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Formulation design and optimization of fast dissolving clonazepam tablets.
S B Shirsand1, Sarasija Suresh, P V Swamy
1Department of Pharmaceutics, H. K. E. Society's College of Pharmacy, Sedam Road, Gulbarga-585 105, India.
Indian Journal of Pharmaceutical Sciences
|May 27, 2010
Summary
New fast dissolving clonazepam tablets were developed using crospovidone and microcrystalline cellulose. Optimized formulations demonstrated significantly faster drug release compared to conventional tablets, enhancing patient compliance.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Formulation Development
Background:
- Patient compliance is crucial for effective treatment, particularly with medications requiring frequent dosing.
- Fast-dissolving tablet formulations offer an alternative to conventional oral dosage forms, potentially improving patient adherence.
- Clonazepam is commonly prescribed for various neurological and psychiatric conditions, necessitating optimized delivery methods.
Purpose of the Study:
- To develop and optimize fast-dissolving tablets (FDTs) of clonazepam using a direct compression method.
- To investigate the impact of crospovidone (superdisintegrant) and microcrystalline cellulose (diluent) on tablet properties and drug release.
- To enhance patient compliance through improved drug dissolution and release profiles.
Main Methods:
- A 3(2) full factorial design was employed to study the effects of crospovidone (2-8%) and microcrystalline cellulose (20-40%) concentrations.
- Tablets were prepared by direct compression using mannitol as a filler.
- Evaluation included hardness, friability, drug content uniformity, in vitro dispersion time, wetting time, water absorption ratio, and in vitro drug release studies.
- Stability studies and drug-excipient interaction assessments were conducted.
Main Results:
- The optimal formulation (2% crospovidone, 40% microcrystalline cellulose) exhibited an in vitro dispersion time of approximately 16 seconds.
- The optimized FDTs showed a nearly five-fold faster drug release compared to conventional commercial tablets (t50% of 3.5 min vs. 16.4 min).
- Short-term stability studies indicated no significant changes in drug content or dispersion time (P<0.05).
Conclusions:
- Fast-dissolving clonazepam tablets can be successfully prepared by direct compression.
- The optimized formulation significantly enhances the dissolution rate of clonazepam, potentially improving therapeutic efficacy.
- This approach offers a promising strategy for improving patient compliance in clonazepam therapy.
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