Abstract

OPTIMIZED FORMULATION AND IN-VITRO ASSESSMENT OF SUSTAINED RELEASE NEBIVOLOL TABLETS USING Î’- CYCLODEXTRIN-BASED SOLID DISPERSIONS

Chaithra R. P.*, Pruthvi A. V.*, Shankrayya M., Venkatesh J. S., Arun Kumar M. K., Chethan Dixit

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Abstract

This study focused on developing and evaluating sustained release (SR) tablets of Nebivolol Hydrochloride using solid dispersion techniques to overcome its poor solubility and low oral bioavailability (~12%) due to first-pass metabolism. Solid dispersions were prepared with β-cyclodextrin at drug-to-carrier ratios of 1:1, 1:3, and 1:5 using the kneading method. FTIR and DSC studies confirmed drug–excipient compatibility, and β-cyclodextrin showed the greatest solubility enhancement. The optimized dispersions were incorporated into SR matrix tablets using HPMC K100M (20%, 25%, and 30% w/w) as polymer by direct compression. All formulations met pharmacopeial standards, showing good flow properties, mechanical strength, and drug content uniformity. In-vitro dissolution revealed sustained release over 12 hours, with F3, F8, and F9 achieving more than 95% drug release. The release followed Higuchi and Korsmeyer–Peppas models, indicating Fickian diffusion. Stability testing of the optimized formulation (F9) for three months under accelerated conditions showed no significant changes. These findings suggest that solid dispersion-based SR tablets can effectively enhance solubility, prolong release, and improve the therapeutic efficacy of Nebivolol.

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