Stability Studies of the Optimized Oral Controlled Release Verapamil Hydrochloride Tablet Formulations (original) (raw)
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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.
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...
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.
AAPS PharmSciTech, 2009
The release of verapamil hydrochloride from tablets with Eudragit RLPO or Kollidon ® SR with different drug-to-polymer ratios were investigated with a view to develop twice-daily sustainedrelease dosage form by solid dispersion (SD) technique. The SDs containing Eudragit RLPO or Kollidon®SR at drug-polymer ratios of 1:1, 1:2, and 1:3 with verapamil hydrochloride were developed using solvent evaporation technique. The physical mixtures of drug and both polymers were prepared by using simple mixing technique at the same ratio as solid dispersion. The physicochemical properties of solid dispersion were evaluated by using Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). The study of DSC, XRD, and FTIR could not show significant interaction between verapamil HCl and Kollidon ® SR or Eudragit RLPO. The solid dispersions or physical mixtures were compressed to tablets. The tablets were prepared with solid dispersions containing Eudragit RLPO or Kollidon ® SR, with all the official requirements of tablet dosage forms fulfilled. Tablets prepared were evaluated for the release of verapamil hydrochloride over a period of 12 h in pH 6.8 phosphate buffer using US Pharmacopoeia type II dissolution apparatus. The in vitro drug release study revealed that the tablet containing Eudragit has extended the release rate for 12 h whereas the tablet containing Kollidon ® SR at the same concentration has extended the release rate up to 8 h. The in vitro release profile and the mathematical models indicate that release of verapamil hydrochloride can be effectively controlled from a tablet containing solid dispersions of Eudragit RLPO. The reduction of size fraction of the SD system from 200-250 to 75-125 μm had a great effect on the drug release.
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.
Comparative release profile of sustained release matrix tablets of verapamil HCl
International Journal of Pharmaceutical Investigation, 2013
Introduction: Verapamil hydrochloride (VH) is a calcium channel blocking agent used in the treatment of hypertension, cardiac arrhythmia and angina pectoris. The short half-life and high frequency of administration of VH makes it a suitable candidate for designing sustained drug delivery system. The aim of the present investigation was to develop a sustained release matrix tablet of verapamil hydrochloride (VH) using ethyl cellulose, methyl cellulose, Eudragit RS 100, hydroxypropyl methylcellulose and carboxymethyl cellulose and to evaluate the drug release kinetics. Materials and Methods: In order to achieve the required sustained release profile, the tablets were prepared by a wet granulation method using avicel PH 101 and magnesium stearate as binder and lubricant, respectively. Results: The formulated tablets were characterized for pre-compression and post-compression parameters and they were in the acceptable limits. The drug release data obtained after an in vitro dissolution study was fitted to various release kinetic models in order to evaluate the release mechanism and kinetics. The criterion for selecting the best fit model was linearity (coefficient of correlation). Drug release mechanism was found to follow a complex mixture of diffusion, swelling and erosion. Furthermore, to minimize the initial burst drug release, batches were coated by using Eudragit RS100 polymer. After coating the tablets, a better release profile of the formulated tablets was expected and the release rate of the drug was compared with the marketed SR tablet of VH. Conclusion: The dosage form holds the potential to control the release rate of drug and extend the duration of action of a drug.
Formulation Development of Verapamil Hydrochloride Tablet by Effervescent Method
Stamford Journal of Pharmaceutical Sciences, 2011
Fast disintegrating tablets of Verapamil Hydrochloride were designed to achieve increased absorption as well as quick onset of pharmacological action of the active ingredient with a view to enhance patient compliance by effervescent method. Different combinations and ratios of sodium bicarbonate, anhydrous citric acid, sodium starch glycolate, Micro-crystalline cellulose (MCC) and lactose were used in order to get optimum result. The prepared formulations were evaluated for hardness, friability, thickness, diameter, taste of the solution to be administered and in-vitro dispersion time. The acceptable dispersion time was achieved by using a combination of citric acid and sodium bi carbonate in the same amount along with sodium starch glycolate, micro-crystalline cellulose (MCC) & lactose. Acceptable taste of the solution to be administered was obtained with a combination of sucrose, aspartame and sodium saccharine. Key words: Effervescent method; Verapamil Hydrochloride; Dispersion t...
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.
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.
Verapamil hydrochloride (VCL) is a drug with narrow therapeutic index commonly used in the treatment of mild or moderate systemic arterial hypertension and myocardial ischemia. We have performed pharmaceutical equivalence and comparative dissolution profile studies between reference (R) and several generic (G) medications comprising immediate release coated tablets of VCL (80mg). The analyses were carried out according to the general methods and monograph provided by the Brazilian Pharmacopoeia. The generic medications G1, G2, G3 and G4 were pharmaceutical equivalents to the R, as they were approved in tests of average weight, hardness, friability, disintegration, drug content and uniformity of unit dose. The R, G1, G3 and G4 were all approved at the stage 1 of the dissolution test, while G2 was approved at stage 2. However, none of the G presented dissolution profile similar to the R (18.36 ≤ F2 ≤ 45.15), which may indirectly impair their therapeutical efficacy. Data arising from this study reinforce the necessity of more commitment from the companies producing generic medications in Brazil with the Good Manufacturing Practices and quality of such products, aiming at the promotion of health and overall wellness.