Formulation and Characterization of Sustained Release Matrix Tablets of Ivabradine Using 32 Full Factorial Design

Abstract

Objective: Ivabradine (IB) is anti-Ischemic drug and used for the symptomatic management of stable angina pectoris. IB acts by reducing the heart rate in a mechanism different from beta blockers and calcium channel blockers, two commonly prescribed anti-anginal drugs. IB has a short biological half-life and the dose of 5/7.5 mg twice a day. In this present study, an attempt has been made to prepare sustained release tablet of IB to achieve the desired drug release. Methods:The sustained release polymers, hydroxypropyl methylcellulose K100M (HPMC K100M), guar gum (GG) and xanthan gum (XG) were taken for the preliminary trail from which guar gum and xanthan gum had shown better drug release. Initially, drug-excipients compatibility studies were carried out by using Fourier transformed infrared spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) which showed no interaction between drug and excipients. Tablets were prepared by wet granulation technique and evaluated for pre-compression and postcompression parameters.Results: 3 2 full factorial design was applied to achieve controlled drug release up to 24 h. The concentration of GG (X1) and XG (X2) were selected as independent variables and the % CDR at 2 h. (Y1) and 18 h. (Y2) were taken as dependent variables. In vitro drug release study revealed that as the amount of polymers increased, % CDR decreased. Conclusion:Contour as well as response surface plots were constructed to show the effect of X1 and X2 on % CDR and predicted at the concentration of independent variables X1 (10 mg) and X2 (10 mg) for a maximized response. The optimized batch (O1) was kept for stability study at 40±2 °C/75±5 %RH for a period of 6mo according to ICH guidelines and found to be stable.

Prediction of Absorption, Distribution, Metabolism, and Excretion Activity of the Components of Madhuca Longifolia and Its Inhibiting Target Molecule

“…The underlying goal and end-game for all ADME studies are to better understand a compound's metabolite-mediated toxicity and safety profile to make a concrete decision on whether the compound can progress to late-stage preclinical and clinical studies to enable filing for an investigational new drug, new drug agreement, or a biologics licensing agreement. ADME studies can be used in molecular docking, pharmacophore modeling, de novo designing, fragment-based screening, to find structure-activity relationships [25,26]. Transporters play an important role in the ADME of drugs.…”

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“…Here in equation 3, b 2 value is more negative than b 1 which indicated that EC had more release retardant effect compare to the HPMC K100M at 1 h [ Figures 4 and 5]. [20] Regression analysis for the effect of X 1 and X 2 on in vitro drug release at 4 h […”

Development and Evaluation of Sustain Release Microparticles of Metoproproprolol Succinate

“…A factor was considered to influence the response if the effects are significant (p<0.05). A positive value indicates a synergistic effect that favors optimization, while a negative sign represents an antagonistic effect or inverse effect of the factor on the selected response [13]. When we study the optimization of formulation for 100 mg constant drug amount considering 70% CPR at 8 h and 100% Drug Entrapment Efficiency it was observed that 200 mg total polymer, 30% gelatin wrt total polymer and 6 h oxidation reaction time is the predicted optimized formula for around 91% DEE and 72%CPR at 8 h. This prediction matches with the formulation No.…”