Novel montelukast sodium-loaded stable oral suspension bioequivalent to the commercial granules in rats

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• 作者：Dong Wuk Kim ; Young Hun Kim ; Abid Mehmood Yousaf…
• 关键词：Montelukast sodium ; Oral suspension ; Stability ; Dissolution ; Bioavailability
• 刊名：Archives of Pharmacal Research
• 出版年：2016
• 出版时间：April 2016
• 年：2016
• 卷：39
• 期：4
• 页码：539-546
• 全文大小：527 KB
• 参考文献：Aagaard, L., and E.H. Hansen. 2014. Adverse drug reactions associated with asthma medications in children: systematic review of clinical trials. International Journal of Clinical Pharmacy 36(2): 243–252.CrossRef PubMed
  Ahmed, T.A., H.M. Ibrahim, A.M. Samy, A. Kaseem, M.T. Nutan, and M.D. Hussain. 2014. Biodegradable injectable in situ implants and microparticles for sustained release of montelukast: in vitro release, pharmacokinetics, and stability. AAPS PharmSciTech 15(3): 772–780.CrossRef PubMed PubMedCentral
  Al Omari, M.M., R.M. Zoubi, E.I. Hasan, T.Z. Khader, and A.A. Badwan. 2007. Effect of light and heat on the stability of montelukast in solution and in its solid state. Journal of Pharmaceutical and Biomedical Analysis 45(3): 465–471.CrossRef PubMed
  Amirav, I., A.S. Luder, N. Kruger, Y. Borovitch, I. Babai, D. Miron, M. Zuker, G. Tal, and A. Mandelberg. 2008. A double-blind, placebo-controlled, randomized trial of montelukast for acute bronchiolitis. Pediatrics 122(6): e1249–1255.CrossRef PubMed
  Balani, S.K., X. Xu, V. Pratha, M.A. Koss, R.D. Amin, C. Dufresne, R.R. Miller, B.H. Arison, G.A. Doss, M. Chiba, A. Freeman, S.D. Holland, J.I. Schwartz, K.C. Lasseter, B.J. Gertz, J.I. Isenberg, J.D. Rogers, J.H. Lin, and T.A. Baillie. 1997. Metabolic profiles of montelukast sodium (Singulair), a potent cysteinyl leukotriene1 receptor antagonist, in human plasma and bile. Drug Metabolism and Disposition 25(11): 1282–1287.PubMed
  Bennett, G., and T. Craig. 2015. Hereditary angioedema with a focus on the child. Allergy and Asthma Proceedings 36(1): 70–73.CrossRef PubMed
  Cho, K.H., and H.G. Choi. 2013. Development of novel bepotastine salicylate salt bioequivalent to the commercial bepotastine besilate in beagle dogs. Drug Development and Industrial Pharmacy 39(6): 901–908.CrossRef PubMed
  Cho, K.H., Y.K. Choi, J.H. Kang, H.G. Choi, C.S. Yong, and Y.J. Park. 2010. Development of a novel combination tablet containing trimebutine maleate and mosapride citrate for the treatment of functional dyspepsia. International Journal of Pharmaceutics 400: 145–152.CrossRef PubMed
  Chong, J.K., and B.F. Chauhan. 2014. Addition of antileukotriene agents to inhaled corticosteroids in children with persistent asthma. Paediatrics and Child Health 19(9): 473–474.PubMed PubMedCentral
  Fey, C., U. Thyroff-Friesinger, and S. Jones. 2014. Bioequivalence of two formulations of montelukast sodium 4 mg oral granules in healthy adults. Clinical and Translational Allergy 4: 29.CrossRef PubMed PubMedCentral
  Gibson, P.G., J.L. Simpson, N.M. Ryan, and A.E. Vertigan. 2014. Mechanisms of cough. Current Opinion in Allergy and Clinical Immunology 14(1): 55–61.CrossRef PubMed
  Jin, S.G., A.M. Yousaf, M.W. Son, S.W. Jang, D.W. Kim, J.O. Kim, C.S. Yong, J.H. Kim, and H.G. Choi. 2015. Mechanical properties, skin permeation and in vivo evaluations of dexibuprofen-loaded emulsion gel for topical delivery. Archives of Pharmaceutical Research 38(2): 216–222.CrossRef
  Kim, Y.H., D.W. Kim, M.S. Kwon, T.K. Kwon, J.H. Park, S.G. Jin, K.S. Kim, Y.I. Kim, J.H. Park, J.O. Kim, C.S. Yong, J.S. Woo, and H.G. Choi. 2015. Novel montelukast sodium-loaded clear oral solution prepared with hydroxypropyl-β-cyclodextrin as a solubilizer and stabilizer: enhanced stability and bioequivalence to commercial granules in rats. Journal of Inclusion Phenomena and Macrocyclic Chemistry 82: 479–487.CrossRef
  Kim, Y.I., K.S. Kim, K.H. Suh, S. Shanmugam, J.S. Woo, C.S. Yong, and H.G. Choi. 2011. New clopidogrel napadisilate salt and its solid dispersion with improved stability and bioequivalence to the commercial clopidogrel bisulphate salt in beagle dogs. International Journal of Pharmaceutics 415: 129–139.CrossRef PubMed
  Li, J., G. Xiao, C. Chen, R. Li, and D. Yan. 2013. Superior dispersions of reduced grapheme oxide synthesized by using gallic acid as a reductant and stabilizer. Journal of Materials Chemistry A 1: 1481–1487.CrossRef
  Lim, H.T., P. Balakrishnan, D.H. Oh, K.H. Joe, Y.R. Kim, D.H. Hwang, Y.B. Lee, C.S. Yong, and H.G. Choi. 2010. Development of novel sibutramine base-loaded solid dispersion with gelatin and HPMC: physicochemical characterization and pharmacokinetics in beagle dogs. International Journal of Pharmaceutics 397: 225–230.CrossRef PubMed
  Losada-Barreiro, S., V. Sánchez-Paz, and C. Bravo-Díaz. 2013. Effects of emulsifier hydrophile–lipophile balance and emulsifier concentration on the distributions of gallic acid, propyl gallate, and α–tocopherol in corn oil emulsions. Journal of Colloid and Interface Science 389: 1–9.CrossRef PubMed
  Mahajan, H.S., and S.A. Gundare. 2014. Preparation, characterization and pulmonary pharmacokinetics of xyloglucan microspheres as dry powder inhalation. Carbohydrate Polymers 102: 529–536.CrossRef PubMed
  Medina, A.P., F.J. Olaya, M.P. Navas, A.M. Tilano, and E. Muñoz. 2012. Bioequivalence study of montelukast 5 mg chewable tablets. Biomedica 32(3): 399–407.CrossRef PubMed
  Muppavarapu, R., S. Guttikar, M. Rajappan, K. Kamarajan, and R. Mullangi. 2014. Sensitive LC-MS/MS-ESI method for simultaneous determination of montelukast and fexofenadine in human plasma: application to a bioequivalence study. Biomedical Chromatography 28(8): 1048–1056.CrossRef PubMed
  Neves, J.S., A.L. Radke, and P.F. Weller. 2010. Cysteinyl leukotrienes acting via granule membrane-expressed receptors elicit secretion from within cell-free human eosinophil granules. Journal of Allergy and Clinical Immunology 125(2): 477–482.CrossRef PubMed PubMedCentral
  Okamoto, Y., M. Yokota, S. Kawazoe, H. Kubota, H. Nagaoka, Y. Arakida, and M. Takeuchi. 2006. A novel dual antagonist of thromboxane A2 and leukotriene D4 receptors: synthesis and structure-activity relationships of chloroquinolylvinyl derivatives. Chemical & Pharmaceutical Bulletin 54(5): 603–610.CrossRef
  Okumu, A., M. DiMaso, and R. Löbenberg. 2008. Dynamic dissolution testing to establish in vitro/in vivo correlations for montelukast sodium, a poorly soluble drug. Pharmaceutical Research 25(12): 2778–2785.CrossRef PubMed
  Patil-Gadhe, A., and V. Pokharkar. 2014. Montelukast-loaded nanostructured lipid carriers: part I oral bioavailability improvement. European Journal of Pharmaceutics and Biopharmaceutics 88(1): 160–168.CrossRef PubMed
  Paul, S.P., and J.M. Bhatt. 2014. Preschool wheeze is not asthma: a clinical dilemma. Indian Journal of Pediatrics 81(11): 1193–1195.CrossRef PubMed
  Rana, N.S., K.S. Rajesh, N.N. Patel, P.R. Patel, U. Limbachiya, and T.Y. Pasha. 2013. Development and validation of RP-HPLC method for the simultaneous estimation of montelukast sodium and ebastine in tablet dosage form. Indian Journal of Pharmaceutical Sciences 75(5): 599–602.PubMed PubMedCentral
  Stelmach, I., J. Jerzynska, and P. Kuna. 2002. A randomized, double-blind trial of the effect of glucocorticoid, antileukotriene and beta-agonist treatment on IL-10 serum levels in children with asthma. Clinical and Experimental Allergy 32(2): 264–269.CrossRef PubMed
  Strauch, E., O. Moske, S. Thoma, K. Storm Van’s Gravesande, G. Ihorst, M. Brandis, and J. Kuehr. 2003. A randomized controlled trial on the effect of montelukast on sputum eosinophil cationic protein in children with corticosteroid-dependent asthma. Pediatric Research 54(2): 198–203.CrossRef PubMed
  Tril, U., J. Fernández-López, J.A.P. Álvarez, and M. Viuda-Martos. 2014. Chemical, physicochemical, technological, antibacterial and antioxidant properties of rich-fibre powder extract obtained from tamarind (Tamarindus indica L.). Industrial Crops and Products 55: 155–162.CrossRef
  Varshosaz, J., S. Eskandari, and M. Tabbakhian. 2012. Freeze-drying of nanostructure lipid carriers by different carbohydrate polymers used as cryoprotectants. Carbohydrate Polymers 88: 1157–1163.CrossRef
  Wang, K., S.S. Birring, K. Taylor, N.K. Fry, A.D. Hay, M. Moore, J. Jin, R. Perera, A. Farmer, P. Little, T.G. Harrison, D. Mant, and A. Harnden. 2014. Montelukast for postinfectious cough in adults: a double-blind randomised placebo-controlled trial. Lancet Respiratory Medicine 2(1): 35–43.CrossRef PubMed
  Zaid, A.N., S. Natour, A. Qaddomi, and A. Abu Ghoush. 2013. Formulation and in vitro and in vivo evaluation of film-coated montelukast sodium tablets using Opadry® yellow 20A82938 on an industrial scale. Drug Design, Development and Therapy 7: 83–91.CrossRef PubMed PubMedCentral
  Zhao, G.H., N. Kapur, B. Carlin, E. Selinger, and J.T. Guthrie. 2011. Characterisation of the interactive properties of microcrystalline cellulose-carboxymethyl cellulose hydrogels. International Journal of Pharmaceutics 415: 95–101.CrossRef PubMed
  Zietsman, S., G. Killian, M. Worthington, and C. Stubbs. 2007. Formulation development and stability studies of aqueous metronidazole benzoate suspensions containing various suspending agents. Drug Development and Industrial Pharmacy 33: 191–197.CrossRef PubMed
  
• 作者单位：Dong Wuk Kim (1)
  Young Hun Kim (1) (2)
  Abid Mehmood Yousaf (1)
  Dong Shik Kim (1)
  Taek Kwan Kwon (2)
  Jung Hee Park (2)
  Yong Il Kim (2)
  Jae-Hyun Park (2)
  Sung Giu Jin (1)
  Kyung Soo Kim (1)
  Kwan Hyung Cho (3) (4)
  Dong Xun Li (5)
  Jong Oh Kim (3)
  Chul Soon Yong (3)
  Jong Soo Woo (2)
  Han-Gon Choi (1)
  
  1. College of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-Gu, Ansan, 426-791, South Korea
  2. Pharmaceutical Research Centre, Hanmi Pharm. Co., Paltan-Myeon, 893-5, Hwaseong, Gyeonggi-Do, 445-913, South Korea
  3. College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan, 712-749, South Korea
  4. College of Pharmacy, Inje University, Inje-ro 197, Gimhae, 621-749, South Korea
  5. National Pharmaceutical Engineering Centre for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang, Jiangxi, 330006, China
  
• 刊物主题：Pharmacy; Pharmacology/Toxicology;
• 出版者：Springer Netherlands
• ISSN：1976-3786

文摘

To develop a montelukast sodium–loaded stable oral suspension bioequivalent to the commercial granules in rats, several montelukast sodium-loaded suspensions were prepared with a suspending agent, stabilizers and anti-aggregation agents, and their stabilities were investigated by visually observing the sedimentation phenomenon and determining the concentration of the degradation product. Moreover, dissolution and pharmacokinetic studies of the optimized formulation were examined in rats compared to commercial montelukast sodium-loaded granules. Avicel RC-591 (Avicel), a suspending agent, prevented the sedimentation of these suspensions at >2.496 (w/v) per cent composition. Amongst the stabilizers tested, fumaric acid provided the lowest concentration of montelukast sulphoxide (a degradation product) in these suspensions at 40 °C, demonstrating its excellent stabilizing activity. Furthermore, as an anti-aggregation agent, glycerin gave lower amounts of degradation product than those with poloxamer 407 and Tween 80. In particular, montelukast-loaded oral suspension, an aqueous suspension containing montelukast sodium/Avicel/fumaric acid/glycerin at a concentration of 312/2496/15.6/62.4 (mg/100 ml), and the commercial granules exhibited similar dissolution profiles in 0.5 % (w/v) aqueous solution of sodium lauryl sulphate. Moreover, the pharmacokinetics in rats provided by this suspension was comparable to that of the commercial granules, suggesting that they were bioequivalent. In addition, it was physically and chemically stable at 40 °C for at least 6 months. Thus, this montelukast sodium-loaded oral suspension, with bioequivalence to the commercial granules and excellent stability, could be a prospective dosage form for the treatment of asthma.