scholarly journals Development of Mebeverine HCl Prolonged release Mini-tablets by thermoplastic granulation technique

Author(s):  
KETAN B. RAMANI ◽  
Vipul Patel

Mebeverine HCl is a BCS class-I drug and thus it possesses high solubility in aqueous media across the biological pH range. The marketed reference product is a multi-unit particulate system (MUPS) containing prolonged release pellets filled in hard gelatin capsule. In conventional manufacturing process, a huge quantity of solvents (aqueous and/or organic) is used to manufacture such dosage form. Additionally, it demands more processing time and efforts. Therefore, a prolonged release capsules dosage form of Mebeverine HCl was formulated using thermoplastic (melt) granulation technique without usage of any solvent. Prolonged release minitablets sized 2 mm in diameter were developed as per quality by design principles. A 23 full-factorial design of experiment was applied to optimize levels of drug release controlling ingredients which includes a hydrophobic meltable binder (hydrogenated castor oil) cum matrixing agent, a hydrophilic meltable binder (polyethylene glycol) which may act as pore former also, and a release controlling polymer (ethyl cellulose). The optimized formulation was found stable. Dissolution profiles of the optimized formulation were found similar to the marketed reference product in different media across the physiological pH range. In conclusion, the explored solvent less process was capable to manufacture the MUPS dosage form of Mebeverine HCl prolonged-release capsules, which is stable and pharmaceutically equivalent with the reference product. The developed process is more beneficial to small and medium scale industry, as it does not require any special and costly equipment, significantly decreases manufacturing cost and increases productivity compared to conventional process, which is mentioned in literature.

2015 ◽  
Vol 89 (1) ◽  
pp. 128-136
Author(s):  
Rareș Iuliu Iovanov ◽  
Ioan Tomuță ◽  
Sorin Emilian Leucuța

Background and aims. Felodipine is a dihydropyridine calcium antagonist that presents good characteristics to be formulated as prolonged release preparations. The aim of the study was the formulation and in vitro characterization of a reservoir type prolonged release system with felodipine, over a 12 hours period using the Simplex method.Methods. The first step of the Simplex method was to study the influence of the granules coating method on the felodipine release. Furthermore the influence of the coating polymer type, the percent of the coating polymer and the percent of pore forming agent in the coating on the felodipine release were studied. Afterwards these two steps of the experimental design the percent of Surelease applied on the felodipine loaded granules and the percent of pore former in the polymeric coating formulation variables were studied. The in vitro dissolution of model drug was performed in phosphate buffer solution (pH 6.5) with 1% sodium lauryl sulfate. The released drug quantification was done using an HPLC method. The release kinetics of felodipine from the final granules was assessed using different mathematical models.Results. A 12 hours release was achieved using granules with the size between 315 – 500 µm coated with 45% Surelease with different pore former ratios in the coating via the top-spray method.Conclusion. We have prepared prolonged release coated granules with felodipine using a fluid bed system based on the Simplex method. The API from the studied final formulations was released over a 12 hours period and the release kinetics of the model drug substance from the optimized preparations fitted best the Higuchi and Peppas kinetic models. 


2010 ◽  
Vol 64 ◽  
pp. 7-12
Author(s):  
Marju Mannila ◽  
Antti Häkkinen

The object of the research was to compare the corrosion resistance of three types of multioxide technical ceramics in hydrofluoric acid containing aqueous media according to a full factorial experimental plan with pH and fluoride ion concentration as variables. The samples were a silicon carbide doped aluminum silicate material, and two membrane coated aluminum silicates with one containing a membrane on both sides of the ceramic plate. The substrates contained more additives on alumina, while the membrane coats were of higher grade aluminum oxide. The samples were shaken in containers for up to two weeks, and their remaining hardness and weight losses were measured. Daily samples drawn from the liquid phase were analyzed for dissolved components. With respect to all measured properties, fluoride concentration affected the materials more detrimentally than alterations in pH.


2009 ◽  
Vol 63 (6) ◽  
Author(s):  
Chirleanny Mendes ◽  
Marília Brito ◽  
Tatiana Porto ◽  
Ana Porto ◽  
Ranilson Bezerra ◽  
...  

AbstractIntestine proteases of Nile tilapia (Oreochromis niloticus) were partially purified by heat treatment (purification factor of 3.5, enzyme activity remained almost constant) to reach the maximum activity and stability within an alkaline pH range of 7.2–11.0. The optimum temperature and stability over a 120 min period were found to be at 55°C and at 35–45°C, respectively. The proteases’ activity was not affected by a 1 vol. % saponin surfactant, inactivated by 0.01 g mL−1 sodium dodecylsulphate after 120 min, and it remained stable for 30 min in a 5 vol. % and 10 vol. % hydrogen peroxide solutions. The proteases were slightly activated by Ca2+, Mg2+, and K+ and the substrate most effectively hydrolysed was casein (40.0 U mg−1). A 24 full factorial design used to evaluated the influence of independent variables showed that the enzyme extract, detergent concentration and the incubation time had a significant influence on the enzymatic activity. The best conditions to be used concerning detergent additive were found with 0.3 mg mL−1 of protein and 3.0 mg mL−1 of detergent for 30 min in the presence of Astrus® detergent.


2004 ◽  
Vol 69 (8-9) ◽  
pp. 683-688 ◽  
Author(s):  
Jurij Vucina ◽  
Dagoljub Lukic ◽  
Milovan Stoiljkovic

The conditions for the efficient separation of tungsten(VI) and rhenium (VII) on alumina were established. The distribution coefficients K d for tungstate and perrhenate anions, as well as the separation factors ?(? = KdWO42-/Kd ReO4-) were determined using hydrochloric or nitric acid as the aqueous media. Asolution of sodium chloride in the pH range 2?6 was also examined. Under all the tested experimental conditions, alumina is a much better adsorbent for tungsten than for rhenium. The obtained results indicated that the best separation of these two elements is achieved when 0.01? 0.1 mol dm-3HCl or 1.0mol dm-3 HNO3 are used as the aqueous media. If NaCl is used as the aqueous phase, the best separation is achieved with 0.20 mol dm-3 NaCl pH 4?6. Under these experimental conditions, the breakthrough and saturation capacities of alumina for tungsten at pH4 are 17 and 26 mg W/g Al2O3 respectively. With increasing pH, these values decrease. Thus, at pH 6 they are only 4 and 13 mg W/g Al2O3, respectively.


2020 ◽  
Author(s):  
Anderson Fiamingo ◽  
Sergio Paulo Campana Filho ◽  
Osvaldo Novais Oliveira Junior

<p>The preparation of chitosans soluble in physiological conditions has been sought for years, but so far solubility in non-acidic aqueous media has only been achieved at the expense of lowering chitosan molecular weight. In this work, we applied the multistep ultrasound-assisted deacetylation process (USAD process) to β-chitin and obtained extensively deacetylated chitosans with high molecular weights (Mw ≥ 1,000,000 g mol<sup>-1</sup>). The homogeneous <i>N</i>-acetylation of a chitosan sample resulting from three consecutive USAD procedures allowed us to produce chitosans with a high weight average degree of polymerization (DPw ≈ 6,000) and tunable degrees of acetylation (DA from 5 to 80%). <i>N</i>-acetylation was carried out under mild conditions to minimize depolymerization, while preserving a predominantly random distribution of 2-amino-2-deoxy-D-glucopyanose (<i>GlcN</i>) and 2-acetamido-2-deoxy-D-glucopyanose (<i>GlcNAc</i>) units. This close to random distribution, inferred with deconvolution of nuclear magnetic resonance (<sup>1</sup>H NMR) spectra, is considered as responsible for the solubility within a wide pH range. Two of the highly <i>N</i>-acetylated chitosans (DA ≈ 60 % and ≈ 70 %) exhibited full water solubility even at neutral pH, which can expand the biomedical applications of chitosans. </p>


2020 ◽  
Vol 63 (9) ◽  
pp. 83-89
Author(s):  
Larisa N. Maskaeva ◽  
◽  
Anastasia V. Beltseva ◽  
Andrew V. Pozdin ◽  
Vyatcheslav F. Markov ◽  
...  

Analysis of the literature showed that narrow-gap lead sulfide PbS (0.4 eV at 300 K), due to its unique properties, has found wide application in such devices as photodetectors with a wide (from infrared to ultraviolet) radiation range, solar energy converters, chemical sensors, temperature sensors, flame detectors, etc. Doping of lead sulfide with various metal ions can affect the bandgap, and hence expand the scope of its application. Of particular interest is the preparation of thin film solid solutions in the PbS – FeS system, which can lead to the appearance of ferromagnetism in lead sulfide. To obtain doped films of lead sulfide and solid solutions based on it, the method of chemical deposition from aqueous media is considered promising, which, in addition to its cost-effectiveness and simplicity of the process, allows one to determine in advance the areas of formation of the semiconducting metal chalcogenides of interest. The analysis of ionic equilibria in the systems "PbAc2 – FeCl2 – Na3Cit – NH4OH – N2H4CS", "PbAc2 – FeCl2 – NaAc – NH4OH – N2H4CS "and " PbAc2 – FeCl2 – Na2С2О4 – NH4OH – N2H4CS "made it possible to reveal predominantly forms of metals in a given pH range. To assess the conditions for the deposition of the main and impurity phases by thermodynamic calculations taking into account the sizes of critical nuclei, the boundary conditions and regions of the formation of FeS, PbS, Fe(OH)2, Pb(OH)2 in the reaction systems under study were found. It is shown that the most promising for the preparation of the three-component PbFeS compound, which does not contain impurity phases of lead and iron hydroxides, is the reaction system "PbAc2 – FeCl2 – Na3Cit – NH4OH – N2H4CS". The possibility of obtaining PbS: Fe films with a uniform iron distribution of ~ 0.5 at.% and deviation from stoichiometry towards Pb deficiency (47.7 at.%) and S excess (50.7 at.%) was experimentally demonstrated.


2011 ◽  
Vol 2011 ◽  
pp. 1-8
Author(s):  
Shailesh T. Prajapati ◽  
Amit N. Patel ◽  
Chhagan N. Patel

The present investigation describes the influence of the concentration of PEG 6000 as a melt binder and ratio of HPMC K4M : PVP on Zolpidem tartrate controlled-release tablet formulations using 32 full factorial design. The ratio of HPMC K4M and PVP K30 () and the concentration of melt binder () were selected as independent variables, and drug release at 1 hr (), 4 hr (), 8 hr (), diffusion coefficient (), and release rate constant () were selected as a dependent variable. Tablets were prepared by melt granulation technique and evaluated for various evaluation parameters. It was observed that concentration of melt binder had significant effect on , , , and Binder concentration 25% w/w was found optimum. Optimized formulation () showed good similarity with theoretical profile of drug. The variable had a significant effect on dependent variables, and the variable had no significant effect on dependent variables.


2021 ◽  
Vol 10 (2) ◽  
pp. 20-26
Author(s):  
Yaduwanshi Payal ◽  
Goswami Anindya ◽  
Malviya Neelesh

The study deals with formulation optimization and evaluation of tinidazole gel by using sodium alginate as gelling agent calcium chloride, sodium citrate were used as cross linking agent. The polymeric solution of drug is in solution form before it administered to the body. But after administration when it comes in contact with acidic pH it’s converted into gel form and the drug tinidazole released from the dosage form constantly and slowly. The formulation is effective for the treatment of gastric ulcer because of Helicobacter pylori. 32 full factorial design were used for the optimization of the formulation 12 trial batches were prepared and 9 factorial design batches in which 2 factor 3 level factorial design were used for the optimization. The concentration of sodium alginate, were taken in 3 level low, medium, high and the prepared formulation were evaluated.


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