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Immediate release tablets of telmisartan using superdisintegrant-formulation, evaluation and stability studies.
Vasanthakumar Sekar1, Vijaya Raghavan Chellan
1Department of Pharmaceutics, College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences, Tamil Nadu, India.
Chemical & Pharmaceutical Bulletin
|April 2, 2008
Summary
This study enhanced telmisartan (anti-hypertensive) bioavailability by developing immediate-release tablets using Polyplasdone XL-10. The formulation improved drug dissolution and showed stability over six months.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Telmisartan, an anti-hypertensive drug, exhibits poor water solubility, leading to slow dissolution and limited bioavailability (42%).
- This necessitates formulation strategies to enhance the dissolution rate and improve therapeutic efficacy.
Purpose of the Study:
- To develop immediate-release telmisartan tablets using Polyplasdone XL-10 (Crosspovidone).
- To evaluate the impact of Polyplasdone XL-10 addition at different stages (intragranular, extragranular, or both) on drug release and bioavailability.
Main Methods:
- Telmisartan granules and tablets were prepared with varying concentrations and addition sites of Polyplasdone XL-10.
- Physicochemical properties, hardness, and disintegration times of the formulations were assessed.
- In-vitro dissolution studies were performed on the prepared tablets.
Main Results:
- Polyplasdone XL-10 effectively increased the dissolution rate of telmisartan.
- Optimized formulations exhibited suitable hardness and disintegration times for immediate release.
- Formulation-10 (F10) demonstrated stable in-vitro drug release characteristics over a six-month period.
Conclusions:
- Immediate-release telmisartan tablets with enhanced dissolution and bioavailability can be successfully formulated using Polyplasdone XL-10.
- The use of Polyplasdone XL-10 is a viable strategy to overcome the solubility challenges of telmisartan.
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