Formulation and Evaluation of Enteric Coated Matrix Tablets of Mesalamine for Inflammatory Bowel Disease

Authors

  • Nikita Chourey Truba Institute of Pharmacy, Karond-Gandhi Nagar Bypass Road, Bhopal, 462038
  • Khushi Chouksey Sagar Institute of Pharmacy and Technology (SIPTec), Opposite International Airport, Gandhi Nagar Bhopal (M.P.) 462036

Abstract

Mesalamine is a gold standard anti-inflammatory drug used to treat inflammatory bowel illnesses. It's usually used to treat and keep Ulcerative Colitis in remission in mild to moderate cases. Mesalamine is rapidly cleared from circulation after being consumed orally, with an elimination half-life of only one hour. Oral intake of delayed or slow released matrix formulations can acquire therapeutic concentration in the intestines. The goal of this study was to use guar gum as a carrier to develop colon-specific delivery methods for mesalamine. The matrix tablets were made using the direct compression process, which is today regarded as a cost-effective and straightforward manufacturing method. Dip coating was used to coat the tablets with varied concentrations of Eudragit L100 polymer. Tablets were studied in vitro in a variety of dissolution solutions, including 0.1 N HCl (pH 1.2), phosphate buffers pH 6.8 and 7.4, and others. The optimized formulation was subjected to swelling tests. All of the formulations' physicochemical parameters were confirmed to be in line with pharmacopoeial norms. All formulations were subjected to stability tests in accordance with ICH recommendations. The tablets coated with Eudragit L100 (20 percent w/v) had a sustained release of 78.39 percent over 12 hours, while the uncoated tablets released the medication in 9 hours. Tablet stability tests revealed that under accelerated and room temperature storage settings for 6 months, there was reduced degradation. In the colon, the enteric-coated Eudragit L100 coated matrix tablets of mesalamine demonstrated promising site-specific drug delivery.

Keywords: Mesalamine, Guar gum, Eudragit L100, Direct compression, Inflammatory bowel illnesses

Keywords:

Mesalamine, Guar gum, Eudragit L100, Direct compression, Inflammatory bowel illnesses

DOI

https://doi.org/10.22270/jddt.v12i1.5176

Author Biographies

Nikita Chourey, Truba Institute of Pharmacy, Karond-Gandhi Nagar Bypass Road, Bhopal, 462038

Truba Institute of Pharmacy, Karond-Gandhi Nagar Bypass Road, Bhopal, 462038

Khushi Chouksey, Sagar Institute of Pharmacy and Technology (SIPTec), Opposite International Airport, Gandhi Nagar Bhopal (M.P.) 462036

Sagar Institute of Pharmacy and Technology (SIPTec), Opposite International Airport, Gandhi Nagar Bhopal (M.P.) 462036

References

Ashford M, Fell JT. Targeting drugs to the colon: delivery systems for oral administration. J Drug Target 1994; 2:241 57. https://doi.org/10.3109/10611869408996806

Rubinstein A. Approaches and opportunities in colon-specific drug delivery. Crit Rev Ther Drug Carrier Syst 1995; 12:101 49. https://doi.org/10.1615/CritRevTherDrugCarrierSyst.v12.i2-3.10

Watts PJ, Lllum L. Colonic Drug Delivery. Drug Dev Ind Pharm 1997; 23:893 913. https://doi.org/10.3109/03639049709148695

Kinget R, Kalala W, Vervoort L, Van Der Mooter G. Colonic drug targeting. J Drug Target 1998; 6:129 49. https://doi.org/10.3109/10611869808997888

Niwa K, Takaya T, Morimoto T, Takada K. Preparation and evaluation of a time controlled release capsule made of ethylcellulose for colon delivery of drugs. J Drug Target 1995; 3:83 9. https://doi.org/10.3109/10611869509059209

Chourasia MK, Jain SK. Pharmaceutical approaches to colon targeted drug delivery systems. J Pharm Pharm Sci 2003; 6:33 66.

Mura P, Maestrelli F, Cirri M, González Rodríguez ML, Rabasco Alvarez AM. Development of enteric coated pectin-based matrix tablets for colonic delivery of theophylline. J Drug Target 2003; 11:365 71. https://doi.org/10.1080/10611860310001639130

Asghar LF, Azeemuddin M, Jain V, Chandran S. Design and in vitro evaluation of formulations with pH and transit time controlled sigmoidal release profile for colon specific delivery. Drug Deliv 2009; 16:205 13. https://doi.org/10.1080/10717540902823960

Hu Z, Shimokawa T, Ohno T, Kimura G, Mawatari SS, Kamitsuna M, et al. Characterization of norfloxacine release from tablet coated with a new pH sensitive polymer, P 4135F. J Drug Target 1999; 7:223 32. https://doi.org/10.3109/10611869909085505

Qi M, Wang P, Wu D. A novel pH- and time-dependent system for colonic drug delivery. Drug Dev Ind Pharm 2003; 29:661 7. https://doi.org/10.1081/DDC-120021315

Tugcu-Demiroz F, Acarturk F, Takka S, Konus-Boyunaga O. In-vitro and in-vivo evaluation of mesalazine-guar gum matrix tablets for colonic drug delivery. J Drug Target 2004; 12 (2):105-112. https://doi.org/10.1080/10611860410001693751

Hovgaard L, Brondsted H. Current applications of polysaccharides in colon targeting. Crit Rev Ther Drug Carrier Syst 1996; 13:185-223. https://doi.org/10.1615/CritRevTherDrugCarrierSyst.v13.i3-4.10

Vandamme F, Lenourry A, Charrueau C, Chaumeil J-C. The use of polysaccharides to target drugs to the colon. Carbohydr Polym 2002; 48:219-231. https://doi.org/10.1016/S0144-8617(01)00263-6

Yu K, Wong D, Friend JD. Guar gum In: Florey, A.T., ed., Analytical Profiles of Drug Substances and Excipients (Academic Press, New York), 1998; Vol. 24, pp 245-276.

Sinha VR, Kumria R. Polysaccharides in colon-specific drug delivery. Int J Pharm 2001; 224:19-38. https://doi.org/10.1016/S0378-5173(01)00720-7

Khan MZ, Stedul HP, Kurjaković N. A pH dependent colon-targeted oral drug delivery system using methacrylic acid copolymers. II. Manipulation of drug release using Eudragit L100 and Eudragit S100 combinations. Drug Dev Ind Pharm 2000; 26:549 54. https://doi.org/10.1081/DDC-100101266

Asghar LF, Chandran S. Design and evaluation of matrices of Eudragit with polycarbophil and carbopol for colon specific delivery. J Drug Target 2008; 16:741-57. https://doi.org/10.1080/10611860802473345

Prakash A, Markham A. Oral delayed-release mesalazine. Drugs 1999; 57: 383-408. https://doi.org/10.2165/00003495-199957030-00013

Steed KP, Hooper G, Monti N, Strolin Benedetti M, Fornasini G, Wilding IR. The use of pharmacoscintigraphy to focus the development strategy for a novel 5-ASA colon targeting system (TIME CLOCKw system), J Control Release 1997; 49:115-122. https://doi.org/10.1016/S0168-3659(97)00062-X

Sinko PJ. Physical Pharmacy and Pharmaceutical Sciences, Lippincott Williams and Wilkins, 5th Edition, 2006.

Chein YW. Novel Drug Delivery Systems, Marcel Dekker, INC, 2nd edition, 1992, 140.

Gautam SP, Rai JP, Billshaiya U, Jain N, Vikram P, Jain DK. Formulation and evaluation of mouth dissolving tablet of loperamide. Int J Pharm Sci Res. 2013; 4(5): 1782-1788.

Patel P, Rai JP, Jain DK, Banweer J. Formulation, development and evaluation of cefaclor extended release matrix tablet. Int J Pharm Pharm Sci 2012; 4(4):355-357.

Pandey SP, Khan MA, Dhote V, Dhote K, Jain DK. Formulation development of sustained release matrix tablet containing metformin hydrochloride and study of various factors affecting dissolution rate. Sch Acad J Pharm 2019; 8 (3):57-73.

Jain P, Nair S, Jain N, Jain DK, Jain S. Formulation and evaluation of solid dispersion of lomefloxacin hydrochloride. Int J Res Pharm Sci 2012; 3(4):604-608.

Published

2022-01-15
Statistics
Abstract Display: 1009
PDF Downloads: 934
PDF Downloads: 620

How to Cite

1.
Chourey N, Chouksey K. Formulation and Evaluation of Enteric Coated Matrix Tablets of Mesalamine for Inflammatory Bowel Disease. J. Drug Delivery Ther. [Internet]. 2022 Jan. 15 [cited 2026 Jan. 21];12(1):56-61. Available from: https://jddtonline.info/index.php/jddt/article/view/5176

How to Cite

1.
Chourey N, Chouksey K. Formulation and Evaluation of Enteric Coated Matrix Tablets of Mesalamine for Inflammatory Bowel Disease. J. Drug Delivery Ther. [Internet]. 2022 Jan. 15 [cited 2026 Jan. 21];12(1):56-61. Available from: https://jddtonline.info/index.php/jddt/article/view/5176