Tablet Formulation Studies on Recrystallized Active Pharmaceutical Ingredients of Valsartan and Olmesartan Medoxomil
Abstract
Both the Valsartan (VAL) and Olmesartan medoxomil (OLM) are widely prescribed anti-hypertensive agents with angiotensin II type I receptor antagonistic activity. Both VAL and OLM are type of BCS class II drugs and having a low and variable oral bioavailability. Recrystallization of VAL and OLM from different organic solvents improved its aqueous solubility and thereby in vitro dissolution properties. In the present investigation, tablets containing Valsartan (VAL), Olmesartan medoxomil (OLM and) recrystallized products were prepared by direct compression method and evaluated for drug content, uniformity of weight, hardness, friability, disintegration time and dissolution properties. All the tablets fulfilled the compendial requirements with regarding to weight variation, friability and disintegration time etc for immediate release tablets. The DP15 (drug percent dissolved at 15 min) values for V-1 (tablets of VAL), V-4 (tablets of methanol recrystallized product with crospovidone as disintegrant) and DIOVAN™ 40mg tablet formulations are 45.97, 98.95 and 82.65 respectively and V-4 formulation showed higher dissolution rate when compared to other formulations. The DP15 values of O-1(tablets of OLM), O-4 (tablets of acetonitrile recrystallized product with crospovidone as disintegrant and OLMY™ (20mg) tablet formulations are 29.25, 99.93 and 84.82 respectively. O-4 tablet formulations showed higher dissolution rate when compared to other tablet formulations.
Keywords: Valsartan, Olmesartan medoxomil, Recrystallization, Aqueous solubility
Keywords:
Valsartan, Olmesartan medoxomil, Recrystallization, Aqueous solubilityDOI
https://doi.org/10.22270/jddt.v11i6-S.5091References
Flesch G, Lloyd P, Müller PH. Absolute bioavailability and pharmacokinetics of valsartan, an angiotensin II receptor antagonist. Eur J Clin Pharmacol., 1997; 52:115-120. https://doi.org/10.1007/s002280050259
Nadeem S, Asif H, Lakshita C, Shamsher MA, Mitra M, Parminder SB. Pharmacological and Pharmaceutical Profile of Valsartan: A Review. Journal of Applied Pharmaceutical Science, 2011; 01(04):12-19.
Warner GT, Jarvis B. Olmesartan Medoxomil. Drugs, 2002; 62:1345-53. https://doi.org/10.2165/00003495-200262090-00005
Laeis P, Puchler K, Kirch W. The pharmacokinetic and metabolic profile of olmesartan medoxomil limits the risk of clinically relevant drug interaction. J. Hypertens. Suppl., 2001; 19:21-32. https://doi.org/10.1097/00004872-200106001-00004
Sarwar B, Suryakanta S, Rizwan Md, Irfanuddin Md, Shobha DM. Bioavailability Enhancement Strategies: Basics, Formulation Approaches and Regulatory Considerations. Current Drug Delivery, 2011; 8(6):691-702. https://doi.org/10.2174/156720111797635504
Dixit AR, Rajput SJ, Patel SG. Preparation and Bioavailability Assessment of SMEDDS Containing Valsartan. AAPS Pharm Sci Tech, 2010; 11(1):314-321. https://doi.org/10.1208/s12249-010-9385-0
Yana YD, Sunga JH, Kima KK, Kimb DW, Kima JO, Leec BJ, Yonga CS, Choi HG. Novel valsartan-loaded solid dispersion with enhanced bioavailability and no crystalline changes. International Journal of Pharmaceutics, 2012; 422(1-2):202-210. https://doi.org/10.1016/j.ijpharm.2011.10.053
Qiuping M, Hongrui S, Erxi C, Xin Z, Tongying J, Changshan S, Siling W. Uniform nano-sized valsartan for dissolution and bioavailability enhancement: Influence of particle size and crystalline state. International Journal of Pharmaceutics, 2012; 441 (1-2):75-81. https://doi.org/10.1016/j.ijpharm.2012.12.025
De Matos Jensen CE, Dos Santos RAS, Denadai AML, Santos CFF, Braga ANG; Sinisterra RD. Pharmaceutical Composition of Valsartan: β-Cyclodextrin: Physico-chemical characterization and anti-hypertensive evaluation. Molecules, 2010; 15:4067-4084. https://doi.org/10.3390/molecules15064067
Chirag R, Neha J, patel J, Upadhyay UM. Enhanced Oral Bioavailability of Olmesartan by using Novel Solid Self Emulsifying Drug Delivery System. International Journal of Advanced Pharmaceutics, 2012; 2(2):82-92.
Kang MJ, Hyung SK, Jeon HS, Park JH, Lee BS, Byeong KA. In Situ Intestinal Permeability and In Vivo absorption Characteristics of Olmesartan Medoxomil in Self-Micoremulsifying Drug Delivery System. Drug Development and Industrial Pharmacy, 2011; 38(5):587-596. https://doi.org/10.3109/03639045.2011.619194
Hetal PT, Bindesh VP, Sneha PT. Development and Characterization of Nanosuspensions of Olmesartan Medoxomil for Bioavailability Enhancement. J Pharm Bioallied Sci., 2011; 3(3):426-434. https://doi.org/10.4103/0975-7406.84459
Amit C, Upendra N, Neha G, Sharma VK, Khosa RL. Enhancement of solubilization and bioavailability of poorly soluble drugs by physical and chemical modifications: A recent review. Journal of Advanced Pharmacy Education & Research, 2012; 2(1):32-67.
Nalluri BN, Ramya KM, Rao TP, Peter AC. Effect of Recrystallization on the Pharmaceutical Properties of Valsartan for Improved Therapeutic Efficacy. Journal of Applied Pharmaceutical Science, 2012; 2(10):126-132. https://doi.org/10.7324/JAPS.2012.21025
Rao TP, Murali B, Devala RG, Srinivas BP. Improvement of Pharmaceutical Properties of Olmesartan by Recrystallization Technique. Journal of Chemical and Pharmaceutical Sciences, 2014; 7(2):162-164.
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