Colon targeted tablets of Albendazole with enhanced solubility by Complexation and Micellar Solubilization
DOI:
https://doi.org/10.21276/IJRDPL.2278-0238.2019.8(3).12-19Keywords:
Albendazole, ?-Cyclodextrin, sodium lauryl sulfate, guar gum. xanthan gum, pectinAbstract
Albendazole (AZ) is a drug used for the treatment of gastrointestinal nematode infections. Phase solubility study was performed to investigate the optimized ratio of AZ: β-cyclodextrin (β-CD) solid dispersion (SD). Increase in the solubility of optimized AZ: β-CD SD was further enhanced by addition sodium lauryl sulfate (SLS) in different ratios was studied. Matrix tablets of the optimized ratio of AZ: β-CD SD with SLS and various proportions (10%, 15%, and 20%) of guar gum (GG). xanthan gum (XG) and pectin (PT) were prepared by non-aqueous wet granulation with PVP K30. Standard calibration curve for AZ was performed in three buffers like 0.1 N HCl, pH 6.8 phosphate buffer solution (PBS) and pH 7.4 PBS and absorbance were measured at 295 nm. Tablets were evaluated for various physical characteristics such as thickness, hardness, and drug content uniformity. The matrix tablets were subjected to in vitro drug release studies in 0.1 N HCl (2 h), pH 6.8 PBS (3 h) and pH 7.4 PBS (19 h) with and without rat caecal content medium. Formulation F9 shows 70.65% and 95.62% of AZ in with and without rat caecal content media respectively is selected as optimized one. Optimized formulation F9 passed the test for stability up to 3 months as per ICH guidelines.
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References
Adkin DA, Davis SS, Sparrow RA, Wilding IR. Colonic transit of different sized tablets in healthy subjects. J Control Rel. 1993; 23: 147- 156.
Jaime ND, William AR, Textbook of Organic Medicinal and Pharmaceutical Chemistry, 10th Ed, Lippincolt Publishers, New York, p: 235-52, 1988.
Rang HB, Dale MM, Rither JM, Pharmacology, 4th Ed, Churchill Livingstone, New York, p: 725-731, 1999.
Indian Pharmacopoeia, Vol. II, Indian Pharmacopoeia Commission, Ghaziabad, p: 692-93, 2007.
British Pharmacopoeia, Vol. I: British Pharmacopoeia Commission, London, p: 76-77, 2008.
United States Pharmacopoeia 26 and National Formulary 21, United States Pharmacopoeial Convention, Rockville, p: 2439-42, 2003.
Swathi. H, T. Shekshavali. In Vitro Evaluation of Anthelmintic activity of Rhus mysorensis leaves. Res. J. Pharmacology & Pharmacodynamics. 2016; 8(3): 115-117.
Gabriel Onn Kit Loh, Yvonne Tze Fung Tan, Kok-Khiang Peh. Enhancement of norfloxacin solubility via inclusion complexation with β-cyclodextrin and its derivative hydroxypropyl-β-cyclodextrin. Asian J Pharm Sci. 2016; 2: 536-546.
Lachman L, Liberman H, Kanig J, The theory and practice of industrial Pharmacy, 3rd Ed, Varghese Publishing House, Mumbai, 1991.
Indian Pharmacopoeia, Vol. II, Indian Pharmacopoeia Commission, Ghaziabad, p: A-145 to A-169, 2007.
United States Pharmacopoeia 26 and National Formulary 21, United States Pharmacopoeial Convention, Rockville, 2003.
Sinha VR, Mittal BR, Bhutani KK, Kumria R. Colonic drug delivery of 5-fluorouracil: an in vitro evaluation. Int J Pharm. 2004; 269(1); 101-08.
Yang L. Biorelevant dissolution testing of colon specific delivery system activated by colonic microflora. J Control Rel. 2008; 125(2); 77-86.
Yang L, Chu JS, Fix JA. Colon specific drug delivery: new approaches and in vitro/in vivo evaluation. Int J Pharm. 2002; 235(1-2); 1-15.
Gautam Singhvi, Mahaveer Singh. Review: In vitro Drug Release Characterization Models. Int J Pharm Studies Res. 2011; 2(1): 77-84.
Higuchi T. Rate of release of medicaments from ointment bases containing drugs in suspension. J Pharm Sci. 1961; 50; 874-75.
Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm. 1983; 15(1); 25-35.
Anjana M. N., Jipnomon Joseph and Sreeja C. Nair. Solubility and bioavailability enhancement of albendazole by complexing with hydroxy propyl β cyclodextrin. J Chem Pharm Res. 2015; 7(4): 1131-41.
Krishnaiah YS, Veer RP, Dinesh KB, Bhaskar P, Satyanarayana V. Development of colon targeted drug delivery systems for mebendazole. J Control Rel. 2001; 77(1-2); 87-95.
J.W. Skoug, M.V. Mikelsons, C.N. Vigneron, N.L. Stemm. Qualitative evaluation of the mechanism of release of matrix sustained release dosage forms by measurement of polymer release. J Control Rel. 1993; 27: 227-245.
L.S. Wan, P.W. Heng, L.F. Wong. Relationship between swelling and drug release in a hydrophilic matrix, Drug Dev Ind Pharm.1993; 19: 1201-1210.
Masheer Ahmed Khan. Effect of Swelling and Drug Release Relationship of Sustained Release Matrices containing different Grades of Hydroxypropyl Methylcellulose. Res J Pharma Dosage Forms and Tech. 2013; 5(4): 232-236.
Mughal MA, Iqbal Z, Neau SH. Guar Gum, Xanthan Gum, and HPMC can define release mechanisms and sustain release of Propranolol Hydrochloride. AAPS Pharm SciTech. 2011; 12(1): 77-87.
How to cite this article:
Thulluru A, Anuradha K. C., Saravanakumar K., Mahammed N, Kumar Ch SP, K. Mohan SJ. Colon targeted tablets of Albendazole with enhanced solubility by Complexation and Micellar Solubilization. Int. J. Res. Dev. Pharm. L. Sci. 2019; 8(3): 12-19. doi: 10.13040/IJRDPL.2278-0238.8(3).12-19
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