9 Citations (Scopus)

Abstract

Introduction: In this study, we present the development of a chronomodulated delivery system consisting of a fast-swelling tablet core containing montelukast sodium coated with a blend of different ratios of ethyl cellulose (gastrointestinal tract (GIT)-insoluble polymer) and Eudragit L100 (enteric polymer). Montelukast sodium is a leukotriene receptor antagonist commonly prescribed for patients of asthma and allergic rhinitis. Asthma and allergic rhinitis share a common core pathophysiology and have almost similar temporal pattern in their occurrence or exacerbation of their respective symptoms, suggesting a role for chronotherapy. Methods: The developed formulation was optimized statistically using central composite design to achieve desired release profile. The coated tablets were studied for water uptake, bursting time, and in vitro release study. Results: The bursting time (lag time) of coated tablet was affected by the pH of buffer, molarity of ions, and concentration of different types of surfactant in dissolution media. With increasing percentage of Eudragit L100 in coating composition, the lag time decreased and release rates significantly increased - could be attributed due to increase in water uptake and polymer leaching. As expected, with increasing coating level, lag time increased and release rate decreased due to the increased diffusion pathways. In vivo study revealed comparative pharmacokinetic profiles of core tablets and pulsatile release tablets (PRTs); however, T max of 2 h for core tablets and 6 h for PRTs were observed. Conclusion: Thus, designed PRTs were found to be suitable in treating episodic attack of asthma in early morning and associated allergic rhinitis.

Original languageEnglish
Pages (from-to)95-105
Number of pages11
JournalJournal of Pharmaceutical Innovation
Volume9
Issue number2
DOIs
Publication statusPublished - 2014

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Tablets
montelukast
Polymers
Asthma
Chronotherapy
Leukotriene Antagonists
In Vitro Techniques
ethyl cellulose
methylmethacrylate-methacrylic acid copolymer
Water
Surface-Active Agents
Gastrointestinal Tract
Buffers
Pharmacokinetics
Ions
Allergic Rhinitis

All Science Journal Classification (ASJC) codes

  • Drug Discovery
  • Pharmaceutical Science

Cite this

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title = "Optimization of chronomodulated delivery system coated with a blend of ethyl cellulose and Eudragit L100 by central composite design: In vitro and in vivo evaluation",
abstract = "Introduction: In this study, we present the development of a chronomodulated delivery system consisting of a fast-swelling tablet core containing montelukast sodium coated with a blend of different ratios of ethyl cellulose (gastrointestinal tract (GIT)-insoluble polymer) and Eudragit L100 (enteric polymer). Montelukast sodium is a leukotriene receptor antagonist commonly prescribed for patients of asthma and allergic rhinitis. Asthma and allergic rhinitis share a common core pathophysiology and have almost similar temporal pattern in their occurrence or exacerbation of their respective symptoms, suggesting a role for chronotherapy. Methods: The developed formulation was optimized statistically using central composite design to achieve desired release profile. The coated tablets were studied for water uptake, bursting time, and in vitro release study. Results: The bursting time (lag time) of coated tablet was affected by the pH of buffer, molarity of ions, and concentration of different types of surfactant in dissolution media. With increasing percentage of Eudragit L100 in coating composition, the lag time decreased and release rates significantly increased - could be attributed due to increase in water uptake and polymer leaching. As expected, with increasing coating level, lag time increased and release rate decreased due to the increased diffusion pathways. In vivo study revealed comparative pharmacokinetic profiles of core tablets and pulsatile release tablets (PRTs); however, T max of 2 h for core tablets and 6 h for PRTs were observed. Conclusion: Thus, designed PRTs were found to be suitable in treating episodic attack of asthma in early morning and associated allergic rhinitis.",
author = "Ranjan, {Om Prakash} and Nayak, {Usha Y.} and Reddy, {M. Sreenivasa} and Dengale, {Swapnil J.} and Musmade, {Prashant B.} and Nayanabhirama Udupa",
year = "2014",
doi = "10.1007/s12247-014-9176-3",
language = "English",
volume = "9",
pages = "95--105",
journal = "Journal of Pharmaceutical Innovation",
issn = "1872-5120",
publisher = "Springer New York",
number = "2",

}

TY - JOUR

T1 - Optimization of chronomodulated delivery system coated with a blend of ethyl cellulose and Eudragit L100 by central composite design

T2 - In vitro and in vivo evaluation

AU - Ranjan, Om Prakash

AU - Nayak, Usha Y.

AU - Reddy, M. Sreenivasa

AU - Dengale, Swapnil J.

AU - Musmade, Prashant B.

AU - Udupa, Nayanabhirama

PY - 2014

Y1 - 2014

N2 - Introduction: In this study, we present the development of a chronomodulated delivery system consisting of a fast-swelling tablet core containing montelukast sodium coated with a blend of different ratios of ethyl cellulose (gastrointestinal tract (GIT)-insoluble polymer) and Eudragit L100 (enteric polymer). Montelukast sodium is a leukotriene receptor antagonist commonly prescribed for patients of asthma and allergic rhinitis. Asthma and allergic rhinitis share a common core pathophysiology and have almost similar temporal pattern in their occurrence or exacerbation of their respective symptoms, suggesting a role for chronotherapy. Methods: The developed formulation was optimized statistically using central composite design to achieve desired release profile. The coated tablets were studied for water uptake, bursting time, and in vitro release study. Results: The bursting time (lag time) of coated tablet was affected by the pH of buffer, molarity of ions, and concentration of different types of surfactant in dissolution media. With increasing percentage of Eudragit L100 in coating composition, the lag time decreased and release rates significantly increased - could be attributed due to increase in water uptake and polymer leaching. As expected, with increasing coating level, lag time increased and release rate decreased due to the increased diffusion pathways. In vivo study revealed comparative pharmacokinetic profiles of core tablets and pulsatile release tablets (PRTs); however, T max of 2 h for core tablets and 6 h for PRTs were observed. Conclusion: Thus, designed PRTs were found to be suitable in treating episodic attack of asthma in early morning and associated allergic rhinitis.

AB - Introduction: In this study, we present the development of a chronomodulated delivery system consisting of a fast-swelling tablet core containing montelukast sodium coated with a blend of different ratios of ethyl cellulose (gastrointestinal tract (GIT)-insoluble polymer) and Eudragit L100 (enteric polymer). Montelukast sodium is a leukotriene receptor antagonist commonly prescribed for patients of asthma and allergic rhinitis. Asthma and allergic rhinitis share a common core pathophysiology and have almost similar temporal pattern in their occurrence or exacerbation of their respective symptoms, suggesting a role for chronotherapy. Methods: The developed formulation was optimized statistically using central composite design to achieve desired release profile. The coated tablets were studied for water uptake, bursting time, and in vitro release study. Results: The bursting time (lag time) of coated tablet was affected by the pH of buffer, molarity of ions, and concentration of different types of surfactant in dissolution media. With increasing percentage of Eudragit L100 in coating composition, the lag time decreased and release rates significantly increased - could be attributed due to increase in water uptake and polymer leaching. As expected, with increasing coating level, lag time increased and release rate decreased due to the increased diffusion pathways. In vivo study revealed comparative pharmacokinetic profiles of core tablets and pulsatile release tablets (PRTs); however, T max of 2 h for core tablets and 6 h for PRTs were observed. Conclusion: Thus, designed PRTs were found to be suitable in treating episodic attack of asthma in early morning and associated allergic rhinitis.

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U2 - 10.1007/s12247-014-9176-3

DO - 10.1007/s12247-014-9176-3

M3 - Article

VL - 9

SP - 95

EP - 105

JO - Journal of Pharmaceutical Innovation

JF - Journal of Pharmaceutical Innovation

SN - 1872-5120

IS - 2

ER -