Physical characterizations and sustained release profiling of gastroretentive drug delivery systems with improved floating and swelling capabilities

Ying Chen Chen, Hsiu O. Ho, Tzu Yu Lee, Ming Thau Sheu

Research output: Contribution to journalArticle

29 Citations (Scopus)

Abstract

The aim was to develop gastroretentive drug delivery systems (GRDDSs) by combining floating and swelling. GRDDS tablets formulated with hydroxyethylcellulose (HEC), chitosan (CS) and sodium bicarbonate (SB) for evaluating floating capacity (floating lag time and duration) and swelling characteristics. CS was used because it was swellable in acidic media and biocompatible. Losartan was incorporated into the optimized formulations for sustained release profiling. Results demonstrated that for those formulations at HEC:CS ratio of 5:5 containing CS, both the floating lag time and floating duration were optimal and reached the preferred swelling effect and sustain for 24 h. Adding SB improved the floating capabilities for all ratios of HEC:CS, but reduced the swelling ability for those formulations containing a higher portion of low viscosity grade CS. Sustained release profiles for losartan in those formulations were achievable, using all viscosity grades of CS at all examined HEC:CS ratios; however, it is more adjustable at different HEC:CS ratios when using a lower viscosity grade of CS. Optimized GRDDS formulations for losartan composed of an equivalent ratio of HEC to CS with 20 mg SB resulted in the tablets floating for more than 16 h and an adjustable sustained release profile.

Original languageEnglish
Pages (from-to)162-169
Number of pages8
JournalInternational Journal of Pharmaceutics
Volume441
Issue number1-2
DOIs
Publication statusPublished - Jan 30 2013

Fingerprint

Chitosan
Drug Delivery Systems
Sodium Bicarbonate
Losartan
Viscosity
Tablets
hydroxyethylcellulose

Keywords

  • Chitosan
  • Floating
  • Gastroretentive drug delivery system
  • Hydroxyethylcellulose
  • Losartan
  • Swelling

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

@article{d9956f2614554873a303feb302b769cb,
title = "Physical characterizations and sustained release profiling of gastroretentive drug delivery systems with improved floating and swelling capabilities",
abstract = "The aim was to develop gastroretentive drug delivery systems (GRDDSs) by combining floating and swelling. GRDDS tablets formulated with hydroxyethylcellulose (HEC), chitosan (CS) and sodium bicarbonate (SB) for evaluating floating capacity (floating lag time and duration) and swelling characteristics. CS was used because it was swellable in acidic media and biocompatible. Losartan was incorporated into the optimized formulations for sustained release profiling. Results demonstrated that for those formulations at HEC:CS ratio of 5:5 containing CS, both the floating lag time and floating duration were optimal and reached the preferred swelling effect and sustain for 24 h. Adding SB improved the floating capabilities for all ratios of HEC:CS, but reduced the swelling ability for those formulations containing a higher portion of low viscosity grade CS. Sustained release profiles for losartan in those formulations were achievable, using all viscosity grades of CS at all examined HEC:CS ratios; however, it is more adjustable at different HEC:CS ratios when using a lower viscosity grade of CS. Optimized GRDDS formulations for losartan composed of an equivalent ratio of HEC to CS with 20 mg SB resulted in the tablets floating for more than 16 h and an adjustable sustained release profile.",
keywords = "Chitosan, Floating, Gastroretentive drug delivery system, Hydroxyethylcellulose, Losartan, Swelling",
author = "Chen, {Ying Chen} and Ho, {Hsiu O.} and Lee, {Tzu Yu} and Sheu, {Ming Thau}",
year = "2013",
month = "1",
day = "30",
doi = "10.1016/j.ijpharm.2012.12.002",
language = "English",
volume = "441",
pages = "162--169",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-2",

}

TY - JOUR

T1 - Physical characterizations and sustained release profiling of gastroretentive drug delivery systems with improved floating and swelling capabilities

AU - Chen, Ying Chen

AU - Ho, Hsiu O.

AU - Lee, Tzu Yu

AU - Sheu, Ming Thau

PY - 2013/1/30

Y1 - 2013/1/30

N2 - The aim was to develop gastroretentive drug delivery systems (GRDDSs) by combining floating and swelling. GRDDS tablets formulated with hydroxyethylcellulose (HEC), chitosan (CS) and sodium bicarbonate (SB) for evaluating floating capacity (floating lag time and duration) and swelling characteristics. CS was used because it was swellable in acidic media and biocompatible. Losartan was incorporated into the optimized formulations for sustained release profiling. Results demonstrated that for those formulations at HEC:CS ratio of 5:5 containing CS, both the floating lag time and floating duration were optimal and reached the preferred swelling effect and sustain for 24 h. Adding SB improved the floating capabilities for all ratios of HEC:CS, but reduced the swelling ability for those formulations containing a higher portion of low viscosity grade CS. Sustained release profiles for losartan in those formulations were achievable, using all viscosity grades of CS at all examined HEC:CS ratios; however, it is more adjustable at different HEC:CS ratios when using a lower viscosity grade of CS. Optimized GRDDS formulations for losartan composed of an equivalent ratio of HEC to CS with 20 mg SB resulted in the tablets floating for more than 16 h and an adjustable sustained release profile.

AB - The aim was to develop gastroretentive drug delivery systems (GRDDSs) by combining floating and swelling. GRDDS tablets formulated with hydroxyethylcellulose (HEC), chitosan (CS) and sodium bicarbonate (SB) for evaluating floating capacity (floating lag time and duration) and swelling characteristics. CS was used because it was swellable in acidic media and biocompatible. Losartan was incorporated into the optimized formulations for sustained release profiling. Results demonstrated that for those formulations at HEC:CS ratio of 5:5 containing CS, both the floating lag time and floating duration were optimal and reached the preferred swelling effect and sustain for 24 h. Adding SB improved the floating capabilities for all ratios of HEC:CS, but reduced the swelling ability for those formulations containing a higher portion of low viscosity grade CS. Sustained release profiles for losartan in those formulations were achievable, using all viscosity grades of CS at all examined HEC:CS ratios; however, it is more adjustable at different HEC:CS ratios when using a lower viscosity grade of CS. Optimized GRDDS formulations for losartan composed of an equivalent ratio of HEC to CS with 20 mg SB resulted in the tablets floating for more than 16 h and an adjustable sustained release profile.

KW - Chitosan

KW - Floating

KW - Gastroretentive drug delivery system

KW - Hydroxyethylcellulose

KW - Losartan

KW - Swelling

UR - http://www.scopus.com/inward/record.url?scp=84872784389&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84872784389&partnerID=8YFLogxK

U2 - 10.1016/j.ijpharm.2012.12.002

DO - 10.1016/j.ijpharm.2012.12.002

M3 - Article

VL - 441

SP - 162

EP - 169

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -