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Published on:November 2019
Indian Journal of Pharmaceutical Education and Research, 2019; 53(4s):s554-s562
Original Article | doi:10.5530/ijper.53.4s.150

Solvent-free Hot Melt Extrusion Technique in Improving Mesalamine Release for Better Management of Inflammatory Bowel Disease


Authors and affiliation (s):

Rudra Narayan Sahoo1, Ananya De2, Vishal Kataria3, Subrata Mallick1,*

1School of Pharmaceutical Sciences, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar, Odisha, INDIA.

2Department of Pharmaceutics, Siksha 'O' Anusandhan (Deemed to be University), Bhubaneshwar, Odisha, INDIA.

3PriviLSLLP, Bangalore, Karnataka, INDIA.

Abstract:

Background: Poor oral bioavailability of mesalamine (Mes) is due to extensive metabolism in the intestinal epithelial cells in addition to the liver. Purpose: Improved mesalamine release by Hot-Melt Extrusion (HME) technique could be utilized for better management of Inflammatory Bowel Disease (IBD). Methods: Mes and hydrophilic polymers like Eudragit- EPO, KollidonVA-64 and PEG 6000 were hot-melt extruded using a co-rotating twin-screw laboratory extruder. Results: The minor shifting with significantly reduced intensity and disappearance of peak in the Differential Scanning Calorimetry (DSC) thermogram could be attributed to some solid–solid interaction and not necessarily any incompatibility. Fourier-Transform Infrared Spectroscopy (FTIR) and Scanning Electron Microscopy (SEM) confirmed the transformation of individual drug crystal into accumulations of small crystallites due to partial or almost complete amorphization. Continuous manufacturing of stable amorphous solid dispersion by solvent-free drug loading Hot-melt extrusion technique has been found feasible in improving drug release compared to mesalamine alone in simulated gastric fluid (f1= 0.3 to 11.1 and f2 = 26 to 49). Conclusion: Melt dispersion samples have exhibited significantly improved mesalamine release and could be utilized for better management of Inflammatory Bowel Disease (IBD).

Key words: Hot-melt extrusion, Solvent-free drug loading, Mesalamine, Feret diameter, Improving Release.

 

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IJPER - An Official Publication of Association of Pharmaceutical Teachers of India is pleased to announce continued growth in the 2019 Release of Journal Citation Reports (source: 2018 Web of Science Data).

 

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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

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