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Microspheres and tablet in capsule system: A novel chronotherapeutic system of ketorolac tromethamine for site and time specific delivery

The objective of the present work was to develop a novel delivery system of ketorolac tromethamine (KT) for dual pulse release based on microspheres and tablet in capsule system (MATICS) as a treatment modality for rheumatoid arthritis. The design consisted of an impermeable hard gelatin capsule bod...

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Autores principales: Shahi, Priya, Kumari, Neeraj, Pathak, Kamla
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4522866/
https://www.ncbi.nlm.nih.gov/pubmed/26258058
http://dx.doi.org/10.4103/2230-973X.160854
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author Shahi, Priya
Kumari, Neeraj
Pathak, Kamla
author_facet Shahi, Priya
Kumari, Neeraj
Pathak, Kamla
author_sort Shahi, Priya
collection PubMed
description The objective of the present work was to develop a novel delivery system of ketorolac tromethamine (KT) for dual pulse release based on microspheres and tablet in capsule system (MATICS) as a treatment modality for rheumatoid arthritis. The design consisted of an impermeable hard gelatin capsule body, in which a core tablet was (second pulse) placed in the bottom and sealed with a hydrogel plug (HP2). The body was locked with enteric coated cap filled with KT microspheres (first pulse). The microspheres for first pulse were selected by screening the formulations (M1–M6), and M1 with least particle size of 96.38 ± 0.05 μm, highest drug loading of 25.10% ± 0.28% and maximum CDR of 89.32% ± 0.21% was adjudged as the best formulation. The HP2 tablet was selected based on its capability for maintaining a lag period of 6 h. The selection criterion of the second pulse (core tablet: T3) was its disintegration time of 4.02 ± 0.53 min and CDR of 99.10% ± 0.32% in 30 min. All the optimized formulations were assembled in accordance with the proposed design to form pulsatile MATICS and evaluated for in vitro release. MATICS displayed delayed sustained CDR of 80.15% in 8 h from the first pulse (microspheres) after a lag time of 2 h, followed by 97.05% KT release from second pulse (core tablet) in simulated colonic fluid within 10 h. Conclusively, in vitro pulsatile release was a rational combination of delayed sustained and immediate release of KT that has the potential to combat the pain at night and morning stiffness. Incorporation of two pulses in one system offers a reduction in dose frequency and better pain management.
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spelling pubmed-45228662015-08-07 Microspheres and tablet in capsule system: A novel chronotherapeutic system of ketorolac tromethamine for site and time specific delivery Shahi, Priya Kumari, Neeraj Pathak, Kamla Int J Pharm Investig Original Research Article The objective of the present work was to develop a novel delivery system of ketorolac tromethamine (KT) for dual pulse release based on microspheres and tablet in capsule system (MATICS) as a treatment modality for rheumatoid arthritis. The design consisted of an impermeable hard gelatin capsule body, in which a core tablet was (second pulse) placed in the bottom and sealed with a hydrogel plug (HP2). The body was locked with enteric coated cap filled with KT microspheres (first pulse). The microspheres for first pulse were selected by screening the formulations (M1–M6), and M1 with least particle size of 96.38 ± 0.05 μm, highest drug loading of 25.10% ± 0.28% and maximum CDR of 89.32% ± 0.21% was adjudged as the best formulation. The HP2 tablet was selected based on its capability for maintaining a lag period of 6 h. The selection criterion of the second pulse (core tablet: T3) was its disintegration time of 4.02 ± 0.53 min and CDR of 99.10% ± 0.32% in 30 min. All the optimized formulations were assembled in accordance with the proposed design to form pulsatile MATICS and evaluated for in vitro release. MATICS displayed delayed sustained CDR of 80.15% in 8 h from the first pulse (microspheres) after a lag time of 2 h, followed by 97.05% KT release from second pulse (core tablet) in simulated colonic fluid within 10 h. Conclusively, in vitro pulsatile release was a rational combination of delayed sustained and immediate release of KT that has the potential to combat the pain at night and morning stiffness. Incorporation of two pulses in one system offers a reduction in dose frequency and better pain management. Medknow Publications & Media Pvt Ltd 2015 /pmc/articles/PMC4522866/ /pubmed/26258058 http://dx.doi.org/10.4103/2230-973X.160854 Text en Copyright: © International Journal of Pharmaceutical Investigation http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Research Article
Shahi, Priya
Kumari, Neeraj
Pathak, Kamla
Microspheres and tablet in capsule system: A novel chronotherapeutic system of ketorolac tromethamine for site and time specific delivery
title Microspheres and tablet in capsule system: A novel chronotherapeutic system of ketorolac tromethamine for site and time specific delivery
title_full Microspheres and tablet in capsule system: A novel chronotherapeutic system of ketorolac tromethamine for site and time specific delivery
title_fullStr Microspheres and tablet in capsule system: A novel chronotherapeutic system of ketorolac tromethamine for site and time specific delivery
title_full_unstemmed Microspheres and tablet in capsule system: A novel chronotherapeutic system of ketorolac tromethamine for site and time specific delivery
title_short Microspheres and tablet in capsule system: A novel chronotherapeutic system of ketorolac tromethamine for site and time specific delivery
title_sort microspheres and tablet in capsule system: a novel chronotherapeutic system of ketorolac tromethamine for site and time specific delivery
topic Original Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4522866/
https://www.ncbi.nlm.nih.gov/pubmed/26258058
http://dx.doi.org/10.4103/2230-973X.160854
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