IN VITRO AND IN VIVO EVALUATION FOR SUSTAINED RELEASE MATRIX TABLET FORMULATED FROM LYOPHILIZED BENIDIPINE NANOPARTICLES
Authors: Shah T , PATEL S, LEUVA K, PATEL J, YADAV P, VEGAD K AND SHAH H

ABSTRACT
An antihypertensive drug, Benidipine (BND) is considered under Biopharmaceutical Classification System Class-?? drug, it has a high permeability but little solubility, and has lower bioavailability. The present study describes the preparation of lyophilized nanoparticles from nanosuspension and matrix tablet from lyophilized BND nanoparticles using Lyophilization strategy to significantly raise the dissolution and oral bioavailability of the drug including poor solubility and high permeability. Matrix tablet of BND was formulated from lyophilized BND nanoparticles, by using polymers HPMC K4, Chitosan, MCC, magnesium Stearate, lactose and talc in order to prepare the suitable formulation. Matrix tablets of lyophilized BND nanoparticles was formulated to assess extended drug release extended drug release. Matrix tablets of lyophilized BND nanoparticles was formulated in order to study the effect of amount of HPMC K4 and Chitosan respectively) on % drug release in 10 hr (Q10) and time require for 80% drug release (T80)) to evaluate extended drug release. A direct compression approach was used to develop the Matrix tablet from lyophilized BND nanoparticles. To achieve optimal % drug release, various formulations of BND were assessed for in-vitro under stimulated gastric and intestinal conditions. Optimized batch F5 has achieved 99 % drug release in 25 hours. It was determined that physiochemical characteristics of all developed formulations were evaluated andthe results were found feasible. Fourier transform infrared spectroscopy (FTIR) study of optimized F5 batch has been performed to investigate any interaction of BND with polymer. In in-vivo study, Tmax was found 30 mins and Cmax was 1530 ng/ml and 3240 ng/ml respectively, approximately three?fold higher than marketed tablet. Keywords: Benidipine, Lyophilization, Dissolution, Nanoparticles, Pharmacokinetics, Matrix tablet
Publication date: 01/11/2023
    https://ijbpas.com/pdf/2023/November/MS_IJBPAS_2023_7390.pdf
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https://doi.org/10.31032/IJBPAS/2023/12.11.7390