ABSTRACT

An antihypertensive drug, Benidipine (BND) is Biopharmaceutical Classification System Class-II drug having low solubility and high permeability and has lower bioavailability. The present study describes the preparation of matrix tablet from lyophilized BND nanoparticles as lyophilization technique is used in order to improve the dissolution and oral bioavailability of the drugs with poor solubility and high permeability, matrix tablet was formulated to achieve extended drug release and to study its drug release pattern as well. BND has mean half-life 5.3 hr and requires frequent dosing every 5-6 hr to maintain optimal relive and used orally in the treatment of hypertension and angina pectoris, but this frequent administration produces side effects like dizziness and headache. So in present study we have achieved extended drug release for time up to 25 hr for treatment of hypertension, for continuous 24 hr control of blood pressure (BP), 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 using 32 factorial design in order to study the effect of independent variables X1 and X2 (i.e. amount of HPMC K4 and Chitosan respectively) on dependent variable (i.e. % drug release in 10 hr (Q10) and time require for 80% drug release (T80)) to evaluate extended drug release. The tablets were prepared by direct compression method. In-vitro drug release of different formulations was carried out under stimulated gastric and intestinal condition to achieve optimized drug release. Optimized batch F5 has achieved 99% drug release in 25 hr. The physiochemical characterizations of all prepared formulations were found to be satisfactory. Fourier transform infrared spectroscopy (FTIR) study of optimized F5 batch was performed to study any interaction of BND with polymer. Keywords: Benidipine, Bioavailability, lyophilization, hypertension, direct compression method, Matrix Tablet
Publication date: 01/07/2022

https://ijbpas.com/pdf/2022/July/MS_IJBPAS_2022_6194.pdf

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https://doi.org/10.31032/IJBPAS/2022/11.7.6194