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Sustained release of theophylline from hydroxypropylcellulose tablets
Journal of Pharmaceutical Sciences
|April 1, 1983
Summary
Hydroxypropylcellulose viscosity and content impact theophylline release from tablets. Higher viscosity and polymer content resulted in slower drug release, confirmed in human studies.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Theophylline is a common bronchodilator.
- Developing sustained-release formulations is crucial for improving patient compliance and therapeutic efficacy.
Purpose of the Study:
- To investigate the influence of hydroxypropylcellulose (HPC) properties on theophylline release from compressed tablets.
- To evaluate the in vitro and in vivo performance of these sustained-release theophylline tablets.
Main Methods:
- Compressed tablets were formulated using theophylline and varying grades and concentrations of hydroxypropylcellulose.
- In vitro drug release studies were conducted to assess the impact of polymer viscosity and content.
- In vivo salivary theophylline levels were monitored in human volunteers after oral administration.
Main Results:
- Theophylline release rate decreased significantly with increasing hydroxypropylcellulose viscosity grade.
- Higher polymer content in the tablets also led to a reduced drug release rate.
- In vivo studies demonstrated a low but sustained salivary theophylline concentration, confirming sustained drug release.
Conclusions:
- Hydroxypropylcellulose viscosity and content are critical factors in controlling theophylline release from sustained-release tablets.
- The developed tablet formulations show promise for effective in vivo sustained drug delivery.