Enhancement of dissolution rate of racecadotril by liquisolid compact technology
DOI:
https://doi.org/10.1590/s2175-97902022e21044Palavras-chave:
Avicel, Aerosil, Non-volatile vehicle, Liquisolid tablets, DissolutionResumo
The current investigation was used to improve the rate of dissolution of an anti-diarrheal drug i.e., racecadotril (RT) at low pH conditions (i.e., in the stomach) by reducing the water secretion and electrolyte in to the intestine by liquisolid tablets. Different formulations (liquisolid) were prepared using Avicel PH 102 as a carrier. Aerosil 200 as a coating material and sodium starch glycolate used as a disintegrant. Polyethylene glycol 200 was used as a non-volatile vehicle to dissolve the drug. FTIR, DSC, XRD and dissolution studies were conducted to characterise liquisolid tablets. Characterisation studies indicated that no interactions between carrier and drug. Solid state characterization had shown a reduction in crystallinity that further supports increment in solubility and dissolution. The optimised formulation showed a significant increase in dissolution i.e., 99.54±0.62% in 30 min compared to directly compressible tablets (38.47±0.26%). The % dissolution efficiency of racecadotril liquisolid tablets 76.86% compared to marketed tablet (27.56%) and conventional direct compression tablet (17.11%). Significant reduction in mean dissolution time of racecadotril from liquisolid tablets (6.84 min) compared to direct compression tablet (44.57 min), indicating faster release of drug and faster onset of action. Formulation of liquisolid tablets could enhance solubility, dissolution and bioavailability of racecadotril.
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Alam NH, Ashraf H, Khan WA, Karim MM, Fuchs GJ. Efficacy and tolerability of racecadotril in the treatment of cholera in adults: A double blind, randomised, controlled clinical trial. Gut. 2003;52(10):1419-23.
Bhattacharya S, Pasha I, Verma A, Kothapalli R, Jafar F, Hr K. Formulation and evaluation of liquisolid compact of azithromycin dihydrate. J Res Pharm. 2019;23(6):1022-32.
Blagden N, de Matas M, Gavan P, York P. Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates. Adv Drug Deliv Rev. 2007;59(7):617-30.
Chella N, Daravath B, Kumar D, Tadikonda R. Formulation and pharmacokinetic evaluation of polymeric dispersions containing valsartan. Eur J Drug Metab Pharmacokinet. 2016;41(5):517-26.
Chella N, Nalini S, Rama RT. Use of the liquisolid compact technique for improvement of the dissolution rate of valsartan. Acta Pharm Sin B. 2012;2(5):502-8.
Chella N, Narra N, Rama RT. Preparation and characterization of liquisolid compacts for improved dissolution of telmisartan. J Drug Deliv. 2014;2014:1-10.
Cojocaru B, Bocquet N, Timsit S, Wille C, Boursiquot C, Marcombes F, et al. Effect of racecadotril in the management of acute diarrhea in infants and children. Arch Pediatr. 2002;9(8):774-9.
Daravath B, Kumari GP. Improvement of bioavailability of poorly soluble racecadotril by solid dispersion with surface adsorption method: A case study. J Rep Pharm Sci. 2021;10(1):77-86.
Daravath B, Naveen CH, Vemula SK, Tadikonda RR. Solubility and dissolution enhancement of flurbiprofen solid dispersion using hydrophilic carriers. Braz J Pharm Sci. 2017;53(4):1-10.
Daravath B, Swathi, Babu RB. Formulation Development and evaluation of sustained release bioadhesive bilayered buccal tablets of furosemide. Anal Chem Lett. 2017;7(2):215-27.
Daravath B, Tadikonda RR. Formulation and in vitro evaluation of flurbiprofen-polyethylene glycol 20000 solid dispersions. J App Pharm Sci. 2014;4(7):76-81.
Daravath B, Tadikonda RR, Vemula SK. Formulation and pharmacokinetics of gelucire solid dispersions of flurbiprofen. Drug Dev Ind Pharm. 2015;41(8):1254-62.
Elkordy AA, Tan XN, Essa EA. Spironolactone release from liquisolid formulations prepared with Capryol™ 90, Solutol® HS-15 and Kollicoat® SR 30 D as non-volatile liquid vehicles. Eur J Pharm Biopharm. 2013;83(2):203-23.
Fahmy RH, Kassem MA. Enhancement of famotidine dissolution rate through liquisolid tablets formulation: in vitro and in vivo evaluation. Eur J Pharm Biopharm . 2008;69(3):993-1003.
Gubbi SR, Jarag R. Formulation and characterization of atorvastatin calcium liquisolid compacts. Asian J Pharm Sci. 2010;5(2):50-60.
Gursoy RN, Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed Pharmacother. 2004;58(3):173-82.
Javadzadeh Y, Jafari-Navimipour NB, Nokhodchi A. Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine). Int J Pharm. 2007;341(1-2):26-34.
Javadzadeh Y, Shariati H, Movahhed-Danesh E, Nokhodchi A. Effect of some commercial grades of microcrystalline cellulose on flowability, compressibility, and dissolution profile of piroxicam liquisolid compacts. Drug Dev Ind Pharm . 2009;35(2):243-51.
Javadzadeh Y, Siahi-Shadbad MR, Barzegar-Jalali M, Nokhodchi A. An investigation of physicochemical properties of piroxicam liquisolid compacts. Pharm Dev Tech. 2007;12(3):337-343.
Javadzadeh Y, Siahi MR, Barzegar JM, Nokhodchi A. Enhancement of dissolution rate of piroxicam using liquisolid compacts. Farmaco. 2005;60(4):361-65.
Jin X, Zhang Z, Sun E, Li S, Jia X. Statistically designed enzymatic hydrolysis of anicariin/b-cyclodextrin inclusion complex optimized for production of icaritin. Acta Pharm Sin B. 2012;2(1):83-89.
Karmarkar AB, Gonjari ID, Hosmani AH, Dhabale PN, Bhise SB. Dissolution rate enhancement of fenofibrate using liquisolid tablet technique. Lat Am J Pharm. 2009;28(4):219-25.
Khaled KA, Asiri YA, El-Sayed YM. In vivo evaluation of hydrochlorothiazide liquisolid tablets in beagle dogs. Int J Pharm . 2001;222(1):1-6.
Lindo ES, Ponce JS, Woo EC, Gutierrez M. Racecadotril in the treatment of acute watery diarrhea in children. N Engl J Med. 2000;343(3):463-67.
Lu M, Xing HN, Yang TZ, Yu J , Yang Z, Sun Y, et al. Dissolution enhancement of tadalafil by liquisolid technique. Pharm Dev Technol. 2017;22(1):77-89.
Luo Y, Xu L, Xu M, Tao X, Ai R, Tang X. Improvement of dissolution and bioavailability of Ginsenosides by hot melt extrusion and co-grinding. Drug Dev Ind Pharm . 2012;39(1):1-8.
Matheson AJ, Noble S. Racecadotril. Drugs. 2000;59(4):829-35.
Mathews BR. Regulatory aspects of stability testing in Europe. Drug Dev Ind Pharm . 1999;25(7):831-56.
Mie Lu, Xing H, Jiang J, Chen X, Yang T, Wang D, et al. Liquisolid technique and its applications in pharmaceutics. Asian J Pharm Sci . 2017;12(2):115-123.
Nokhodchi A, Hentzschel CM, Leopold CS. Drug release from liquisolid systems: speed it up, slow it down. Expert Opin Drug Deliv 2011;8(2):191-205.
Primi MP, Bueno L, Baumer P, Berard H, Lecomte JM. Racecadotril demonstrates intestinal antisecretory activity in vivo. Aliment Pharmacol Ther. 1999;13(6):3-7.
Saeedi M, Akbari J, Morteza-Semnani K, Enayati-Fard R, Sar-Reshteh-Dar S, Soleymani A. Enhancement of dissolution rate of indomethacin using liquisolid compacts. Iran J Pharm Res. 2011;10(1):25-34.
Singh N, Narayan S. Racecadotril: A Novel Antidiarrheal. Med J Armed Forces India. 2008;64(4):361-62.
Sonoda R, Horibe M, Oshima T, Iwasaki T, Watano S. Improvement of dissolution property of poorly water soluble drug by novel dry coating method using planetary ball mill. Chem Pharm Bull. 2008;56(9):1243-47.
Spireas S, Sadu S. Enhancement of Prednisolone dissolution properties using liquisolid compacts. Int J Pharm . 1998;166(2):177-88.
Spireas S, Sadu S, Grover R. In-vitro release evaluation of hydrocortisone liquisolid tablets. J Pharm Sci. 1998;87(7):867-72.
Spireas S, Wang T, Grover R. Effect of powders substrate on the dissolution properties of methyclothiazide liquisolid compacts. Drug Dev Ind Pharm . 1999;25(2):163-68.
Suliman AS, Anderson RJ, Elkordy AA. Norfloxacin as a model hydrophobic drug with unique release from liquisolid formulations prepared with PEG 200 and Synperonic PE/L-61 non-volatile liquid vehicles. Powder Technol. 2014;257:156-67.
Tadikonda RR, Daravath B. Formulation and evaluation of meclizine hydrochloride fast dissolving tablets using solid dispersion method. Asian J Pharm Clin Res. 2014;7(2):98-102.
Tayel SA, Soliman II, Louis D. Improvement of dissolution properties of carbamazepine through application of the liquisolid tablet technique. Eur J Pharm Biopharm . 2008;69(1):342-47.
Tiong N, Elkordy AA. Effects of liquisolid formulations on dissolution of naproxen. Eur J Pharm Biopharm . 2009;73(3):373-84.
Wong SM, Kellaway IW, Murdan S. Enhancement of the dissolution rate and oral absorption of a poorly water soluble drug by formation of surfactant-containing microparticles. Int J Pharm . 2006;317(1):61-68.
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