Comparative release profile of sustained release matrix tablets of verapamil HCl (original) (raw)
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LATIN AMERICAN JOURNAL OF PHARMACY
. The pharmaceutical attributes of sustained release (SR) oral tablets containing verapamil hy-drochloride prepared by using synthetic polymers (HPMC K4M and Na carboxymethylcellulose) and natural hydrophilic matrix formers (xanthan gum and Acacia) were observed in the present work. Direct compression method was used for the preparation of sustained release matrix tablet using the polymers in different ratios. Compressed tablets were evaluated for hardness, friability, weight variation and in vitro dissolution using USP dissolution apparatus-II. Dissolution profiles of test formulations were obtained in 900 mL distilled water for 12 h at 37 °C. The data was then kinetically evaluated with different mathematical models i.e., Zero Order, First Order, Higuchi, Hixson-Crowell, Baker & Lonsdale, Korsmeyer and Peppas, Weibull, Hoffenberg and Peppas Sahi. Different verapamil hydrochloride matrix tablet formulations have shown different dissolution behavior and it was concluded that the syn...
Asian Journal of Pharmaceutics, 2009
S ustained release tablet of Verapamil hydrochloride (VPH) was prepared by using Precirol ATO 5 (PREC) by direct compression of matrices prepared by using the melt granulation technique. The effect of different concentrations of PREC on the in-vitro drug release of VPH was studied by comparing it with the marketed formulation and percent release given in USP for VPH extended release tablets. Effect of release enhancers such as microcrystalline cellulose (MCC) and lactose on in-vitro drug release was also studied. Biopharmaceutical evaluation of the satisfactory formulation was also performed in order to estimate the maximum concentration of drug in plasma (C max), time required to reach maximum concentration (t max), elimination rate constant (k), elimination rate constant (t 1/2), area under curve (AUC (0-t) and AUC (02a), apparent volume of distribution (V d) and mean residence time. The results showed that PREC can be utilized as the matrix forming agent to sustain the release of VPH. The results of biopharmaceutical evaluation showed that the rate of absorption appeared to be more sustained, resulting in a more uniform plasma concentration profile of VPH. More bioavailability was noted with the sustained release formulation even though the drug has substantial first pass metabolism. The results indicated that it is possible to make once-a-day sustained-release tablet of VPH by using the melt granulation technique.
FORMULATION AND EVALUATION OF MATRIX TABLETS OF VERAPAMIL HYDROCHLORIDE BY SOLID DISPERSION METHOD
ABSTRACT The aim of the study was to improve the solubility and dissolution rate of the drug Verapamil HCL using solid-dispersion-Sustained release matrix tablets by direct compression method. Solid dispersions were prepared by solvent evaporation technique using PEG 6000 poloxamer 188 and Urea as carriers. The solid dispersions were characterized by using FTIR and confirmed that no chemical interaction during entrapment process. The prepared solid dispersions were formulated in matrix tablets evaluated for pre-compression and post-compression parameters. The post compression parameters were evaluated for hardness, friability, weight variation and drug content which were within the acceptable official limits. The drug content was found to be high and uniformly distributed in all formulations. It was shown that with the developed formulations, the release and dissolution of drug from the tablets can be increased by formulating it as solid dispersion tablets. It was concluded that development of sustained release solid-dispersion tablets using poloxamer 188 [97%] with HPMC K4m results highest increase in dissolution rate and optimum rate of drug and reduced crystallinity of Verapamil HCL can account for the faster dissolution of the released drug from the polymer matrix.
Asian Journal of Pharmaceutics, 2011
V erapamil hydrochloride was formulated as oral-controlled release matrix tablets using hydrophilic polymer such as hydroxypropyl methylcellulose K 15 M (HPMC 15 M) along with electrolytes. In this work a new attempt was made for in situ interactions between drug and electrolytes were devised to control the release of highly water soluble drugs from oral hydrophilic monolithic systems. Electrolytes such as aluminum hydroxide and sodium carbonate were used at different concentrations in various formulations, while drug and polymer concentrations were maintained constantly at 1:2 ratios in all the formulations. These electrolytes were used to monitor matrix swelling and gel properties. Electrolytes at higher concentrations exhibited greater inhibition in drug release from the matrix and low concentrations were accounted for controlled release of the drug. The results indicated that the drug released at a controlled rate were due to differential swelling rate and matrix stiffening, and provides a uniform gel layer. These findings indicated that the swelling and gel formation in the presence of ionizable species within the hydrophilic matrices provide an attractive alternative for controlled drug delivery from a simple monolithic system. Accelerated stability studies were carried out as per ICH guidelines for some selected formulations, which indicated that these formulations were stable at accelerated storage conditions.
Development of Hydrophobic Carriers based tablets for Sustained Release of Verapamil
The main aim of the study is to formulate sustained release matrix tablets of verapamil hydrochloride using hydrophobic carriers or meltable binders like stearic acid, carnauba wax and bees wax by melt granulation technique. The influence of a hydrophilic polymer like polyethylene glycol (PEG) was studied on the waxy matrices. Two grades of PEG (4000 and 6000) were used in the preparations. The granules were prepared and compressed into tablets and they are evaluated for their physicochemical properties and in vitro dissolution studies were done. The IR spectral analysis revealed that there are no interactions between drug and the polymers and are compatible with other. The release data were subjected to various release kinetic models and also compared with those of a commercial brand. The tablets prepared fulfilled all the official requirements according to the pharmacopeia. From the dissolution studies it was observed that carnauba wax acts a good retardant (more than 16 h). Among the two grades of PEG used 4000 and 6000, PEG 6000 increases the drug release to a greater extent than PEG 4000. It was concluded that hydrophobic carriers which act as very good retardants of the drug and also PEG can be used as a channeling agent in waxy matrices to regulate the release of the drug.
International Current Pharmaceutical Journal, 2014
The purpose of the current work was to formulate Verapamil Hydrochloride (VH) sustained release matrix tablets by using natural polymers and comparison with leading national brand Calan SR of Searle Pharmaceuticals. Tragacanth and pectin were used in various concentrations. Pre compression studies i.e. angle of repose, bulk density, tapped density, Carr's compressibility index and Hausner's ratio were also performed and found within the Pharmacopoeial limits. Eight formulations (F1-F8) of (VH) were prepared by direct compression method. Post compression studies i.e. Thickness, Hardness, Diameter, Friability and Dissolution studies were conducted. Different kinetic models i.e. zero order, first order, Highuchi model and Korsmeyer Peppas were applied to study release patterns and similarity index was calculated. Dissolution studies were carried out in phosphate buffer of pH 6.8 showed that formulations (F4 and F8) formulated with higher polymers concentration showed comparatively better drug retardation. F5 was the most comparable with the reference product. Verapamil hydrochloride released was observed non-fickian as diffusion following Higuchi model.
In the present study accelerated testing (6 month) and long term testing (12 month) were carried out on Oral Verapamil Hydrochloride control release tablet in order to assess the physical and chemical stability of Verapamil Hydrochloride tablets. All the formulations were tested for disintegration test, % drug content and % drug release over the entire period of testing. These formulations did not show any significant change in any parameter during 12 month and 6 month of testing at 25+5ᵒC/60+5% RH and at 40+2ᵒC/75+5% RH, respectively. All the results were within the acceptable limits. Shelf lives calculated by software R Gui were found to be 43.452, 43.577 and 43.234 months at 1, 3 and 6 months for F4 in accelerated stability. However shelf lives were 44.112, 41.634, 41.867 and 42.896 months at 1, 3, 6 and 12 months respectively in long term stability.
Ankara Universitesi Eczacilik Fakultesi Dergisi, 2004
This work has focused on the effects of different hydroxypropylmethylcellulose (HPMC) types and HPMC:direct tabletting agent (DC-agent) ratio on Verapamil Hydrochloride (VRP HCl) release from monolayered and three-layered matrix tablets. Investigated polymers were Methocel K100LV, K15M, K100M and DC-agent was Ludipress ® LCE. Eight formulations were prepared as monolayered matrix tablets while four formulations were prepared as three-layered matrix tablets by direct compression method. Drug release studies were carried out according to the method given for Delayed Release Articles in USP XXVII. HPMC types and ratios were found to be effective on drug release. Increasing amount and viscosity grade of HPMC resulted in a decrease in release of drug from the matrices. Tablets containing low viscosity grade HPMC at inner and outer layers presented release profiles close to or within the limits of pharmacopeia. Release data of three-layered matrix tablet (F12) and the reference product (Isoptin ®-KKH) which were in agreement with USP XXVII criteria, were evaluated by mathematical models (zero order, first order, Higuchi, Hixson-Crowell, Korsmeyer-Peppas), difference factor (f 1) and similarity factor (f 2). The kinetics of VRP HCl release from F12 showed best fit to Higuchi model and Isoptin ®-KKH well fitted to zero order kinetic model. F12 and Isoptin ®-KKH were both show Anomalous transport mechanism Evren ALĞIN, Müge KILIÇARSLAN, Ayşegül KARATAŞ, Nilüfer YÜKSEL, Tamer BAYKARA 126 according to their n exponent values. Depending on the results of f 1 (5.2) and f 2 (71.4) values, F12 and Isoptin ®-KKH were found to be similar with regard to release kinetics.
2014
The purpose of the current work was to formulate Verapamil Hydrochloride (VH) sustained release matrix tablets by using natural polymers and comparison with leading national brand Calan SR of Searle Pharmaceuticals. Tragacanth and pectin were used in various concentrations. Pre compression studies i.e. angle of repose, bulk density, tapped density, Carr's compressibility index and Hausner's ratio were also performed and found within the Pharmacopoeial limits. Eight formulations (F1-F8) of (VH) were prepared by direct compression method. Post compression studies i.e. Thickness, Hardness, Diameter, Friability and Dissolution studies were conducted. Different kinetic models i.e. zero order, first order, Highuchi model and Korsmeyer Peppas were applied to study release patterns and similarity index was calculated. Dissolution studies were carried out in phosphate buffer of pH 6.8 showed that formulations (F4 and F8) formulated with higher polymers concentration showed comparatively better drug retardation. F5 was the most comparable with the reference product. Verapamil hydrochloride released was observed non-fickian as diffusion following Higuchi model.
FORMULATION DEVELOPMENT AND EVALUATION OF SUSTAINED RELEASE PELLETS OF VERAPAMIL HCl
Objective: The study aims for the design and evaluation of floating tablets of emtricitabine (EMT), post oral administration to sustain the release and enhance gastric residence time (GRT). Methods: EMT is a nucleoside reverse-transcriptase inhibitor for the prevention and treatment of human immunodeficiency virus (HIV) infection. The investigation was considered to formulate a floating tablet of EMT with various agents. The formulation included with various concentrations of hydroxypropyl methylcellulose (HPMC) k4m, ethylcellulose, microcrystalline cellulose, polyvinylpyrrolidone (PVP) by wet granulation method. Various parameters for the prepared formulations were evaluated for weight variation, thickness, hardness, friability, floating lag time (FLT), total floating time (TFT), swelling index, in vitro drug release, and fourier-transform infrared spectroscopy (FTIR) studies. Results: The best formulation F1 exhibited 88.28% release in 24 h duration, with a floating lag time of 7 min and swelling index of 52.1% and drug content was determined to be 98.27%. The release mechanism was determined to be first order with higuchi release kinetics displaying diffusion along with the dissolution of the EMT from the tablet by non fickian mechanism. Conclusion: EMT tablets showed an increased GRT with a sustained release for 24 h thereby allowing a better window for absorption consequently improve the therapeutic effect of the drug.