INTESTINAL ABSORPTION OF EPROSARTAN MESYLATE FROM SELF EMULSIFYING SYSTEM AND CYCLODEXTRIN COMPLEX
DOI:
https://doi.org/10.22159/ijpps.2017v9i2.16215Keywords:
Eprosartan, Self-nano emulsifying, Inclusion complexation, Hydroxypropyl b cyclodextrin, Labrafil, Lauroglycol, TweenAbstract
Objective: The aim of this work was to determine the intestinal membrane transport parameters of eprosartan mesylate (EM) and to investigate self-nano emulsifying drug delivery systems (SNEDDS) and inclusion complexation with hydroxypropyl b cyclodextrin (HPbCD) for enhanced intestinal absorption of eprosartan mesylate.
Methods: The intestinal absorption was monitored using the in situ rabbit intestinal perfusion technique. SNEDDS was developed using labrafil, Lauroglycol with a tween in the presence of ethanol. Inclusion complexation was achieved by construction of phase solubility diagram in the presence of HPbCD. The prepared complex was evaluated using Fourier Transform Infrared Spectroscopy (FTIR) and differential scanning calorimetry (DSC).
Results: The drug was found to be poorly absorbed from the jejuno-ileum and the colon with the absorption being mainly through paracellular pathway. An inclusion complex was developed between the drug and HPβCD. Perfusion of the drug in the nanoemulsion formulation or as an inclusion complex resulted in a significant increase in the intestinal absorption of the drug compared with the control.
Conclusion: SNEDDS and inclusion complexation are promising strategies for enhanced intestinal absorption of eprosartan mesylate.
Downloads
References
Dalvi VJ PDD, Tambe AP, Khanvilkar VV, Kadam VJ. Analytical methods for estimation of eprosartan mesylate: a review. Pharma Sci Monit 2013;4:371-87.
Chandana O, Kumar DS, Babu RR. Method development and validation of eprosartan mesylate and its impurities using reverse phase high-performance liquid chromatography. Int J Curr Pharm Res 2016;8:49-53.
Brooks DP, Ohlstein EH, Ruffolo RR. Pharmacology of eprosartan, an angiotensin ii receptor antagonist: exploring hypotheses from clinical data. Am Heart J 1999;138:S246-S51.
Ram CVS, Rudmann MA. Unique dual mechanism of action of eprosartan: effects on systolic blood pressure, pulse pressure, the risk of stroke and cognitive decline. Expert Rev Cardiovasc Ther 2007;5:1003-11.
Sica DA, Hollenberg NK. The renal profile of eprosartan. Pharmacotherapy 1999;19:86S-94S.
Michel MC, Foster C, Brunner HR, Liu L. A systematic comparison of the properties of clinically used angiotensin ii type 1 receptor antagonists. Pharmacol Rev 2013;65:809-48.
Gudipati MR, Jushchyshyn JM, Palepu NR, Venkatesh GM. Eprosartan arginyl charge-neutralization-complex and a process for its preparation and formulation. US Patent; 2003.
Bhandaru JS, Malothu N, Akkinepally RR. Characterization and solubility studies of pharmaceutical cocrystals of eprosartan mesylate. Cryst Growth Des 2015;15:1173-9.
Sarangi MK, Padhi S. Colon targeted drug delivery system an approach for treating colonic ailments. J Critical Rev 2015;2:12-8.
Jyothi BJ, Sreelakshmi K. Design and evaluation of self-nano emulsifying drug delivery system of flutamide. J Young Pharm 2011;3:4-8.
Ajmera A, Deshpande S, Kharadi S, Rathod K, Patel K, Patel P. Dissolution rate enhancement of atorvastatin, fenofibrate and ezetimibe by inclusion complex with β-cyclodextrin. Asian J Pharm Clin Res 2012;5:73-6.
Mendhe A, Kharwade R, Mahajan U. Dissolution enhancement of poorly water-soluble drug by cyclodextrins inclusion complexation. Int J Appl Pharm 2016;8:60-5.
Loftsson T, Masson M, Brewster ME. Selfâ€association of cyclodextrins and cyclodextrin complexes. J Pharm Sci 2004;93:1091-9.
Rao M, Sunitha K, Harika K. Influence of hydroxypropyl-β-cyclodextrin on repaglinide release from sustained release bioadhesive buccal tablets. Asian J Pharm Clin Res 2013;6:184-90.
Sultan AA, Elâ€Gizawy SA, Osman MA, El Maghraby GM. Colloidal carriers for extended absorption window of furosemide. J Pharm Pharmacol 2016; 68:324-32.
International conference on harmonisation, Q2 (R1) Validation of analytical procedures: Text and methodology; 2005.
Loftsson T, Hreinsdóttir D, Másson M. The complexation efficiency. J Inclusion Phenom Macrocyclic Chem 2007;57:545-52.
Wang SH, Griffiths PR. Resolution enhancement of diffuse reflectance IR spectra of coals by fourier self-deconvolution: 1. Ch stretching and bending modes. Fuel 1985;64:229-36.
Yuan C, Liu B, Liu H. Characterization of hydroxypropyl-β-cyclodextrins with different substitution patterns via ftir, gc–ms, and tg–dta. Carbohydr Polym 2015;118:36-40.
Sheng J, Venkatesh GM, Duddu SP, Grant DJ. Dehydration behavior of eprosartan mesylate dihydrate. J Pharm Sci 1999;88:1021-9.
Danciu C, Soica C, Csanyi E, Ambrus R, Feflea S, Peev C, et al. Changes in the anti-inflammatory activity of soy isoflavonoid genistein versus genistein incorporated in two types of cyclodextrin derivatives. Chem Cent J 2012;6:1-11.
Riad LE, Sawchuk RJ. Absorptive clearance of carbamazepine and selected metabolites in rabbit intestine. Pharm Res 1991;8:1050-5.
Published
How to Cite
Issue
Section
