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Formulation and Preparation of Losartan-Potassium-Loaded Controlled-Release Matrices Using Ethocel Grade 10 to
Kamran Ahmad Khan1, Ashfaq Ahmad2, Carlotta Marini3
1Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan P.O. Box 29050, Pakistan.
Pharmaceutics
|February 24, 2024
Summary
New losartan potassium matrices formulated with Ethocel 10 FP polymer demonstrated pseudo-zero-order release kinetics. In vivo studies showed a strong correlation between in vitro drug release and in vivo absorption, suggesting improved patient compliance.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Losartan potassium is a widely prescribed medication for hypertension.
- Optimizing drug release profiles is crucial for improving therapeutic efficacy and patient adherence.
- Controlled-release formulations aim to provide sustained drug levels, reducing dosing frequency.
Purpose of the Study:
- To formulate and characterize losartan potassium matrices using Ethocel 10 premium and Ethocel 10FP premium polymers.
- To evaluate the in vitro drug release kinetics and in vivo pharmacokinetic profile of the optimized matrices.
- To establish a correlation between in vitro drug release and in vivo drug absorption.
Main Methods:
- Losartan potassium matrices were prepared using direct compression with varying drug-to-polymer ratios (10:3, 10:4, 10:5).
- Physical parameters (hardness, diameter, thickness, friability, weight variation, content uniformity) and in vitro dissolution were assessed.
- Pharmacokinetic parameters (half-life, Tmax, Cmax, AUC, MRT, Cl) were determined in rabbits after oral administration.
- In vitro-in vivo correlation (IVIVC) was established.
Main Results:
- Matrices with Ethocel 10 FP at a 10:4 ratio exhibited pseudo-zero-order release kinetics (n=0.986).
- A strong level-A correlation (r=0.985) was observed between in vitro drug release and in vivo drug absorption.
- Pharmacokinetic analysis in rabbits revealed favorable parameters, including a half-life of 11.78 ± 0.018 h.
Conclusions:
- The developed losartan potassium matrices, particularly those with Ethocel 10 FP at a 10:4 ratio, show promising controlled-release characteristics.
- The established level-A IVIVC validates the predictive capability of the in vitro dissolution test for in vivo performance.
- These optimized matrices have the potential to enhance patient compliance through once-daily dosing and improve therapeutic outcomes.
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