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Design, optimization and evaluation of mesalamine matrix tablet for colon drug delivery system

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Abstract

The aim of the present investigation was to develop and evaluate matrix tablet of mesalamine for colonic delivery by using Eudragit RSPO, RLPO and combination of both. The tablets were further coated with different concentration of pH-dependent methacrylic acid copolymers (Eudragit S100), by dip immerse method. The physicochemical parameters of all the formulations were found to be in compliance with the pharmacopoeial standards. The in vitro drug release study was conducted using sequential dissolution technique at pH 1.2 (0.1N) HCl, phosphate buffers pH 6.8 and 7.4, with or without rat cecal content mimicking different regions of gastro intestinal tract. The result demonstrated that the tablet containing Eudragit RLPO coated with Eudragit S100 (1 %) showed a release of 94.91 % for 24 h whereas in the presence of rat cecal content the drug release increases to about 98.55 % for 24 h. The uncoated tablets released the drug within 6 h. The in vitro release of selected formulation was compared with marketed formulation (Octasa MR). In vitro dissolution kinetics followed the Higuchi model via non-Fickian diffusion controlled release mechanism. The stability studies of tablets showed less degradation during accelerated and room temperature storage conditions. The enteric coated Eudragit S100 coated matrix of mesalamine showing promising site specific drug delivery in the colon region.

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References

  • Ali Asghar LF, Azeemuddin M, Jain V, Chandran S (2009) Design and in vitro evaluation of formulations with pH and transit time controlled sigmoidal release profile for colon-specific delivery. Drug Deliv 16:295–303

    Article  PubMed  Google Scholar 

  • Ahmadi F, Varshosaz J, Emami J, Tavakoli N, Minaiyan M, Mahzouni P, Dorkoosh F (2011) Preparation and in vitro/in vivo evaluation of dextran matrix tablets of budesonide in experimental ulcerative colitis in rats. Drug Deliv 18:122–130

    Article  CAS  PubMed  Google Scholar 

  • Akhgari A, Farahmand F, Afrasiabi Garekani H, Sadeghi F, Vandamme T (2010) The effect of pectin on swelling and permeability characteristics of free films containing Eudragit RL and/or RS as a coating formulation aimed for colonic drug delivery. Daru 18:91–96

    PubMed Central  CAS  PubMed  Google Scholar 

  • Boyapally H, Nukala RK, Douroumis D (2009) Development and release mechanism of diltiazem HCl prolonged release matrix tablets. Drug Deliv 16:67–74

    Article  CAS  PubMed  Google Scholar 

  • Bautzova T, Rabiskova M, Lamprecht A (2011) Multiparticulate system containing 5-aminosalicylic acid for the treatment of inflammatory bowel disease. Drug Dev Ind Pharm 37:1100–1109

    Article  PubMed  Google Scholar 

  • Bursemer T, Otto I, Bodmeier R (2001) Pulsatile drug–delivery systems. Crit Rev Ther Drug Carrier Syst 18:433–458

    Google Scholar 

  • Ceballos A, Cirri M, Maestrelli F, Corti G, Mura P (2005) Influence of formulation and process variables on in vitro release of theophylline from directly-compressed Eudragit matrix tablets. Farmaco 60:913–918

    Article  CAS  PubMed  Google Scholar 

  • Chourasia MK, Jain SK (2004) Polysaccharides for colon targeted drug delivery. Drug Deliv 11:129–148

    Article  CAS  PubMed  Google Scholar 

  • Ebube NK, Hikal AH, Wyandt CM, Beer DC, Miller MG, Jones AB (1997) Sustained release of acetaminophen from heterogeneous matrix tablets: influence of polymer ratio polymer loading and coactive on drug release. Pharm Dev Technol 2:161–170

    Article  CAS  PubMed  Google Scholar 

  • Fu J, Wang X, Xu L, Meng J, Weng Y, Li G, He H, Tang X (2011) Preparation and in vitro-in vivo evaluation of double layer coated and matrix sustained release pellet formulations of diclofenac potassium. Int J Pharm 15:84–90

    Article  Google Scholar 

  • Gaikwad SS, Thombre SK, Kale YK, Gondkar SB, Darekar AB (2014) Design and in vitro characterization of buccoadhesive tablets of timolol maleate. Drug Dev Ind Pharm 40:680–690

    Article  CAS  PubMed  Google Scholar 

  • Gao P, Nie X, Zou M, Shi Y, Cheng G (2011) Recent advances in materials for extended-release antibiotic delivery system. J Antibiot (Tokyo) 64:625–634

    Article  CAS  Google Scholar 

  • Gohel MC, Parikh RK, Nagori SA, Dabhi MR (2008) Design of a potential colonic drug delivery system of mesalamine. Pharm Dev Technol 13:444–456

    Article  Google Scholar 

  • Hamza YS, Aburahma MH (2010) Innovation of novel sustained release compression-coated tablets for lornoxicam: formulation and in vitro investigations. Drug Dev Ind Pharm 36:337–349

    Article  CAS  Google Scholar 

  • Kuksal A, Tiwary AK, Jain NK, Jain S (2006) Formulation and in vitro, in vivo evaluation of extended- release matrix tablet of zidovudine: influence of combination of hydrophilic and hydrophobic matrix formers. AAPS PharmSciTech 3:E1

    Article  Google Scholar 

  • Lopes CM, Sousa Lobo JM, Costa P, Pinto JF (2006) Directly compressed mini matrix tablets containing ibuprofen: preparation and evaluation of sustained release. Drug Dev Ind Pharm 32:95–106

    Article  CAS  PubMed  Google Scholar 

  • Love BL, Miller AD (2012) Extended-release mesalamine granules for ulcerative colitis. Ann Pharmacother 46:1529–1536

    Article  PubMed  Google Scholar 

  • Mehta R, Chawla A, Sharma P, Pawar P (2013) Formulation and in vitro evaluation of Eudragir S-100 coated naproxen matrix tablets for colon-targeted drug delivery system. J Adv Pharm Technol Res 4:31–41

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  • Meier M, John E, Wieckhusen D, Wirth W, Peukert W (2008) Characterization of the grinding behavior in a single particle impact device: studies on pharmaceutical powders. Eur J Pharm Sci 10:45–55

    Article  Google Scholar 

  • Mooter GV (2006) Colon drug delivery. Expert Opin Drug Deliv 3:111–125

    Article  PubMed  Google Scholar 

  • Mundargi RC, Patil SA, Agnihotri SA, Aminabhavi TM (2007) Development of polysaccharide based colon targeted drug delivery systems for the treatment of amoebiasis. Drug Dev Ind Pharm 33:255–264

    Article  CAS  PubMed  Google Scholar 

  • Patel MM, Shah TJ, Amin AF, Shah NN (2009) Design, development and optimization of a novel time and pH-dependent colon targeted drug delivery system. Pharm Dev Technol 14:62–69

    CAS  PubMed  Google Scholar 

  • Patra CN, Kumar AB, Pandit HK, Singh SP, Devi MV (2007) Design and evaluation of sustained release bilayer tablets of propranolol hydrochloride. Acta Pharm 57:479–489

    Article  CAS  PubMed  Google Scholar 

  • Sangalli ME, Maroni A, Foppoli A, Zema L, Giordano F, Gazzaniga A (2004) Different HPMC viscosity grades as coating agents for an oral time and/or site-controlled delivery system: a study on process parameters and in vitro performances. Eur J Pharm Sci 22:469–476

    Article  CAS  PubMed  Google Scholar 

  • Singh BN (2007) Modified-release solid formulations for colonic delivery. Recent Pat Drug Deliv Formul 1:53–63

    Article  CAS  PubMed  Google Scholar 

  • Vassallo M, Camilleri M, Phillips SF, Brown ML, Chapman NJ, Thomforde GM (1992) Transit though the proximal colon influences stool weight in the irritable bowel syndrome. Gastroenterology 102:102–108

    CAS  PubMed  Google Scholar 

  • Von der, Camilleri OM, Kvols LK, Thomforde GM (1993) Motor dysfunction of the small bowel and colon in patients with the carcinoid syndrome and diarrhea. N Engl J Med 329:1073–1077

    Article  Google Scholar 

  • Wadher KJ, Kakde RB, Umekar MJ (2011) Formulation and evaluation of a sustained–release tablets of metformin hydrochloride using hydrophilic synthetic and hydrophilic natural polymers. Indian J Pharm Sci 73:208–215

    Article  PubMed Central  CAS  PubMed  Google Scholar 

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Acknowledgments

All authors (P.K. Pawar, C. Gautam) declare that they have no conflict of interest. The author thanks to Dr. Madhu Chitkara, vice chancellor, Chitkara University Punjab for financial and infrastructure support for the project.

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Authors and Affiliations

  1. Gourishankar Institute of Pharmaceutical Education & Reseach, Satara, Maharashtra, India

    Pravin Kondiba Pawar

  2. Chitkara College of Pharmacy, Chitkara University, Chandigarh-Patiala National Highway, Rajpura, Patiala, Punjab, 140401, India

    Chinanshu Gautam

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  1. Pravin Kondiba Pawar
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  2. Chinanshu Gautam
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Correspondence to Pravin Kondiba Pawar.

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Pawar, P.K., Gautam, C. Design, optimization and evaluation of mesalamine matrix tablet for colon drug delivery system. Journal of Pharmaceutical Investigation 46, 67–78 (2016). https://doi.org/10.1007/s40005-015-0214-z

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