Development and Evaluation of Mesalamine—Glutamine Cocrystal Tablets for Colon Specific Delivery

DOI:

https://doi.org/10.37285/ijpsn.2017.10.5.8

Authors

  • Mamatha T
  • Sama M
  • Husna K Qureshi

Abstract



The objective of the work was to develop the co-crystal formulation of mesalamine with glutamine. It was done to enhance dissolution rate, solubility and physicochemical properties to be used in pharmaceutical composition (tablet) for colon targeting. Co-crystal preparation was carried out by liquid assisted grinding method using glutamine as a co-crystal former (1:1 stoichiometric ratio) and acetonitrile as a solvent giving maximum solubility and dissolution rate. The formation of the co-crystals was confirmed by Fourier Transform – Infra Red spectrometry, Differential Scanning Calorimetry and Powder X-Ray Diffraction. Pre-compression studies included measure-ment of bulk density, tapped density, angle of repose, Hausner’s ratio and compressibility index. The tablets were prepared by direct compression. Post compression parameters for uncoated tablets included hardness, size and thickness, friability and weight variation. Enteric-coated tablets were prepared by dip-coating process using Eudragit RSPO, Triethyl citrate and isopropyl alcohol mixture as coating solution. The coated tablets were further evaluated for disintegration and dissolution testing. All the results were found to be under specified limits. Finally, co-crystal tablets were compared with marketed formulation. In vitro dissolution rate of optimized mesalamine co-crystal tablet was comparatively higher than marketed formulation, which reflects improvement in solubility. Glutamine has good anti-inflammatory property. Formulation with glutamine as co-crystal added more efficacies to mesalamine for treatment in colon related inflammatory diseases. It was concluded that stable co-crystals of mesalamine -glutamine having better anti-inflammatory property, increased solubility and improved in vitro dissolution of mesalamine can be successfully prepared.    

 

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Keywords:

Mesalamine, Co-crystal, Colon targeting, Enteric coating, Glutamine

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Published

2017-09-30

How to Cite

1.
T M, M S, Qureshi HK. Development and Evaluation of Mesalamine—Glutamine Cocrystal Tablets for Colon Specific Delivery. Scopus Indexed [Internet]. 2017 Sep. 30 [cited 2024 May 17];10(5):3866-74. Available from: https://www.ijpsnonline.com/index.php/ijpsn/article/view/867

Issue

Vol. 10 No. 5 (2017): September-October 2017

Section

Research Articles
Crossref
Scopus
Google Scholar
Europe PMC

References

Bauer KH and Kesselhut JF (1995). Novel pharmaceutical excipients for colon targeted drug delivery system. STP Pharm Sci., 5: 54-59.
Bowker MJ, Bastin RJ and Slater BJ (2000). Salt Selection and Optimisation Procedures for Pharmaceutical New Chemical Entities. Org. Proc. Res. Dev., 4(5): 427-435.
Datta S and Grant DJ (2004). Crystal structures of drugs: advances in determination, prediction and engineering. Nat Rev Drug Discov, 3(1): 42-57.
D. Braga, F. Grepioni, L. Maini and M. Polito (2009). Crystal Polymorphism and Multiple Crystal Forms Molecular Networks. Structure and Bonding, 132: 25-50.
Fujita T and Sakurai K (1995). Efficacy of glutamine-enriched enteral nutrition in an experimental model of mucosal ulcerative colitis. Br J Surg. 82(6): 749-51.
Mamatha T, Md. Zubair, Sarah Nasreen N and Md. Ahmeduddin (2015). Formulation and Evaluation of Oro dispersible Tablets of Fosinopril Sodium, Dhaka Univ. J. Pharm. Sci. 14(1): 11-16.
Marvola M, Nykanen P, Rautio S, Isonen N and Autere A (1999). Enteric polymers as binders and coating materials in multiple unit site specific drug delivery system, Eur J Pharm Sci.7(3): 259-267.
Nykanen P, Krogars K, Sakkinen M, Heinamaki J, Jurjenson H, Veski P and Marvola M (1999). Organic acids as excipients in matrix granules for colon-specific drug delivery. Int J Pharm, 184: 251-261.
Patel JK, Patel RP, Amin AF and Patel MM (2005). Formulation and evaluation of mucoadhesive glipizide microspheres. AAPS Pharm Sci Tech. 6(1): E49-E55.
Patil PB, Hajare AA and Awale RP (2011). Development and Evaluation of Mesalamine Tablet Formulation for Colon Delivery Research. J. Pharm. and Tech. 4(11): 1751-1756.
Rambabu D, Reddy JS, Ganesh SV, Ravikumar N, Anand KS, Gopikrishna G and Anil KK (2012). Novel Co-crystals / molecular salts of mesalamine to be used as improved anti-inflammatory drug. (Publication no: Wo/2012/090224; International patent application no: PCT/IN2011/000902).
Seema Badhana, Navneet Garud, and Akanksha Garud (2013). Colon specific drug delivery of mesalamine using eudragit S100-coated chitosan microspheres for the treatment of ulcerative colitis. International Current Pharmaceutical Journal, 2(3): 42-48.
Stahly GP (2007). Diversity in Single- and Multiple-Component Crystals. The Search for and Prevalence of Polymorphs and Cocrystals. Crystal Growth & Design.7 (6):1007-1026.
Stahly GP (2009). A Survey of Co-crystals Reported Prior to 2000. Crystal Growth & Design. 9(10): 4212.
Taylor. R and Kennard O (1982). Crystallographic evidence for the existence of C-H…O, C-H…N, C-H…Cl hydrogen bonds. J. Am. Chem. Soc. 104. 5063-5070.
Valentine C Ibekwe (2006). A comparitive in vitro assessment of the drug release performance of pH-Responsive polymers for ileo-colonic delivery. Int J Pharm, 308: 52-60.
Vijaya M, Sudeesh E and Saravana Kumar K (2011). Design And Evaluation Of Mesalamine Tablet For Colon Specific Drug Delivery. Int. J. Drug Dev. & Res. 3(3): 197-212.
Yang L, Chu JS Chu and Fix JA (2002). Colon specific drug delivery: new approaches and in vitro/in vivo evaluation. Int J Pharm, 235: 1-15.