Method Preparation of sustained release tablet of Nifedipine Formulation F 1 F 2 and F 3 was prepared by wet granulation method (original) (raw)
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Asian Journal of Pharmaceutics, 2010
T he aim of the present work was to develop controlled release matrix formulation of nifedipine and investigate the effects of both hydrophilic and hydrophobic polymers on in vitro drug release. Matrix tablets were prepared by wet granulation technique using different concentration of hydroxy propyl methyl cellulose (HPMC), ethyl cellulose (EC), compressible Eudragits (RSpo and RLpo) and their combination in different ratios to examine their influence on tablet properties and drug release profile. Tablets were evaluated by measurement of hardness, friability, content uniformity, weight variation and drug release pattern. Release studies were carried out using USP type II apparatus in 900 ml of sodium phosphate buffer (pH 7.4) with 0.5% (w/v) SDS. The amount of drug released was determined at 238 nm by UV-visible spectrophotometer. In vitro dissolution studies indicated that hydrophobic polymers significantly reduced the rate of drug release compared to hydrophilic ones in 12 hrs and combination of both polymers exhibited the best release profile to sustain the drug release for prolong period of time. As a result, the tablet containing HPMC:EC in ratio of 0.75:1 showed better controlled release pattern over a period of 12 hrs. In selected formulation, the calculated regression coefficients for release models fitted best to zero-order models.
The purpose of this research work was to formulate and evaluate the sustained release tablets of tablets are prepared by direct compression method. The formulations were optimized by incorporating varying composition of Xanthan gum and guar gum as polymers, lactose as flow aid and magnesium stearate drug, which revealed that there was no physical and chemical interaction occurred. The Pre formulation parameters such as bulk density, tapped density, compressibility index and Hausner's percentage yield was evaluated for tablets. The effect of these variables on drug release also studied. The In using pH 0.1N HCl as dissolution media at 75 rpm speed and temperature of 37 sampling was done at periodic time intervals of 1,4,8,12,16,20 and 24 hours and was replaced by equal volume of dissolution media after each withdraw release at different intervals is estimated using UV method. Based on the evaluation result the formulations F kinetics and Higguchi mechanis the drug release through the matrix was fickian diffusion.
Objective: The aim of the present research is to formulate and evaluate matrix tablet of Nifedipine by using hydrophobic and hydrophilic polymer. Method: The Nifedipine matrix tablets were prepared by wet granulation method. Formulated tablets were characterized by parameters like hardness, friability, content uniformity, weight variation and in- vitro release studies. In vitro drug release studies were carried in dissolution apparatus using 900 ml of 0.1N HCL (pH 1.2 buffer) for first 2 hours and remaining 12 hours in phosphate buffer (pH 6.8) containing 1% w/v sodium lauryl sulfate as dissolution medium. The amount of drug released was determined spectrophotometrically at 235 nm. Result: The results of the present study based on the in- vitro dissolution studies showed that formulation F5 was shown drug release upto 92.53% at 14 hours was selected as the best formulation from Nifedipine formulations. All the formulated tablets were evaluated for various physical parameters such as hardness, thickness, friability weight variation and drug content was found to be within the limit. In selected formulation, the calculated regression coefficients for drug release kinetics follows the Korsemayer-peppas and drug transport mechanism follow anomalous transport and non- fickian diffusion mechanism release. Conclusion: The result of the study demonstrated that combination of both hydrophilic and hydrophobic polymers could be successfully employed for formulating sustained-release matrix tablets of nifedipine.
Novel drug delivery systems are the best choice for current scenario of Pharmaceutical and medical demands. Novel drug delivery systems (NDDS) and technologies are very effective but at the end the manufacturing cost of finished dosage form goes on top, because of new materials, time consuming process and machinery. In the current research work we were aiming to develop a new excipient from few commonly available materials by mixing together and binding with a binder. Granules of corn starch and pre-gelatinized starch or soluble starch at certain ratio with a binder, works as sustain release agent in conventional dosage form. Formulation with newly prepared material exhibit neither very slow nor very fast rates of drug release. Compressed tablets were prepared by direct compression with SRmixK and wet granulation method using different concentration of hydroxy propyl methyl cellulose (HPMC), ethyl cellulose (EC), Eudragits (RS and RL) to scrutinize their influence on tablet properties and drug release profile. In vitro drug release studies were carried out using USP type II apparatus in 900 mL of sodium phosphate buffer (pH 7.4) with 0.5% (w/v) SDS. The total quantity of drug released was determined at 238 nm thru UV-visible spectrophotometer. In vitro dissolution studies designated that hydrophobic polymers significantly reduced the rate of drug release compared to hydrophilic ones in 12 hrs., while SRmixK exhibited the best release profile to sustain the drug release for prolong period.
Formulation and Evaluation of Nifedipine Sustained Release Tablets by Using Different Polymers
Journal of Biomedical and Pharmaceutical Research, 2019
Oral drug delivery has been known for many years because the most generally utilized route of administration among all the routes that are explored for the general delivery of medication via various pharmaceutical products of different dosage forms. The reason that the oral route achieved such quality could also be partly attributed to its simple administration moreover because the ancient belief that by oral administration the drug is well absorbed because the food stuffs that area unit eaten daily. In fact the event of a pharmaceutical product for oral delivery, no matter its physical kind involves variable extents of optimization of dose kind characteristics at intervals the inherent constraints of GI physiology. The rationale for development of a extended release formulation of a drug is to enhance its therapeutic benefits, minimizing its side effects while improving the management of the diseased condition. The aim of the present investigation is to formulate and evaluate mat...
The purpose of the present investigation was to design and evaluate sustained release tablets of a poorly water soluble drug nifedipine, employing hydrophilic polymers Methocel K15M CR and Methocel K100LV CR and to select the best formulation based on pharmacokinetic studies. Direct compression method was used to prepare matrix tablets. The granules were evaluated for angle of repose, loose bulk density, tapped bulk density, compressibility index and drug content. The tablets were subjected to various tests for their physical parameters such as thickness, hardness and friability. In vitro release study was carried out for 12 hours using USP paddle type dissolution apparatus in phosphate buffer with sodium lauryl sulphate (pH 6.8). Quantitative evaluation by mathematical model indicates that formulation containing HPMC K15M CR and HPMC K100LV CR in a ratio of 1:3 showed better dissolution properties compared to other formulations. Korsmeyer's plot indicated that the drug release mechanisms from the matrix tablet followed Fickian mechanism. The study indicates that the hydrophilic matrix tablets of nifedipine prepared using Methocel K15M CR and Methocel K100LV CR can successfully be employed as twice-a-day oral controlled release dosage form in order to improve patient compliance.
Encapsulation and drug release of poorly water soluble nifedipine from bio-carriers
Journal of Non-Crystalline Solids, 2018
Controlled drug delivery is one of the most intruding field in pharmaceutical research. It is desired for most of the drugs due to safety and efficacy reasons. Another emerging field is improving the bioavailability of poorly water-soluble drugs. By encapsulating such drugs into biodegradable polysaccharide materials both, improved bioavailability and controlled drug release is readily expected. Nifedipine, used as a model drug, was encapsulated within polysaccharide gels by the novel ethanol induced gelation method. Wet materials were processed by supercritical technology to retain its form and structure. Swelling and in-vitro dissolution tests were performed to investigate the swelling of aerogels and release behavior of nifedipine within body fluids. It was observed that guar and xanthan are not the best candidates for oral delivery of nifedipine, since the release was prolonged to 14 days. Oppositely, pectin and alginate are both suitable for nifedipine encapsulation as they released 100% of nifedipine within the first 5 h. Higher drug loading was achieved by pectin aerogels most likely due to their higher surface area.
Journal of Applied Polymer Science, 2010
Naturally available carbohydrate polymers such as methylcellulose (MC) and gelatin (Ge) have been widely studied in the previous literature for controlled release (CR) applications. In this study, methyl cellulose-g-acrylamide/gelatin (MC-g-AAm/Ge) microspheres were prepared by water-in-oil (W/O) emulsion method and crosslinked with glutaraldehyde to encapsulate with nifedipine (NFD), an antihypertensive drug. The microspheres prepared were characterized by differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and laser particle size analyzer. DSC thermograms of NFD-loaded AAm-MC/Gel microspheres confirmed the molecular level distribution of NFD in the matrix. SEM indicated the formation of spherical particles.
International Journal of Pharmaceutics, 2000
The aim of the present study was to investigate the effect of hydroxypropylmethylcellulose (HPMC-2208), used as an excipient for controlled release of drug, on the release profiles and bioavailability of the poorly water-soluble nifedipine (NP) from a tablet prepared using macrogol 6000 (PEG) and HPMC. The crushing tolerance of the NP tablet prepared using PEG and HPMC (NP-PEG-HPMC tablet) was markedly increased with increasing compression force used during the preparation from 20 to 200 MPa. The values reached their maximal levels (approximately 13 kg for the NP-PEG-HPMC tablet and 8 kg for the PEG tablet) at the compression force of 100 MPa. Although NP is a poorly water-soluble drug, it was rapidly dissolved from the NP-PEG tablet (without HPMC) due to the improvement of its dissolution rate in the presence of PEG. NP dissolution was complete at the latest within 1 h. On the other hand, dissolution of NP from the NP-PEG-HPMC tablet was significantly delayed with an increase in the concentration of HPMC in the tablet. The dissolution of NP from the NP-PEG-HPMC tablet containing 50% HPMC-2208 was markedly delayed as the viscosity of HPMC also increased. Interestingly, the same peak plasma NP concentration (C max) and the area under the plasma NP concentration-time curve (AUC 0-10) were observed for both the NP-PEG tablet and NP-PEG-HPMC tablets, however, the time to C max (t max) for the NP-PEG-HPMC tablet was significantly higher when the NP-PEG-HPMC tablet was orally administered to rabbits. We describe here a preparation method of a new sustained-release NP-PEG-HPMC tablet using a mixture of NP-PEG granules (prepared with PEG) and HPMC.
Journal of Pharmacy and Pharmacology, 1993
To modify the release rate of nifedipine, a potent calcium channel antagonist, a double-layer tablet was designed, anticipating a more balanced oral bioavailability and a prolonged efficacy than the simple plain tablet. Amorphous nifedipine powders prepared by spray-drying with 2-hydroxypropyl-β-cyclodextrin (HP-β-CyD) and nonionic surfactant HCO-60 were employed as a fast-release portion to attain an initial rapid dissolution of nifedipine. Hydroxypropylcelluloses (HPCs) with different viscosity grades (type L, M, and H) were used for a slow-release portion to provide an appropriate sustained-release. Taking into account the physiological conditions of the gastrointestinal tract (pH and motility), an optimal formulation of the double-layer tablet was obtained by changing the mixing ratios of each component. For example, the tablet consisting of HP-β-CyD with 3% HCO-60/(HPC-L:HPC-M) in the weight ratio 1/2(1:1) provided a sufficient slow release of the drug over a wide pH region fol...