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Formulation and evaluation of dextromethorphan hydrobromide sustained release tablets.
Subramania Nainar Meyyanathan1, Sekar Rajan, Selvadurai Muralidaharan
1Department of Pharmaceutical Analysis, JSS College of Pharmacy, Rocklands, Ootacamund-643 001, India.
Drug Delivery
|August 21, 2008
Summary
Sustained release dextromethorphan hydrobromide tablets were developed using hydroxypropyl methyl cellulose. The optimized formulation showed significantly higher drug absorption due to a longer half-life compared to immediate-release tablets.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Pharmacokinetics
Background:
- Dextromethorphan hydrobromide is commonly formulated as immediate-release tablets.
- There is a need for sustained-release formulations to improve patient compliance and therapeutic efficacy.
- Hydroxypropyl methyl cellulose (HPMC) is a widely used hydrophilic polymer for sustained drug release.
Purpose of the Study:
- To develop and characterize sustained-release (SR) matrix tablets of dextromethorphan hydrobromide.
- To investigate the influence of polymer concentration and fillers on in vitro drug release.
- To evaluate the in vivo bioavailability of the optimized SR formulation compared to immediate-release tablets.
Main Methods:
- Sustained-release matrix tablets were prepared using wet granulation with HPMC-K-100 CR as the rate-controlling polymer.
- In vitro drug release studies were conducted to assess the effect of polymer concentration and fillers.
- A crossover bioavailability study was performed in six healthy male volunteers comparing the optimized SR tablets with a marketed immediate-release formulation.
Main Results:
- Drug release from the SR tablets could be effectively modulated by adjusting the concentration of HPMC and the type of fillers used.
- The optimized sustained-release formulation demonstrated significantly higher extent of drug absorption compared to the marketed immediate-release dextromethorphan hydrobromide tablets.
- The enhanced absorption was attributed to a lower elimination rate and a longer half-life observed with the SR formulation.
Conclusions:
- Hydroxypropyl methyl cellulose is a suitable polymer for developing sustained-release matrix tablets of dextromethorphan hydrobromide.
- The developed SR formulation offers improved bioavailability and pharmacokinetic profile over immediate-release dosage forms.
- This sustained-release technology holds promise for enhancing the therapeutic management of conditions treated with dextromethorphan hydrobromide.
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