaluation of orodispersible tablets of baclofen. Int J Chem Tech Res. 2009 Jul;1(3):517-21.
United States Pharmacopoeia 29’ The Official Compendia of Standards. Asian. Rockville MD: United States Pharmacopoeial Convention Inc. 2006; 714-720.
Sharma D, Singh G, Kumar D, Singh M. Formulation development and evaluation of fast disintegrating tablets of salbutamol sulphate, cetirizine hydrochloride in combined pharmaceutical dosage form: a new era in novel drug delivery for pediatrics and geriatrics. Journal of drug delivery. 2015;2015. Available from: doi. org/10.1155/2015/640529
The guideline, I.H. Stability Testing: Requirements for New Dosage Forms Q1C. 1996.
Daughert y DJ, Marquez A, Calcut t NA, Schubert D. A novel curcumin derivative for the treatment of diabetic neuropathy. Neuropharmacology. 2018 Feb 1;129:26-35. Available from: doi. org/10.1016/j.neuropharm.2017.11.007
Ferreira PE, Lopes CR, Alves AM, Alves ÉP, Linden DR, Zanoni JN, Buttow NC. Diabetic neuropathy: an evaluation of the use of quercetin in the cecum of rats. World Journal of Gastroenterology: WJG. 2013 Oct 14;19(38):6416. Available from: doi: 10.3748/wjg.v19.i38.6416
Tian R, Yang W, Xue Q, Gao L, Huo J, Ren D, Chen X. Rutin ameliorates diabetic neuropathy by lowering plasma glucose and decreasing oxidative stress via Nrf2 signaling pathway in rats. European journal of pharmacology. 2016 Jan 15;771:84-92. Available from: doi.org/10.1016/j.ejphar.2015.12.021
Solanki SS, Paliwal P, Jain S, Sharma P, Sarkar B. Formulation and Evaluation of CurcuminLiquisolid Tablets. Current Research in Pharmaceutical Sciences. 2012 Dec 31:210-214.
Shetake RM, Nanjwade BK, Sarkar AB, Srichana T, Bellad KA. Development and Evaluation of Quercetin Dispersible Tablets.
Mahajan HS, Bhalkar KG. Development and Evaluat ion of Rut in-HPβCD Inclusion Complex Based Mout h Dissolv ing Tablets. International Journal of Pharmaceutical Sciences and Developmental Research. 2017 Jan 21;3(1):1-6. Available from: DOI: 10.17352/ijpsdr.000009
Setty CM, Prasad DV, Gupta VR, Sa B. Development of fast dispersible aceclofenac tablets: effect of functionality of superdisintegrants. Indian journal of pharmaceutical sciences. 2008 Mar;70(2):180. Available from: doi: 10.4103/0250-474X.41452
Mohanachandran PS, Sindhumol PG, Kiran TS. Superdisintegrants: an overview. International journal of pharmaceutical sciences review and research. 2011 Jan;6(1):105-109.
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