Quantitative Appearance Inspection for Film Coated Tablets.

Science.gov (United States)

Yoshino, Hiroyuki; Yamashita, Kazunari; Iwao, Yasunori; Noguchi, Shuji; Itai, Shigeru

2016-01-01

The decision criteria for the physical appearance of pharmaceutical products are subjective and qualitative means of evaluation that are based entirely on human interpretation. In this study, we have developed a comprehensive method for the quantitative analysis of the physical appearance of film coated tablets. Three different kinds of film coated tablets with considerable differences in their physical appearances were manufactured as models, and their surface roughness, contact angle, color measurements and physicochemical properties were investigated as potential characteristics for the quantitative analysis of their physical appearance. All of these characteristics were useful for the quantitative evaluation of the physical appearances of the tablets, and could potentially be used to establish decision criteria to assess the quality of tablets. In particular, the analysis of the surface roughness and film coating properties of the tablets by terahertz spectroscopy allowed for an effective evaluation of the tablets' properties. These results indicated the possibility of inspecting the appearance of tablets during the film coating process.

Pharmacokinetics of hydrocodone extended-release tablets formulated with different levels of coating to achieve abuse deterrence compared with a hydrocodone immediate-release/acetaminophen tablet in healthy subjects.

Science.gov (United States)

Darwish, Mona; Bond, Mary; Tracewell, William; Robertson, Philmore; Yang, Ronghua

2015-01-01

A hydrocodone extended-release (ER) formulation employing the CIMA(®) Abuse-Deterrence Technology platform was developed to provide resistance against rapid release of hydrocodone when tablets are comminuted or taken with alcohol. This study evaluated the pharmacokinetics of three hydrocodone ER tablet prototypes with varying levels of polymer coating to identify the prototype expected to have the greatest abuse deterrence potential based on pharmacokinetic characteristics that maintain systemic exposure to hydrocodone comparable to that of a commercially available hydrocodone immediate-release (IR) product. In this four-period crossover study, healthy subjects aged 18-45 years were randomized to receive a single intact, oral 45-mg tablet of one of three hydrocodone ER prototypes (low-, intermediate-, or high-level coating) or an intact, oral tablet of hydrocodone IR/acetaminophen (APAP) 10/325 mg every 6 h until four tablets were administered, with each of the four treatments administered once over the four study periods. Dosing periods were separated by a minimum 5-day washout. Naltrexone 50 mg was administered to block opioid receptors. Blood samples for pharmacokinetic assessments were collected predose and through 72 h postdose. Parameters assessed included maximum observed plasma hydrocodone concentration (C(max)), time to C(max) (t(max)), and area under the concentration-time curve from time 0 to infinity (AUC(0-∞)). Mean C(max) values were 49.2, 32.6, and 28.4 ng/mL for the low-, intermediate-, and high-level coating hydrocodone ER tablet prototypes, respectively, and 37.3 ng/mL for the hydrocodone IR/APAP tablet; respective median t(max) values were 5.9, 8.0, 8.0, and 1.0 h. Total systemic exposure to hydrocodone (AUC(0-∞)) was comparable between hydrocodone ER tablet prototypes (640, 600, and 578 ng·h/mL, respectively) and hydrocodone IR/APAP (581 ng·h/mL). No serious adverse events or deaths were reported. The most common adverse events included

Multispectral UV imaging for determination of the tablet coating thickness

DEFF Research Database (Denmark)

Novikova, Anna; Carstensen, Jens Michael; Zeitler, J. Axel

2017-01-01

The applicability of off-line multispectral ultraviolet (UV) imaging in combination with multivariate data analysis was investigated to determine the coating thickness and its distribution on the tablet surface during lab scale coating. The UV imaging results were compared with the weight gain...... measured for each individual tablet and the corresponding coating thickness and its distribution measured by terahertz pulsed imaging (TPI). Three different tablet formulations were investigated, two of which contained UV active tablet cores. Three coating formulations were applied: Aquacoat® ECD (a mainly...... translucent coating) and Eudragit® NE (a turbid coating containing solid particles). It was shown that UV imaging is a fast and non-destructive method to predict individual tablet weight gain as well as coating thickness. The coating thickness distribution profiles determined by UV imaging correlated...

Assessing the influence of media composition and ionic strength on drug release from commercial immediate-release and enteric-coated aspirin tablets.

Science.gov (United States)

Karkossa, Frank; Klein, Sandra

2017-10-01

The objective of this test series was to elucidate the importance of selecting the right media composition for a biopredictive in-vitro dissolution screening of enteric-coated dosage forms. Drug release from immediate-release (IR) and enteric-coated (EC) aspirin formulations was assessed in phosphate-based and bicarbonate-based media with different pH, electrolyte composition and ionic strength. Drug release from aspirin IR tablets was unaffected by media composition. In contrast, drug release from EC aspirin formulations was affected by buffer species and ionic strength. In all media, drug release increased with increasing ionic strength, but in bicarbonate-based buffers was delayed when compared with that in phosphate-based buffers. Interestingly, the cation species in the dissolution medium had also a clear impact on drug release. Drug release profiles obtained in Blank CarbSIF, a new medium simulating pH and average ionic composition of small intestinal fluid, were different from those obtained in all other buffer compositions studied. Results from this study in which the impact of various media parameters on drug release of EC aspirin formulations was systematically screened clearly show that when developing predictive dissolution tests, it is important to simulate the ionic composition of intraluminal fluids as closely as possible. © 2017 Royal Pharmaceutical Society.

Demonstration of pharmaceutical tablet coating process by injection molding technology.

Science.gov (United States)

Puri, Vibha; Brancazio, David; Harinath, Eranda; Martinez, Alexander R; Desai, Parind M; Jensen, Keith D; Chun, Jung-Hoon; Braatz, Richard D; Myerson, Allan S; Trout, Bernhardt L

2018-01-15

We demonstrate the coating of tablets using an injection molding (IM) process that has advantage of being solvent free and can provide precision coat features. The selected core tablets comprising 10% w/w griseofulvin were prepared by an integrated hot melt extrusion-injection molding (HME-IM) process. Coating trials were conducted on a vertical injection mold machine. Polyethylene glycol and polyethylene oxide based hot melt extruded coat compositions were used. Tablet coating process feasibility was successfully demonstrated using different coating mold designs (with both overlapping and non-overlapping coatings at the weld) and coat thicknesses of 150 and 300 μm. The resultant coated tablets had acceptable appearance, seal at the weld, and immediate drug release profile (with an acceptable lag time). Since IM is a continuous process, this study opens opportunities to develop HME-IM continuous processes for transforming powder to coated tablets. Copyright © 2017 Elsevier B.V. All rights reserved.

Monitoring tablet surface roughness during the film coating process

DEFF Research Database (Denmark)

Seitavuopio, Paulus; Heinämäki, Jyrki; Rantanen, Jukka

2006-01-01

The purpose of this study was to evaluate the change of surface roughness and the development of the film during the film coating process using laser profilometer roughness measurements, SEM imaging, and energy dispersive X-ray (EDX) analysis. Surface roughness and texture changes developing during...... the process of film coating tablets were studied by noncontact laser profilometry and scanning electron microscopy (SEM). An EDX analysis was used to monitor the magnesium stearate and titanium dioxide of the tablets. The tablet cores were film coated with aqueous hydroxypropyl methylcellulose, and the film...... coating was performed using an instrumented pilot-scale side-vented drum coater. The SEM images of the film-coated tablets showed that within the first 30 minutes, the surface of the tablet cores was completely covered with a thin film. The magnesium signal that was monitored by SEM-EDX disappeared after...

Bioequivalence study of a new sildenafil 100 mg orodispersible film compared to the conventional film-coated 100 mg tablet administered to healthy male volunteers

Directory of Open Access Journals (Sweden)

Radicioni M

2017-04-01

Full Text Available Milko Radicioni,1 Chiara Castiglioni,1 Andrea Giori,2 Irma Cupone,3 Valeria Frangione,4 Stefano Rovati4 1CROSS Research S.A., Phase I Unit, Arzo, Switzerland; 2IBSA Farmaceutici Italia, Lodi, Italy; 3Bouty S.p.A., Strada Padana Superiore, Cassina De’ Pecchi, Italy; 4IBSA Institut Biochimique S.A., Pambio-Noranco, Switzerland Abstract: A new orodispersible film formulation of the phosphodiesterase type 5 inhibitor, sildenafil, has been developed to examine the advantages of an orally disintegrating film formulation and provide an alternative to the current marketed products for the treatment of erectile dysfunction. The pharmacokinetics of the sildenafil 100 mg orodispersible film (IBSA was compared to that of the conventional marketed 100 mg film-coated tablet (Viagra® after single-dose administration to 53 healthy male volunteers (aged 18–51 years in a randomized, open, two-way crossover bioequivalence study. Each subject received a single oral dose of 100 mg of sildenafil as test or reference formulation administered under fasting conditions at each of the two study periods according to a randomized crossover design. There was a washout interval of ≥7 days between the two administrations of the investigational medicinal products. Blood samples for pharmacokinetic analysis were collected up to 24 h post-dosing. The primary objective was to compare the rate (peak plasma concentration; Cmax and extent (area under the curve [AUC] from administration to last observed concentration time; AUC0–t of sildenafil absorption after single-dose administration of test and reference. Secondary endpoints were observed to describe the plasma pharmacokinetic profiles of sildenafil and its metabolite N-desmethyl-sildenafil relative bioavailability and safety profile after single-dose administration. The mean sildenafil and N-desmethyl-sildenafil plasma concentration–time profiles up to 24 h after single-dose administration of sildenafil 100 mg

Influence of polymeric subcoats on the drug release properties of tablets powder-coated with pre-plasticized Eudragit L 100-55.

Science.gov (United States)

Sauer, Dorothea; Watts, Alan B; Coots, Lonique B; Zheng, Weijia C; McGinity, James W

2009-02-09

The aim of the study was to investigate the properties of sodium valproate tablets that were dry powder-coated with pre-plasticized Eudragit L 100-55. Polyethylene glycol 3350 (PEG 3350) was used as primer to facilitate initial coating powder adhesion. Solubility parameters were employed to determine the wetting properties of the PEG 3350 primer. Additional PEG 3350 within the powder coating formulation was required to enable powder adhesion to the tablet cores. The application of a subcoat of either Eudragit E PO or Eudragit RL PO facilitated adhesion of the enteric polymer to the tablet cores and reduced the amount PEG 3350 required in the coating formulation. Since reduction of the PEG 3350 content produced less water-vapor permeable films, the enteric coating level necessary to control the drug release was decreased. PEG 3350 and Methocel K4M were incorporated in both Eudragit E PO and Eudragit RL PO subcoating formulations as pore forming agents. The influence of the pore forming excipients on physicochemical properties of free powder-cast films was investigated. The miscibility of the PEG 3350 and Methocel K4M in the film coating was correlated with their ability to function as pore forming agent.

Multispectral UV Imaging for Determination of the Tablet Coating Thickness.

Science.gov (United States)

Novikova, Anna; Carstensen, Jens M; Zeitler, J Axel; Rades, Thomas; Leopold, Claudia S

2017-06-01

The applicability of off-line multispectral UV imaging in combination with multivariate data analysis was investigated to determine the coating thickness and its distribution on the tablet surface during lab-scale coating. The UV imaging results were compared with the weight gain measured for each individual tablet and the corresponding coating thickness and its distribution measured by terahertz pulsed imaging (TPI). Three different tablet formulations were investigated, 2 of which contained UV-active tablet cores. Three coating formulations were applied: Aquacoat® ECD (a mainly translucent coating) and Eudragit® NE (a turbid coating containing solid particles). It was shown that UV imaging is a fast and nondestructive method to predict individual tablet weight gain as well as coating thickness. The coating thickness distribution profiles determined by UV imaging correlated to the results of the TPI measurements. UV imaging appears to hold a significant potential as a process analytical technology tool for determination of the tablet coating thickness and its distribution resulting from its high measurement speed, high molar absorptivity, and a high scattering coefficient, in addition to relatively low costs. Copyright © 2017 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.

Tablet coating by injection molding technology - Optimization of coating formulation attributes and coating process parameters.

Science.gov (United States)

Desai, Parind M; Puri, Vibha; Brancazio, David; Halkude, Bhakti S; Hartman, Jeremy E; Wahane, Aniket V; Martinez, Alexander R; Jensen, Keith D; Harinath, Eranda; Braatz, Richard D; Chun, Jung-Hoon; Trout, Bernhardt L

2018-01-01

We developed and evaluated a solvent-free injection molding (IM) coating technology that could be suitable for continuous manufacturing via incorporation with IM tableting. Coating formulations (coating polymers and plasticizers) were prepared using hot-melt extrusion and screened via stress-strain analysis employing a universal testing machine. Selected coating formulations were studied for their melt flow characteristics. Tablets were coated using a vertical injection molding unit. Process parameters like softening temperature, injection pressure, and cooling temperature played a very important role in IM coating processing. IM coating employing polyethylene oxide (PEO) based formulations required sufficient room humidity (>30% RH) to avoid immediate cracks, whereas other formulations were insensitive to the room humidity. Tested formulations based on Eudrajit E PO and Kollicoat IR had unsuitable mechanical properties. Three coating formulations based on hydroxypropyl pea starch, PEO 1,000,000 and Opadry had favorable mechanical (35% elongation, >95×10 4 J/m 3 toughness) and melt flow (>0.4g/min) characteristics, that rendered acceptable IM coats. These three formulations increased the dissolution time by 10, 15 and 35min, respectively (75% drug release), compared to the uncoated tablets (15min). Coated tablets stored in several environmental conditions remained stable to cracking for the evaluated 8-week time period. Copyright © 2017 Elsevier B.V. All rights reserved.

Clinical Efficacy and Residue Depletion of 10% Enrofloxacin Enteric-Coated Granules in Pigs.

Science.gov (United States)

Lei, Zhixin; Liu, Qianying; Yang, Bing; Xiong, Jincheng; Li, Kun; Ahmed, Saeed; Hong, Liping; Chen, Pin; He, Qigai; Cao, Jiyue

2017-01-01

A new, more palatable formulation of 10% enrofloxacin enteric-coated granules was investigated to evaluate the pharmacokinetic effect in plasma, the residue elimination in tissues and the clinical efficacy against Actinobacillus pleuropneumonia (APP) and Mycoplasam suis (MS) in pigs. In this study, the enrofloxacin concentrations in plasma and tissues were detected using high-performance liquid chromatography with phosphate buffer (pH = 3) and acetonitrile. The pharmacokinetics and elimination of enrofloxacin enteric-coated granules were performed after oral administration at a single dose of 10 mg/kg body weight (bw) and 5 mg/kg twice per day for 5 consecutive days, respectively. The in vivo antibacterial efficacy and clinical effectiveness of enrofloxacin enteric-coated granules against APP and MS were assayed at 2.5, 5, 10 mg/kg, compared with tiamulin (8 mg/kg) based on establishment of APP and MS infection models. 56 APP strains were selected and tested for in vitro antibacterial activity of enrofloxacin enteric-coated granules. The main parameters of elimination half-life (t 1/2β ), T max , and area under the curve (AUC) were 14.99 ± 4.19, 3.99 ± 0.10, and 38.93 ± 1.52 μg h/ml, respectively, revealing that the enrofloxacin concentration remained high and with a sustainable distribution in plasma. Moreover, the analysis on the evaluation of enrofloxacin and ciprofloxacin in muscle, fat, liver and kidney showed that the recovery were more than 84% recovery in accordance with the veterinary drug residue guidelines of United States pharmacopeia, and the withdrawal periods were 4.28, 3.81, 4.84, and 3.51 days, respectively, suggesting that the withdrawal period was 5 d after oral administration of 5 mg/kg twice per day. The optimal dosage of enrofloxacin enteric-coated granules against APP and MS was 5 mg/kg, with over 90% efficacy, which was significantly different ( p enrofloxacin enteric-coated granules had significant potential for treating APP and MS

Drug Resistance and Pseudoresistance: An Unintended Consequence of Enteric Coating Aspirin

Science.gov (United States)

Grosser, Tilo; Fries, Susanne; Lawson, John A.; Kapoor, Shiv C.; Grant, Gregory R.; FitzGerald, Garret A.

2013-01-01

Background Low dose aspirin reduces the secondary incidence of myocardial infarction and stroke. Drug resistance to aspirin might result in treatment failure. Despite this concern, no clear definition of “aspirin resistance” has emerged and estimates of its incidence have varied remarkably. We aimed to determine the commonality of a mechanistically consistent, stable and specific phenotype of true pharmacological resistance to aspirin – such as might be explained by genetic causes. Methods and Results Healthy volunteers (n=400) were screened for their response to a single oral dose of 325 mg immediate release or enteric coated aspirin. Response parameters reflected the activity of aspirin's molecular target, cyclooxygenase-1. Individuals who appeared “aspirin resistant” on one occasion underwent repeat testing and if still “resistant” were exposed to low dose enteric coated aspirin (81 mg) and clopidogrel (75 mg) for one week each. Variable absorption caused a high frequency of apparent resistance to a single dose of 325 mg enteric coated aspirin (up to 49%) but not to immediate release aspirin (0%). All individuals responded to aspirin upon repeated exposure, extension of the post dosing interval or addition of aspirin to their platelets ex vivo. Conclusions Pharmacological resistance to aspirin is rare; this study failed to identify a single case of true drug resistance. Pseudoresistance, reflecting delayed and reduced drug absorption, complicates enteric coated but not immediate release aspirin administration. Clinical Trial Registration Information clinicaltrials.gov. Identifier: NCT00948987. PMID:23212718

Clinical Efficacy and Residue Depletion of 10% Enrofloxacin Enteric-Coated Granules in Pigs

Directory of Open Access Journals (Sweden)

Zhixin Lei

2017-05-01

Full Text Available A new, more palatable formulation of 10% enrofloxacin enteric-coated granules was investigated to evaluate the pharmacokinetic effect in plasma, the residue elimination in tissues and the clinical efficacy against Actinobacillus pleuropneumonia (APP and Mycoplasam suis (MS in pigs. In this study, the enrofloxacin concentrations in plasma and tissues were detected using high-performance liquid chromatography with phosphate buffer (pH = 3 and acetonitrile. The pharmacokinetics and elimination of enrofloxacin enteric-coated granules were performed after oral administration at a single dose of 10 mg/kg body weight (bw and 5 mg/kg twice per day for 5 consecutive days, respectively. The in vivo antibacterial efficacy and clinical effectiveness of enrofloxacin enteric-coated granules against APP and MS were assayed at 2.5, 5, 10 mg/kg, compared with tiamulin (8 mg/kg based on establishment of APP and MS infection models. 56 APP strains were selected and tested for in vitro antibacterial activity of enrofloxacin enteric-coated granules. The main parameters of elimination half-life (t1/2β, Tmax, and area under the curve (AUC were 14.99 ± 4.19, 3.99 ± 0.10, and 38.93 ± 1.52 μg h/ml, respectively, revealing that the enrofloxacin concentration remained high and with a sustainable distribution in plasma. Moreover, the analysis on the evaluation of enrofloxacin and ciprofloxacin in muscle, fat, liver and kidney showed that the recovery were more than 84% recovery in accordance with the veterinary drug residue guidelines of United States pharmacopeia, and the withdrawal periods were 4.28, 3.81, 4.84, and 3.51 days, respectively, suggesting that the withdrawal period was 5 d after oral administration of 5 mg/kg twice per day. The optimal dosage of enrofloxacin enteric-coated granules against APP and MS was 5 mg/kg, with over 90% efficacy, which was significantly different (p < 0.05 to the 2.5 mg/kg group, but not to the 10 mg/kg group or the positive

ESR accident dosimetry using medicine tablets coated with sugar

International Nuclear Information System (INIS)

Kai, A.; Miki, T.; Ikeya, M.

1990-01-01

Properties of radiation-induced radicals in medicine tablets were investigated using electron spin resonance (ESR). A sharp ESR signal sensitive to gamma ray irradiation was observed in the sugar coating part of the tablets. The signal has anisotropic g values of g 1 = 2.0009, g 2 = 2.0007 and g 3 = 2.0002. The signal grows linearly with dose at least up to about 20 Gy. No fading was observed at room temperature even when exposed to sunlight. The dose to artificially irradiated tablets was estimated using the signal intensity and a previously determined calibration curve. The signal in sugar coated tablets can be utilised for dose measurements. In particular, the wide distribution of sugar coated tablets allows the use of the tablets as accident dosemeters. (author)

Effect of protective coating of aspirin tablets with acrylatemethacrylate copolymers on tablet disintegration times and dissolution rates

OpenAIRE

Okor R; Eichie F; Uhumwangho M; Aka-Aha A

2007-01-01

Tablets of aspirin (a moisture degradable drug) have been film coated with two analogous Eudragit RL and RS copolymers designated here as A and B which differ only in their cation content in the ratio 2:1 (A:B). A, is therefore more hydrophilic than B. The tablets were film coated with ethanol solutions of these two polymers. Film coating with either A or B significantly reduced the moisture uptake potentials of the tablets but caused an increase in the disintegration times of the tablets and...

Development of enteric coated tablets from spray dried extract of feverfew (Tanacetum parthenium L:

Directory of Open Access Journals (Sweden)

Juliana Siqueira Chaves

2009-09-01

Full Text Available Tanacetum parthenium (feverfew is an herb that is commercialized worldwide as a therapeutic treatment for migraine. Its pharmacological effect is mainly due to the presence of the sesquiterpene lactone parthenolide as well as of flavonoids. So far, there are no studies on standardization of pre-formulations or phytomedicines containing this herb. The present study aimed at developing a pre-formulation using a standardized spray-dried extract of feverfew and further designing and standardizing enteric coated tablets. In this work, the spray-dried extract of feverfew was evaluated for its parthenolide, santin and total flavonoid content, parthenolide solubility, particle size, tapped density, hygroscopicity, angle of repose and moisture content. Tablets containing the spray-dried extract were tested for their average weight, friability, hardness, and disintegration time. The total flavonoid and parthenolide contents in the spray-dried extract were 1.31 % and 0.76% w/w, respectively. The spray-dried extract presented consistent pharmacotechnical properties and allowed its tableting by direct compression. Tablet properties were in accordance with the proposed specifications. The procedures described herein can be used to prepare and evaluate pre-formulations of feverfew with adequate properties for the development of a high-quality phytomedicine.Tanacetum parthenium (tanaceto é uma planta medicinal comercializada no mundo todo para tratamento de enxaqueca. Seu efeito farmacológico é creditado principalmente à lactona sesquiterpênica partenolídeo e flavonóides. Até o momento não existem estudos sobre a padronização de pré-formulações ou o desenvolvimento de fitoterápicos com tanaceto. Logo, o objetivo deste trabalho foi obter comprimidos de revestimento entérico a partir de extrato seco e padronizado de tanaceto. Neste trabalho, o extrato seco do tanaceto obtido pelo método de spray drying foi avaliado quanto ao teor de partenol

Correlating bilayer tablet delamination tendencies to micro-environmental thermodynamic conditions during pan coating.

Science.gov (United States)

Zacour, Brian M; Pandey, Preetanshu; Subramanian, Ganeshkumar; Gao, Julia Z; Nikfar, Faranak

2014-06-01

The objective of this study was to determine the impact that the micro-environment, as measured by PyroButton data loggers, experienced by tablets during the pan coating unit operation had on the layer adhesion of bilayer tablets in open storage conditions. A full factorial design of experiments (DOE) with three center points was conducted to study the impact of final tablet hardness, film coating spray rate and film coating exhaust temperature on the delamination tendencies of bilayer tablets. PyroButton data loggers were placed (fixed) at various locations in a pan coater and were also allowed to freely move with the tablet bed to measure the micro-environmental temperature and humidity conditions of the tablet bed. The variance in the measured micro-environment via PyroButton data loggers accounted for 75% of the variance in the delamination tendencies of bilayer tablets on storage (R(2 )= 0.75). A survival analysis suggested that tablet hardness and coating spray rate significantly impacted the delamination tendencies of the bilayer tablets under open storage conditions. The coating exhaust temperature did not show good correlation with the tablets' propensity to crack indicating that it was not representative of the coating micro-environment. Models created using data obtained from the PyroButton data loggers outperformed models created using primary DOE factors in the prediction of bilayer tablet strength, especially upon equipment or scale transfers. The coating micro-environment experienced by tablets during the pan coating unit operation significantly impacts the strength of the bilayer interface of tablets on storage.

Bioavailability of everolimus administered as a single 5 mg tablet versus five 1 mg tablets: a randomized, open-label, two-way crossover study of healthy volunteers.

Science.gov (United States)

Thudium, Karen; Gallo, Jorge; Bouillaud, Emmanuel; Sachs, Carolin; Eddy, Simantini; Cheung, Wing

2015-01-01

The mammalian target of rapamycin (mTOR) inhibitor everolimus has a well-established pharmacokinetics profile. We conducted a randomized, single-center, open-label, two-sequence, two-period crossover study of healthy volunteers to assess the relative bioavailability of everolimus administered as one 5 mg tablet or five 1 mg tablets. Subjects were randomized 1:1 to receive everolimus dosed as one 5 mg tablet or as five 1 mg tablets on day 1, followed by a washout period on days 8-14 and then the opposite formulation on day 15. Blood sampling for pharmacokinetic evaluation was performed at prespecified time points, with 17 samples taken for each treatment period. Primary variables for evaluation of relative bioavailability were area under the concentration-time curve from time zero to infinity (AUCinf) and maximum blood concentration (Cmax). Safety was assessed by reporting the incidence of adverse events (AEs). Twenty-two participants received everolimus as one 5 mg tablet followed by five 1 mg tablets (n=11) or the opposite sequence (n=11). The Cmax of five 1 mg tablets was 48% higher than that of one 5 mg tablet (geometric mean ratio, 1.48; 90% confidence interval [CI], 1.35-1.62). AUCinf was similar (geometric mean ratio, 1.08; 90% CI, 1.02-1.16), as were the extent of absorption and the distribution and elimination kinetics. AEs, all grade 1 or 2, were observed in 54.5% of subjects. Although the extent of absorption was similar, the Cmax of five 1 mg tablets was higher than that of one 5 mg tablet, suggesting these formulations lead to different peak blood concentrations and are not interchangeable at the dose tested.

Formulation and process strategies to minimize coat damage for compaction of coated pellets in a rotary tablet press: A mechanistic view.

Science.gov (United States)

Xu, Min; Heng, Paul Wan Sia; Liew, Celine Valeria

2016-02-29

Compaction of multiple-unit pellet system (MUPS) tablets has been extensively studied in the past few decades but with marginal success. This study aims to investigate the formulation and process strategies for minimizing pellet coat damage caused by compaction and elucidate the mechanism of damage sustained during the preparation of MUPS tablets in a rotary tablet press. Blends containing ethylcellulose-coated pellets and cushioning agent (spray dried aggregates of micronized lactose and mannitol), were compacted into MUPS tablets in a rotary tablet press. The effects of compaction pressure and dwell time on the physicomechanical properties of resultant MUPS tablets and extent of pellet coat damage were systematically examined. The coated pellets from various locations at the axial and radial peripheral surfaces and core of the MUPS tablets were excavated and assessed for their coat damage individually. Interestingly, for a MUPS tablet formulation which consolidates by plastic deformation, the tablet mechanical strength could be enhanced without exacerbating pellet coat damage by extending the dwell time in the compaction cycle during rotary tableting. However, the increase in compaction pressure led to faster drug release rate. The location of the coated pellets in the MUPS tablet also contributed to the extent of their coat damage, possibly due to uneven force distribution within the compact. To ensure viability of pellet coat integrity, the formation of a continuous percolating network of cushioning agent is critical and the applied compaction pressure should be less than the pellet crushing strength. Copyright © 2015 Elsevier B.V. All rights reserved.

Characterization of the coating and tablet core roughness by means of 3D optical coherence tomography.

Science.gov (United States)

Markl, Daniel; Wahl, Patrick; Pichler, Heinz; Sacher, Stephan; Khinast, Johannes G

2018-01-30

This study demonstrates the use of optical coherence tomography (OCT) to simultaneously characterize the roughness of the tablet core and coating of pharmaceutical tablets. OCT is a high resolution non-destructive and contactless imaging methodology to characterize structural properties of solid dosage forms. Besides measuring the coating thickness, it also facilitates the analysis of the tablet core and coating roughness. An automated data evaluation algorithm extracts information about coating thickness, as well as tablet core and coating roughness. Samples removed periodically from a pan coating process were investigated, on the basis of thickness and profile maps of the tablet core and coating computed from about 480,000 depth measurements (i.e., 3D data) per sample. This data enables the calculation of the root mean square deviation, the skewness and the kurtosis of the assessed profiles. Analyzing these roughness parameters revealed that, for the given coating formulation, small valleys in the tablet core are filled with coating, whereas coarse features of the tablet core are still visible on the final film-coated tablet. Moreover, the impact of the tablet core roughness on the coating thickness is analyzed by correlating the tablet core profile and the coating thickness map. The presented measurement method and processing could be in the future transferred to in-line OCT measurements, to investigate core and coating roughness during the production of film-coated tablets. Copyright © 2017. Published by Elsevier B.V.

Biomaterial-Derived Calcium Carbonate Nanoparticles for Enteric Drug Delivery

Directory of Open Access Journals (Sweden)

Diane Render

2016-01-01

Full Text Available Oral drug delivery systems provide the most convenient, noninvasive, readily acceptable alternatives to parenteral systems. In the current work, eggshell-derived calcium carbonate (CaCO3 nanoparticles were used to develop enteric drug delivery system in the form of tablets. CaCO3 nanoparticles were manufactured using top-down ball-milling method and characterized by X-ray diffractometry (XRD and transmission electron microscopy (TEM and loaded with 5-fluorouracil as a model drug. Tablets with varying CaCO3 core and binder compositions were fabricated and coated with Eudragit S100 or Eudragit L100. Suitability for enteric delivery of the tablets was tested by oral administration to rabbits and radiography. Radiograph images showed that the tablet remained in the stomach of the rabbit for up to 3 hours. Further modifications of these biomaterial-derived nanoparticles and the coatings will enable manufacturing of stable formulations for slow or controlled release of pharmaceuticals for enteric delivery.

Optimasi Formula Tablet Salut Enterik Natrium Diklofenak dengan Bahan Penyalut Kollicoat 30 D

Directory of Open Access Journals (Sweden)

Nanang Yunarto

2015-05-01

Full Text Available Diclofenac sodium is an analgetic and antiinflammation drug and commonly used by oral administration. Because of it’s side effects that can cause stomach irritation, nausea and vomiting, it’s made in the form of enteric-coated. Enteric-coated formulations developed used organic solvent having toxicity and flammability risks. The aim of this study is to develop diclofenac sodium enteric-coated tablets with a water-based coating material. Coating material used is Kollicoat 30 D which is a derivative of acrylic polymer that can dispersed in water. Optimalization of the formula is done by the weight gain 4%, 6% and 8%. The result showed that enteric coated tablets used coating material with weight gain 8% gave the best result with all parameters meet the requirements of the test, there was no change in acid medium for 2 hours and stable released active ingredient

Two Contrasting Failure Modes of Enteric Coated Beads.

Science.gov (United States)

Shi, Galen H; Dong, Xia; Lytle, Michelle; Kemp, Craig A J; Behme, Robert J; Hinds, Jeremy; Xiao, Zhicheng

2018-04-09

This study aimed to elucidate the mechanisms and kinetics of coating failure for enteric coated beads exposed to high-humidity conditions at different storage temperatures. Enteric coated beads were placed on high-humidity conditions (75 to 98% relative humidity (RH)) in the temperature range of 5 to 40°C. These stability samples of beads were tested for acid dissolution and water activity and also analyzed with SEM, X-ray CT, and DMA. Exposure of enteric coated beads to high humidity led to increased gastric release of drug which eventually failed the dissolution specification. SEM showed visible cracks on the surface of beads exposed to 5°C/high humidity and fusion of enteric beads into agglomerates at 40°C/high humidity. In a non-destructive time elapse study, X-ray CT demonstrated swelling of microcrystalline cellulose cores, crack initiation, and propagation through the API layer within days under 5°C/98% RH storage conditions and ultimately fracture through the enteric coating. DMA data showed a marked reduction in T g of the enteric coating materials after exposure to humidity. At 5°C/high humidity, the hygroscopic microcrystalline cellulose core absorbed moisture leading to core swelling and consequent fracture through the brittle API and enteric layers. At 40°C (high humidity) which is above the T g of the enteric polymer, enteric coated beads coalesced into agglomerates due to melt flow of the enteric coating. We believe it is the first report on two distinct failure models of enteric coated dosage forms.

Development and evaluation of a dimensionless mechanistic pan coating model for the prediction of coated tablet appearance.

Science.gov (United States)

Niblett, Daniel; Porter, Stuart; Reynolds, Gavin; Morgan, Tomos; Greenamoyer, Jennifer; Hach, Ronald; Sido, Stephanie; Karan, Kapish; Gabbott, Ian

2017-08-07

A mathematical, mechanistic tablet film-coating model has been developed for pharmaceutical pan coating systems based on the mechanisms of atomisation, tablet bed movement and droplet drying with the main purpose of predicting tablet appearance quality. Two dimensionless quantities were used to characterise the product properties and operating parameters: the dimensionless Spray Flux (relating to area coverage of the spray droplets) and the Niblett Number (relating to the time available for drying of coating droplets). The Niblett Number is the ratio between the time a droplet needs to dry under given thermodynamic conditions and the time available for the droplet while on the surface of the tablet bed. The time available for drying on the tablet bed surface is critical for appearance quality. These two dimensionless quantities were used to select process parameters for a set of 22 coating experiments, performed over a wide range of multivariate process parameters. The dimensionless Regime Map created can be used to visualise the effect of interacting process parameters on overall tablet appearance quality and defects such as picking and logo bridging. Copyright © 2017 Elsevier B.V. All rights reserved.

Automated pharmaceutical tablet coating layer evaluation of optical coherence tomography images

International Nuclear Information System (INIS)

Markl, Daniel; Sacher, Stephan; Khinast, Johannes G; Hannesschläger, Günther; Leitner, Michael; Buchsbaum, Andreas

2015-01-01

Film coating of pharmaceutical tablets is often applied to influence the drug release behaviour. The coating characteristics such as thickness and uniformity are critical quality parameters, which need to be precisely controlled. Optical coherence tomography (OCT) shows not only high potential for off-line quality control of film-coated tablets but also for in-line monitoring of coating processes. However, an in-line quality control tool must be able to determine coating thickness measurements automatically and in real-time. This study proposes an automatic thickness evaluation algorithm for bi-convex tables, which provides about 1000 thickness measurements within 1 s. Beside the segmentation of the coating layer, optical distortions due to refraction of the beam by the air/coating interface are corrected. Moreover, during in-line monitoring the tablets might be in oblique orientation, which needs to be considered in the algorithm design. Experiments were conducted where the tablet was rotated to specified angles. Manual and automatic thickness measurements were compared for varying coating thicknesses, angles of rotations, and beam displacements (i.e. lateral displacement between successive depth scans). The automatic thickness determination algorithm provides highly accurate results up to an angle of rotation of 30°. The computation time was reduced to 0.53 s for 700 thickness measurements by introducing feasibility constraints in the algorithm. (paper)

Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics

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Sateesh Kumar Vemula

2013-01-01

Full Text Available The rationale of the present study is to formulate flurbiprofen colon targeted compression coated tablets using guar gum to improve the therapeutic efficacy by increasing drug levels in colon, and also to reduce the side effects in upper gastrointestinal tract. Direct compression method was used to prepare flurbiprofen core tablets, and they were compression coated with guar gum. Then the tablets were optimized with the support of in vitro dissolution studies, and further it was proved by pharmacokinetic studies. The optimized formulation (F4 showed almost complete drug release in the colon (99.86% within 24 h without drug loss in the initial lag period of 5 h (only 6.84% drug release was observed during this period. The pharmacokinetic estimations proved the capability of guar gum compression coated tablets to achieve colon targeting. The Cmax of colon targeted tablets was 11956.15 ng/mL at Tmax of 10 h whereas it was 15677.52 ng/mL at 3 h in case of immediate release tablets. The area under the curve for the immediate release and compression coated tablets was 40385.78 and 78214.50 ng-h/mL and the mean resident time was 3.49 and 10.78 h, respectively. In conclusion, formulation of guar gum compression coated tablets was appropriate for colon targeting of flurbiprofen.

A New Application of Lipid Nanoemulsions as Coating Agent, Providing Zero-Order Hydrophilic Drug Release from Tablets

Directory of Open Access Journals (Sweden)

Nicolas Anton

2012-01-01

Full Text Available The objective of the present investigation was to evaluate potential of nanoemulsions as a coating material for the tablets. The nanoemulsion of size less than 100 nm was prepared using a simple and low-energy spontaneous emulsification method. Conventional tablets containing theophylline as a model hydrophilic drug were prepared. The theophylline tablets were coated with the nanoemulsion using a fluid bed coater. The effect of different levels of the nanoemulsion coating on the theophylline release was evaluated. The theophylline tablets containing different levels of the nanoemulsion coating could be successfully prepared. Interestingly, the coating of tablet with the nanoemulsion resulted in zero-order release of theophylline from the tablets. The noncoated theophylline tablets release the entire drug in less than 2 minutes, whereas nanoemulsion coating delayed the release of theophylline from tablets. This investigation establishes the proof of concept for the potential of nanoemulsions as a coating material for tablets.

Repackaged sodium valproate tablets--Meeting quality and adherence to ensure seizure control.

Science.gov (United States)

Redmayne, Nichola; Robertson, Sherryl; Kockler, Jutta; Llewelyn, Victoria; Haywood, Alison; Glass, Beverley

2015-09-01

Sodium valproate, which is commonly repacked to assist with adherence to ensure seizure control, is hygroscopic and therefore sensitive to moisture. The aim of this study was thus to determine the stability implications of removing the enteric coated tablets from their original packaging and repackaging into a Dose Administration Aid (DAA) with storage under various environmental conditions. Physicochemical stability of enteric coated sodium valproate tablets repackaged into a DAA and stored at controlled room temperature, accelerated and refrigerated conditions was evaluated for 28 days. A validated high performance liquid chromatography method was used for the quantitation of the drug content. Although the chemical stability (sodium valproate between 95 and 105% of labelled content) was maintained for 28 days for all storage conditions, for those tablets stored under accelerated conditions the integrity of the enteric coat was compromised after only 8 days. Repackaging of enteric coated sodium valproate should be undertaken with caution and be informed by storage climate. This is particularly relevant for those patients living in hot, humid environments where they should be advised to store their DAA in a refrigerator. Copyright © 2015 British Epilepsy Association. Published by Elsevier Ltd. All rights reserved.

COMPARISON OF HYDROCORTISONE 10 MG TABLETS: TABLET HARDNESS OPTIMISED FOR ADULT USE HAS NEGATIVE CONSEQUENCES FOR PAEDIATRIC USE.

Science.gov (United States)

Saimbi, Sarina; Madden, Valerie; Stirling, Heather; Yahyouche, Asma; Batchelor, Hannah

2016-09-01

Children's medicines are not always readily available as an age appropriate product and manipulation of adult products is often required. Recently the commercial manufacturing process for 10 mg hydrocortisone tablets has changed and the compression force increased due to tablets fracturing on removal from the blister pack. However, this change led to parents of children requiring hydrocortisone reporting that the tablets were more difficult to manipulate.This study evaluated 10 mg hydrocortisone tablets for their suitability for manipulation in order to deliver an appropriate dose to children (2 mg dose). The physical properties of tablets with the old and new compression force were compared as well as the accuracy of obtaining the paediatric dose. The tablets compared were hydrocortisone Auden 10 mg tablets (Brand A, PL16876/002)-these are the newer, harder tablets- and hydrocortisone 10 mg tablets (Brand B, PL17507/0097). Tablet physical properties including friability (Copley FRV200) and tablet hardness (Copley TBF1000) were compared. The accuracy of split doses (halve and quarter tablets) were recorded on a Sartorius analytical balance. The accuracy of the 2 mg paediatric dosing was assessed by crushing the tablet, adding 10 mL of water and extracting 2 mL. The concentration was measured using UV analysis (Jenway Genova Plus) according to a calibration curve (wavelength=246 nm). Two devices were used to crush the tablets: a spoon onto a plate and a commercially available crushing device (Apothecary Ezy Crush Pill Crusher With Ergo Grip). As anticipated Brand A tablets were harder (51.85 ±5.1 N) compared to Brand B (30.99±4.1 N). Brand A tablets passed the friability testing with Auden tablets which are known to be harder tablets and therefore more force is required to crush these. Some of the experimental work within this project was conducted by Andrew Hackett and Kameron Paul-Thaper whilst at the University of Birmingham on work

Angular circulation speed of tablets in a vibratory tablet coating pan.

Science.gov (United States)

Kumar, Rahul; Wassgren, Carl

2013-03-01

In this work, a single tablet model and a discrete element method (DEM) computer simulation are developed to obtain the angular circulation speed of tablets in a vibratory tablet coating pan for range of vibration frequencies and amplitudes. The models identify three important dimensionless parameters that influence the speed of the tablets: the dimensionless amplitude ratio (a/R), the Froude number (aω2/g), and the tablet-wall friction coefficient, where a is the peak vibration amplitude at the drum center, ω is the vibration angular frequency, R is the drum radius, and g is the acceleration due to gravity. The models predict that the angular circulation speed of tablets increases with an increase in each of these parameters. The rate of increase in the angular circulation speed is observed to decrease for larger values of a/R. The angular circulation speed reaches an asymptote beyond a tablet-wall friction coefficient value of about 0.4. Furthermore, it is found that the Froude number should be greater than one for the tablets to start circulating. The angular circulation speed increases as Froude number increases but then does not change significantly at larger values of the Froude number. Period doubling, where the motion of the bed is repeated every two cycles, occurs at a Froude number larger than five. The single tablet model, although much simpler than the DEM model, is able to predict the maximum circulation speed (the limiting case for a large value of tablet-wall friction coefficient) as well as the transition to period doubling.

Studies on Novel Pantoprazole and Cefuroxime Axetil Tablets for Site Specific Delivery.

OpenAIRE

Putta Rajesh Kumar

2012-01-01

In this study core in coat tablets containing enteric coated Pantaprazole (PP) core and Cefuroxime axetil (CA) floating type coat formulation as single unit prepared by compression coating method. The tablets were evaluated for their various pre-compression, compression characteristics, in vitro drug release kinetics and stability studies. The analytical estimation of drugs was found to be accurate and precise. The results of rheological characteristics indicated that, the powder beds of both...

Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics

Science.gov (United States)

Bontha, Vijaya Kumar

2013-01-01

The rationale of the present study is to formulate flurbiprofen colon targeted compression coated tablets using guar gum to improve the therapeutic efficacy by increasing drug levels in colon, and also to reduce the side effects in upper gastrointestinal tract. Direct compression method was used to prepare flurbiprofen core tablets, and they were compression coated with guar gum. Then the tablets were optimized with the support of in vitro dissolution studies, and further it was proved by pharmacokinetic studies. The optimized formulation (F4) showed almost complete drug release in the colon (99.86%) within 24 h without drug loss in the initial lag period of 5 h (only 6.84% drug release was observed during this period). The pharmacokinetic estimations proved the capability of guar gum compression coated tablets to achieve colon targeting. The C max of colon targeted tablets was 11956.15 ng/mL at T max of 10 h whereas it was 15677.52 ng/mL at 3 h in case of immediate release tablets. The area under the curve for the immediate release and compression coated tablets was 40385.78 and 78214.50 ng-h/mL and the mean resident time was 3.49 and 10.78 h, respectively. In conclusion, formulation of guar gum compression coated tablets was appropriate for colon targeting of flurbiprofen. PMID:24260738

Preparation of Porous Hydroxyapatite Tablets and Porous Hydroxyapatite Coatings for Orthopaedic Use

International Nuclear Information System (INIS)

Mendez-Gonzalez, M.

2004-01-01

Porous hydroxyapatite tablets and coatings on metal substrates were obtained by the addition of polymeric additives and liofilization. Both tablets and coatings were characterized by scanning electron microscopy and x-ray diffraction. Coatings obtained by plasma spraying also exhibited interconnected porous of 100 μm while coatings obtained by laser ablation did not show any porosity. The diffraction patterns of the deposited HA were similar to that of the powder obtained by the precipitation method suggesting that no significant changes occurred during the coating procedure

Statistical evaluation of tablet coating processes: influence of pan design and solvent type

Directory of Open Access Journals (Sweden)

Valdomero Pereira de Melo Junior

2010-12-01

Full Text Available Partially and fully perforated pan coaters are among the most relevant types of equipment currently used in the process of coating tablets. The goal of this study was to assess the performance differences among these types of equipment employing a factorial design. This statistical approach allowed the simultaneous study of the process variables and verification of interactions among them. The study included partially-perforated and fully-perforated pan coaters, aqueous and organic solvents, as well as hypromellose-based immediate-release coating. The dependent variables were process time, energy consumption, mean weight of tablets and process yield. For the tests, placebo tablets with a mean weight of 250 mg were produced, divided into eight lots of two kilograms each and coated in duplicate, using both partially perforated pan and fully perforated pan coaters. The results showed a significant difference between the type of equipment used (partially and fully perforated pan coaters with regard to process time and energy consumption, whereas no significant difference was identified for mean weight of the coated tablets and process yield.Entre os tipos de equipamentos de maior relevância utilizados atualmente no processo de revestimento de comprimidos estão os de tambor parcial e totalmente perfurados. A proposta desse trabalho foi avaliar as diferenças de desempenho entre esses equipamentos empregando projeto fatorial. Essa abordagem estatística possibilitou o estudo simultâneo das variáveis do processo, permitindo verificar interações entre elas. O trabalho incluiu equipamento com tambor parcialmente perfurado e totalmente perfurado, solventes aquoso e orgânico, assim como revestimento de liberação imediata à base de hipromelose. As variáveis dependentes ou respostas foram tempo de processo, consumo de energia, peso médio e rendimento do processo. Para os ensaios, foram produzidos comprimidos de placebo de 250 mg de peso m

Development of fi lm forming formulation and technology of polymeric fi lm coating on Indotril tablets

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L. I. Kucherenko

2013-09-01

Full Text Available Introduction. In previous researches we grounded expedience of «Indotril» tablets development; formulation and technology of "Indotril" tablet cores were developed. Received tablet cores should be covered by protective polymeric film with the purpose of unpleasant taste elimination, increase of tablets expiration date. Objective. The aim of our investigation was to develop the film forming composition and technology of polymeric film coating on «Indotril» tablets in pseudo-fluidized layer. Materials and Methods. As “Indotril” tablets cores should be covered by protective polymeric film we performed research designed to select efficient film forming solution. Thus modern filming agents were studied, besides such factors were investigated: concentration of film forming suspension, increase of tablet coat in mass, air temperature under gas distribution grid. Obtained tablets were checked according to pharmacopeia methods. Results and discussion. First we studied tablet compression force influence on main parameters of «Indotril» cores tablets: on crushing strength, abrasion in pseudo-fluidized layer unit and disintegration. Then for further investigation we chose «Indotril» cores tablets with crushing strength near 70 H, abrasion - up to 0,5% and disintegration time - not more than 10 minutes. We performed research to select film forming solution for covering “Indotril” tablets in pseudo-fluidized layer unit. As filming agents we used different samples of hydroxypropyl methylcellulose (HPMC by Japan company Shin-Etsu Chemical Co and English company Colorcon. Water HPMC solutions were prepared which contained plasticizer (propylene glycol, pigment (titanium IV dioxide and dye (tartrazine. Coating process of “Indotril” tablets was performed in laboratory pseudo-fluidized layer unit with the air temperature 75ºC under gas distribution grid. Variance analysis of experimental data on quality of coat surface showed insignificance as

Structural changes of polymer-coated microgranules and excipients on tableting investigated by microtomography using synchrotron X-ray radiation.

Science.gov (United States)

Kajihara, Ryusuke; Noguchi, Shuji; Iwao, Yasunori; Suzuki, Yoshio; Terada, Yasuko; Uesugi, Kentaro; Itai, Shigeru

2015-03-15

Multiple-unit tablets consisting of polymer-coated microgranules and excipients have a number of advantageous pharmaceutical properties. Polymer-coated microgranules are known to often lose their functionality because of damage to the polymer coating caused by tableting, and the mechanism of polymer coating damage as well as the structural changes of excipients upon tableting had been investigated but without in-situ visualization and quantitative analysis. To elucidate the mechanism of coating damage, the internal structures of multiple-unit tablets were investigated by X-ray computed microtomography using synchrotron X-rays. Cross sectional images of the tablets with sub-micron spatial resolution clearly revealed that void spaces remained around the compressed excipient particles in the tablets containing an excipient composed of cellulose and lactose (Cellactose(®) 80), whereas much smaller void spaces remained in the tablets containing an excipient made of sorbitol (Parteck(®) SI 150). The relationships between the void spaces and the physical properties of the tablets such as hardness and disintegration were investigated. Damage to the polymer coating in tablets was found mainly where polymer-coated microgranules were in direct contact with each other in both types of tablets, which could be attributed to the difference in hardness of excipient particles and the core of the polymer-coated microgranules. Copyright © 2015 Elsevier B.V. All rights reserved.

Enteric-coated mycophenolate sodium.

Science.gov (United States)

Gabardi, Steven; Tran, Jennifer L; Clarkson, Michael R

2003-11-01

To review the pharmacology, pharmacokinetics, efficacy, and safety of mycophenolate sodium. Primary literature was obtained via a MEDLINE search (1966-June 2003). Abstracts were obtained from the manufacturer and included in the analysis. All studies and abstracts evaluating mycophenolate sodium in solid organ transplantation were considered for inclusion. English-language studies and abstracts were selected for inclusion, but were limited to those consisting of human subjects. Mycophenolate sodium, a mycophenolic acid prodrug, is an inhibitor of T-lymphocyte proliferation. Mycophenolic acid reduces the incidence of acute rejection in renal transplantation. Mycophenolate sodium is enteric coated and has been suggested as a potential method to reduce the gastrointestinal adverse events seen with mycophenolate mofetil. Both mycophenolate mofetil and mycophenolate sodium have been shown to be therapeutically equivalent at decreasing the incidence of allograft rejection and loss. The frequency of adverse events is similar between both compounds, with the most common events being diarrhea and leukopenia. Mycophenolate sodium is effective in preventing acute rejection in renal transplant recipients. At doses of 720 mg twice daily, the efficacy and safety profiles are similar to those of mycophenolate mofetil 1000 mg twice daily. Mycophenolate sodium has been approved in Switzerland; approval in the US is pending.

Optimization of process parameters for a quasi-continuous tablet coating system using design of experiments.

Science.gov (United States)

Cahyadi, Christine; Heng, Paul Wan Sia; Chan, Lai Wah

2011-03-01

The aim of this study was to identify and optimize the critical process parameters of the newly developed Supercell quasi-continuous coater for optimal tablet coat quality. Design of experiments, aided by multivariate analysis techniques, was used to quantify the effects of various coating process conditions and their interactions on the quality of film-coated tablets. The process parameters varied included batch size, inlet temperature, atomizing pressure, plenum pressure, spray rate and coating level. An initial screening stage was carried out using a 2(6-1(IV)) fractional factorial design. Following these preliminary experiments, optimization study was carried out using the Box-Behnken design. Main response variables measured included drug-loading efficiency, coat thickness variation, and the extent of tablet damage. Apparent optimum conditions were determined by using response surface plots. The process parameters exerted various effects on the different response variables. Hence, trade-offs between individual optima were necessary to obtain the best compromised set of conditions. The adequacy of the optimized process conditions in meeting the combined goals for all responses was indicated by the composite desirability value. By using response surface methodology and optimization, coating conditions which produced coated tablets of high drug-loading efficiency, low incidences of tablet damage and low coat thickness variation were defined. Optimal conditions were found to vary over a large spectrum when different responses were considered. Changes in processing parameters across the design space did not result in drastic changes to coat quality, thereby demonstrating robustness in the Supercell coating process. © 2010 American Association of Pharmaceutical Scientists

A novel in-line NIR spectroscopy application for the monitoring of tablet film coating in an industrial scale process.

Science.gov (United States)

Möltgen, C-V; Puchert, T; Menezes, J C; Lochmann, D; Reich, G

2012-04-15

Film coating of tablets is a multivariate pharmaceutical unit operation. In this study an innovative in-line Fourier-Transform Near-Infrared Spectroscopy (FT-NIRS) application is described which enables real-time monitoring of a full industrial scale pan coating process of heart-shaped tablets. The tablets were coated with a thin hydroxypropyl methylcellulose (HPMC) film of up to approx. 28 μm on the tablet face as determined by SEM, corresponding to a weight gain of 2.26%. For a better understanding of the aqueous coating process the NIR probe was positioned inside the rotating tablet bed. Five full scale experimental runs have been performed to evaluate the impact of process variables such as pan rotation, exhaust air temperature, spray rate and pan load and elaborate robust and selective quantitative calibration models for the real-time determination of both coating growth and tablet moisture content. Principal Component (PC) score plots allowed each coating step, namely preheating, spraying and drying to be distinguished and the dominating factors and their spectral effects to be identified (e.g. temperature, moisture, coating growth, change of tablet bed density, and core/coat interactions). The distinct separation of HPMC coating growth and tablet moisture in different PCs enabled a real-time in-line monitoring of both attributes. A PLS calibration model based on Karl Fischer reference values allowed the tablet moisture trajectory to be determined throughout the entire coating process. A 1-latent variable iPLS weight gain calibration model with calibration samples from process stages dominated by the coating growth (i.e. ≥ 30% of the theoretically applied amount of coating) was sufficiently selective and accurate to predict the progress of the thin HPMC coating layer. At-line NIR Chemical Imaging (NIR-CI) in combination with PLS Discriminant Analysis (PLSDA) verified the HPMC coating growth and physical changes at the core/coat interface during the initial

A new formulation for orally disintegrating tablets using a suspension spray-coating method.

Science.gov (United States)

Okuda, Y; Irisawa, Y; Okimoto, K; Osawa, T; Yamashita, S

2009-12-01

The aim of this study was to design a new orally disintegrating tablet (ODT) that has high tablet hardness and a fast oral disintegration rate using a new preparation method. To obtain rapid disintegration granules (RDGs), a saccharide, such as trehalose, mannitol, or lactose, was spray-coated with a suspension of corn starch using a fluidized-bed granulator (suspension method). As an additional disintegrant, crospovidone, light anhydrous silicic acid, or hydroxypropyl starch was also included in the suspension. The RDGs obtained possessed extremely large surface areas, narrow particle size distribution, and numerous micro-pores. When tabletting these RDGs, it was found that the RDGs increased tablet hardness by decreasing plastic deformation and increasing the contact frequency between granules. In all tablets, a linear relationship was observed between tablet hardness and oral disintegration time. From each linear correlation line, a slope (D/H value) and an intercept (D/H(0) value) were calculated. Tablets with small D/H and D/H(0) values could disintegrate immediately in the oral cavity regardless of the tablet hardness and were considered to be appropriate for ODTs. Therefore, these values were used as key parameters to select better ODTs. Of all the RDGs prepared in this study, mannitol spray-coated with a suspension of corn starch and crospovidone (2.5:1 w/w ratio) showed most appropriate properties for ODTs; fast in vivo oral disintegration time, and high tablet hardness. In conclusion, this simple method to prepare superior formulations for new ODTs was established by spray-coating mannitol with a suspension of appropriate disintegrants.

A gamma scintigraphic study of gastric coating by Expidet, tablet and liquid formulations

International Nuclear Information System (INIS)

Washington, N.; Wilson, C.G.; Greaves, J.L.; Norman, S.

1989-01-01

The gastric residence time and gastric coating properties of 10 mg of radiolabelled micronised resin incorporated into Expidet formulations, chewable tablets and 10 ml of a liquid formulation were measued by gamma scintigraphy in twelve fasted, healthy subjects. All preparations emptied from the stomach in a similar manner for the first 1.5 h; however, the final 10% of the activity from the Expidet formulation emptied considerably more slowly than the initial phase. The total mean gastric emptying times for the three formulations were 2.3, 2.5 and 5.5 h for the tablet, liquid and Expidet formulation, respectively. The amount of activity following administration of the table or Expidet formulation was the same in the three regions of the stomach, but the coating of the mucosa by the Expidet formulation within each area was observed to be more uniform due to the greater dispersion of the dose form. The table broke up into a number of small discrete pieces. The gastric residence time of 99m Tc-labelled resin delivered in an Expidet formulation is significantly longer than the same marker administered in a table or in 10 ml of a liquid formulation. Moreover, coating of the gastric mucosa was more uniform with the Expidet formulation than the other two formulations studied. (author) 10 refs.; 6 figs

Assessment of the pharmaceutical quality of marketed enteric coated pantoprazole sodium sesquihydrate products.

Science.gov (United States)

Mostafa, Haitham F; Ibrahim, Mohamed A; Mahrous, Gamal M; Sakr, Adel

2011-04-01

Pantoprazole sodium sesquihydrate (PSS) is a proton pump inhibitor, used in acid-related disorders, like peptic ulcer and gastroesophageal reflux. Increasing the number of pantoprazole containing products in the market, raises questions of its efficacy and generic substitution. The pharmaceutical quality of 6 generic PSS enteric coated tablets in 2 local markets was assessed relative to the innovator product (pantozol®). Uniformity of dosage unit, disintegration and in vitro drug release were determined using United States pharmacopeia for delayed release tablets. The similarity factor (f2) was assessed using the FDA recommended approach (f2 similarity factor). The content uniformity of the innovator product was 98.39% of the labeled claim with RSD value of 1.08%, while the content of generic products ranged from 96.98% to 98.80% with RSD values of 1.24-2.19%. All the products showed no disintegration, cracks or swelling in 0.1 N HCl, except product 1, which showed complete disintegration after 20 min. However, the disintegration of all the products in phosphate buffer met USP requirements. Dissolution of tablets in 0.1 N HCl showed no drug release after 2 h except product 1 in which one tablet showed a drug release more than 10% at acid stage level A1. In addition, three tablets of this product showed dissolution of 45%, 48% and 69% at acid stage level A2. The similarity factor f2 of the products was between 71 and 74 indicating the similarity in dissolution profiles of all the products in accordance to FDA requirements, except product 1 in which f2 value was 18.67.

Effect of the External Lubrication Method for a Rotary Tablet Press on the Adhesion of the Film Coating Layer.

Science.gov (United States)

Kondo, Hisami; Toyota, Hiroyasu; Kamiya, Takayuki; Yamashita, Kazunari; Hakomori, Tadashi; Imoto, Junko; Kimura, Shin-Ichiro; Iwao, Yasunori; Itai, Shigeru

2017-01-01

External lubrication is a useful method which reduces the adhesion of powder to punches and dies by spraying lubricants during the tableting process. However, no information is available on whether the tablets prepared using an external lubrication system can be applicable for a film coating process. In this study, we evaluated the adhesion force of the film coating layer to the surface of tablets prepared using an external lubrication method, compared with those prepared using internal lubrication method. We also evaluated wettability, roughness and lubricant distribution state on the tablet surface before film coating, and investigated the relationship between peeling of the film coating layer and these tablet surface properties. Increasing lubrication through the external lubrication method decreased wettability of the tablet surface. However, no change was observed in the adhesion force of the film coating layer. On the other hand, increasing lubrication through the internal lubrication method, decreased both wettability of the tablet surface and the adhesion force of the film coating layer. The magnesium stearate distribution state on the tablet surface was assessed using an X-ray fluorescent analyzer and lubricant agglomerates were observed in the case of the internal lubrication method. However, the lubricant was uniformly dispersed in the external lubrication samples. These results indicate that the distribution state of the lubricant affects the adhesion force of the film coating layer, and external lubrication maintained sufficient lubricity and adhesion force of the film coating layer with a small amount of lubricant.

Bilayer tablets of Paliperidone for Extended release osmotic drug delivery

Science.gov (United States)

Chowdary, K. Sunil; Napoleon, A. A.

2017-11-01

The purpose of this study is to develop and optimize the formulation of paliperidone bilayer tablet core and coating which should meet in vitro performance of trilayered Innovator sample Invega. Optimization of core formulations prepared by different ratio of polyox grades and optimization of coating of (i) sub-coating build-up with hydroxy ethyl cellulose (HEC) and (ii).enteric coating build-up with cellulose acetate (CA). Some important influence factors such as different core tablet compositions and different coating solution ingredients involved in the formulation procedure were investigated. The optimization of formulation and process was conducted by comparing different in vitro release behaviours of Paliperidone. In vitro dissolution studies of Innovator sample (Invega) with formulations of different release rate which ever close release pattern during the whole 24 h test is finalized.

Notes from the field: national shortage of isoniazid 300 mg tablets.

Science.gov (United States)

2012-12-21

On November 16, 2012, the Illinois State tuberculosis (TB) program notified CDC's Division of Tuberculosis Elimination of a national shortage of 300 mg tablets of the antituberculosis medication isoniazid (INH). Subsequently, other state TB programs (e.g., California, Indiana, Maryland, New York, Virginia, and Wisconsin) reported difficulty obtaining INH 300 mg tablets. Other programs (e.g., San Diego) have experienced difficulties obtaining at least one of the commercially available anti-TB preparations containing the combination of rifampin and INH (IsonaRif [VersaPharm]).

Formulation and optimization of chronomodulated press-coated tablet of carvedilol by Box–Behnken statistical design

Directory of Open Access Journals (Sweden)

Satwara RS

2012-08-01

Full Text Available Rohan S Satwara, Parul K PatelDepartment of Pharmaceutics, Babaria Institute of Pharmacy, Vadodara, Gujarat, IndiaObjective: The primary objective of the present investigation was to formulate and optimize chronomodulated press-coated tablets to deliver the antihypertensive carvedilol at an effective quantity predawn, when a blood pressure spike is typically observed in most hypertensive patients.Experimental work: Preformulation studies and drug excipient compatibility studies were carried out for carvedilol and excipients. Core tablets (6 mm containing carvedilol and 10-mm press-coated tablets were prepared by direct compression. The Box–Behnken experimental design was applied to these press-coated tablets (F1–F15 formula with differing concentrations of rate-controlling polymers. Hydroxypropyl methyl cellulose K4M, ethyl cellulose, and K-carrageenan were used as rate-controlling polymers in the outer layer. These tablets were subjected to various precompression and postcompression tests. The optimized batch was derived both by statistically (using desirability function and graphically (using Design Expert® 8; Stat-Ease Inc. Tablets formulated using the optimized formulas were then evaluated for lag time and in vitro dissolution.Results and discussion: Results of preformulation studies were satisfactory. No interaction was observed between carvedilol and excipients by ultraviolet, Fourier transform infrared spectroscopy, and dynamic light scattering analysis. The results of precompression studies and postcompression studies were within limits. The varying lag time and percent cumulative carvedilol release after 8 h was optimized to obtain a formulation that offered a release profile with 6 h lag time, followed by complete carvedilol release after 8 h. The results showed no significant bias between predicted response and actual response for the optimized formula.Conclusion: Bedtime dosing of chronomodulated press-coated tablets may offer a

Determination of drug, excipients and coating distribution in pharmaceutical tablets using NIR-CI

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Anna Palou

2012-04-01

Full Text Available The growing interest of the pharmaceutical industry in Near Infrared-Chemical Imaging (NIR-CI is a result of its high usefulness for quality control analyses of drugs throughout their production process (particularly of its non-destructive nature and expeditious data acquisition. In this work, the concentration and distribution of the major and minor components of pharmaceutical tablets are determined and the spatial distribution from the internal and external sides has been obtained. In addition, the same NIR-CI allowed the coating thickness and its surface distribution to be quantified. Images were processed to extract the target data and calibration models constructed using the Partial Least Squares (PLS algorithms. The concentrations of Active Pharmaceutical Ingredient (API and excipients obtained for uncoated cores were essentially identical to the nominal values of the pharmaceutical formulation. But the predictive ability of the calibration models applied to the coated tablets decreased as the coating thickness increased. Keywords: Near infrared Chemical Imaging (NIR-CI, Hyperspectral imaging, Component distribution, Tablet coating distribution, Partial Least Squares (PLS regression

Multiple-unit tablet of probiotic bacteria for improved storage stability, acid tolerability, and in vivo intestinal protective effect

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Park HJ

2016-04-01

Full Text Available Hee Jun Park,1 Ga Hyeon Lee,1 Joonho Jun,1 Miwon Son,1 Myung Joo Kang2 1Dong-A Pharmaceutical Co. Ltd., Yongin, Gyeonggi, 2College of Pharmacy, Dankook University, Cheonan, Chungnam, Korea Abstract: The aim of this study was to formulate probiotics-loaded pellets in a tablet form to improve storage stability, acid tolerability, and in vivo intestinal protective effect. Bacteria-loaded pellets primarily prepared with hydroxypropyl methylcellulose acetate succinate were compressed into tablets with highly compressible excipients and optimized for flow properties, hardness, and disintegration time. The optimized probiotic tablet consisted of enteric-coated pellets (335 mg, microcrystalline cellulose (Avicel PH102, 37.5 mg, and porous calcium silicate (25 mg and allowed whole survival of living bacteria during the compaction process with sufficient tablet hardness (13 kp and disintegration time (14 minutes. The multiple-unit tablet showed remarkably higher storage stability under ambient conditions (25°C/60% relative humidity over 6 months and resistance to acidic medium compared to uncoated strains or pellets. Repeated intake of this multiple-unit tablet significantly lowered plasma level of endotoxin, a pathogenic material, compared to repeated intake of bare probiotics or marketed products in rats. These results, therefore, suggest that the multiple-unit tablet is advantageous to better bacterial viability and gain the beneficial effects on the gut flora, including the improvement of intestinal barrier function. Keywords: probiotics, multiple-unit tablet, bacterial viability, acid resistance, intestinal barrier function

Study of the 50 mg Propylthiouracil tablets stability

International Nuclear Information System (INIS)

Valdes Bendoyro, Maria Olga; Garcia Penna, Caridad Margarita; Lugones Fernandez, Juan

2010-01-01

Authors developed a stability study of 50 mg Propylthiouracil tablets and determination of its expiry date. This study was conducted by fixed life methods and of accelerated stability by high-performance liquid chromatography, validated in Drugs Research and Development Center. Fixed life study was conducted during 24 months at room temperature; whereas the accelerated stability study was conducted exposing the product to light influence, humidity and temperature; during 3 months a analysis was performed for the two first ones and over 6 months in the case of temperature study. Propylthiouracil formula (50 mg tablets) fulfilled the quality specifications described in Pharmacopeia. Results of stability study by fixed life after 24 months showed that thr product maintain the parameter determining its quality during this period, and in the accelerated studies there was not a significant degradation of product. Two years was the expity date established in above mentioned conditions

Dry coating of micronized API powders for improved dissolution of directly compacted tablets with high drug loading.

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Han, Xi; Ghoroi, Chinmay; Davé, Rajesh

2013-02-14

Motivated by our recent study showing improved flow and dissolution rate of the active pharmaceutical ingredient (API) powders (20 μm) produced via simultaneous micronization and surface modification through continuous fluid energy milling (FEM) process, the performance of blends and direct compacted tablets with high drug loading is examined. Performance of 50 μm API powders dry coated without micronization is also considered for comparison. Blends of micronized, non-micronized, dry coated or uncoated API powders at 30, 60 and 70% drug loading, are examined. The results show that the blends containing dry coated API powders, even micronized ones, have excellent flowability and high bulk density compared to the blends containing uncoated API, which are required for direct compaction. As the drug loading increases, the difference between dry coated and uncoated blends is more pronounced, as seen in the proposed bulk density-FFC phase map. Dry coating led to improved tablet compactibility profiles, corresponding with the improvements in blend compressibility. The most significant advantage is in tablet dissolution where for all drug loadings, the t(80) for the tablets with dry coated APIs was well under 5 min, indicating that this approach can produce nearly instant release direct compacted tablets at high drug loadings. Copyright © 2012 Elsevier B.V. All rights reserved.

Implementation of quality by design approach in manufacturing process optimization of dry granulated, immediate release, coated tablets - a case study.

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Teżyk, Michał; Jakubowska, Emilia; Milanowski, Bartłomiej; Lulek, Janina

2017-10-01

The aim of this study was to optimize the process of tablets compression and identification of film-coating critical process parameters (CPPs) affecting critical quality attributes (CQAs) using quality by design (QbD) approach. Design of experiment (DOE) and regression methods were employed to investigate hardness, disintegration time, and thickness of uncoated tablets depending on slugging and tableting compression force (CPPs). Plackett-Burman experimental design was applied to identify critical coating process parameters among selected ones that is: drying and preheating time, atomization air pressure, spray rate, air volume, inlet air temperature, and drum pressure that may influence the hardness and disintegration time of coated tablets. As a result of the research, design space was established to facilitate an in-depth understanding of existing relationship between CPPs and CQAs of intermediate product (uncoated tablets). Screening revealed that spray rate and inlet air temperature are two most important factors that affect the hardness of coated tablets. Simultaneously, none of the tested coating factors have influence on disintegration time. The observation was confirmed by conducting film coating of pilot size batches.

Evaluating the effect of coating equipment on tablet film quality using terahertz pulsed imaging

DEFF Research Database (Denmark)

Haaser, Miriam; Naelapaa, Kaisa; Gordon, Keith C

2013-01-01

In this study, terahertz pulsed imaging (TPI) was employed to investigate the effect of the coating equipment (fluid bed and drum coater) on the structure of the applied film coating and subsequent dissolution behaviour. Six tablets from every batch coated with the same delayed release coating fo...

Development and Efficacy Assessment of an Enteric Coated Porous Tablet Loaded With F4 Fimbriae for Oral Vaccination of Piglets against F4+ Escherichia coli Infections.

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Srivastava, Atul; Gowda, D V; Madhunapantula, SubbaRao V; Siddaramaiah

2016-01-01

Enterotoxigenic Escherichia coli (ETEC) infection is one of the major causes contributing to the development of diarrhoea and mortality in new born, suckling and newly weaned piglets. To date, no preventive/treatment strategy showed promising results, which could be due to the lack of potent vaccines, and/or due to the development of resistance of ETEC to antibiotics. Therefore, in the present investigation, a novel porous sodium alginate (SA) tablet formulation loaded with F4 fimbriae antigen was developed and tested for efficacy against ETEC infections in piglet models. Precompression parameters of the powder mixes and post compression parameters of tablets have been evaluated and results were found to be satisfactory. Loading of F4 fimbrial antigens into the tablets was achieved by inducing pores in the tablets via the sublimation of camphor followed by incubation with purified F4 fimbriae. The loaded tablets have been coated with Eudragit L100 to protect the F4 fimbriae from (a) highly acidic gastric environment; (b) proteolytic cleavage by pepsin; and (c) to promote subsequent release in the intestine. Evaluation of developed F4 fimbrial tablets in a Pig model demonstrated induction of mucosal immunity, and a significant reduction of F4+ E. coli in faeces. Therefore, F4 fimbriae loaded porous tablets could be a novel oral vaccination candidate to induce mucosal and systemic immunity against ETEC infections.

A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets.

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Vemula, Sateesh Kumar

2015-12-01

A significant plan is executed in the present study to study the effect of double-compression coating on flurbiprofen core mini-tablets to achieve the pulsatile colonic delivery to deliver the drug at a specific time as per the patho-physiological need of the disease that results in improved therapeutic efficacy. In this study, pulsatile double-compression-coated tablets were prepared based on time-controlled hydroxypropyl methylcellulose K100M inner compression coat and pH-sensitive Eudragit S100 outer compression coat. Then, the tablets were evaluated for both physical evaluation and drug-release studies, and to prove these results, in vivo pharmacokinetic studies in human volunteers were conducted. From the in vitro drug-release studies, F6 tablets were considered as the best formulation, which retarded the drug release in the stomach and small intestine (3.42 ± 0.12% in 5 h) and progressively released to the colon (99.78 ± 0.74% in 24 h). The release process followed zero-order release kinetics, and from the stability studies, similarity factor between dissolution data before and after storage was found to be 88.86. From the pharmacokinetic evaluation, core mini-tablets producing peak plasma concentration (C max) was 14,677.51 ± 12.16 ng/ml at 3 h T max and pulsatile colonic tablets showed C max = 12,374.67 ± 16.72 ng/ml at 12 h T max. The area under the curve for the mini and pulsatile tablets was 41,238.52 and 72,369.24 ng-h/ml, and the mean resident time was 3.43 and 10.61 h, respectively. In conclusion, development of double-compression-coated tablets is a promising way to achieve the pulsatile colonic release of flurbiprofen.

An Evaluation of Theraphy with Fluconazole 150 mg Tablets Compared to Fluconazole 150 mg Tablets Plus Dermoxen Lenitiva Cream in The Time to Reduce Simptomatology in Women with Vulvovaginal Candidiasis

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Davide Carati

2014-06-01

Full Text Available Aim of the study. Authors investigated first of all the time to onset of first relief of symptoms. Secondary measures included the time to overall relief of symptoms and the reoccurrence rate over the first 45 days after the first visit. Methods. A randomized, open-label, parallel study evaluated 47 women with moderate to severe symptoms of Vulvo Vaginal Candidiasis (VVC. Patients were divided into two groups of treatment: group 1 followed a therapy with Fluconazole 150 mg tablets, while group 2 had a therapy based on Fluconazole 150 mg tablets coadjuvated by Dermoxen Lenitiva cream. Results. The time at which 50% of patients experienced first relief of symptoms was 24.6 hours for Group 1, while for Group 2 it was 12.4 hours (P<0.05. There were significant differences between the two groups in respect to the time of first relief of symptoms and reoccurrence of infection within 45 days of treatment. Conclusions. Combined treatment with Fluconazole 150 mg tablets and by Dermoxen Lenitiva cream provides statistically significant improvement in the time of first relief of symptoms, complete relief of symptoms and relapse time in the treatment of VVC compared to fluconazole 150 mg tablets only.

Pharmacokinetic comparison using two tablets of an evogliptin/metformin XR 2.5/500 mg fixed dose combination vs. 1 tablet each of evogliptin 5 mg and metformin XR 1,000 mg
.

Science.gov (United States)

Yoon, Sumin; Rhee, Su-Jin; Park, Sang-In; Yoon, Seo Hyun; Cho, Joo-Youn; Jang, In-Jin; Lee, SeungHwan; Yu, Kyung-Sang

2017-06-01

The aim of this study was to compare the pharmacokinetic (PK) characteristics of evogliptin and metformin following the administration of 2 evogliptin/metformin extended-release (XR) 2.5/500 mg FDC tablets with the coadministration of separate evogliptin 5-mg and metformin XR 1,000-mg tablets (separate formulations). A randomized, two-period, two-sequence crossover study was conducted. Subjects were randomly assigned to receive 2 FDC tablets or the individual tablets, followed by a 14-day washout period and the administration of the alternate treatment. Blood samples were collected predose and up to 72 hours postdose for each period. PK parameters including Cmax and AUClast were calculated. The geometric mean ratios (GMRs) and the 90% confidence intervals (CIs) between FDC and the separate formulations were calculated for the Cmax and AUClast of evogliptin and metformin. 33 subjects completed the study. The GMR (90% CI) values of Cmax and AUClast for evogliptin were 1.011 (0.959 - 1.066) and 1.010 (0.977 - 1.043), respectively. The GMR (90% CI) values of Cmax and AUClast for metformin were 0.892 (0.827 - 0.963) and 0.893 (0.841 - 0.947), respectively. There was no significant difference between the FDC and separate formulations regarding the occurrence of adverse events. All drug-related adverse events were considered to be mild and resolved without any treatment. Two FDC tablets of evogliptin/metformin XR 2.5/500 mg showed a similar PK profile to the separate formulations of evogliptin 5 mg and metformin XR 1,000 mg. All of the 90% CIs of GMR satisfied the regulatory bioequivalence criteria of 0.800 - 1.250.
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New insights on poly(vinyl acetate)-based coated floating tablets: characterisation of hydration and CO2 generation by benchtop MRI and its relation to drug release and floating strength.

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Strübing, Sandra; Abboud, Tâmara; Contri, Renata Vidor; Metz, Hendrik; Mäder, Karsten

2008-06-01

The purpose of this study was to investigate the mechanism of floating and drug release behaviour of poly(vinyl acetate)-based floating tablets with membrane controlled drug delivery. Propranolol HCl containing tablets with Kollidon SR as an excipient for direct compression and different Kollicoat SR 30 D/Kollicoat IR coats varying from 10 to 20mg polymer/cm2 were investigated regarding drug release in 0.1N HCl. Furthermore, the onset of floating, the floating duration and the floating strength of the device were determined. In addition, benchtop MRI studies of selected samples were performed. Coated tablets with 10mg polymer/cm2 SR/IR, 8.5:1.5 coat exhibited the shortest lag times prior to drug release and floating onset, the fastest increase in and highest maximum values of floating strength. The drug release was delayed efficiently within a time interval of 24 h by showing linear drug release characteristics. Poly(vinyl acetate) proved to be an appropriate excipient to ensure safe and reliable drug release. Floating strength measurements offered the possibility to quantify the floating ability of the developed systems and thus to compare different formulations more efficiently. Benchtop MRI studies allowed a deeper insight into drug release and floating mechanisms noninvasively and continuously.

Guargum and Eudragit ® coated curcumin liquid solid tablets for colon specific drug delivery.

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S Kumar, Vrinda; Rijo, John; M, Sabitha

2018-04-15

Colorectal cancer, also known as bowel cancer, is the uncontrolled cell growth in the colon or rectum (parts of the large intestine), or in the appendix. The colon specific drug delivery would alleviate the systemic side effects and would assure the safe therapy for colonic disorders with minimum dose and duration of therapy. The liquisolid technique refers to solubilisation of drug in a non-volatile solvent combined with inclusion of appropriate carrier and coating agent required for tableting. Colon specific degradation of natural polymer, guar gum and pH dependant degradative (pH-7) property of eudragit L100 restricts the delivery of curcumin in gastric and intestinal pH. Formulated curcumin liquisolid powder was evaluated for the micrometric properties, solubility and by differential thermal analysis, X ray powder diffraction and scanning electron microscopy. Curcumin loaded liquisolid tablet showed more anticancer activity against HCT-15 compared with free curcumin. Bioavailability study of the coated and uncoated liquisolid tablets were performed using Newzealand white rabbits. The present study concludes that liquisolid technique is a promising alternative for improving oral bioavailability and dissolution rate of water insoluble drug and coating liquisolid tablet with colon sensitive polymers showed site specific release of drug in the colon. Copyright © 2018 Elsevier B.V. All rights reserved.

Pharmaceutical equivalence of gabapentin tablets with various extragranular binders Pharmaceutical equivalence of gabapentin tablets with various extragranular binders

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SWATI C. JAGDALE

2010-06-01

Full Text Available Gabapentin is a high-dose drug widely used as an oral anti-epilepticagent. Due to high crystalline and has poor compaction properties it is difficult to form tablets by direct compression. The aim of this study was to develop gabapentin tablets, pharmaceutically equivalent to the reference product Neurontin (marketed in USA. Gabapentin 800mg tablets were produced by wet granulation by keeping intragranular binder as well as its concentration constant and by changing with various extragranular binders with its concentration (A = PVPK 30, B = HPMC 15 cps, C = Kollidon VA 64, D =Klucel EXF.The tablet having no weight, thickness and hardness variation and having appropriate, friability as well as disintegration profile were coated with a 3% film coating solution .Seven formulations F1 (A in lower concentration F2 (A in higher concentration, F3 (B in lower concentration and F4 (B in higher concentration, F5 (C in lower concentration, F6 (C in higher concentration, F7 (D in lower concentration were formulated. Among them F6 demonstrated adequate hardness, friability, disintegration, uniformity of content, and total drug dissolution after 45minutes. The dissimilarity factor (f1 is 5.93 and the similarity factor (f2 is 67.85. So F6 was found to be equivalent to Neurontin.Gabapentin is widely used as an oral anti-epileptic agent. However, owing to its high crystallinity and poor compaction properties, it is difficult to form tablets of this drug by direct compression. The aim of this study was to develop gabapentin tablets, pharmaceutically equivalent to the brand-name pioneer product Neurontin® (marketed in USA. Gabapentin 800mg tablets were produced by wet granulation with a constant concentration of intragranular binder and a varying concentration of extragranular binders (A = polyvinylpyrrolidone K30, B = hydroxypropylmethylcellulose 15 cps, C = Kollidon VA64, D =Klucel EXF. The tablets that did not vary in weight, thickness or hardness and had

Stability of a formulation of zidovudine 300 mg tablets

International Nuclear Information System (INIS)

Ibannez Calvo, Sergio; Garcia Penna, Caridad Margarita; Leon Rodriguez, Rafael

2010-01-01

Authors developed a validation of analytical method by high-performance liquid applicable to stability study of Zidovudine (300 mg tablets). The validated analytical method was linear, specific and exact. Above mentioned study was developed determing its expiry date. This study was conducted by fixed life and of accelerated stability methods by high-performance liquid chromatography, validated in Drugs Research and Development Center (Havana, Cuba). Fixed life study was conducted during 24 months at room temperature whereas the accelerated stability study was conducted exposing the product to light influence and humidity during three months and to temperature during 6 months. Zidovudine formula (300 mg tablets) fulfilled the quality specifications described in Pharmacopeia. After 24 months results of stability study by fixed life showed that product maintained the parameters determining its quality during that period and in accelerated studies there was not a significant degradation of product. Two years was established as expiry date in above mentioned conditions

Development and Evaluation of a Novel Pellet-Based Tablet System for Potential Colon Delivery of Budesonide

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Jaleh Varshosaz

2012-01-01

Full Text Available Budesonide, a potent glucocorticoid, is used for the treatment of inflammatory bowel diseases. Current available oral formulations of budesonide have low efficacy against ulcerative colitis because of the premature drug release in the upper part of the gastrointestinal tract. In this paper a pH- and time-controlled colon-targeted pellet-based tablet of budesonide was established. Pellet cores were prepared by extrusion-spheronization method and further coated with xanthan gum (barrier layer, Eudragit NE30D and L30D55 combination (inner layer, and Eudragit FS30 (as enteric layer sequentially to achieve the required release profile. The coated pellets then compressed into tablets using inert tabletting granules of Cellactose or Pearlitol. Release studies, performed in simulated gastric, intestinal, and colon pH were used in sequence to mimic the gastrointestinal transit. The influence of formulation variables like barrier layer thickness, inner layer composition, and enteric coat thickness on drug release were investigated and the coated pellets that contained 12% weight gain in xanthan gum layer, Eudragit L30D55 and Eudragit NE30D with a ratio of 3 : 7 in inner layer with 30% weight gain and 25% weight gain in Eudragit FS layer were found to protect the drug release in stomach and small intestine and 83.35 ± 2.4 of budesonide was released at 24 h. The drug release from the tablets prepared using 40% Cellactose 80 as tableting excipient was found to be closely similar to that of uncompressed pellets.

Formulation and in vitro and in vivo evaluation of film-coated montelukast sodium tablets using Opadry® yellow 20A82938 on an industrial scale

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Zaid AN

2013-02-01

Full Text Available Abdel Naser Zaid,1 Salam Natur,2 Aiman Qaddumi,2 Abeer Abu Ghoush11Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine; 2Pharmacare PLC, Ramallah, PalestinePurpose: The aim of this study was to formulate stable film-coated montelukast sodium (MS tablets using Opadry® yellow 20A82938 (Montikast® tablets and to evaluate their in vitro and in vivo release profile.Methods: MS core tablets were manufactured using a direct compression method. Opadry yellow 20A82938 aqueous coating dispersion was used as the film-coating material. Dissolution of the film-coated tablets was tested in 900 mL of 0.5% sodium lauryl sulfate solution and the bioequivalence of the tablets was tested by comparing them with a reference formulation – Singulair® tablets. In vitro–in vivo correlation was evaluated. The stability of the obtained film-coated tablets was evaluated according to International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use guidelines.Results: The efficiency of the film coating was determined by subjecting the coated tablets to gastric pH and drug release was analyzed using high-performance liquid chromatography. The coated tablets had no obvious defects. MS release met the study criterion of not less than 80% dissolved after 30 minutes in 0.5% sodium lauryl sulfate solution. Statistical comparison of the main pharmacokinetic parameters clearly indicated no significant difference between test and reference in any of the calculated pharmacokinetic parameters. Level A correlation between in vitro drug release and in vivo absorption was found to be satisfactory.Conclusion: These findings suggest that aqueous film coating with Opadry yellow 20A82938 is an easy, reproducible, and economical approach for preparing stable MS film-coated tablets without affecting the drug-release characteristics.Keywords: coating, stability, aqueous

Development and evaluation of microporous osmotic tablets of diltiazem hydrochloride

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Afifa Bathool

2012-01-01

Full Text Available Microporous osmotic tablet of diltiazem hydrochloride was developed for colon targeting. These prepared microporous osmotic pump tablet did not require laser drilling to deliver the drug to the specific site of action. The tablets were prepared by wet granulation method. The prepared tablets were coated with microporous semipermeable membrane and enteric polymer using conventional pan coating process. The incorporation of sodium lauryl sulfate (SLS, a leachable pore-forming agent, could form in situ delivery pores while coming in contact with gastrointestinal medium. The effect of formulation variables was studied by changing the amounts of sodium alginate and NaCMC in the tablet core, osmogen, and that of pore-forming agent (SLS used in the semipermeable coating. As the amount of hydrophilic polymers increased, drug release rate prolonged. It was found that drug release was increased as the concentration of osmogen and pore-former was increased. Fourier transform infrared spectroscopy and Differential scanning calorimetry results showed that there was no interaction between drug and polymers. Scanning electron microscopic studies showed the formation of pores after predetermined time of coming in contact with dissolution medium. The formation of pores was dependent on the amount of pore former used in the semipermeable membrane. in vitro results showed acid-resistant, timed release at an almost zero order up to 24 hours. The developed osmotic tablets could be effectively used for prolonged delivery of Diltiazem HCl.

Development and evaluation of a hot-melt coating technique for enteric coating

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Arun Trambak Patil

2012-03-01

Full Text Available Conventional enteric coating requires the use of organic based polymers which are equally hazardous to the environment and operating personnel. Hot-melt coating avoids the use of solvents and is a safer and time-saving process. The present study was designed to assess the efficacy of hot-melt coating (HMC as an enteric coating technique. Pellets prepared by extrusion spheronization were selected as the core formulation for a model of the gastric irritant drug diclofenac sodium (DFS because of their innate advantages over single-unit formulations. Stearic acid (SA and palmitic acid (PA were evaluated as enteric hot-melt coating materials. HMC was carried out in a specially modified coating pan by applying SA and PA in molten state onto preheated pellets to achieve a coating level of 5-15 %w/w. Hot-melt coated pellets were evaluated for disintegration pH and in vitro dissolution in the pH range 1.2 to 6.8, along with basic micromeritics. SEM of coated pellets showed a uniform and smooth coating. These results indicated that HMC of both SA and PA exhibited very good enteric coating ability. The coated pellets showed negligible drug release in acidic pH. As the pellets were subsequently transferred to a higher pH level, a gradual increase in release of the drug from the pellets was observed with increasing pH of the dissolution media. The release was dependent upon coating extent, providing sustained enteric release as opposed to abrupt release with mixed release kinetics.O revestimento entérico convencional requer o uso de polímeros orgânicos os quais são igualmente danosos ao meio ambiente e ao pessoal que o executa. O revestimento por fusão a quente evita o uso de solventes e é processo mais seguro e que consome menos tempo. O presente estudo foi planejado para avaliar a eficácia do revestimento por fusão a quente (RFQ como técnica de revestimento entérico. Os péletes preparados por esferonização por extrusão foram selecionados como

In Vitro Evaluation of Eslicarbazepine Delivery via Enteral Feeding Tubes.

Science.gov (United States)

Reindel, Kristin; Zhao, Fang; Hughes, Susan; Dave, Vivek S

2017-12-01

Purpose: The feasibility of preparing an eslicarbazepine acetate suspension using Aptiom tablets for administration via enteral feeding tubes was evaluated. Methods: Eslicarbazepine acetate suspension (40 mg/mL) was prepared using Aptiom tablets after optimizing the tablet crushing methods and the vehicle composition. A stability-indicating high-performance liquid chromatography (HPLC) method was developed to monitor the eslicarbazepine stability in the prepared suspension. Three enteric feeding tubes of various composition and dimensions were evaluated for the delivery of the suspensions. The suspension was evaluated for the physical and chemical stability for 48 hours. Results: The reproducibility and consistency of particle size reduction was found to be best with standard mortar/pestle. The viscosity analysis and physical stability studies showed that ORA-Plus:water (50:50 v/v) was optimal for suspending ability and flowability of suspension through the tubes. The developed HPLC method was found to be stability indicating and suitable for the assay of eslicarbazepine acetate in the prepared suspension. The eslicarbazepine concentrations in separately prepared suspensions were within acceptable range (±3%), indicating accuracy and reproducibility of the procedure. The eslicarbazepine concentrations in suspensions before and after delivery through the enteric feeding tubes were within acceptable range (±4%), indicating absence of any physical/chemical interactions of eslicarbazepine with the tubes and a successful delivery of eslicarbazepine dosage via enteric feeding tubes. The stability study results showed that eslicarbazepine concentration in the suspension remained unchanged when stored at room temperature for 48 hours. Conclusion: The study presents a convenient procedure for the preparation of a stable suspension of eslicarbazepine acetate (40 mg/mL) using Aptiom tablets, for administration via enteral feeding tubes.

In vitro disintegration and dissolution studies of once-weekly copies of alendronate sodium tablets (70 mg) and in vivo implications.

Science.gov (United States)

Dansereau, Richard J; Crail, Debbie J; Perkins, Alan C

2008-04-01

The aim of this study was to evaluate the in vitro disintegration and dissolution of 26 alendronic acid tablets (70 mg) on the market in Canada, Germany, the Netherlands, and the United Kingdom compared to the branded product (Fosamax). The disintegration and dissolution times were determined using the methods described in the United States Pharmacopeia 30 (USP 30). The disintegration of four orally disintegrating tablets (non-bisphosphonates) and branded film-coated risedronate sodium tablets were included for comparison. The mean disintegration times of the alendronic acid tablets ranged from 14 s for Pharmachemie (Netherlands) to 342 s (5.7 min) for Betapharm (Germany). The mean disintegration time of the branded product tablets ranged from 43 to 78 s. Six of the 26 companies market alendronic acid tablets with very rapid disintegration times which are similar to those of orally disintegrating tablets (non-bisphosphonates). The alendronic acid tablets with very rapid mean disintegration times are as follows: Pharmachemie (Netherlands), 14 s; Novopharm (Canada), 13-24 s; GRY-Pharma (Germany), 21 s; Juta Pharma (Germany), 30 s; APS/Teva (United Kingdom), 26 and 37 s; and Teva (UK), 14-29 s. Since there is no established disintegration time for alendronic acid tablets there can be no assurance that the copy tablets are equivalent to the branded product in terms of esophageal drug exposure. However, the in vitro disintegration times have not been correlated with in vivo disintegration and performance. The dissolution of all the bisphosphonate tablets was rapid with greater than 80% dissolved in 15 min and all products conformed to the USP 30 specification. The dissolution of all alendronic acid tablets was rapid and complete and conformed to the established USP 30 specifications which should ensure adequate drug absorption from the copy products. However, copies of alendronic acid tablets are approved based on the results of single-dose bioavailability studies in

Enteric coating of granules containing the probiotic Lactobacillus acidophilus

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Pyar Hassan

2014-06-01

Full Text Available In the present study, a capsule formulation composed of enteric coated granules of Lactobacillus acidophilus ATCC 4962 was developed using Eudragit L30D-55 as enteric polymer. Optimization of the capsule formulation was achieved with a maximum viable cell count after 2 h of incubation in acid medium and disintegration time of 1 h in buffer pH 6.8. The amount of Eudragit L30D-55 in the capsules correlated with gastric juice resistance. The best protective qualities against artificial gastric juice were observed when capsules were prepared from granules composed of L. acidophilus, corn starch, lactose monohydrate, polyvinylpyrrolidone and coated with 12.5 % (m/V of Eudragit L30D-55. Capsule formulation of L. acidophilus in edible broth medium suspension serves as a cheap alternative to the expensive freeze-drying procedure for preparing L. acidophilus. In addition, the enteric coating using Eudragit L30D-55 could protect probiotics from the acidic gastric environment and enhance the bioactivity of probiotics along with replacement of pathogenic microbes in human intestine

How do tablet properties influence swallowing behaviours?

Science.gov (United States)

Yamamoto, Shinya; Taniguchi, Hiroshige; Hayashi, Hirokazu; Hori, Kazuhiro; Tsujimura, Takanori; Nakamura, Yuki; Sato, Hideaki; Inoue, Makoto

2014-01-01

Behavioural performance of tablet swallowing was evaluated with different tablet conditions in terms of size, number and surface coating. Four different types of tablets were prepared: small or large, and with or without a surface coating. Fourteen normal male adults were instructed to swallow the prepared tablets with 15 ml of water. The number of tablets in one trial was changed from one to three. To evaluate swallowing and tablet transport, electromyographic activity was recorded in the left suprahyoid muscles, and videofluorographic images were examined. All tablet conditions (size, number and surface coating) affected the swallowing performance in terms of total number of swallows, electromyographic burst patterns and location of remaining tablets. Increases in the size and number of tablets increased the number of swallows and electromyographic burst area and duration. In addition, all of these parameters increased while swallowing tablets without a coating compared with tablets with a coating. Location of the remaining tablets was mainly within the mouth. This study only clarified the normal pattern of tablet swallowing under several conditions in healthy subjects, but the results may facilitate comprehensive evaluation and treatment planning in terms of administering medication to dysphagic patients. © 2013 Royal Pharmaceutical Society.

Effect of binders on 500mg metformin hydrochloride tablets produced by wet granulation

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LUCIANA CATIA BLOCK

2009-12-01

Full Text Available Metformin hydrochloride (MH is an oral hypoglycemic agent and a high-dose drug that has poor flow and compression properties. In this study, the feasibility of developing adequate, low cost 500mg tablets of metformin hydrochloride by wet granulation was tested with several binders (Starch / PVP K30®; Starch 1500® /PVP K30®, PVP K30® and PVP K90® in a simple tablet press of the type used in small pharmaceutical laboratories. The drug powder was tested for ability to flow, by determining Carr’s Index (CI and the Hausner ratio (HR. Differential scanning calorimetry and thermogravimetric analysis were carried out on isolated MH and 1:1 (w/w binary mixtures with the excipients. The size distribution, friability, flow properties and drug content of the granules were analyzed, as were the hardness, friability, disintegration, dissolution and uniformity of the dosage form. The drug powder showed CI > 22% and HR > 1.25, characteristic of a poor flow powder, and no significant incompatibilities with the excipients. All the granules showed adequate flow properties and were suitable for pressing into tablets, all of which complied with pharmacopeial specifications. The starch /PVP K30® and starch 1500® /PVP K30® mixtures were best for producing 500 mg MH tablets. Keywords: Metformin hydrochloride. Tablets. Wet granulation. Binders.

Eudragit L/HPMCAS blend enteric-coated lansoprazole pellets: enhanced drug stability and oral bioavailability.

Science.gov (United States)

Fang, Yu; Wang, Guozheng; Zhang, Rong; Liu, Zhihua; Liu, Zhenghua; Wu, Xiaohui; Cao, Deying

2014-06-01

The objectives of the present work were to use blends of Eudragit L and hydroxypropyl methylcellulose acetate succinate (HPMCAS) as enteric film coatings for lansoprazole (LSP) pellets. The enteric-coated pellets were prepared with a fluid-bed coater. The influence of the blend ratio, type of plasticizer, plasticizer level, coating level, and curing conditions on gastric stability in vitro drug release and drug stability was evaluated. Furthermore, the bioavailability of the blend-coated pellets in beagle dogs was also performed. The blend-coated pellets exhibited significant improvement of gastric stability and drug stability compared to the pure polymer-coated pellets. Moreover, the AUC values of blend-coated pellets were greater than that of the pure polymer-coated pellets. It was concluded that the using blends of Eudragit L and HPMCAS as enteric film coatings for LSP pellets improved the drug stability and oral bioavailability.

In-vitro studies of enteric coated diclofenac sodium-carboxymethylcellulose microspheres.

Science.gov (United States)

Arica, B; Arica, M Y; Kaş, H S; Hincal, A A; Hasirci, V

1996-01-01

MIcrospheres containing diclofenac sodium (DS) were prepared using carboxymethylcellulose (CMC) as the main support material (1.0, 2.0, 3.0% (w/v)) and aluminum chloride as the crosslinker. Drug to polymer ratios of 1:1, 1:2 and 1:4 were used to obtain a range of microspheres. The microspheres were then coated with an enteric coating material, Eudragit S-100, efficiency, % yield value, particle sizes an in-vitro dissolution behaviour were investigated. The surface of the enteric coated microspheres seemed to be all covered with Eudragit S-100 from scanning electron microscopy observation. It was also observed that increasing the CMC concentration led to an increase in the encapsulation efficiency, % yield value and particle size and decreased the release rate. Eudragit S-100 coating did not significantly alter the size but the release rate was significantly lower even when the lower concentration solution was used.

Tablet potency of Tianeptine in coated tablets by near infrared spectroscopy: model optimisation, calibration transfer and confidence intervals.

Science.gov (United States)

Boiret, Mathieu; Meunier, Loïc; Ginot, Yves-Michel

2011-02-20

A near infrared (NIR) method was developed for determination of tablet potency of active pharmaceutical ingredient (API) in a complex coated tablet matrix. The calibration set contained samples from laboratory and production scale batches. The reference values were obtained by high performance liquid chromatography (HPLC) and partial least squares (PLS) regression was used to establish a model. The model was challenged by calculating tablet potency of two external test sets. Root mean square errors of prediction were respectively equal to 2.0% and 2.7%. To use this model with a second spectrometer from the production field, a calibration transfer method called piecewise direct standardisation (PDS) was used. After the transfer, the root mean square error of prediction of the first test set was 2.4% compared to 4.0% without transferring the spectra. A statistical technique using bootstrap of PLS residuals was used to estimate confidence intervals of tablet potency calculations. This method requires an optimised PLS model, selection of the bootstrap number and determination of the risk. In the case of a chemical analysis, the tablet potency value will be included within the confidence interval calculated by the bootstrap method. An easy to use graphical interface was developed to easily determine if the predictions, surrounded by minimum and maximum values, are within the specifications defined by the regulatory organisation. Copyright © 2010 Elsevier B.V. All rights reserved.

Stabilization Mechanism of Roxithromycin Tablets under Gastric pH Conditions.

Science.gov (United States)

Inukai, Koki; Noguchi, Shuji; Kimura, Shin-Ichiro; Itai, Shigeru; Iwao, Yasunori

2018-05-31

Macrolide antibiotics are widely used at clinical sites. Clarithromycin (CAM), a 14-membered macrolide antibiotic, was reported to gelate under acidic conditions. Gelation allows oral administration of acid-sensitive CAM without enteric coating by hindering the penetration of gastric fluid into CAM tablets. However, it is unknown whether this phenomenon occurs in other macrolide antibiotics. In this study, we examined the gelation ability of three widely used macrolide antibiotics, roxithromycin (RXM), erythromycin A (EM), and azithromycin (AZM). The results indicated that not only CAM but also RXM gelated under acidic conditions. EM and AZM did not gelate under the same conditions. Gelation of RXM delayed the disintegration of the tablet and release of RXM from the tablet. Disintegration and release were also delayed in commercial RXM tablets containing disintegrants. This study showed that two of the four macrolides gelated, which affects tablet disintegration and dissolution and suggests that this phenomenon might also occur in other macrolides. Copyright © 2018. Published by Elsevier Inc.

Application of a tablet film coating model to define a process-imposed transition boundary for robust film coating.

Science.gov (United States)

van den Ban, Sander; Pitt, Kendal G; Whiteman, Marshall

2018-02-01

A scientific understanding of interaction of product, film coat, film coating process, and equipment is important to enable design and operation of industrial scale pharmaceutical film coating processes that are robust and provide the level of control required to consistently deliver quality film coated product. Thermodynamic film coating conditions provided in the tablet film coating process impact film coat formation and subsequent product quality. A thermodynamic film coating model was used to evaluate film coating process performance over a wide range of film coating equipment from pilot to industrial scale (2.5-400 kg). An approximate process-imposed transition boundary, from operating in a dry to a wet environment, was derived, for relative humidity and exhaust temperature, and used to understand the impact of the film coating process on product formulation and process control requirements. This approximate transition boundary may aid in an enhanced understanding of risk to product quality, application of modern Quality by Design (QbD) based product development, technology transfer and scale-up, and support the science-based justification of critical process parameters (CPPs).

Comparison of the pharmacokinetics of a new 30 mg modified-release tablet formulation of metoclopramide for once-a-day administration versus 10 mg immediate-release tablets: a single and multiple-dose, randomized, open-label, parallel study in healthy male subjects.

Science.gov (United States)

Bernardo-Escudero, Roberto; Alonso-Campero, Rosalba; Francisco-Doce, María Teresa de Jesús; Cortés-Fuentes, Myriam; Villa-Vargas, Miriam; Angeles-Uribe, Juan

2012-12-01

The study aimed to assess the pharmacokinetics of a new, modified-release metoclopramide tablet, and compare it to an immediate-release tablet. A single and multiple-dose, randomized, open-label, parallel, pharmacokinetic study was conducted. Investigational products were administered to 26 healthy Hispanic Mexican male volunteers for two consecutive days: either one 30 mg modified-release tablet every 24 h, or one 10 mg immediate-release tablet every 8 h. Blood samples were collected after the first and last doses of metoclopramide. Plasma metoclopramide concentrations were determined by high-performance liquid chromatography. Safety and tolerability were assessed through vital signs measurements, clinical evaluations, and spontaneous reports from study subjects. All 26 subjects were included in the analyses [mean (SD) age: 27 (8) years, range 18-50; BMI: 23.65 (2.22) kg/m², range 18.01-27.47)]. Peak plasmatic concentrations were not statistically different with both formulations, but occurred significantly later (p 0.05)]. One adverse event was reported in the test group (diarrhea), and one in the reference group (headache). This study suggests that the 30 mg modified-release metoclopramide tablets show features compatible with slow-release formulations when compared to immediate-release tablets, and is suitable for once-a-day administration.

Investigation of the potential for direct compaction of a fine ibuprofen powder dry-coated with magnesium stearate.

Science.gov (United States)

Qu, Li; Zhou, Qi Tony; Gengenbach, Thomas; Denman, John A; Stewart, Peter J; Hapgood, Karen P; Gamlen, Michael; Morton, David A V

2015-05-01

Intensive dry powder coating (mechanofusion) with tablet lubricants has previously been shown to give substantial powder flow improvement. This study explores whether the mechanofusion of magnesium stearate (MgSt), on a fine drug powder can substantially improve flow, without preventing the powder from being directly compacted into tablets. A fine ibuprofen powder, which is both cohesive and possesses a low-melting point, was dry coated via mechanofusion with between 0.1% and 5% (w/w) MgSt. Traditional low-shear blending was also employed as a comparison. No significant difference in particle size or shape was measured following mechanofusion. For the low-shear blended powders, only marginal improvement in flowability was obtained. However, after mechanofusion, substantial improvements in the flow properties were demonstrated. Both XPS and ToF-SIMS demonstrated high degrees of a nano-scale coating coverage of MgSt on the particle surfaces from optimized mechanofusion. The study showed that robust tablets were produced from the selected mechanofused powders, at high-dose concentration and tablet tensile strength was further optimized via addition of a Polyvinylpyrrolidone (PVP) binder (10% w/w). The tablets with the mechanofused powder (with or without PVP) also exhibited significantly lower ejection stress than those made of the raw powder, demonstrating good lubrication. Surprisingly, the release rate of drug from the tablets made with the mechanofused powder was not retarded. This is the first study to demonstrate such a single-step dry coating of model drug with MgSt, with promising flow improvement, flow-aid and lubrication effects, tabletability and also non-inhibited dissolution rate.

Application of process analytical technology in tablet process development using NIR spectroscopy : Blend uniformity, content uniformity and coating thickness measurements

NARCIS (Netherlands)

Moes, Johannes J; Ruijken, Marco M; Gout, Erik; Frijlink, Henderik W; Ugwoke, Michael I

2008-01-01

Near-infrared (NIR)spectroscopy was employed as a process analytical technique in three steps of tabletting process: to monitor the blend homogeneity, evaluate the content uniformity of tablets and determine the tablets coating thickness. A diode-array spectrometer mounted on a lab blender (SP15 NIR

Effects of tablet formulation and subsequent film coating on the supersaturated dissolution behavior of amorphous solid dispersions.

Science.gov (United States)

Sakai, Toshiro; Hirai, Daiki; Kimura, Shin-Ichiro; Iwao, Yasunori; Itai, Shigeru

2018-04-05

The effects of tablet preparation and subsequent film coating with amorphous solid dispersion (ASD) particles that were composed of a drug with poor water solubility and hydrophilic polymers were investigated. ASD particles were prepared with a drug and vinylpyrrolidone-vinyl acetate copolymer (PVPVA) or polyvinylpyrrolidone (PVP) at a weight ratio of 1:1 or 1:2 using a melt extrusion technique. Tablets were prepared by conventional direct compression followed by pan coating. A mathematical model based on the Noyes-Whitney equation assuming that stable crystals precipitated at the changeable surface area of the solid-liquid interface used to estimate drug dissolution kinetics in a non-sink dissolution condition. All the ASD particles showed a maximum dissolution concentration approximately ten times higher than that of the crystalline drug. The ASD particles with PVPVA showed higher precipitation rate with lower polymer ratio, while PVP did not precipitate within 960 min regardless of the polymer ratio, suggesting the ASD particles of 1:1 drug:PVPVA (ASD-1) were the most unstable among the ASD particles considered. The dissolution of a core tablet with ASD-1 showed less supersaturation and a much higher precipitation rate than those of ASD-1 particles. However, a film-coated tablet or core tablet with a trace amount of hydroxypropylmethylcellulose (HPMC) showed a similar dissolution profile to that of the ASD-1 particles, indicating HPMC had a remarkable precipitation inhibition effect. Overall, these results suggest that tablet preparation with ASD may adversely affect the maintenance of supersaturation; however, this effect can be mitigated by adding an appropriate precipitation inhibitor to the formulation. Copyright © 2018 Elsevier B.V. All rights reserved.

Film coated tablets (ColoPulse technology) for targeted delivery in the lower intestinal tract : influence of the core composition on release characteristics

NARCIS (Netherlands)

Schellekens, Reinout C. A.; Baltink, Jan H.; Woesthuis, Ellen M.; Stellaard, Frans; Kosterink, Jos G. W.; Woerdenbag, Herman J.; Frijlink, Henderik W.

2010-01-01

The design of a film coating technology which allows a tablet to deliver the drug in the ileocolonic segment would offer new treatment possibilities. The objective is to develop a platform technology that is suitable for a broad range of drug compounds. We developed a coated tablet with a delayed,

Ficus deltoidea Standardization: Analytical Methods for Bioactive Markers in Deltozide Tablet 200 MG

International Nuclear Information System (INIS)

Hazlina Ahmad Hassali; Zainah Adam; Rosniza Razali

2016-01-01

Standardization of herbal materials based on their chemical and biological profile is an important prerequisite for development of herbal product. The phyto pharmaceutical product that has been developed by Medical Technology Division, Malaysian Nuclear Agency is DELTOZIDE TABLET 200 MG containing 200 mg of spray-dried aqueous extract of Ficus deltoidea var kunstleri leaf as the active ingredient. Ficus deltoidea Jack or locally known as Mas Cotek is a South East Asian native plant traditionally used to treat several diseases. Pharmacological data showed that this plant exhibited good antioxidant, anti-diabetic and anti-inflammatory properties. It is important to establish the chemical profiles and determine the phytochemicals content of this plant as it is popularly used in traditional medicines. Thus, the present study reports on the comprehensive phytochemicals evaluation of bioactive markers from this extract for the development of DELTOZIDE TABLET 200 MG . Characterization of extract using LCMS/ MS Triple TOF System showed the presence of major constituents representing vitexin, isovitexin, gallic acid, catechinic, api genin, epicatechin and caffeoylquinic acid along with other minor constituents. The extract was standardized by ultra-high performance liquid chromatography (UHPLC) using two pharmacologically active markers, vitexin and isovitexin. Furthermore, qualitative determination of phytochemicals showed the presence of important phyto-constituents namely anthraquinones, terpenoids, flavonoids, tannins, phlobatannins, alkaloids, saponins, cardiac glycosides, steroids and phenols in the aqueous extract of Ficus deltoidea. Quantitative determination of phytochemicals revealed that the amount of total phenolic content (TPC; Gallic acid as standard) and total flavonoid content (TFC; Quercetin as standard) were 126.67±3.98 mg GAE/ g extract and 9.08±0.36 mg QE/ g extract respectively. The generated data provides some explanation for its wide usage in

Effect of combination tablets containing amlodipine 10 mg and irbesartan 100 mg on blood pressure and cardiovascular risk factors in patients with hypertension

Directory of Open Access Journals (Sweden)

Yagi S

2015-01-01

Full Text Available Shusuke Yagi,1 Akira Takashima,1 Minoru Mitsugi,2 Toshihiro Wada,2 Junko Hotchi,1 Ken-ichi Aihara,3 Tomoya Hara,1 Masayoshi Ishida,1 Daiju Fukuda,4 Takayuki Ise,1 Koji Yamaguchi,1 Takeshi Tobiume,1 Takashi Iwase,1 Hirotsugu Yamada,1 Takeshi Soeki,1 Tetsuzo Wakatsuki,1 Michio Shimabukuro,4 Masashi Akaike,5 Masataka Sata11Department of Cardiovascular Medicine, Graduate School of Health Biosciences, University of Tokushima, Tokushima, 2Department of Internal Medicine, Shikoku Central Hospital, Shikokuchuo, 3Department of Medicine and Bioregulatory Sciences, 4Department of Cardio-Diabetes Medicine, 5Department of Medical Education, Graduate School of Health Biosciences, University of Tokushima, Tokushima, JapanBackground: Hypertension is one of the major risk factors for cardiovascular and cerebrovascular disease and mortality. Patients who receive insufficient doses of antihypertensive agents or who are poorly adherent to multidrug treatment regimens often fail to achieve adequate blood pressure (BP control. The aim of this study was to determine the efficacy of an angiotensin II receptor blocker (ARB and calcium channel blocker (CCB combination tablet containing a regular dose of irbesartan (100 mg and a high dose of amlodipine (10 mg with regard to lowering BP and other risk factors for cardiovascular disease.Methods: We retrospectively evaluated data from 68 patients with essential hypertension whose treatment regimen was changed either from combination treatment with an independent ARB and a low-dose or regular-dose CCB or from a combination tablet of ARB and a low-dose or regular-dose CCB to a combination tablet containing amlodipine 10 mg and irbesartan 100 mg, because of incomplete BP control. Previous treatments did not include irbesartan as the ARB.Results: The combination tablet decreased systolic and diastolic BP. In addition, it significantly decreased serum uric acid, low-density lipoprotein cholesterol, and increased high

Effect of Mg content on microstructure and corrosion behavior of hot dipped Zn–Al–Mg coatings

Energy Technology Data Exchange (ETDEWEB)

Yao, Caizhen; Lv, Haibing [Research Centre of Laser Fusion, CAEP, P.O.Box 919-988-5, Mianyang, Sichuan 621900 (China); Zhu, Tianping [Department of Chemical and Materials Engineering, The University of Auckland, PB 92019, Auckland 1142 (New Zealand); Zheng, Wanguo [Research Centre of Laser Fusion, CAEP, P.O.Box 919-988-5, Mianyang, Sichuan 621900 (China); Yuan, Xiaodong, E-mail: xdyuan@caep.cn [Research Centre of Laser Fusion, CAEP, P.O.Box 919-988-5, Mianyang, Sichuan 621900 (China); Gao, Wei, E-mail: w.gao@auckland.ac.nz [Department of Chemical and Materials Engineering, The University of Auckland, PB 92019, Auckland 1142 (New Zealand)

2016-06-15

In this article, Zn–Al–Mg coatings were prepared by hot dipping method. The surface morphology, cross–section microstructure, microhardness, composition, corrosion behaviour of ZAM coatings were investigated by using X–ray diffraction (XRD), Optical microscope, Environmental scanning electron microscopy equipped with EDS (FESEM–EDS), Microhardness tester and Electrochemical analysis respectively. Corrosion test was also performed in a standard salt fog spray chamber. Microstructure studies indicates that Zn grain size was refined and eutectic areas at Zn grain boundary areas increased with increasing Mg content. ZA5M1.5 and ZA5M2 coatings have two distinct layers. Mg tends to exist in the outer layer while Al is in the inner layer. The inner layer is composed of Al{sub 5}Fe{sub 2}Zn{sub 0.4} intermetallic, which may to contribute to the microhardness. The outer layer is Zn grains surrounded by Zn–Mg etutectics, which may improve the corrosion resistance. The microhardness is more than 700 HV{sub 50g} for Al-rich layer and around 151 HV{sub 25g} for Mg-rich layer. The improved corrosion resistance of Zn–5%Al-1.5%Mg coating comes from the corrosion product of flocculent type simonkolleite, which prolongs the micro-path and impedes the movement of O{sub 2} and H{sub 2}O, ultimately retards the overall corrosion process. - Highlights: • Two-layer structured Zn–Al–Mg coatings were prepared by hot dipping method. • Mg exists in the outer layer while Al exists in the inner layer of Zn–Al–Mg coating. • Zn–Al–Mg coating has better protective ability than Zn and Zn–Al coatings. • The Mg-modified simonkolleite is the reason of the enhanced corrosion resistance.

Comparative Evaluation and Optimization of Film Coating ...

African Journals Online (AJOL)

In this study, hydroxypropyl methylcellulose phthalate (HPMCP) and two polymethacrylates, Wangit L30D-55® and Wangit L-100® were investigated for their enteric coating properties using diclofenac sodium tablets as core. Both polymers showed acid protective effect at the weight gain of 6%. Polymethacrylate based ...

Effect of magnesium stearate concentration on dissolution properties of ranitidine hydrochloride coated tablets.

Science.gov (United States)

Uzunović, Alija; Vranić, Edina

2007-08-01

Most pharmaceutical formulations also include a certain amount of lubricant to improve their flowability and prevent their adhesion to the surfaces of processing equipment. Magnesium stearate is an additive that is most frequently used as a lubricant. Magnesium stearate is capable of forming films on other tablet excipients during prolonged mixing, leading to a prolonged drug liberation time, a decrease in hardness, and an increase in disintegration time. It is hydrophobic, and there are many reports in the literature concerning its adverse effect on dissolution rates. The objective of this study was to evaluate the effects of two different concentrations of magnesium stearate on dissolution properties of ranitidine hydrochloride coated tablet formulations labeled to contain 150 mg. The uniformity content was also checked. During the drug formulation development, several samples were designed for choice of the formulation. For this study, two formulations containing 0,77 and 1,1% of magnesium stearate added in the manufacture of cores were chosen. Fraction of ranitidine hydrochloride released in dissolution medium was calculated from calibration curves. The data were analyzed using pharmacopeial test for similarity of dissolution profiles ( f2 equation), previously proposed by Moore and Flanner. Application of f2 equation showed differences in time-course of ranitidine hydrochloride dissolution properties. The obtained values indicate differences in drug release from analyzed ranitidine hydrochloride formulations and could cause differences in therapeutic response.

Mg-MOF-74/MgF₂ Composite Coating for Improving the Properties of Magnesium Alloy Implants: Hydrophilicity and Corrosion Resistance.

Science.gov (United States)

Liu, Wei; Yan, Zhijie; Ma, Xiaolu; Geng, Tie; Wu, Haihong; Li, Zhongyue

2018-03-07

Surface modification on Mg alloys is highly promising for their application in the field of bone repair. In this study, a new metal-organic framework/MgF₂ (Mg-MOF-74/MgF₂) composite coating was prepared on the surface of AZ31B Mg alloy via pre-treatment of hydrofluoric acid and in situ hydrothermal synthesis methods. The surface topography of the composite coating is compact and homogeneous, and Mg-MOF-74 has good crystallinity. The corrosion resistance of this composite coating was investigated through Tafel polarization test and immersion test in simulated body fluid at 37 °C. It was found that Mg-MOF-74/MgF₂ composite coating significantly slowed down the corrosion rate of Mg alloy. Additionally, Mg-MOF-74/MgF₂ composite coating expresses super-hydrophilicity with the water contact angle of nearly 0°. In conclusion, on the basis of MgF₂ anticorrosive coating, the introduction of Mg-MOF-74 further improves the biological property of Mg alloys. At last, we propose that the hydrophilicity of the composite coating is mainly owing to the large number of hydroxyl groups, the high specific surface area of Mg-MOF-74, and the rough coating produced by Mg-MOF-74 particles. Hence, Mg-MOF-74 has a great advantage in enhancing the hydrophilicity of Mg alloy surface.

Mg substituted apatite coating from alkali conversion of acidic calcium phosphate

Energy Technology Data Exchange (ETDEWEB)

Navarro da Rocha, Daniel, E-mail: dnr.navarro@gmail.com [Military Institute of Engineering-IME, Pça. Gen. Tiburcio, 80, P. Vermelha, Urca, Rio de Janeiro, R.J. (Brazil); Cruz, Leila Rosa de Oliveira [Military Institute of Engineering-IME, Pça. Gen. Tiburcio, 80, P. Vermelha, Urca, Rio de Janeiro, R.J. (Brazil); Campos, José Brant de [Rio de Janeiro State University - UERJ, Rio de Janeiro, R.J. (Brazil); Marçal, Rubens L. Santana Blazutti [Military Institute of Engineering-IME, Pça. Gen. Tiburcio, 80, P. Vermelha, Urca, Rio de Janeiro, R.J. (Brazil); Mijares, Dindo Q.; Coelho, Paulo G. [Department of Biomaterials and Biomimetics, New York University College of Dentistry (NYU), New York, NY (United States); Prado da Silva, Marcelo H. [Military Institute of Engineering-IME, Pça. Gen. Tiburcio, 80, P. Vermelha, Urca, Rio de Janeiro, R.J. (Brazil)

2017-01-01

In this work, two solutions were developed: the first, rich in Ca{sup 2+}, PO{sub 4}{sup 3−} ions and the second, rich in Ca{sup 2+}, PO{sub 4}{sup 3−} and Mg{sup 2+}, defined as Mg-modified precursor solution. For each Mg-modified precursor solution, the concentrations of Mg{sup 2+} ions were progressively increased by 5%, 10% and 15%wt. The aims of this research were to investigate the influence of magnesium ions substitution in calcium phosphate coatings on titanium surface and to evaluate these coatings by bioactivity assay in McCoy culture medium. The obtained coatings were characterized by X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR) analysis, and the presence of Mg ions was confirmed by the inductively coupled plasma atomic emission spectroscopy (ICP) analysis. In vitro bioactivity assay in McCoy culture medium showed bioactivity after 14 days in incubation for the HA and 10% Mg-monetite coatings. The high chemical stability of Mg-HA coatings was verified by the bioactivity assays, and no bone-like apatite deposition, characteristic of bioactivity, was observed for Mg-HA coatings, for the time period used in this study. - Highlights: • The presence of Mg ions influenced the final apatite phase present in the produced coatings. • A lower efficiency in heterogeneous deposition and an exposure of Ti substrate in 5% Mg-monetite coatings was soon verified. • McCoy culture medium was effective in predicting the coatings bioactivity.

Effect of Mg on the Microstructure and Corrosion Resistance of the Continuously Hot-Dip Galvanizing Zn-Mg Coating

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Anping Dong

2017-08-01

Full Text Available The microstructure of continuously hot-dip galvanizing Zn-Mg coating was investigated in order to obtain the mechanism of the effects of Mg on the corrosion resistance. In this paper, the vertical section of the Zn-0.20 wt % Al-Mg ternary phase diagram near the Al-low corner was calculated. The results indicates that the phase composition of the Zn-0.20 wt % Al-Mg ternary phase diagram near the Al-low corner is the same as Zn-Mg binary phase diagram, suggesting Al in the Zn-Mg (ZM coatings mainly concentrates on the interfacial layer between the coating and steel substrate. The microstructure of continuously hot-dip galvanizing ZM coatings with 0.20 wt % Al containing 1.0–3.0 wt % Mg was investigated using tunneling electron microscopy (TEM. The morphology of Zn in the coating changes from bulk to strip and finally to mesh-like, and the MgZn2 changes from rod-like to mesh-like with the Mg content increasing. Al in the ZM coatings mainly segregates at the Fe2Al5 inhibition layer and the Mg added to the Zn bath makes this inhibition layer thinner and uneven. Compared to GI coating, the time of the first red rust appears increases by more than two-fold and expansion rate of red rust reduces by more than four-fold in terms of salt spray experiment. The ZM coating containing 2.0 wt % Mg has the best corrosion resistance. The enhanced corrosion resistance of ZM coatings mainly depends on different corrosion products.

A Pharmacokinetic Bioequivalence Study Comparing Pirfenidone Tablet and Capsule Dosage Forms in Healthy Adult Volunteers.

Science.gov (United States)

Pan, Lin; Belloni, Paula; Ding, Han Ting; Wang, Jianshuang; Rubino, Christopher M; Putnam, Wendy S

2017-09-01

Pirfenidone film-coated tablets were developed to offer an alternative to the marketed capsule formulation. This study assessed the bioequivalence of the tablet and capsule formulations under fed and fasted states. A Phase I, open-label, randomized, four-treatment-period, four-sequence, crossover pharmacokinetics study (NCT02525484) was conducted. Each subject received an 801-mg single dose of pirfenidone as three 267-mg capsules or one 801-mg tablet under fasted and fed conditions. Pirfenidone plasma C max , AUC 0-t and AUC 0-∞ were used to assess bioequivalence. Forty-four subjects were randomized to treatment. The 801-mg tablet in the fasted state met bioequivalence criteria [90% confidence intervals (CI) 80.00-125.00%] for the GLSM ratios of natural log-transformed C max , AUC 0-t and AUC 0-∞ . Under fed conditions, the 801-mg tablet met the bioequivalence criteria for AUC 0-t and AUC 0-∞ , but slightly exceeded the bioequivalence criteria for the C max (90% CI of 108.26-125.60%). The tablet C max was approximately 17% higher than that of the capsules. In the fed state, the tablet C max , and both AUC 0-t and AUC 0-∞ were reduced by 39% and 17%, respectively, relative to the fasted state. The tablet and capsules had acceptable tolerability profiles. The pirfenidone 801-mg tablet met bioequivalence criteria when compared with three 267-mg capsules in the fasted state. The tablet C max was slightly higher relative to capsules in the fed state, but this is not expected to have a clinically meaningful impact on the benefit-risk profile of pirfenidone. This work was supported by F. Hoffmann-La Roche Ltd.

Tablet splitting and weight uniformity of half-tablets of 4 medications in pharmacy practice.

Science.gov (United States)

Tahaineh, Linda M; Gharaibeh, Shadi F

2012-08-01

Tablet splitting is a common practice for multiple reasons including cost savings; however, it does not necessarily result in weight-uniform half-tablets. To determine weight uniformity of half-tablets resulting from splitting 4 products available in the Jordanian market and investigate the effect of tablet characteristics on weight uniformity of half-tablets. Ten random tablets each of warfarin 5 mg, digoxin 0.25 mg, phenobarbital 30 mg, and prednisolone 5 mg were weighed and split by 6 PharmD students using a knife. The resulting half-tablets were weighed and evaluated for weight uniformity. Other relevant physical characteristics of the 4 products were measured. The average tablet hardness of the sampled tablets ranged from 40.3 N to 68.9 N. Digoxin, phenobarbital, and prednisolone half-tablets failed the weight uniformity test; however, warfarin half-tablets passed. Digoxin, warfarin, and phenobarbital tablets had a score line and warfarin tablets had the deepest score line of 0.81 mm. Splitting warfarin tablets produces weight-uniform half-tablets that may possibly be attributed to the hardness and the presence of a deep score line. Digoxin, phenobarbital, and prednisolone tablet splitting produces highly weight variable half-tablets. This can be of clinical significance in the case of the narrow therapeutic index medication digoxin.

Bioequivalence of 2 Formulations of Sildenafil Oral Soluble Film 100 mg and Sildenafil Citrate (Viagra) 100 mg Oral Tablets in Healthy Male Volunteers.

Science.gov (United States)

Dadey, Eric

Sildenafil citrate tablets (VIAGRA; Pfizer Inc) have been used since 1998 as an oral therapy for the treatment of erectile dysfunction. However, in some cases, patients may have difficulty in swallowing tablets, and the need to use water to aid in the oral administration of the tablets has the potential to interrupt the sexual encounter, reduce spontaneity, and therefore decrease the quality of the experience. Two oral soluble film (OSF) formulations of sildenafil were developed using MonoSol Rx's proprietary PharmFilm technology. Both films were formulated to dissolve rapidly on the tongue, thereby releasing the drug into the oral cavity, whereupon it is swallowed without the use of water. From a patient perspective, it is anticipated that the film formulations of sildenafil citrate will provide a more compliant and discreet dosage form. The purpose of this clinical study was to compare the bioequivalence of the 2 sildenafil OSF 100 mg formulations (MonoSol Rx, LLC) with the sildenafil citrate 100 mg tablets. The design was a single-dose, randomized, open-label, 3-period, 6-sequence, 3-treatment, single-center, crossover study conducted in 18 healthy, nonsmoking male volunteers under fasting conditions, with each treatment period separated by a 7-day washout period. Plasma sildenafil concentrations were measured predose and then periodically to 24 hours after dosing. The 90% confidence intervals for plasma sildenafil AUC0-t, AUC0-∞, and Cmax for both sildenafil OSF formulations as compared with sildenafil citrate tablets were all within the 80%-125% range, indicating bioequivalence of both film formulations to sildenafil citrate tablets. Overall, the demonstrated bioequivalence coupled with the performance advantages of an OSF dosage form (ie, rapid dissolution in the mouth, can be taken without water, and can be dosed discreetly) suggest that the sildenafil OSF may provide an attractive alternative to sildenafil citrate oral tablets.

Effects of food on the pharmacokinetics of gemigliptin/metformin sustained-release 50/1,000 mg (25/500 mg x 2 tablets) fixeddose combination tablet in healthy male volunteers.

Science.gov (United States)

Choi, Hee Youn; Noh, Yook-Hwan; Kim, Yo Han; Kim, Mi Jo; Lee, Shi Hyang; Kim, Jeong-Ae; Kim, Bogyeong; Lim, Hyeong-Seok; Bae, Kyun-Seop

2014-05-01

For patient convenience, a gemigliptin/metformin sustainedrelease fixed-dose combination (FDC) tablet was developed. This study was conducted to investigate the effects of food on the pharmacokinetic (PK) profile of the FDC tablets. This was an open-label, randomized, single dose, 2-period, 2-sequence crossover study in 24 healthy male volunteers. The FDC tablets (25/500 mg × 2 tablets) were administered in high-fat fed and fasted states on separate occasions, and each subject was randomly allocated to each sequence with a 7-day washout period. PK blood samplings were conducted from predose to 48 hours after dosing. Tolerability assessments were performed throughout the study. Nine adverse events (AEs) of mild intensity were reported from 8 subjects after study drug administration, and the AE frequency was similar between treatments. No serious AEs were reported. The PK parameters of gemigliptin and metformin were compared between fasting and fed states. For gemigliptin, the geometric mean ratios (GMRs) (fed : fasted state) of the Cmax and AUClast were 0.886 (90% confidence interval (CI) 0.781 - 1.006) and 1.021 (90% CI 0.949 - 1.099), respectively. For metformin, the GMRs of the Cmax and AUClast were 0.811 (90% CI 0.712 - 0.923) and 1.144 (90% CI 1.013 - 1.291), respectively. A prolonged tmax for metformin was observed. These results are similar to the effects of food on each component. The FDC tablet may have a similar PK profile as that of individual drugs and is generally tolerable when administered with food. These results indicate that the FDC tablet can be administered in the same dosing regimen as each component, especially that of metformin sustained-release.

Effect of Magnesium Stearate Concentration on Dissolution Properties of Ranitidine Hydrochloride Coated Tablets

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Alija Uzunović

2007-08-01

Full Text Available Most pharmaceutical formulations also include a certain amount of lubricant to improve their flowability and prevent their adhesion to the surfaces of processing equipment. Magnesium stearate is an additive that is most frequently used as a lubricant. Magnesium stearate is capable of forming films on other tablet excipients during prolonged mixing, leading to a prolonged drug liberation time, a decrease in hardness, and an increase in disintegration time. It is hydrophobic, and there are many reports in the literature concerning its adverse effect on dissolution rates.The objective of this study was to evaluate the effects of two different concentrations of magnesium stearate on dissolution properties of ranitidine hydrochloride coated tablet formulations labeled to contain 150 mg. The uniformity content was also checked.During the drug formulation development, several samples were designed for choice of the formulation. For this study, two formulations containing 0,77 and 1,1% of magnesium stearate added in the manufacture of cores were chosen. Fraction of ranitidine hydrochloride released in dissolution medium was calculated from calibration curves. The data were analyzed using pharmaco-peial test for similarity of dissolution profiles (f2 equation, previously proposed by Moore and Flanner.Application of f2 equation showed differences in time-course of ranitidine hydrochloride dissolution properties. The obtained values indicate differences in drug release from analyzed ranitidine hydrochloride formulations and could cause differences in therapeutic response.

Effect of Sampling Frequency for Real-Time Tablet Coating Monitoring Using Near Infrared Spectroscopy.

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Igne, Benoît; Arai, Hiroaki; Drennen, James K; Anderson, Carl A

2016-09-01

While the sampling of pharmaceutical products typically follows well-defined protocols, the parameterization of spectroscopic methods and their associated sampling frequency is not standard. Whereas, for blending, the sampling frequency is limited by the nature of the process, in other processes, such as tablet film coating, practitioners must determine the best approach to collecting spectral data. The present article studied how sampling practices affected the interpretation of the results provided by a near-infrared spectroscopy method for the monitoring of tablet moisture and coating weight gain during a pan-coating experiment. Several coating runs were monitored with different sampling frequencies (with or without co-adds (also known as sub-samples)) and with spectral averaging corresponding to processing cycles (1 to 15 pan rotations). Beyond integrating the sensor into the equipment, the present work demonstrated that it is necessary to have a good sense of the underlying phenomena that have the potential to affect the quality of the signal. The effects of co-adds and averaging was significant with respect to the quality of the spectral data. However, the type of output obtained from a sampling method dictated the type of information that one can gain on the dynamics of a process. Thus, different sampling frequencies may be needed at different stages of process development. © The Author(s) 2016.

Stannate conversion coatings on Mg-8Li alloy

International Nuclear Information System (INIS)

Yang Lihui; Zhang Milin; Li Junqing; Yu Xiang; Niu Zhongyi

2009-01-01

The stannate conversion coatings (SnCC) on Mg-8Li alloy were investigated by simple immersion method. The surface morphology and composition were studied by scanning electron microscopy (SEM), energy dispersive spectroscopy (EDS) and X-ray diffraction spectroscopy (XRD) techniques. The corrosion resistance was assessed by means of potentiodynamic polarization measurements and electrochemical impedance spectra (EIS). The effects of time of a stannate bath on the quality of stannate conversion coatings were investigated by SEM and EIS. It was found that the coating particles were mainly composed of hemispherical particles MgSnO 3 .3H 2 O. A comparison of results revealed the coating treated for 60 min exhibited the most uniform, dense and corrosion-resistant

Terahertz Technology: A Boon to Tablet Analysis

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Wagh, M. P.; Sonawane, Y. H.; Joshi, O. U.

2009-01-01

The terahertz gap has a frequency ranges from ∼0.3 THz to ∼10 THz in the electromagnetic spectrum which is in between microwave and infrared. The terahertz radiations are invisible to naked eye. In comparison with x-ray they are intrinsically safe, non-destructive and non-invasive. Terahertz spectroscopy enables 3D imaging of structures and materials, and the measurement of the unique spectral fingerprints of chemical and physical forms. Terahertz radiations are produced by a dendrimer based high power terahertz source and spectroscopy technologies. It resolves many of the questions left unanswered by complementary techniques, such as optical imaging, Raman and infrared spectra. In the pharmaceutical industries it enables nondestructive, internal, chemical analysis of tablets, capsules, and other dosage forms. Tablet coatings are a major factor in drug bioavailability. Therefore tablet coatings integrity and uniformity are of crucial importance to quality. Terahertz imaging gives an unparalleled certainty about the integrity of tablet coatings and the matrix performance of tablet cores. This article demonstrates the potential of terahertz pulse imaging for the analysis of tablet coating thickness by illustrating the technique on tablets. PMID:20490288

Enteric-coated epichlorohydrin crosslinked dextran microspheres for site-specific delivery to colon.

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Rai, Gopal; Yadav, Awesh K; Jain, Narendra K; Agrawal, Govind P

2015-01-01

Enteric-coated epichlorohydrin crosslinked dextran microspheres containing 5-Fluorouracil (5-FU) for colon drug delivery was prepared by emulsification-crosslinking method. The formulation variables studied includes different molecular weights of dextran, volume of crosslinking agent, stirring speed, time and temperature. Dextran microspheres showed mean entrapment efficiencies ranging between 77 and 87% and mean particle size ranging between 10 and 25 µm. About 90% of drug was released from uncoated dextran microspheres within 8 h, suggesting the fast release and indicated the drug loaded in uncoated microspheres, released before they reached colon. Enteric coating (Eudragit-S-100 and Eudragit-L-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method. The release study of 5-FU from coated dextran microspheres was complete retardation in simulated gastric fluid (pH 1.2) and once the coating layer of enteric polymer was dissolved at higher pH (7.4 and 6.8), a controlled release of the drug from the microspheres was observed. Further, the release of drug was found to be higher in the presence of dextranase and rat caecal contents, indicating the susceptibility of dextran microspheres to colonic enzymes. Organ distribution and pharmacokinetic study in albino rats was performed to establish the targeting potential of optimized formulation in the colon.

In vitro study of nanostructured diopside coating on Mg alloy orthopedic implants

International Nuclear Information System (INIS)

Razavi, Mehdi; Fathi, Mohammadhossein; Savabi, Omid; Vashaee, Daryoosh; Tayebi, Lobat

2014-01-01

The high corrosion rate of Mg alloys has hindered their application in various areas, particularly for orthopedic applications. In order to decrease the corrosion rate and to improve the bioactivity, mechanical stability and cytocompatibility of the Mg alloy, nanostructured diopside (CaMgSi 2 O 6 ) has been coated on AZ91 Mg alloy using a combined micro arc oxidation (MAO) and electrophoretic deposition (EPD) method. The crystalline structure, the morphology and the composition of the samples were characterized by X-ray diffraction (XRD), scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR). Electrochemical corrosion test, immersion test, and compression test were used to evaluate the corrosion resistance, the in vitro bioactivity and the mechanical stability of the samples, respectively. The cytocompatibility of the samples was tested by the cell viability and the cell attachment of L-929 cells. The results confirmed that the diopside coating not only slows down the corrosion rate, but also enhances the in vitro bioactivity, mechanical stability and cytocompatibility of AZ91 Mg alloy. Therefore, Mg alloy coated with nanostructured diopside offers a promising approach for biodegradable bone implants. - Highlights: • The diopside coating was applied on Mg alloy using the combined MAO and EPD methods. • The corrosion resistance of the diopside coated Mg alloy was noticeably improved. • The in vitro bioactivity of the diopside coated Mg alloy was considerably increased. • The mechanical stability of biodegradable Mg alloy was enhanced by diopside coating. • The cytocompatibility of the Mg alloy was improved employing diopside coating

In vitro study of nanostructured diopside coating on Mg alloy orthopedic implants

Energy Technology Data Exchange (ETDEWEB)

Razavi, Mehdi, E-mail: mehdi.razavi@okstate.edu [Biomaterials Research Group, Department of Materials Engineering, Isfahan University of Technology, Isfahan 84156-83111 (Iran, Islamic Republic of); Torabinejad Dental Research Center, School of Dentistry, Isfahan University of Medical Sciences, Isfahan 81746-73461 (Iran, Islamic Republic of); School of Materials Science and Engineering, Helmerich Advanced Technology Research Center, Oklahoma State University, Tulsa, OK 74106 (United States); School of Electrical and Computer Engineering, Helmerich Advanced Technology Research Center, Oklahoma State University, Tulsa, OK 74106 (United States); Fathi, Mohammadhossein [Biomaterials Research Group, Department of Materials Engineering, Isfahan University of Technology, Isfahan 84156-83111 (Iran, Islamic Republic of); Dental Materials Research Center, Isfahan University of Medical Sciences, Isfahan (Iran, Islamic Republic of); Savabi, Omid [Torabinejad Dental Research Center, School of Dentistry, Isfahan University of Medical Sciences, Isfahan 81746-73461 (Iran, Islamic Republic of); Vashaee, Daryoosh [School of Electrical and Computer Engineering, Helmerich Advanced Technology Research Center, Oklahoma State University, Tulsa, OK 74106 (United States); Tayebi, Lobat, E-mail: lobat.tayebi@okstate.edu [School of Materials Science and Engineering, Helmerich Advanced Technology Research Center, Oklahoma State University, Tulsa, OK 74106 (United States); School of Chemical Engineering, Oklahoma State University, Stillwater, OK 74078 (United States)

2014-08-01

The high corrosion rate of Mg alloys has hindered their application in various areas, particularly for orthopedic applications. In order to decrease the corrosion rate and to improve the bioactivity, mechanical stability and cytocompatibility of the Mg alloy, nanostructured diopside (CaMgSi{sub 2}O{sub 6}) has been coated on AZ91 Mg alloy using a combined micro arc oxidation (MAO) and electrophoretic deposition (EPD) method. The crystalline structure, the morphology and the composition of the samples were characterized by X-ray diffraction (XRD), scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR). Electrochemical corrosion test, immersion test, and compression test were used to evaluate the corrosion resistance, the in vitro bioactivity and the mechanical stability of the samples, respectively. The cytocompatibility of the samples was tested by the cell viability and the cell attachment of L-929 cells. The results confirmed that the diopside coating not only slows down the corrosion rate, but also enhances the in vitro bioactivity, mechanical stability and cytocompatibility of AZ91 Mg alloy. Therefore, Mg alloy coated with nanostructured diopside offers a promising approach for biodegradable bone implants. - Highlights: • The diopside coating was applied on Mg alloy using the combined MAO and EPD methods. • The corrosion resistance of the diopside coated Mg alloy was noticeably improved. • The in vitro bioactivity of the diopside coated Mg alloy was considerably increased. • The mechanical stability of biodegradable Mg alloy was enhanced by diopside coating. • The cytocompatibility of the Mg alloy was improved employing diopside coating.

Specifications development for "Karbatril" codenamed tablets

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L. I. Kucherenko

2017-08-01

Full Text Available Introduction. According to current legislation of Ukraine the specifications of tablets include the following indicators: description, identification, average weight, disintegration and assay. The aim of the study. The development of specifications and project of quality control methods for "Karbatril" codenamed tablets. Materials and methods. During the study we analyzed 6 series of tablets "Karbatril." For the description, identification, determination of the average mass, disintegration, active ingredients quantify of "Karbatril" codenamed tablets we used appropriate methods and instruments. Results and discussion. Tablets "Karbatril" were analyzed for the following parameters: - Overview - Tablets white or nearly white; - Average weight - during the study the average weight of 6 series of obtained tablets ranged from 339,0 mg to 369,9 mg according to SPU from 337,0 mg to 373,0 mg; - Disintegration – according to SPU the disintegration for tablet without shell shall not exceed 15 min. Analyzed tablets disintegrated in the period from 5 to 10 minutes; - Identification and quantification of the active ingredients of tablets were conducted using modified HPLC methods. During the identification obtained chromatograms show compliance with SPU. In quantitative determination of the active ingredients content in "Karbatril" codenamed tablets we found carbamazepine from 148.18 mg to 150.19 mg, thiotriazoline - from 98.93 mg to 99.71 mg. This data is consistent to SPU which regulates content of carbamazepine - 150 mg ± 7,5%, thiotriazoline - 100 mg ± 10%. Conclusions. This study has developed specification for "Karbatril" codenamed tablets and also methods of HPLC qualitative and quantitative determination of active ingredients. In the specification the following parameters are included: description, identification, average weight, disintegration and assay. The study drafted quality control methods which are planned to be later offered to the

Captopril 25 mg tablets stability assessment in different primary packing materials

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Flávia Costa Mendes Paiva

2017-11-01

Full Text Available Introduction: Packaging is used to provide protection and information, from the production to the administration of a formulation. It is essential to define the primary packaging, for keeping the therapeutic efficacy of drugs, safety of users and for protecting drugs from instability. Objectives: The main objective of this study was to assess the stability of captopril 25 mg tablets in different primary packaging materials. Method: The characterization (IR, DSC and physical tests of the packaging materials used for captopril was carried out prior to the manufacture of tablets. Tablets were also characterized by physical-chemical analysis, comparative dissolution profile and stability studies. Results: The characterization of packaging materials was crucial for understanding the behavior of captopril when packed in each material. Materials with significant barrier, as blisters PVC/PVdC 90 g.m-² and hard aluminum and PVC/PE/PVdC and hard aluminum showed satisfactory results in a second stage, S2. On the contrary, lower barrier materials as blisters PVC/PVdC 40 g.m-² and hard aluminum did not present dissolution analysis S2. Conclusions: The aluminum strip presented the best results. And the batch in glass bottle, although packaged in excellent material, was disapproved in accelerated stability.

An oral modified-release nifedipine tablet (Adalat LA) and its appearance on double contrast barium enema

International Nuclear Information System (INIS)

Bleehen, Robert E.

2000-01-01

Adalat LA 30 mg and 60 mg tablets are widely prescribed oral modified release nifedipine preparations with a porous, non-digestible plastic tablet coating which is required in order to effect the osmotically driven slow release mechanism. These tablets may therefore be seen anywhere along the gastrointestinal tract and are passed apparently whole in the faeces. An example of the appearance within the rectum of Adalat LA 30 (Bayer) on double contrast barium enema is shown and the main features described. A review of the literature is given. Recognition of the appearances during the barium enema examination will prompt those performing the procedure to question the drug history where relevant and will reduce the incidence of false-positive reporting. Bleehen, R.E. (2000)

Mycophenolic acid agents: is enteric coating the answer?

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Manitpisitkul W

2011-03-01

Full Text Available Wana Manitpisitkul1, Sabrina Lee2, Matthew Cooper31Department of Pharmacy, University of Maryland Medical Center, Baltimore, MD, USA; 2Solid Organ Transplant Program, University of Utah Health Care, Salt Lake City, UT, USA; 3Department of Surgery, University of Maryland School of Medicine, Baltimore, MD, USAAbstract: Addition of mycophenolate mofetil (MMF to calcineurin-based immunosuppressive therapy has led to a significant improvement in graft survival and reduction of acute rejection in renal transplant recipients. However, in clinical practice, MMF dose reduction, interruption, or discontinuation due to hematological and gastrointestinal (GI side-effects occurred in up to 50% of the patients. Large retrospective analyses have demonstrated that patients requiring MMF dose manipulation due to adverse events experienced a higher rate of rejection and graft loss. Enteric-coated mycophenolate sodium (EC-MPS was developed with the goal of improving upper GI side-effects. Here, we review the efficacy and safety of EC-MPS in de novo kidney transplant recipient, and in stable renal transplant patients who were converted from MMF. The changes in GI-related adverse events using patient-reported outcome instruments are also reviewed.Keywords: enteric-coated mycophenolate sodium, mycophenolate mofetil, kidney transplant, efficacy, gastrointestinal tolerability

Coating of graphite flakes with MgO/carbon nanocomposite via gas state reaction

International Nuclear Information System (INIS)

Sharif, M.; Faghihi-Sani, M.A.; Golestani-Fard, F.; Saberi, A.; Soltani, Ali Khalife

2010-01-01

Coating of graphite flakes with MgO/carbon nanocomposite was carried out via gaseous state reaction between mixture of Mg metal, CO gas and graphite flakes at 1000 o C. XRD and FE-SEM analysis of coating showed that the coating was comprised of MgO nano particles and amorphous carbon distributed smoothly and covered the graphite surface evenly. Thermodynamic calculations were employed to predict the reaction sequences as well as phase stability. The effect of coating on water wettability and oxidation resistance of graphite was studied using contact angle measurement and TG analysis, respectively. It was demonstrated that the reaction between Mg and CO could result in MgO/C nanocomposite deposition. The coating improved water wettability of graphite and also enhanced the oxidation resistance of graphite flakes significantly. Also the graphite coating showed significant phenolic resin-wettabilty owing to high surface area of such hydrophilic nano composite coating. The importance of graphite coating is explained with emphasis on its potential application in graphite containing refractories.

Comparing the Electrochemical Performance of LiFePO4/C Modified by Mg Doping and MgO Coating

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Jianjun Song

2013-01-01

Full Text Available Supervalent cation doping and metal oxide coating are the most efficacious and popular methods to optimize the property of LiFePO4 lithium battery material. Mg-doped and MgO-coated LiFePO4/C were synthesized to analyze their individual influence on the electrochemical performance of active material. The specific capacity and rate capability of LiFePO4/C are improved by both MgO coating and Mg doping, especially the Mg-doped sample—Li0.985Mg0.015FePO4/C, whose discharge capacity is up to 163 mAh g−1, 145.5 mAh g−1, 128.3 mAh g−1, and 103.7 mAh g−1 at 1 C, 2 C, 5 C, and 10 C, respectively. The cyclic life of electrode is obviously increased by MgO surface modification, and the discharge capacity retention rate of sample LiFePO4/C-MgO2.5 is up to 104.2% after 100 cycles. Comparing samples modified by these two methods, Mg doping is more prominent on prompting the capacity and rate capability of LiFePO4, while MgO coating is superior in terms of improving cyclic performance.

Corrosion properties of the Mg alloy coated with polypyrrole films

International Nuclear Information System (INIS)

Grubač, Zoran; Rončević, Ivana Škugor; Metikoš-Huković, Mirjana

2016-01-01

Highlights: • Electropolymerization of pyrrole on Mg-alloy surface in presence of salicylate. • Salicylate dual role in PPy deposition: passivation and electron transfer mediation. • Redox potential of salicylate corresponds to potential of PPy nucleation. • EIS and polarization corrosion studies of PPy coated Mg-alloy in Hanks’ solution. • Polypyrrole significantly slowdown Mg alloy corrosion in Hanks’ solution. - Abstract: In the present study the reactive surface of Mg alloy was coated with the nontoxic biocompatible polypyrrole (PPy) film synthesized by electrochemical oxidation from an aqueous salicylate solution. Salicylate ions prevent Mg dissolution and act as an electron transfer mediator during the PPy film nucleation, formation and growth on the alloy surface. Kinetics of the pyrrole polymerization as well as corrosion resistance of the PPy coated Mg alloy in the Hanks’ solution were investigated using dc electrochemical methods and electrochemical impedance spectroscopy (EIS). Characterization of the surface film was performed by optical and Fourier transform infrared spectroscopy (FTIR).

Stabilization and target delivery of Nattokinase using compression coating.

Science.gov (United States)

Law, D; Zhang, Z

2007-05-01

The aim of the work is to develop a new formulation in order to stabilize a nutraceutical enzyme Nattokinase (NKCP) in powders and to control its release rate when it passes through the gastrointestinal tract of human. NKCP powders were first compacted into a tablet, which was then coated with a mixture of an enteric material Eudragit L100-55 (EL100-55) and Hydroxypropylcellulose (HPC) by direct compression. The activity of the enzyme was determined using amidolytic assay and its release rates in artificial gastric juice and an intestinal fluid were quantified using bicinchoninic acid assay. Results have shown that the activity of NKCP was pressure independent and the coated tablets protected NKCP from being denatured in the gastric juice, and realized its controlled release to the intestine based on in vitro experiments.

Development of a chitosan based double layer-coated tablet as a platform for colon-specific drug delivery

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Kim MS

2016-12-01

Full Text Available Min Soo Kim,1,* Dong Woo Yeom,1,* Sung Rae Kim,1 Ho Yub Yoon,1 Chang Hyun Kim,1 Ho Yong Son,1 Jin Han Kim,1 Sangkil Lee,2 Young Wook Choi1 1College of Pharmacy, Chung-Ang University, Seoul, 2College of Pharmacy, Keimyung University, Daegu, South Korea *These authors contributed equally to this work Abstract: A double layer-coated colon-specific drug delivery system (DL-CDDS was developed, which consisted of chitosan (CTN based polymeric subcoating of the core tablet containing citric acid for microclimate acidification, followed by an enteric coating. The polymeric composition ratio of Eudragit E100 and ethyl cellulose and amount of subcoating were optimized using a two-level factorial design method. Drug-release characteristics in terms of dissolution efficiency and controlled-release duration were evaluated in various dissolution media, such as simulated colonic fluid in the presence or absence of CTNase. Microflora activation and a stepwise mechanism for drug release were postulated. Consequently, the optimized DL-CDDS showed drug release in a controlled manner by inhibiting drug release in the stomach and intestine, but releasing the drug gradually in the colon (approximately 40% at 10 hours and 92% at 24 hours in CTNase-supplemented simulated colonic fluid, indicating its feasibility as a novel platform for CDD. Keywords: chitosan, colon-specific delivery, acidification, microflora, factorial design, controlled release

Clinical efficacy and safety of a new 1000-mg suspension versus twice-daily 500-mg tablets of MPFF in patients with symptomatic chronic venous disorders: a randomized controlled trial.

Science.gov (United States)

Carpentier, Patrick; van Bellen, Bonno; Karetova, Debora; Hanafiah, Harunarashid; Enriquez-Vega, Elizabeth; Kirienko, Alexander; Dzupina, Andrej; Sabovic, Miso; Reina Gutierrez, Lourdes; Subwongcharoen, Somboom; Tüzün, Hasan; Maggioli, Arnaud

2017-10-01

Chronic venous disorders (CVD) is estimated to affect 30% to 50% of women and 10% to 30% of men. The most widely prescribed treatment for CVD worldwide is micronized purified flavonoid fraction 500 mg (MPFF). The aim of this clinical trial was to develop a new once daily 1000-mg oral suspension of MPFF. In an international, randomized, double-blind, parallel-group study, symptomatic individuals classified CEAP C0s to C4s were randomized in either treatment arm and treated for 8 weeks. Lower limb symptoms (discomfort, pain and heaviness) were assessed using Visual Analog Scales (VAS), and quality of life (QoL) was measured with the CIVIQ-20 Questionnaire. A total of 1139 patients were included in the study. Both MPFF treatment regimens were well tolerated and associated with a significant reduction in lower limb symptoms. A non-inferiority of MPFF 1000-mg oral suspension once daily compared to MPFF 500-mg tablet twice daily (P1000 mg and -3.37 cm for MPFF 500 mg), leg pain (-3.27 cm for MPFF 1000 mg and -3.31 cm for MPFF 500 mg) and leg heaviness (-3.41 cm for MPFF 1000 mg and -3.46 cm for MPFF 500 mg). The patients' QoL was improved by about 20 points on the CIVIQ scale in both groups (19.33 points for MPFF 1000 mg and 20.28 points for MPFF 500 mg). MPFF 1000-mg oral suspension and MPFF 500-mg tablets treatments were associated with similar reductions in lower limb symptoms and QoL improvement. The new once daily MPFF1000-mg oral suspension has a similar safety profile to two tablets of MPFF 500 mg, with the advantage of one daily intake, potentially associated with improved patient adherence and easier CVD management.

Broadband Acoustic Resonance Dissolution Spectroscopy (BARDS): A rapid test for enteric coating thickness and integrity of controlled release pellet formulations.

Science.gov (United States)

Alfarsi, Anas; Dillon, Amy; McSweeney, Seán; Krüse, Jacob; Griffin, Brendan; Devine, Ken; Sherry, Patricia; Henken, Stephan; Fitzpatrick, Stephen; Fitzpatrick, Dara

2018-04-12

There are no rapid dissolution based tests for determining coating thickness, integrity and drug concentration in controlled release pellets either during production or post-production. The manufacture of pellets requires several coating steps depending on the formulation. The sub-coating and enteric coating steps typically take up to six hours each followed by additional drying steps. Post production regulatory dissolution testing also takes up to six hours to determine if the batch can be released for commercial sale. The thickness of the enteric coating is a key factor that determines the release rate of the drug in the gastro-intestinal tract. Also, the amount of drug per unit mass decreases with increasing thickness of the enteric coating. In this study, the coating process is tracked from start to finish on an hourly basis by taking samples of pellets during production and testing those using BARDS (Broadband Acoustic Resonance Dissolution Spectroscopy). BARDS offers a rapid approach to characterising enteric coatings with measurements based on reproducible changes in the compressibility of a solvent due to the evolution of air during dissolution. This is monitored acoustically via associated changes in the frequency of induced acoustic resonances. A steady state acoustic lag time is associated with the disintegration of the enteric coatings in basic solution. This lag time is pH dependent and is indicative of the rate at which the coating layer dissolves. BARDS represents a possible future surrogate test for conventional USP dissolution testing as its data correlates directly with the thickness of the enteric coating, its integrity and also with the drug loading as validated by HPLC. Copyright © 2018 Elsevier B.V. All rights reserved.

In vitro disintegration studies of weekly generic alendronate sodium tablets (70 mg) available in the US.

Science.gov (United States)

Dansereau, Richard J; Crail, Debbie J; Perkins, Alan C

2009-02-01

Bisphosphonates as a class have the potential to cause upper gastrointestinal irritation. Although the generic alendronate sodium tablets are bioequivalent to the branded product, a potential concern is that the pharmaceutical attributes of the various generic formulations my affect the potential for local irritation and tolerability. The in vitro disintegration times were determined using the method described in the US Pharmacopeia 30 (USP 30). The disintegration of three generic alendronate sodium tablets 70 mg available in the United States was compared to that of the branded product. The mean disintegration times of the generic alendronate sodium tablets ranged from 9 to 10 s for the Barr lots to 108 s for the Watson lot. The disintegration time of the branded product (Fosamax) was 53 s. The three Barr lots and one Teva lot had rapid disintegration times which were similar to the disintegration standards (disintegrating tablets. Since there is no established disintegration time for alendronate sodium tablets there can be no assurance that the generic tablets are equivalent to the branded product in terms of esophageal exposure. However, the in vitro disintegration times have not been correlated with in vivo disintegration performance. Copies of generic alendronate sodium tablets are approved based on the results of single-dose bioavailability studies in healthy subjects and this is not considered adequate to establish similar disintegration characteristics.

Influence of disintegrants in different substrate physical form on dimensional recovery of multi-component tablet.

Science.gov (United States)

Sarkar, Srimanta; Ooi, Shing Ming; Liew, Celine Valeria; Tan, Bing Xun; Heng, Paul Wan Sia

2014-11-20

This study investigated the influence of different disintegrants, present in different substrate physical forms, on dimensional recovery of multi-component tablets prepared at different compression pressures. Formulations containing model drug, metformin, (10%, w/w), different disintegrants (10%, w/w), and lactose (80%, w/w) were compressed directly or after granulation using polyvinyl pyrrolidone (1%, w/w) as binder, into tablets (350 mg, 10mm diameter) at 150, 200, and 250 N/mm(2) compression pressures. Tablets were characterized for immediate dimensional recovery (IR) after ejection from the die, latent dimensional recovery (LR) over 24 h, tensile strength, and disintegration. The IR was predominantly contributed by crystalline components whereas LR was brought about by polymeric materials. With increased compression pressure, higher degree of plastic deformation of the polymeric disintegrants resulted in tablet with lower LR and higher tensile strength. Presence of polyvinyl pyrrolidone in the granules contributed considerably to plastic deformation, and the tablets produced had lower LR, higher tensile strength, and longer disintegration time. This study indicated that use of granules as the feed substrate physical form and a prudent selection of components may enable the coating of resultant tablets immediately after compression without the risk of coat damage due to LR. Copyright © 2014 Elsevier B.V. All rights reserved.

Coating of graphite flakes with MgO/carbon nanocomposite via gas state reaction

Energy Technology Data Exchange (ETDEWEB)

Sharif, M., E-mail: Sharif_m@metaleng.iust.ac.i [Iran University of Science and Technology, Tehran (Iran, Islamic Republic of); Faghihi-Sani, M.A. [Sharif University of Technology, Tehran (Iran, Islamic Republic of); Golestani-Fard, F. [Iran University of Science and Technology, Tehran (Iran, Islamic Republic of); Saberi, A. [Tabriz University (Iran, Islamic Republic of); Soltani, Ali Khalife [Iran University of Science and Technology, Tehran (Iran, Islamic Republic of)

2010-06-18

Coating of graphite flakes with MgO/carbon nanocomposite was carried out via gaseous state reaction between mixture of Mg metal, CO gas and graphite flakes at 1000 {sup o}C. XRD and FE-SEM analysis of coating showed that the coating was comprised of MgO nano particles and amorphous carbon distributed smoothly and covered the graphite surface evenly. Thermodynamic calculations were employed to predict the reaction sequences as well as phase stability. The effect of coating on water wettability and oxidation resistance of graphite was studied using contact angle measurement and TG analysis, respectively. It was demonstrated that the reaction between Mg and CO could result in MgO/C nanocomposite deposition. The coating improved water wettability of graphite and also enhanced the oxidation resistance of graphite flakes significantly. Also the graphite coating showed significant phenolic resin-wettabilty owing to high surface area of such hydrophilic nano composite coating. The importance of graphite coating is explained with emphasis on its potential application in graphite containing refractories.

Sol-Gel Derived Hydroxyapatite Coating on Mg-3Zn Alloy for Orthopedic Application

Science.gov (United States)

Singh, Sanjay; Manoj Kumar, R.; Kuntal, Kishor Kumar; Gupta, Pallavi; Das, Snehashish; Jayaganthan, R.; Roy, Partha; Lahiri, Debrupa

2015-04-01

In recent years, magnesium and its alloys have gained a lot of interest as orthopedic implant constituents because their biodegradability and mechanical properties are closer to that of human bone. However, one major concern with Mg in orthopedics is its high corrosion rate that results in the reduction of mechanical integrity before healing the bone tissue. The current study evaluates the sol-gel-derived hydroxyapatite (HA) coating on a selected Mg alloy (Mg-3Zn) for decreasing the corrosion rate and increasing the bioactivity of the Mg surface. The mechanical integrity of the coating is established as a function of the surface roughness of the substrate and the sintering temperature of the coating. Coating on a substrate roughness of 15-20 nm and sintering at 400°C shows the mechanical properties in similar range of bone, thus making it suitable to avoid the stress-shielding effect. The hydroxyapatite coating on the Mg alloy surface also increases corrosion resistance very significantly by 40 times. Bone cells are also found proliferating better in the HA-coated surface. All these benefits together establish the candidature of sol-gel HA-coated Mg-3Zn alloy in orthopedic application.

Corrosion Resistance of the Superhydrophobic Mg(OH2/Mg-Al Layered Double Hydroxide Coatings on Magnesium Alloys

Directory of Open Access Journals (Sweden)

Fen Zhang

2016-04-01

Full Text Available Coatings of the Mg(OH2/Mg-Al layered double hydroxide (LDH composite were formed by a combined co-precipitation method and hydrothermal process on the AZ31 alloy substrate in alkaline condition. Subsequently, a superhydrophobic surface was successfully constructed to modify the composite coatings on the AZ31 alloy substrate using stearic acid. The characteristics of the composite coatings were investigated by means of X-ray diffractometer (XRD, Fourier transform infrared spectroscopy (FTIR, X-ray photoelectron spectroscopy (XPS, scanning electronic microscope (SEM and contact angle (CA. The corrosion resistance of the coatings was assessed by potentiodynamic polarization, the electrochemical impedance spectrum (EIS, the test of hydrogen evolution and the immersion test. The results showed that the superhydrophobic coatings considerably improved the corrosion resistant performance of the LDH coatings on the AZ31 alloy substrate.

Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent.

Science.gov (United States)

Qi, Xiaole; Chen, Haiyan; Rui, Yao; Yang, Fengjiao; Ma, Ning; Wu, Zhenghong

2015-07-15

To prolong the residence time of dosage forms within gastrointestinal trace until all drug released at desired rate was one of the real challenges for oral controlled-release drug delivery system. Herein, we developed a fine floating tablet via compression coating of hydrophilic polymer (hydroxypropyl cellulose) combined with effervescent agent (sodium bicarbonate) to achieve simultaneous control of release rate and location of ofloxacin. Sodium alginate was also added in the coating layer to regulate the drug release rate. The effects of the weight ratio of drug and the viscosity of HPC on the release profile were investigated. The optimized formulations were found to immediately float within 30s and remain lastingly buoyant over a period of 12 h in simulated gastric fluid (SGF, pH 1.2) without pepsin, indicating a satisfactory floating and zero-order drug release profile. In addition, the oral bioavailability experiment in New Zealand rabbits showed that, the relative bioavailability of the ofloxacin after administrated of floating tablets was 172.19%, compared to marketed common release tablets TaiLiBiTuo(®). These results demonstrated that those controlled-released floating tables would be a promising gastro-retentive delivery system for drugs acting in stomach. Copyright © 2015 Elsevier B.V. All rights reserved.

Development of modified release 3D printed tablets (printlets) with pharmaceutical excipients using additive manufacturing.

Science.gov (United States)

Goyanes, Alvaro; Fina, Fabrizio; Martorana, Annalisa; Sedough, Daniel; Gaisford, Simon; Basit, Abdul W

2017-07-15

The aim of this study was to manufacture 3D printed tablets (printlets) from enteric polymers by single filament fused deposition modeling (FDM) 3D printing (3DP). Hot melt extrusion was used to generate paracetamol-loaded filaments from three different grades of the pharmaceutical excipient hypromellose acetate succinate (HPMCAS), grades LG, MG and HG. One-step 3DP was used to process these filaments into enteric printlets incorporating up to 50% drug loading with two different infill percentages (20 and 100%). X-ray Micro Computed Tomography (Micro-CT) analysis revealed that printlets with 20% infill had cavities in the core compared to 100% infill, and that the density of the 50% drug loading printlets was higher than the equivalent formulations loaded with 5% drug. In biorelevant bicarbonate dissolution media, drug release from the printlets was dependent on the polymer composition, drug loading and the internal structure of the formulations. All HPMCAS-based printlets showed delayed drug release properties, and in the intestinal conditions, drug release was faster from the printlets prepared with polymers with a lower pH-threshold: HPMCAS LG > HPMCAS MG > HPMCAS HG. These results confirm that FDM 3D printing makes it possible not only to manufacture delayed release printlets without the need for an outer enteric coating, but it is also feasible to adapt the release profile in response to the personal characteristics of the patient, realizing the full potential of additive manufacturing in the development of personalised dose medicines. Copyright © 2017 Elsevier B.V. All rights reserved.

Tablet splitting: is it worthwhile? Analysis of drug content and weight uniformity for half tablets of 16 commonly used medications in the outpatient setting.

Science.gov (United States)

Helmy, Sally A

2015-01-01

Tablet splitting is a well-established medical practice in clinical settings for multiple reasons, including cost savings and ease of swallowing. However, it does not necessarily result in weight-uniform half tablets. To (a) investigate the effect of tablet characteristics on weight and content uniformity of half tablets, resulting from splitting 16 commonly used medications in the outpatient setting and (b) provide recommendations for safe tablet-splitting prescribing practices. Ten random tablets from each of the selected medications were weighed and split by 5 volunteers (2 men and 3 women aged 25-44 years) using a knife. The selected medications were mirtazapine 30 mg, bromazepam 3 mg, oxcarbazepin 150 mg, sertraline 50 mg, carvedilol 25 mg, bisoprolol fumarate 10 mg, losartan 50 mg, digoxin 0.25 mg, amiodarone HCl 200 mg, metformin HCl 1,000 mg, glimepiride 4 mg, montelukast 10 mg, ibuprofen 600 mg, celecoxib 200 mg, meloxicam 15 mg, and sildenafil citrate 50 mg. The resulting half tablets were evaluated for weight and drug content uniformity in accordance with proxy United States Pharmacopeia (USP) specification (95%-105% for digoxin and 90%-110% for the other 15 drugs). Weight and drug content uniformity were assessed by comparing weight or drug content of the half tablets with one-half of the mean weight or drug content for all whole tablets in the sample. The percentages by which the weight and drug content of each whole tablet or half tablet differed from sample mean values were calculated. Other relevant physical characteristics of the 16 products were measured. A total of 52 of 320 half tablets (16.2%) and 48 of 320 half tablets (15.0%) fell outside of the proxy USP specification for weight and drug content, respectively. Bromazepam, carvedilol, bisoprolol, losartan, digoxin, and meloxicam half tablets failed the weight and content uniformity test; however, the half tablets for the rest of the medications passed the test. Mean percent weight loss after

Actual use of and adherence to ibuprofen 400 mg tablet dosing instructions in a simulated OTC environment
.

Science.gov (United States)

Meeves, Suzanne; Leyva, Rina; Richardson, Clark; Wilson, Brenda; Savastano, David M

2017-07-01

Evaluate adherence of US consumers to proposed label directions for a new 400 mg ibuprofen formulation. In this single-arm, open-label, multicenter, 30-day study simulating an over-the-counter (OTC)-like environment, US analgesic consumers reviewed proposed product packaging for a new 400 mg ibuprofen formulation and made a purchase decision. Purchasers used the product as needed and recorded use over 30 days. Outcomes included the percentage of participants who exhibited correct or acceptable product use for the primary endpoint (not exceeding 1,200 mg/day > 2 times during the study) or secondary endpoint (not exceeding 400 mg/dose > 2 times during the study) and adherence to the labeled dosing interval of 6 - 8 hours. Primary endpoint success was met if the lower bound of the 95% confidence interval (CI) was ≥ 85%. Of 685 purchasers providing use data, correct or acceptable use behavior occurred in 95.2% (95% CI: 93.6%, 96.8%) regarding total daily dose and in 84.4% (95% CI: 81.7%, 87.1%) regarding the number of tablets taken per dosing occasion. Most participants (87.3%) never used > 1,200 mg/day or took > 1 tablet/dose (78.1%). Nearly 43% of subjects re-dosed within 6 hours of the previous dose; of these, ~ 82% re-dosed between the 4- and 6-hour time intervals. Adverse events were consistent with prior ibuprofen 200 mg experience. This study provides evidence that a majority of US consumers would be able to use OTC ibuprofen 400 mg tablets in a manner consistent with product labeling. Misuse rates were low and unlikely to generate an excess risk of clinically important adverse events.
.

Rare earth conversion coating on Mg-8.5Li alloys

International Nuclear Information System (INIS)

Yang Xiaowei; Wang Guixiang; Dong Guojun; Gong Fan; Zhang Milin

2009-01-01

The conversion coating formed by immersion in a solution containing rare earth salt on Mg-8.5Li alloy was studied and the corrosion resistance was evaluated as well. The surface morphology was observed by scanning electron microscopy (SEM), and the chemical composition was characterized by X-ray photoelectron spectroscopy (XPS). The corrosion behaviors of Mg-8.5Li alloy and conversion coating were assessed by means of potentiodynamic polarization curves, electrochemical impedance spectra (EIS) and immersion tests. The experimental results indicated that the coating with cracked morphology was homogeneous. It was mainly composed of La 2 O 3 , CeO 2 , Mn 2 O 3 and MnO 2 as detected by XPS. The results of electrochemical measurements and immersion tests revealed that the rare earth conversion coating possessed better corrosion resistance than bare alloy and chromate conversion coating.

Corrosion protection of Mg-5Li alloy with epoxy coatings containing polyaniline

International Nuclear Information System (INIS)

Shao Yawei; Huang Hui; Zhang Tao; Meng Guozhe; Wang Fuhui

2009-01-01

The protective ability of epoxy coating containing polyaniline (PANI coating) on Mg-5Li alloy in 3.5% NaCl aqueous solution has been studied by means of EIS and electrochemical noise measurements (EN). The results of EN and EIS revealed that the PANI coating protected Mg-5Li alloy from corrosion perfectly. XPS results indicated that the presence of polyaniline changed the chemical structure of the corrosion film on the alloy surface. An analysis of the electrochemical noise data based on stochastic analysis indicated that the corrosion growth probability of Mg-5Li alloy beneath the coating was decreased by the addition of polyaniline.

Development of an automation system for a tablet coater

DEFF Research Database (Denmark)

Ruotsalainen, Mirja; Heinämäki, Jyrki; Rantanen, Jukka

2002-01-01

An instrumentation and automation system for a side-vented pan coater with a novel air-flow rate measurement system for monitoring the film-coating process of tablets was designed and tested. The instrumented coating system was tested and validated by film-coating over 20 pilot-scale batches...... and automated pan-coating system described, including historical data storage capability and a novel air-flow measurement system, is a useful tool for controlling and characterizing the tablet film-coating process. Monitoring of critical process parameters increases the overall coating process efficiency...

Enteric-coated sustained-release nanoparticles by coaxial electrospray: preparation, characterization, and in vitro evaluation

Science.gov (United States)

Hao, Shilei; Wang, Bochu; Wang, Yazhou; Xu, Yingqian

2014-02-01

Enteric-coated formulations can delay the release of drugs until they have passed through the stomach. However, high concentration of drugs caused by rapidly released in the small intestine leads to the intestinal damage, and frequent administration would increase the probability of missing medication and reduce the patient compliance. To solve the above-mentioned problems, aspirin-loaded enteric-coated sustained-release nanoparticles with core-shell structure were prepared via one-step method using coaxial electrospray in this study. Eudragit L100-55 as pH-sensitive polymer and Eudragit RS as sustained-release polymer were used for the outer coating and inner core of the nanoparticles, respectively. The maximum loading capacity of nanoparticles was 23.66 % by changing the flow rate ratio of outer/inner solutions, and the entrapment efficiency was nearly 100 %. Nanoparticles with core-shell structure were observed via fluorescence microscope and transmission electron microscope. And pH-sensitive and sustained drug release profiles were observed in the media with different pH values (1.2 and 6.8). In addition, mild cytotoxicity in vitro was detected, and the nanoparticles could be taken up by Caco-2 cells within 1.0 h in cellular uptake study. These results indicate that prepared enteric-coated sustained-release nanoparticles would be a more safety and effective carrier for oral drug delivery.

Iodine tablets and a nuclear accident

International Nuclear Information System (INIS)

Paile, W.

1992-01-01

Radioactive iodine is one of the major substances released during severe nuclear accidents. Radioactive iodine is easily gasified, and if present in fallout it can enter the lungs, and thereby the circulatory system, with the inhalation of air. Once in a body, radioactive iodine accumulates in the thyroid and may result in tumours in the thyroid and, in extreme cases, impaired thyroid function. Accumulation of radioactive iodine can be prevented by taking non-radioactive, 'cold' iodine as tablets. Iodine tablets dilute the radioactive iodine that has entered the body. A dose of iodine also paralyses the thyroid temporarily by saturating its iodine-carrying capacity. To be useful iodine tablets should be taken immediately when a radioactive emission has occurred. If the tablets are taken too early or too late, they give little protection. Iodine tablets should not be taken just to be on the safe side, since their use may involve harmful side effects. Dosing instructions should also be followed with care. (orig.)

Magnesium substituted hydroxyapatite formation on (Ti,Mg)N coatings produced by cathodic arc PVD technique

International Nuclear Information System (INIS)

Onder, Sakip; Kok, Fatma Nese; Kazmanli, Kursat; Urgen, Mustafa

2013-01-01

In this study, formation of magnesium substituted hydroxyapatite (Ca 10−x Mg x (PO 4 ) 6 (OH) 2 ) on (Ti,Mg)N and TiN coating surfaces were investigated. The (Ti 1−x ,Mg x )N (x = 0.064) coatings were deposited on titanium substrates by using cathodic arc physical vapor deposition technique. TiN coated grade 2 titanium substrates were used as reference to understand the role of magnesium on hydroxyapatite (HA) formation. The HA formation experiments was carried out in simulated body fluids (SBF) with three different concentrations (1X SBF, 5X SBF and 5X SBF without magnesium ions) at 37 °C. The coatings and hydroxyapatite films formed were characterized by scanning electron microscope (SEM), X-ray diffraction (XRD) and FTIR Spectroscopy techniques. The energy dispersive X-ray spectroscopy (EDS) analyses and XRD investigations of the coatings indicated that magnesium was incorporated in the TiN structure rather than forming a separate phase. The comparison between the TiN and (Ti, Mg)N coatings showed that the presence of magnesium in TiN structure facilitated magnesium substituted HA formation on the surface. The (Ti,Mg)N coatings can potentially be used to accelerate the HA formation in vivo conditions without any prior hydroxyapatite coating procedure. - Highlights: • Mg incorporated in (Ti,Mg)N coating structure and did not form a separate phase • Mg dissolution in SBF solution facilitated Mg-substituted hydroxyapatite formation • (Ti,Mg)N acted as Mg-source for Mg-substituted hydroxyapatite formation in SBF

Formulation of Dihydroartemisinin-Piperaquine (DHP Generic Tablet as Antimalarials Drug

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Nanang Yunarto

2016-09-01

Full Text Available The incidence of malaria in Indonesia is about two million cases annually. Dihydroartemisinin-piperaquine (DHP is the first line therapy recommended for uncomplicated malaria treatment, whereas  DHP is still fully imported. The generic DHP tablet formulation has the potential to become the first of DHP drug which is locally produced. This study is aimed to formulate generic DHP film coated tablets for antimalaria drug. Tablets were compressed with the combination of wet granulation for piperaquine phosphate (PQP and direct compression method for DHA and coated with a moisture barier coating material. The parameters to evaluate the quality of DHP tablets are physical properties, assay, and dissolution test. DHA and PQP assay were performed by HPLC method. The dissolution testing was conducted by in house method using HCl 0.1 N medium. The result shows physical properties of film-coated tablets meet the requirement, i.e. uniform weight, 7.0-8.5 kp hardness, 0.02% friability and 3 minute 22 seconds disintegration. The assay to determine  DHA in tablet was 95.17% and PQP was 97.05%. The result of dissolution testing shows the content of DHA and PQP in the tablet were 113.51% and 96.55%, respesctively. The formulation which is developed meets the general requirement of API in tablet 90–110% and dissolution requirement >75%.

Bioequivalence of two film-coated tablets of imatinib mesylate 400 mg: a randomized, open-label, single-dose, fasting, two-period, two-sequence crossover comparison in healthy male South American volunteers.

Science.gov (United States)

Parrillo-Campiglia, Susana; Ercoli, Mónica Cedres; Umpierrez, Ofelia; Rodríguez, Patricia; Márquez, Sara; Guarneri, Carolina; Estevez-Parrillo, Francisco T; Laurenz, Marilena; Estevez-Carrizo, Francisco E

2009-10-01

Imatinib is a tyrosine kinase inhibitor that has been established as a highly effective therapy for chronic myelogenous leukemia and gastrointestinal stromal tumors. A new generic, once-daily 400-mg tablet of imatinib has been developed by a pharmaceutical company in Argentina, where the regulatory standard for marketing authorization of an imatinib generic is in vitro dissolution testing. The aim of this study was to assess the bioequivalence of a new generic film-coated test tablet formulation versus a film-coated reference tablet formulation of imatinib 400 mg. The local manufacturer seeks to validate the in vitro performance of this new formulation with a bioequivalence study. A randomized, open-label, single-dose, fasting, 2-period, 2-sequence crossover design with a 2-week washout period was used in this study. The study population consisted of healthy male South American (Uruguayan) volunteers, who were assigned in a 1:1 ratio to a randomized sequence (test-reference or reference-test). In each period, the test or reference formulation was administered after an overnight fast. During the 72-hour follow-up period, participants were monitored for vital signs and symptoms. Blood samples were collected at 15 time points, including baseline, until 72 hours. Physical examination and laboratory tests (blood, urine) were repeated 1 week after study completion. A noncompartmental model was used to determine the pharmacokinetic parameters of imatinib. The 90% CIs of the test/reference ratios for AUC(0-infinity) and C(max) were determined; the test and reference formulations were considered bioequivalent if the 90% CIs were between 0.80 and 1.25. Adverse events were assessed by a nurse who administered a questionnaire while the healthy volunteers were admitted in the unit. The bioequivalence study was conducted in 30 Uruguayan male volunteers. Demographic characteristics (mean [SD]) included age, 27.8 (6.5) years; weight, 71.2 (9.8) kg; height, 1.71 (0.09) m; and body

Pharmacokinetic bioequivalence studies of a fixed-dose combination of tamsulosin and dutasteride in healthy volunteers.

Science.gov (United States)

Fossler, Michael J; Collins, David A; Thompson, Meg M; Nino, Antonio; Bianco, Joseph J; Chetty, Dushen

2014-05-01

The combination of dutasteride and tamsulosin may be more effective for the treatment of symptomatic benign prostatic hyperplasia than either treatment alone. We report the results of three pharmacokinetics and tolerability studies, which used a dutasteride/tamsulosin HCl (0.5 mg/0.2 mg) fixed-dose combination (FDC) capsules containing a small dutasteride soft gelatin capsule (smaller than commercial Avodart™) and modified-release tamsulosin pellets that have different amounts of enteric coating. These studies compared the test products to commercial Avodart™ (dutasteride 0.5 mg) and two different commercial tamsulosin HCl 0.2 mg products, Harnal™ Capsules or Harnal-D™ Tablets, which are reportedly bioequivalent to each other. All three studies were randomized single-dose studies in healthy male adults. Study 1 [N = 86 (NCT01254071)] was a two-period crossover study of a dutasteride/tamsulosin HCl FDC versus coadministered Avodart™ and Harnal-D™ Tablets. The pharmacokinetics of both dutasteride and tamsulosin were studied. Study 2 [N = 27 (NCT01471678)] was a four-period crossover study of dutasteride/tamsulosin HCl FDC formulations versus Avodart™ and Harnal™ Capsules or Harnal-D™ Tablets. Only the pharmacokinetics of tamsulosin were studied. Study 3 [N = 40 (NCT01495026)] was a two-period study of dutasteride/tamsulosin HCl FDC formulations versus coadministered Avodart™ and Harnal-D™ Tablets. In this study, only the pharmacokinetics of tamsulosin were studied. Study 2 assessed fed-state pharmacokinetics. Studies 1 and 3 assessed fed- and fasted-state pharmacokinetics. All dutasteride/tamsulosin HCl FDC formulations and coadministered treatments were well-tolerated. In Study 1, the FDC dutasteride was bioequivalent to Avodart™ coadministered with tamsulosin under fed and fasted conditions. In Study 1, the FDC tamsulosin had a slower release than commercial Harnal-D™ Tablets coadministered with dutasteride (fed and fasted

Development and properties of duplex MgF2/PCL coatings on biodegradable magnesium alloy for biomedical applications.

Science.gov (United States)

Makkar, Preeti; Kang, Hoe Jin; Padalhin, Andrew R; Park, Ihho; Moon, Byoung-Gi; Lee, Byong Taek

2018-01-01

The present work addresses the performance of polycaprolactone (PCL) coating on fluoride treated (MgF2) biodegradable ZK60 magnesium alloy (Mg) for biomedical application. MgF2 conversion layer was first produced by immersing Mg alloy substrate in hydrofluoric acid solution. The outer PCL coating was then prepared using dip coating technique. Morphology, elements profile, phase structure, roughness, mechanical properties, invitro corrosion, and biocompatibility of duplex MgF2/PCL coating were then characterized and compared to those of fluoride coated and uncoated Mg samples. The invivo degradation behavior and biocompatibility of duplex MgF2/PCL coating with respect to ZK60 Mg alloy were also studied using rabbit model for 2 weeks. SEM and TEM analysis showed that the duplex coating was uniform and comprised of porous PCL film (~3.3 μm) as upper layer with compact MgF2 (~2.2 μm) as inner layer. No significant change in microhardness was found on duplex coating compared with uncoated ZK60 Mg alloy. The duplex coating showed improved invitro corrosion resistance than single layered MgF2 or uncoated alloy samples. The duplex coating also resulted in better cell viability, cell adhesion, and cell proliferation compared to fluoride coated or uncoated alloy. Preliminary invivo studies indicated that duplex MgF2/PCL coating reduced the degradation rate of ZK60 Mg alloy and exhibited good biocompatibility. These results suggested that duplex MgF2/PCL coating on magnesium alloy might have great potential for orthopedic applications.

The Formulation of Diclofenac Sodium Hydrogel Tablets | Onyechi ...

African Journals Online (AJOL)

The dissolution data fitted to Higuchi and Hixson-Crowell equations indicating the existence of diffusion mechanism controlling diclofenac release from the tablets. Keywords: Sustained release, diclofenac sodium hydrogel tablets, Voltarol retard tablets, film coating, dissolution profiles. Nigerian Journal of Pharmaceutical ...

Estudio de estabilidad de tabletas de propiltiouracilo 50 mg Study of the 50 mg Propylthiouracil tablets stability

Directory of Open Access Journals (Sweden)

María Olga Valdés Bendoyro

2010-03-01

Full Text Available Se desarrolló el estudio de estabilidad de las tabletas de propiltiouracilo 50 mg y se determinó su fecha de vencimiento. Este estudio se realizó por los métodos de vida de estante y de estabilidad acelerada mediante cromatografía líquida de alta eficiencia, validados en el Centro de Investigación y Desarrollo de Medicamentos. El estudio de vida de estante se desarrolló por un periodo de 24 meses a temperatura ambiente; mientras que el estudio de estabilidad acelerada se efectuó sometiendo el producto a la influencia de la luz, la humedad y la temperatura; se realizó el análisis durante 3 meses, para los 2 primeros y durante 6 meses para el estudio de la temperatura. La formulación de propiltiouracilo tabletas 50 mg cumplió con las especificaciones de calidad descritas en la farmacopea. Los resultados del estudio de estabilidad por vida de estante después de transcurridos los 24 meses indicaron que el producto mantenía los parámetros que determinan su calidad durante ese tiempo, y en los estudios acelerados no se observó degradación significativa del producto. Se estableció 2 años como fecha de vencimiento en las condiciones señaladas.Autors developed a stability study of 50 mg Propylthiouracil tablets and determination of its expiry date. This study was conducted by fixed life methods and of accelerated stability by high-performance liquid chromatography, validated in Drugs Research and Development Center. Fixed life study was conducted during 24 months at room temperature; whereas the accelerated stability study was conducted exposing the product to light influence, humidity and temperature; during 3 months a analysis was performed for the two first ones and over 6 months in the case of temperature study. Propylthiouracil formula (50 mg tablets fulfilled the quality specifications described in Pharmacopeia. Results of stability study by fixed life after 24 monhts showed that thr product maintain the parameter determining

Substantial reduction of inappropriate tablet splitting with computerised decision support: a prospective intervention study assessing potential benefit and harm

Directory of Open Access Journals (Sweden)

Quinzler Renate

2009-06-01

Full Text Available Abstract Background Currently ambulatory patients break one in four tablets before ingestion. Roughly 10% of them are not suitable for splitting because they lack score lines or because enteric or modified release coating is destroyed impairing safety and effectiveness of the medication. We assessed impact and safety of computerised decision support on the inappropriate prescription of split tablets. Methods We performed a prospective intervention study in a 1680-bed university hospital. Over a 15-week period we evaluated all electronically composed medication regimens and determined the fraction of tablets and capsules that demanded inappropriate splitting. In a subsequent intervention phase of 15 weeks duration for 10553 oral drugs divisibility characteristics were indicated in the system. In addition, an alert was generated and displayed during the prescription process whenever the entered dosage regimen demanded inappropriate splitting (splitting of capsules, unscored tablets, or scored tablets unsuitable for the intended fragmentation. Results During the baseline period 12.5% of all drugs required splitting and 2.7% of all drugs (257/9545 required inappropriate splitting. During the intervention period the frequency of inappropriate splitting was significantly reduced (1.4% of all drugs (146/10486; p = 0.0008. In response to half of the alerts (69/136 physicians adjusted the medication regimen. In the other half (67/136 no corrections were made although a switch to more suitable drugs (scored tablets, tablets with lower strength, liquid formulation was possible in 82% (55/67. Conclusion This study revealed that computerised decision support can immediately reduce the frequency of inappropriate splitting without introducing new safety hazards.

Magnesium-Based Sacrificial Anode Cathodic Protection Coatings (Mg-Rich Primers for Aluminum Alloys

Directory of Open Access Journals (Sweden)

Michael D. Blanton

2012-09-01

Full Text Available Magnesium is electrochemically the most active metal employed in common structural alloys of iron and aluminum. Mg is widely used as a sacrificial anode to provide cathodic protection of underground and undersea metallic structures, ships, submarines, bridges, decks, aircraft and ground transportation systems. Following the same principle of utilizing Mg characteristics in engineering advantages in a decade-long successful R&D effort, Mg powder is now employed in organic coatings (termed as Mg-rich primers as a sacrificial anode pigment to protect aerospace grade aluminum alloys against corrosion. Mg-rich primers have performed very well on aluminum alloys when compared against the current chromate standard, but the carcinogenic chromate-based coatings/pretreatments are being widely used by the Department of Defense (DoD to protect its infrastructure and fleets against corrosion damage. Factors such as reactivity of Mg particles in the coating matrix during exposure to aggressive corrosion environments, interaction of atmospheric gases with Mg particles and the impact of Mg dissolution, increases in pH and hydrogen gas liberation at coating-metal interface, and primer adhesion need to be considered for further development of Mg-rich primer technology.

Molybdate and molybdate/permanganate conversion coatings on Mg-8.5Li alloy

International Nuclear Information System (INIS)

Wang Guixiang; Zhang Milin; Wu Ruizhi

2012-01-01

A novel environment-friendly conversion coating for Mg-8.5Li alloy was obtained by immersing in a solution of molybdate. The concentration of ammonium molybdate and the addition of potassium permanganate were discussed in this experiment. The surface morphology of the conversion coatings was observed by scanning electron microscopy (SEM), and the chemical composition was investigated by X-ray photoelectron spectroscopy (XPS) and X-ray diffraction (XRD). The corrosion resistance of Mg-8.5Li alloy and conversion coatings were investigated by means of potentiodynamic polarization, electrochemical impedance spectroscopy (EIS) and weight loss measurement. The results showed that the coatings with cracked morphology were homogeneous and uniform. The conversion coatings were mainly composed of metal-oxide as detected by XPS. The results of electrochemical measurement and weight loss measurement revealed that the molybdate conversion coating had better corrosion resistance than bare alloy and chromate conversion coating, and the molybdate/permanganate conversion coating had lower corrosion current density and higher coating resistance than the molybdate conversion coating.

Molybdate and molybdate/permanganate conversion coatings on Mg-8.5Li alloy

Energy Technology Data Exchange (ETDEWEB)

Wang Guixiang, E-mail: wgx0357@126.com [Key Laboratory of Superlight Material and Surface Technology, College of Materials Science and Chemical Engineering, Harbin Engineering University, Harbin 150001 (China); Zhang Milin; Wu Ruizhi [Key Laboratory of Superlight Material and Surface Technology, College of Materials Science and Chemical Engineering, Harbin Engineering University, Harbin 150001 (China)

2012-01-15

A novel environment-friendly conversion coating for Mg-8.5Li alloy was obtained by immersing in a solution of molybdate. The concentration of ammonium molybdate and the addition of potassium permanganate were discussed in this experiment. The surface morphology of the conversion coatings was observed by scanning electron microscopy (SEM), and the chemical composition was investigated by X-ray photoelectron spectroscopy (XPS) and X-ray diffraction (XRD). The corrosion resistance of Mg-8.5Li alloy and conversion coatings were investigated by means of potentiodynamic polarization, electrochemical impedance spectroscopy (EIS) and weight loss measurement. The results showed that the coatings with cracked morphology were homogeneous and uniform. The conversion coatings were mainly composed of metal-oxide as detected by XPS. The results of electrochemical measurement and weight loss measurement revealed that the molybdate conversion coating had better corrosion resistance than bare alloy and chromate conversion coating, and the molybdate/permanganate conversion coating had lower corrosion current density and higher coating resistance than the molybdate conversion coating.

Molecular insights into shellac film coats from different aqueous shellac salt solutions and effect on disintegration of enteric-coated soft gelatin capsules.

Science.gov (United States)

Al-Gousous, J; Penning, M; Langguth, P

2015-04-30

The purpose of this investigation was to study the effect of using different salts of shellac on the disintegration properties of shellac-based enteric coatings. In the last two decades, shellac has been increasingly used as an aqueous solution for enteric coating purposes, with the ammonium salt being the form typically used. Little investigation has been performed on using other salts, and therefore, this was the focus of our work. Enteric coatings, based on different shellac salts (ammonium, sodium, potassium and composite ammonium-sodium), were applied onto soft gelatin capsules. Disintegration testing of the coated soft gelatin capsules showed that alkali metal salts promote faster disintegration than ammonium salts. In order to determine the causes behind these differences, the solubility, thermal and spectroscopic properties of films cast from the different salts were investigated. The results show that films cast from ammonium-based salts of shellac are, unlike those cast from alkali metal-based salts, water-insoluble. Spectroscopic evidence suggests that this might be due to partial salt dissociation resulting in loss of ammonium as ammonia and reduced degree of shellac ionization during drying. In addition, oxidation of shellac aldehyde groups of the ammonium-based shellac salts could also play a role. And possible higher extent of shellac hydrolysis during the preparation of alkali metal salts might also be a factor. Therefore, the nature of the shellac salt used in the preparation of shellac-based aqueous coating solutions is a significant formulation factor affecting product performance. Copyright © 2014 Elsevier B.V. All rights reserved.

Microwave-assisted synthesis of lanthanum conversion coating on Mg-Li alloy and its corrosion resistance

International Nuclear Information System (INIS)

Song Dalei; Jing Xiaoyan; Wang Jun; Lu Shanshan; Yang Piaoping; Wang Yanli; Zhang Milin

2011-01-01

Graphical abstract: Highlights: → The method of microwave is used to synthesize lanthanum conversion coating. → Lanthanum conversion coating on Mg-Li alloy was studied. → Different conditions between room temperature and microwave were compared. → The corrosion behavior of lanthanum conversion coatings was studied. → The corrosion mechanism of lanthanum conversion coatings was studied. - Abstract: Lanthanum-based conversion coating on Mg-Li alloy has been prepared by a microwave-assisted method. X-ray diffractions (XRD) indicate that the intermetallic compounds of lanthanum are formed on Mg-Li alloy surface. Scanning electron microscopy (SEM) images show that the coating has different morphologies and special structures. The corrosion resistance was assessed by means of potentiodynamic polarization curves and electrochemical impedance spectra (EIS). The results indicate that this coating significantly reduces the corrosion rate of Mg-Li alloy in NaCl solution. A comparing experiment indicates that the coating prepared by microwave-assisted process has superior corrosion resistance to the coating obtained at room temperature.

Comparison study of different coatings on degradation performance and cell response of Mg-Sr alloy

International Nuclear Information System (INIS)

Shangguan, Yongming; Sun, Lina; Wan, Peng; Tan, Lili; Wang, Chengyue; Fan, Xinmin; Qin, Ling; Yang, Ke

2016-01-01

To solve the problem of rapid degradation for magnesium-based implants, surface modification especially coating method is widely studied and showed the great potential for clinical application. However, as concerned to the further application and medical translation for biodegradable magnesium alloys, there are still lack of data and comparisons among different coatings on their degradation and biological properties. This work studied three commonly used coatings on Mg-Sr alloy, including micro-arc oxidation coating, electrodeposition coating and chemical conversion coating, and compared these coatings for requirements of favorable degradation and biological performances, how each of these coating systems has performed. Finally the mechanism for the discrepancy between these coatings is proposed. The results indicate that the micro-arc oxidation coating on Mg-Sr alloy exhibited the best corrosion resistance and cell response among these coatings, and is proved to be more suitable for the orthopedic application. - Highlights: • The MAO, PED and Sr-P coating were fabricated on Mg-Sr alloy to evaluate the degradation. • The MAO coating showed the greatest degradation performance among these three coatings. • The PED coating exhibited worse corrosion resistance even than Mg-Sr substrate. • The value of cell proliferation and ALP activity were ranked in the following order: MAO > Sr-P > PED.

Comparison study of different coatings on degradation performance and cell response of Mg-Sr alloy

Energy Technology Data Exchange (ETDEWEB)

Shangguan, Yongming [Department of Materials Science and Engineering, Nanjing University of Science and Technology, Nanjing 210094 (China); Institute of Metal Research, Chinese Academy of Sciences, 72 Wenhua Road, Shenyang 110016 (China); Sun, Lina [Jinzhou Medical University, Jinzhou 121000 (China); Wan, Peng, E-mail: pwan@imr.ac.cn [Institute of Metal Research, Chinese Academy of Sciences, 72 Wenhua Road, Shenyang 110016 (China); Department of Orthopaedics and Traumatology, The Chinese University of Hong Kong, Hong Kong SAR (China); Tan, Lili [Institute of Metal Research, Chinese Academy of Sciences, 72 Wenhua Road, Shenyang 110016 (China); Wang, Chengyue [Jinzhou Medical University, Jinzhou 121000 (China); Fan, Xinmin [Department of Materials Science and Engineering, Nanjing University of Science and Technology, Nanjing 210094 (China); Qin, Ling [Department of Orthopaedics and Traumatology, The Chinese University of Hong Kong, Hong Kong SAR (China); Yang, Ke, E-mail: kyang@imr.ac.cn [Institute of Metal Research, Chinese Academy of Sciences, 72 Wenhua Road, Shenyang 110016 (China)

2016-12-01

To solve the problem of rapid degradation for magnesium-based implants, surface modification especially coating method is widely studied and showed the great potential for clinical application. However, as concerned to the further application and medical translation for biodegradable magnesium alloys, there are still lack of data and comparisons among different coatings on their degradation and biological properties. This work studied three commonly used coatings on Mg-Sr alloy, including micro-arc oxidation coating, electrodeposition coating and chemical conversion coating, and compared these coatings for requirements of favorable degradation and biological performances, how each of these coating systems has performed. Finally the mechanism for the discrepancy between these coatings is proposed. The results indicate that the micro-arc oxidation coating on Mg-Sr alloy exhibited the best corrosion resistance and cell response among these coatings, and is proved to be more suitable for the orthopedic application. - Highlights: • The MAO, PED and Sr-P coating were fabricated on Mg-Sr alloy to evaluate the degradation. • The MAO coating showed the greatest degradation performance among these three coatings. • The PED coating exhibited worse corrosion resistance even than Mg-Sr substrate. • The value of cell proliferation and ALP activity were ranked in the following order: MAO > Sr-P > PED.

Bio-Corrosion Behavior of Ceramic Coatings Containing Hydroxyapatite on Mg-Zn-Ca Magnesium Alloy

Directory of Open Access Journals (Sweden)

Hong-Yan Ding

2018-04-01

Full Text Available Ceramic coatings containing hydroxyapatite (HA were fabricated on a biodegradable Mg66Zn29Ca5 magnesium alloy through micro-arc oxidation by adding HA particles into the electrolytes. The phase composition and surface morphology of the coatings were characterized by X-ray diffraction and scanning electron microscopy analyses, respectively. Electrochemical experiments and immersion tests were performed in Hank’s solution at 37 °C to measure the corrosion resistance of the coatings. Blood compatibility was evaluated by in vitro blood platelet adhesion tests and static water contact angle measurement. The results show that the typical ceramic coatings with a porous structure were prepared on the magnesium alloy surface with the main phases of MgO and MgSiO3 and a small amount of Mg3(PO42 and HA. The optimal surface morphology appeared at HA concentration of 0.4 g/L. The electrochemical experiments and immersion tests reveal a significant improvement in the corrosion resistance of the ceramic coatings containing HA compared with the coatings without HA or bare Mg66Zn29Ca5 magnesium alloy. The static water contact angle of the HA-containing ceramic coatings is 18.7°, which is lower than that of the coatings without HA (40.1°. The in vitro blood platelet adhesion tests indicate that the HA-containing ceramic coatings possess improved blood compatibility compared with the coatings without HA. Utilizing HA-containing ceramic coatings may be an effective way to improve the surface biocompatibility and corrosion resistance of magnesium alloys.

A novel biodegradable nicotinic acid/calcium phosphate composite coating on Mg-3Zn alloy

Energy Technology Data Exchange (ETDEWEB)

Song, Yingwei, E-mail: ywsong@imr.ac.cn; Shan, Dayong; Han, En-Hou

2013-01-01

A novel biodegradable composite coating is prepared to reduce the biodegradation rate of Mg-3Zn alloy. The Mg-3Zn substrate is first immersed into 0.02 mol L{sup -1} nicotinic acid (NA) solution, named as vitamin B{sub 3}, to obtain a pretreatment film, and then the electrodeposition of calcium phosphate coating with ultrasonic agitation is carried out on the NA pretreatment film to obtain a NA/calcium phosphate composite coating. Surface morphology is observed by scanning electron microscopy (SEM). Chemical composition is determined by X-ray diffraction (XRD) and EDX. Protection property of the coatings is evaluated by electrochemical tests. The biodegradable behavior is investigated by immersion tests. The results indicate that a thin but compact bottom layer can be obtained by NA pretreatment. The electrodeposition calcium phosphate coating consists of many flake particles and ultrasonic agitation can greatly improve the compactness of the coating. The composite coating is biodegradable and can reduce the biodegradation rate of Mg alloys in stimulated body fluid (SBF) for twenty times. The biodegradation process of the composite coating can be attributed to the gradual dissolution of the flake particles into chippings. - Highlights: Black-Right-Pointing-Pointer NA/calcium phosphate composite coating is prepared to protect Mg-3Zn alloy implant. Black-Right-Pointing-Pointer Nicotinic acid (vitamin B{sub 3}) is available to obtain a protective bottom film. Black-Right-Pointing-Pointer Ultrasonic agitation greatly improves the compactness of calcium phosphate coating. Black-Right-Pointing-Pointer The composite coating can reduce the biodegradation rate of Mg-3Zn twenty times. Black-Right-Pointing-Pointer The composite coating is biodegraded by the dissolution of flakes into chippings.

Nanocontainer-Enhanced Self-Healing for Corrosion-Resistant Ni Coating on Mg Alloy.

Science.gov (United States)

Xie, Zhi-Hui; Li, Dan; Skeete, Zakiya; Sharma, Anju; Zhong, Chuan-Jian

2017-10-18

The ability to manipulate the functionalization of Ni coating is of great importance in improving the corrosion resistance of magnesium (Mg) alloy for many industrial applications. In the present work, MCM-41 type mesoporous silica nanocontainers (MSNs) loaded with corrosion inhibitor (NaF) were synthesized and employed as smart reinforcements to enhance the integrity and corrosion inhibition of the Ni coating. The incorporation of the F-loaded MSNs (F@MSNs) to enhance the corrosion resistant capacity of a metallic coating is reported for the first time. The mesoporous structures of the as-prepared MSNs and F@MSNs were confirmed by transmission electron microscopy (TEM), small angle X-rays scattering (SAXS), and N 2 adsorption-desorption isotherms. The X-ray photoelectron spectroscopy (XPS) data demonstrated the successful immobilization of fluoride ion on the MSNs and formation of a magnesium fluoride (MgF 2 ) protective film at the corrosion sites of the Mg alloy upon soaking in a F@MSNs-containing NaCl solution. The results from potentiodynamic polarization (PDP) and electrochemical impedance spectroscopy (EIS) for both bare Mg alloy and Ni coatings with and without F@MSNs have revealed a clear decrease in corrosion rate in a corrosive solution for a long-time immersion due to the introduction of F@MSNs. These findings open new opportunities in the exploration of self-healing metallic coatings for highly enhanced anticorrosion protection of Mg alloy.

Bioactive glass–ceramic coating for enhancing the in vitro corrosion resistance of biodegradable Mg alloy

International Nuclear Information System (INIS)

Ye Xinyu; Cai Shu; Dou Ying; Xu Guohua; Huang Kai; Ren Mengguo; Wang Xuexin

2012-01-01

Highlights: ► Sol–gel derived 45S5 glass–ceramic coating was prepared on Mg alloy substrate. ► The corrosion resistance of glass–ceramic coated Mg alloy was markedly improved. ► The corrosion behavior of the coated sample varied due to the cracking of coating. - Abstract: In this work, a bioactive 45S5 glass–ceramic coating was synthesized on magnesium (Mg) alloy substrate by using a sol–gel dip-coating method, to improve the initial corrosion resistance of AZ31 Mg alloy. The surface morphology and phase composition of the glass–ceramic coating were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). The coating composed of amorphous phase and crystalline phase Na 2 Ca 2 Si 3 O 9 , with the thickness of ∼1.0 μm, exhibited a uniform and crack-free surface morphology. The corrosion behavior of the uncoated and coated Mg alloy substrates was investigated by the electrochemical measurements and immersion tests in simulated body fluid (SBF). Potentiodynamic polarization tests recorded an increase of potential (E corr ) form −1.60 V to −1.48 V, and a reduction of corrosion current density (i corr ) from 4.48 μA cm −2 to 0.16 μA cm −2 , due to the protection provided by the glass–ceramic coating. Immersion tests also showed the markedly improved corrosion resistance of the coated sample over the immersion period of 7 days. Moreover, after 14 days of immersion in SBF, the corrosion resistance of the coated sample declined due to the cracking of the glass–ceramic coating, which was confirmed by electrochemical impedance spectroscopy (EIS) analysis. The results suggested that the 45S5 glass–ceramic coated Mg alloy could provide a suitable corrosion behavior for use as degradable implants.

Preparation of venlafaxine hydrochloride sustained-release tablets

Directory of Open Access Journals (Sweden)

GUO Lingling

2013-08-01

Full Text Available To prepare venlafxine hydrochloride sustained-release tablets.Hydroxypropylmethyl cellulose(HPMC and methyl cellulose(MC were used as main materials to prepare sustained-release tablets of velafaxine hydrochloride and the influence of important factors on in vitro release curves of venlafaxine hydrochloride sustained-release tablets was investigated.Results:The optimal prescription included 100 mg HPMC,25 mg MC,and 2.5% glidant in one tablet prepared with 30kN.The tablets were prepared with the method of wet granulation by NO.16 mesh sieve.The tablets exhibited good sustained-release property in phosphate buffered solution (pH=6.8.The as-prepared venlafxine hydrochloride sustained-release tablets have good sustained-release property.

Mechanism by Which Magnesium Oxide Suppresses Tablet Hardness Reduction during Storage.

Science.gov (United States)

Sakamoto, Takatoshi; Kachi, Shigeto; Nakamura, Shohei; Miki, Shinsuke; Kitajima, Hideaki; Yuasa, Hiroshi

2016-01-01

This study investigated how the inclusion of magnesium oxide (MgO) maintained tablet hardness during storage in an unpackaged state. Tablets were prepared with a range of MgO levels and stored at 40°C with 75% relative humidity for up to 14 d. The hardness of tablets prepared without MgO decreased over time. The amount of added MgO was positively associated with tablet hardness and mass from an early stage during storage. Investigation of the water sorption properties of the tablet components showed that carmellose water sorption correlated positively with the relative humidity, while MgO absorbed and retained moisture, even when the relative humidity was reduced. In tablets prepared using only MgO, a petal- or plate-like material was observed during storage. Fourier transform infrared spectrophotometry showed that this material was hydromagnesite, produced when MgO reacts with water and CO2. The estimated level of hydromagnesite at each time-point showed a significant negative correlation with tablet porosity. These results suggested that MgO suppressed storage-associated softening by absorbing moisture from the environment. The conversion of MgO to hydromagnesite results in solid bridge formation between the powder particles comprising the tablets, suppressing the storage-related increase in volume and increasing tablet hardness.

Pharmacokinetics of colon-specific pH and time-dependent flurbiprofen tablets.

Science.gov (United States)

Vemula, Sateesh Kumar; Veerareddy, Prabhakar Reddy; Devadasu, Venkat Ratnam

2015-09-01

Present research deals with the development of compression-coated flurbiprofen colon-targeted tablets to retard the drug release in the upper gastro intestinal system, but progressively release the drug in the colon. Flurbiprofen core tablets were prepared by direct compression method and were compression coated using sodium alginate and Eudragit S100. The formulation is optimized based on the in vitro drug release study and further evaluated by X-ray imaging and pharmacokinetic studies in healthy humans for colonic delivery. The optimized formulation showed negligible drug release (4.33 ± 0.06 %) in the initial lag period followed by progressive release (100.78 ± 0.64 %) for 24 h. The X-ray imaging in human volunteers showed that the tablets reached the colon without disintegrating in the upper gastrointestinal tract. The C max of colon-targeted tablets was 12,374.67 ng/ml at T max 10 h, where as in case of immediate release tablets the C max was 15,677.52 ng/ml at T max 3 h, that signifies the ability of compression-coated tablets to target the colon. Development of compression-coated tablets using combination of time-dependent and pH-sensitive approaches was suitable to target the flurbiprofen to colon.

Comparative effects of enteric-coated pancreatin microsphere therapy after conventional and pylorus-preserving pancreatoduodenectomy

NARCIS (Netherlands)

Bruno, M. J.; Borm, J. J.; Hoek, F. J.; Delzenne, B.; Hofmann, A. F.; de Goeij, J. J.; van Royen, E. A.; van Gulik, T. M.; de Wit, L. T.; Gouma, D. J.; van Leeuwen, D. J.; Tytgat, G. N.

1997-01-01

BACKGROUND: A comparative study was performed between patients with exocrine pancreatic insufficiency after conventional pancreatoduodenectomy (Whipple's procedure) and pylorus-preserving pancreatoduodenectomy (PPPD). In these patients the pharmacodynamics of 2-mm enteric-coated pancreatin

Characterization and corrosion property of nano-rod-like HA on fluoride coating supported on Mg-Zn-Ca alloy.

Science.gov (United States)

Feng, Yashan; Zhu, Shijie; Wang, Liguo; Chang, Lei; Yan, Bingbing; Song, Xiaozhe; Guan, Shaokang

2017-06-01

The poor corrosion resistance of biodegradable magnesium alloys is the dominant factor that limits their clinical application. In this study, to deal with this challenge, fluoride coating was prepared on Mg-Zn-Ca alloy as the inner coating and then hydroxyapatite (HA) coating as the outer coating was deposited on fluoride coating by pulse reverse current electrodeposition (PRC-HA/MgF 2 ). As a comparative study, the microstructure and corrosion properties of the composite coating with the outer coating fabricated by traditional constant current electrodeposition (TED-HA/MgF 2 ) were also investigated. Scanning electron microscopy (SEM) images of the coatings show that the morphology of PRC-HA/MgF 2 coating is dense and uniform, and presents nano-rod-like structure. Compared with that of TED-HA/MgF 2 , the corrosion current density of Mg alloy coated with PRC-HA/MgF 2 coatings decreases from 5.72 × 10 -5 A/cm 2 to 4.32 × 10 -7 A/cm 2 , and the corrosion resistance increases by almost two orders of magnitude. In immersion tests, samples coated with PRC-HA/MgF 2 coating always show the lowest hydrogen evolution amount, and could induce deposition of the hexagonal structure-apatite on the surface rapidly. The results show that the corrosion resistance and the bioactivity of the coatings have been improved by adopting double-pulse current mode in the process of preparing HA on fluoride coating, and the PRC-HA/MgF 2 coating is worth of further investigation.

Evaluation of the disintegration properties of commercial famotidine 20 mg orally disintegrating tablets using a simple new test and human sensory test.

Science.gov (United States)

Harada, Tsutomu; Narazaki, Ryuichi; Nagira, Shinsuke; Ohwaki, Takayuki; Aoki, Shigeru; Iwamoto, Kiyoshi

2006-08-01

The purpose of this study was to demonstrate the usefulness and broad-applicability of a simple disintegration test method for orally disintegrating tablets (ODT). Eight types of commercial famotidine 20 mg orally disintegrating tablets with different physical properties (formulation, manufacturing method, tablet weight, shape, diameter, thickness, etc.), were used. Disintegration times of these tablets were evaluated employing human sensory test, conventional disintegration test, and the new proposed disintegration test. The human sensory test was performed in 5 healthy volunteers. In the conventional disintegration test, the disintegration apparatus described in the Japanese Pharmacopeia (JP 1(st)) was used. Our proposed new test which is characterized by a rotating shaft with a low weight (10, 15 g) and rotation speed (10, 25, 50 rpm) was evaluated using tablets with and without storage under severe conditions (60 degrees C/75%RH for 1 week). The disintegration times of famotidine 20 mg orally disintegrating tablets in human sensory test varied from 9 to 32 s. In contrast, disintegration times in the conventional test were prolonged to over 300 s. Disintegration times in the new proposed test were close to those in human sensory test. Especially, when the new test was conducted with 15 or 10 g weight and 25 rpm, the slope (human sensory test vs. new proposed test) was almost 1. We were able to demonstrate that the new proposed test was useful to estimate the actual human disintegration time.

Construction of a novel pH-sensitive drug release system from mesoporous silica tablets coated with Eudragit

Science.gov (United States)

Xu, Yingpu; Qu, Fengyu; Wang, Yu; Lin, Huiming; Wu, Xiang; Jin, Yingxue

2011-03-01

A novel pH-sensitive drug release system has been established by coating Eudragit (Eud) on drug-loaded mesoporous silica (MS) tablets. The release rate of ibuprofen (IBU) from the MS was retarded by coating with Eudragit S-100, and the higher retardation was due to the increase of coating concentration and the coating layers. The target position of the release depended on the pH of the release medium, which was confirmed by the drug release from IBU/MS/Eud increasing rapidly with the change of medium pH from 1.2 to 7.4. This drug delivery system could prohibit irritant drug from leaking in the stomach and make it only release in the intestine. The loaded and unloaded drug samples were characterized by powder X-ray diffraction (XRD), Fourier transform infrared spectrometer (FTIR), N 2 adsorption/desorption, scanning electron microscopy (SEM), and transmission electron microscopy (TEM).

Bioactive glass-ceramic coating for enhancing the in vitro corrosion resistance of biodegradable Mg alloy

Energy Technology Data Exchange (ETDEWEB)

Ye Xinyu [Key Laboratory for Advanced Ceramics and Machining Technology of Ministry of Education, Tianjin University, Tianjin 300072 (China); Cai Shu, E-mail: caishu@tju.edu.cn [Key Laboratory for Advanced Ceramics and Machining Technology of Ministry of Education, Tianjin University, Tianjin 300072 (China); Dou Ying [Key Laboratory for Advanced Ceramics and Machining Technology of Ministry of Education, Tianjin University, Tianjin 300072 (China); Xu Guohua [Shanghai Changzheng Hospital, Shanghai 200003 (China); Huang Kai; Ren Mengguo; Wang Xuexin [Key Laboratory for Advanced Ceramics and Machining Technology of Ministry of Education, Tianjin University, Tianjin 300072 (China)

2012-10-15

Highlights: Black-Right-Pointing-Pointer Sol-gel derived 45S5 glass-ceramic coating was prepared on Mg alloy substrate. Black-Right-Pointing-Pointer The corrosion resistance of glass-ceramic coated Mg alloy was markedly improved. Black-Right-Pointing-Pointer The corrosion behavior of the coated sample varied due to the cracking of coating. - Abstract: In this work, a bioactive 45S5 glass-ceramic coating was synthesized on magnesium (Mg) alloy substrate by using a sol-gel dip-coating method, to improve the initial corrosion resistance of AZ31 Mg alloy. The surface morphology and phase composition of the glass-ceramic coating were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). The coating composed of amorphous phase and crystalline phase Na{sub 2}Ca{sub 2}Si{sub 3}O{sub 9}, with the thickness of {approx}1.0 {mu}m, exhibited a uniform and crack-free surface morphology. The corrosion behavior of the uncoated and coated Mg alloy substrates was investigated by the electrochemical measurements and immersion tests in simulated body fluid (SBF). Potentiodynamic polarization tests recorded an increase of potential (E{sub corr}) form -1.60 V to -1.48 V, and a reduction of corrosion current density (i{sub corr}) from 4.48 {mu}A cm{sup -2} to 0.16 {mu}A cm{sup -2}, due to the protection provided by the glass-ceramic coating. Immersion tests also showed the markedly improved corrosion resistance of the coated sample over the immersion period of 7 days. Moreover, after 14 days of immersion in SBF, the corrosion resistance of the coated sample declined due to the cracking of the glass-ceramic coating, which was confirmed by electrochemical impedance spectroscopy (EIS) analysis. The results suggested that the 45S5 glass-ceramic coated Mg alloy could provide a suitable corrosion behavior for use as degradable implants.

Microstructure and corrosion behavior of electrodeposited nano-crystalline nickel coating on AZ91 Mg alloy

Energy Technology Data Exchange (ETDEWEB)

Zarebidaki, Arman, E-mail: arman.zare@iauyazd.ac.ir; Mahmoudikohani, Hassan, E-mail: hassanmahmoudi.k@gmail.com; Aboutalebi, Mohammad-Reza

2014-12-05

Highlights: • Activation, zincating, and Cu electrodeposition were used as pretreatment processes for electrodeposition of nickel coatings. • Nano-crystalline nickel coatings were successfully electrodeposited onto the AZ91 Mg alloys. • Effect of nickel electrodeposited coating on the corrosion resistance of AZ91 Mg alloy has been studied. - Abstract: In order to enhance the corrosion resistance, nickel coating was electrodeposited onto AZ91 Mg alloy. Activation, zincating, and Cu electrodeposition used as pretreatment processes for better adhesion and corrosion performance of the nickel over layer. The corrosion properties of the AZ91 Mg alloy, nickel electroplated AZ91 Mg alloy, and pure nickel was assessed via polarization and electrochemical impedance spectroscopy (EIS) methods in 3.5 wt% NaCl solution. Moreover, the structure of the coating was investigated by means of X-ray diffraction, whereas specimen’s morphology and elemental composition were analyzed using scanning electron microscope (SEM) equipped with energy dispersive spectrometer (EDS). Measurements revealed that the coating has a nano-crystalline structure with the grain size of 95 nm. Corrosion results showed superior corrosion resistance for the coated AZ91 Mg alloy as the corrosion current density decreased from 2.5 × 10{sup −4} A cm{sup −2}, for the uncoated sample, to 1.5 × 10{sup −5} A cm{sup −2}, for coated specimen and the corrosion potential increased from −1.55 V to −0.98 V (vs. Ag/AgCl) at the same condition.

Formulation development and optimization of Lamivudine 300 mg and Tenofovir Disoproxil Fumarate (TDF 300 mg FDC tablets by D-optimal mixture design

Directory of Open Access Journals (Sweden)

Prosper Tibalinda

2016-12-01

Full Text Available The usage of fixed dose combination (FDC tablets of Lamivudine and Tenofovir Disoproxil Fumarate (TDF is increasing due to increased incidences of HIV/Hepatitis B and HIV/TB co-infections. This is likely to increase the financial crisis due to limited resources for funding procurement of ready-made products from the pharmaceuticals manufacturing leading countries. Therefore, production of local oral tablets containing Lamivudine and TDF FDC is inevitable. Lamivudine 300 mg/TDF 300 mg tablets were developed and optimized by D-optimal mixture design and produced by direct compression technique. Twenty trial formulations with independent variables, including PVP-CL 1–12.00%, PVP-K30 1–10.00%, starch-1500 2.5–12.5% and Avicel-PH102 2–19.25% were prepared by direct compression technique. The formulations were assessed on assay, dissolution, friability, weight variation and disintegration time. It was found that assay ranged from 98.13–101.95% for Lamivudine, 98.25–102.84 for TDF, both were within the in-house assay specification of 95 to 105%. Dissolution at single point was above 80% for Lamivudine 93.96–100.55% and 95.85–103.15% for TDF, disintegration time was between 1.92–66.33 min and friability 0.06–12.56%. Out of twenty formulation trials, eight formulations had all parameters in proven acceptable range. On optimization, one formulation with independent variables, PVP-CL 5.67%, PVP-K30 1.00%, Starch-1500 5.76% was selected. The optimized formulation was comparable to the reference product on the market with similarity factor (f2 and difference factor (f1 within the acceptable range for both Lamivudine and TDF.

Assessing gastrointestinal motility and disintegration profiles of magnetic tablets by a novel magnetic imaging device and gamma scintigraphy.

Science.gov (United States)

Goodman, Kirsteen; Hodges, Lee Ann; Band, Janet; Stevens, Howard N E; Weitschies, Werner; Wilson, Clive G

2010-01-01

To validate Magnetic Moment Imaging (MMI) for the investigation of gastrointestinal transit and disintegration of solid dosage forms and to correlate the MMI findings with the corresponding gamma scintigraphic data. Three magnetic tablets (MTs) were investigated using in vitro and in vivo tests. The clinical study was a four-way, crossover study with the following arms: (a) immediate-release tablets administered in fasted state; (b) immediate-release tablets administered after 400mL of Clinutren ISO; (c) enteric-coated tablets administered in the fasted state; and (d) non-disintegrating tablets studied in the lightly fed state (100mL of Clinutren ISO). In both the in vitro and in vivo studies, tablets were detected successfully by MMI and scintigraphy. There was a good correlation between gastric residence times and positional data (in the x, y and y, z-axes). In addition, MMI revealed early swelling behaviour of the tablet matrix. There was excellent agreement for the disintegration times of MT(A) in the fasted arm (scintigraphy 12.0+/-4.4min, MMI 11.8+/-4.4min). In the MT(A)-fed arm, onset times determined by scintigraphy were delayed in three subjects when compared to the corresponding MMI results. Delayed disintegration was observed with MT(A) administered after food (pdisintegration of a magnetic tablet through the gastrointestinal tract. Copyright 2009 Elsevier B.V. All rights reserved.

Hydrothermal synthesis and corrosion behavior of the protective coating on Mg-2Zn-Mn-Ca-Ce alloy

Directory of Open Access Journals (Sweden)

Dan Song

2016-12-01

Full Text Available Protective coatings were synthesized on the Mg-2Zn-Mn-Ca-Ce Mg alloy through the hydrothermal method with de-ionized water as the reagent. The coatings were composed of Mg hydroxide, generally uniform and compact. Hydrogen evolution tests and electrochemical tests in the Hanks’ solution demonstrated that the Mg(OH2 coatings effectively decreased the bio-degradation rate of the Mg alloy substrate. Microstructure observation showed that the coating formation on the secondary phases was more difficult than that on the α-Mg matrix, which led to micro cracks and pores on the secondary phases after drying. Over synthesizing time, the coating layer on secondary phases gradually becomes more compact and uniform. Meanwhile, owing to the thicker and more compact coatings, the corrosion resistance and protective efficiency were significantly improved with longer synthesizing time as well.

Mg-containing hydroxyapatite coatings produced by plasma electrolytic oxidation of titanium

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Antonio, Cesar Augusto; Rangel, Elidiane Cipriano; Durrant, Steven Frederick; Cruz, Nilson Cristino da, E-mail: cesar.augustoa@hotmail.com [Universidade Estadual Paulista Julio de Mesquita Filho (UNESP), Sorocaba, SP (Brazil). Lab. de Plasmas Tecnologicos; Delgado-Silva, Adriana de Oliveira [Universidade Federal de Sao Carlos (UFSCar), Sorocaba, SP (Brazil); Tabacniks, Manfredo H. [Universidade de Sao Paulo (USP), SP (Brazil). Instituto de Fisica

2017-07-15

Plasma Electrolytic Oxidation (PEO) is promising for the processing of biomaterials because it enables the production of surfaces with adjustable composition and structure. In this work, aimed at the improvement of the bioactivity of titanium, PEO has been used to grow calcium phosphide coatings on titanium substrates. The effects of the addition of magnesium acetate to the electrolytes on the composition of the coatings produced during 120 s on Ti disks using bipolar voltage pulses and solutions of calcium and magnesium acetates and sodium glycerophosphate as electrolytes have been studied. Scanning electron microscopy, X-ray energy dispersive spectroscopy, Rutherford backscattering spectroscopy, X-ray diffractometry with Rietveld refinement and profilometry were used to characterize the modified samples. Coatings composed of nearly 50 % of Mg-doped hydroxyapatite have been produced. In certain conditions up to 4% Mg can be incorporated into the coating without any observable significant structural modifications of the hydroxyapatite. (author)

Key Technical Aspects Influencing the Accuracy of Tablet Subdivision.

Science.gov (United States)

Teixeira, Maíra T; Sá-Barreto, Lívia C L; Gratieri, Taís; Gelfuso, Guilherme M; Silva, Izabel C R; Cunha-Filho, Marcílio S S

2017-05-01

Tablet subdivision is a common practice used mainly for dose adjustment. The aim of this study was to investigate how the technical aspects of production as well as the method of tablets subdivision (employing a tablet splitter or a kitchen knife) influence the accuracy of this practice. Five drugs commonly used as subdivided tablets were selected. For each drug, the innovator drug product, a scored-generic and a non-scored generic were investigated totalizing fifteen drug products. Mechanical and physical tests, including image analysis, were performed. Additionally, comparisons were made between tablet subdivision method, score, shape, diluent composition and coating. Image analysis based on surface area was a useful tool as an alternative assay to evaluate the accuracy of tablet subdivision. The tablet splitter demonstrates an advantage relative to a knife as it showed better results in weight loss and friability tests. Oblong, coated and scored tablets had better results after subdivision than round, uncoated and non-scored tablets. The presence of elastic diluents such as starch and dibasic phosphate dehydrate conferred a more appropriate behaviour for the subdivision process than plastic materials such as microcrystalline cellulose and lactose. Finally, differences were observed between generics and their innovator products in all selected drugs with regard the quality control assays in divided tablet, which highlights the necessity of health regulations to consider subdivision performance at least in marketing authorization of generic products.

Studies on portal systemic circulation by oral administration of 201Tl enclosed enteric coated capsule

International Nuclear Information System (INIS)

Tonami, Norihisa; Nakajima, Kenichi; Watanabe, Naoto

1986-01-01

Thallium-201 enclosed enteric coated capsule was prepared and administered orally to evaluate portal systemic circulation in 11 control subjects and 31 patients with various liver diseases by investigating scintigraphic appearance and the heart-to-liver uptake ratio (H/L ratio). In 10 patients with liver cirrhosis and one with chronic hepatitis, the results of H/L ratio were compared to those obtained by 201 Tl per-rectal administration. 1. It was fundamentally confirmed that 201 Tl enclosed enteric coated capsule was not broken down in the artificial gastric juice, but nearly completely melted 15 minutes after soaking in the artificial intestinal juice. 2. Clinical study was successfully completed in 36 out of 42 cases (86 %). Unsuccessful cases were found in 2 with capsule collapse in the stomach and 4 with its poor moving to the duodenum. 3. In control subjects the liver was clearly visualized and the mean value of H/L ratio was 0.32 which is lower than that of 201 Tl per-rectal administration previously reported. H/L ratio in patients with chronic and acute hepatitis was nearly equal to that in control subjects. H/L ratio in patients with liver cirrhosis was slightly higher than that in control subjects, but there was no significant difference between them. In cases with esophageal varices, H/L ratio was not so high compared to that in control subjects. Out of 7 patients showing high H/L ratio more than 0.8 in 201 Tl per-rectal administration, only one showed similar high ratio (1.07) in oral administration of 201 Tl enclosed enteric coated capsule. In this case the shunting from superior mesenteric vein to inferior vena cava connection was confirmed. From these results, it was considered that the shunting volume of superior mesenteric vein through esophageal varices is small. 4. A possibility of a new administration of radioisotope with enteric coated capsule was emphasized. (author)

Impact of salt form and molecular weight of chitosan on swelling and drug release from chitosan matrix tablets.

Science.gov (United States)

Huanbutta, Kampanart; Cheewatanakornkool, Kamonrak; Terada, Katsuhide; Nunthanid, Jurairat; Sriamornsak, Pornsak

2013-08-14

Magnetic resonance imaging (MRI) and gravimetric techniques were used to assess swelling and erosion behaviors of hydrophilic matrix tablets made of chitosan. The impact of salt form, molecular weight (MW) and dissolution medium on swelling behavior and drug (theophylline) release was studied. The matrix tablets made of chitosan glycolate (CGY) showed the greatest swelling in both acid and neutral media, compared to chitosan aspartate, chitosan glutamate and chitosan lactate. MRI illustrated that swelling region of CGY in both media was not different in the first 100 min but glassy region (dry core) in 0.1N HCl was less than in pH 6.8 buffer. The tablets prepared from chitosan with high MW swelled greater than those of low MW. Moreover, CGY can delay drug release in the acid condition due to thick swollen gel and low erosion rate. Therefore, CGY may be suitably applied as sustained drug release polymer or enteric coating material. Copyright © 2013 Elsevier Ltd. All rights reserved.

Glass-ceramic coated Mg-Ca alloys for biomedical implant applications.

Science.gov (United States)

Rau, J V; Antoniac, I; Fosca, M; De Bonis, A; Blajan, A I; Cotrut, C; Graziani, V; Curcio, M; Cricenti, A; Niculescu, M; Ortenzi, M; Teghil, R

2016-07-01

Biodegradable metals and alloys are promising candidates for biomedical bone implant applications. However, due to the high rate of their biodegradation in human body environment, they should be coated with less reactive materials, such, for example, as bioactive glasses or glass-ceramics. Fort this scope, RKKP composition glass-ceramic coatings have been deposited on Mg-Ca(1.4wt%) alloy substrates by Pulsed Laser Deposition method, and their properties have been characterized by a number of techniques. The prepared coatings consist of hydroxyapatite and wollastonite phases, having composition close to that of the bulk target material used for depositions. The 100μm thick films are characterized by dense, compact and rough morphology. They are composed of a glassy matrix with various size (from micro- to nano-) granular inclusions. The average surface roughness is about 295±30nm due to the contribution of micrometric aggregates, while the roughness of the fine-texture particulates is approximately 47±4nm. The results of the electrochemical corrosion evaluation tests evidence that the RKKP coating improves the corrosion resistance of the Mg-Ca (1.4wt%) alloy in Simulated Body Fluid. Copyright © 2016 Elsevier B.V. All rights reserved.

21 CFR 520.1510 - Nitenpyram tablets.

Science.gov (United States)

2010-04-01

... and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... order of a licensed veterinarian. (d) Conditions of use—(1) Dogs—(i) Amount—(A) One 11.4-mg tablet for dogs weighing less than 25 pounds (lb) or one 57-mg tablet for dogs weighing more than 25 lb, as needed...

Biological activity evaluation of magnesium fluoride coated Mg-Zn-Zr alloy in vivo.

Science.gov (United States)

Jiang, Hongfeng; Wang, Jingbo; Chen, Minfang; Liu, Debao

2017-06-01

To explore the biodegradable characteristics and biological properties, which could promote new bone formation, of MgF 2 coated magnesium alloy (Mg-3wt%Zn-0.5wt%Zr) in rabbits. Magnesium alloy with MgF 2 coating was made and the MgF 2 /Mg-Zn-Zr was implanted in the femoral condyle of rabbits. Twelve healthy adult Japanese white rabbits in weight of 2.8-3.2kg were averagely divided into A(Mg-Zn-Zr) group and B(MgF 2 /MgZn-Zr) group. Indexes such as microstructural evolution, SEM scan, X-ray, Micro-CT and mechanical properties were observed and detected at 1th day, 2th, 4th, 8th, 12th, 24th week after implantation. Low-density regions occurred around the cancellous bone, and the regions gradually expanded during the 12weeks after implantation. The implant was gradually absorbed from 12 to 24weeks. The density of surrounding cancellous bone increased compared with the 12th week data. The degradation rate of B group was lower than that of A group (Pmagnesium ions. The biological properties of the coating itself presented good biocompatibility and bioactivity. Copyright © 2017 Elsevier B.V. All rights reserved.

Authentication of gold nanoparticle encoded pharmaceutical tablets using polarimetric signatures.

Science.gov (United States)

Carnicer, Artur; Arteaga, Oriol; Suñé-Negre, Josep M; Javidi, Bahram

2016-10-01

The counterfeiting of pharmaceutical products represents concerns for both industry and the safety of the general public. Falsification produces losses to companies and poses health risks for patients. In order to detect fake pharmaceutical tablets, we propose producing film-coated tablets with gold nanoparticle encoding. These coated tablets contain unique polarimetric signatures. We present experiments to show that ellipsometric optical techniques, in combination with machine learning algorithms, can be used to distinguish genuine and fake samples. To the best of our knowledge, this is the first report using gold nanoparticles encoded with optical polarimetric classifiers to prevent the counterfeiting of pharmaceutical products.

Development of modified-release tablets of zolpidem tartrate by biphasic quick/slow delivery system.

Science.gov (United States)

Mahapatra, Anjan Kumar; Sameeraja, N H; Murthy, P N

2015-06-01

Zolpidem tartrate is a non-benzodiazepine analogue of imidazopyridine of sedative and hypnotic category. It has a short half-life with usual dosage regimen being 5 mg, two times a day, or 10 mg, once daily. The duration of action is considered too short in certain circumstances. Thus, it is desirable to lengthen the duration of action. The formulation design was implemented by preparing extended-release tablets of zolpidem tartrate using the biphasic delivery system technology, where sodium starch glycolate acts as a superdisintegrant in immediate-release part and hydroxypropyl methyl cellulose as a release retarding agent in extended-release core. Tablets were prepared by direct compression. Both the core and the coat contained the drug. The pre-compression blends were evaluated for angle of repose, bulk density, and compressibility index. The tablets were evaluated for thickness, hardness, weight variation test, friability, and in vitro release studies. No interaction was observed between zolpidem tartrate and excipients from the Fourier transform infrared spectroscopy and differential scanning calorimetry analysis. The results of all the formulations prepared were compared with reference product Stilnoct®. Optimized formulations showed release patterns that match the United States Pharmacopeia (USP) guidelines for zolpidem tartrate extended-release tablets. The mechanism of drug release was studied using different mathematical models, and the optimized formulation has shown Fickian diffusion. Accelerated stability studies were performed on the optimized formulation.

Development and optimization of enteric coated mucoadhesive microspheres of duloxetine hydrochloride using 32 full factorial design

Science.gov (United States)

Setia, Anupama; Kansal, Sahil; Goyal, Naveen

2013-01-01

Background: Microspheres constitute an important part of oral drug delivery system by virtue of their small size and efficient carrier capacity. However, the success of these microspheres is limited due to their short residence time at the site of absorption. Objective: The objective of the present study was to formulate and systematically evaluate in vitro performance of enteric coated mucoadhesive microspheres of duloxetine hydrochloride (DLX), an acid labile drug. Materials and Methods: DLX microspheres were prepared by simple emulsification phase separation technique using chitosan as carrier and glutaraldehyde as a cross-linking agent. Microspheres prepared were coated with eudragit L-100 using an oil-in-oil solvent evaporation method. Eudragit L-100was used as enteric coating polymer with the aim to release the drug in small intestine The microspheres prepared were characterized by particle size, entrapment efficiency, swelling index (SI), mucoadhesion time, in vitro drug release and surface morphology. A 32 full factorial design was employed to study the effect of independent variables polymer-to-drug ratio (X1) and stirring speed (X2) on dependent variables, particle size, entrapment efficiency, SI, in vitro mucoadhesion and drug release up to 24 h (t24). Results: Microspheres formed were discrete, spherical and free flowing. The microspheres exhibited good mucoadhesive property and also showed high percentage entrapment efficiency. The microspheres were able to sustain the drug release up to 24 h. Conclusion: Thus, the prepared enteric coated mucoadhesive microspheres may prove to be a potential controlled release formulation of DLX for oral administration. PMID:24167786

Bioactive glass-ceramic coating for enhancing the in vitro corrosion resistance of biodegradable Mg alloy

Science.gov (United States)

Ye, Xinyu; Cai, Shu; Dou, Ying; Xu, Guohua; Huang, Kai; Ren, Mengguo; Wang, Xuexin

2012-10-01

In this work, a bioactive 45S5 glass-ceramic coating was synthesized on magnesium (Mg) alloy substrate by using a sol-gel dip-coating method, to improve the initial corrosion resistance of AZ31 Mg alloy. The surface morphology and phase composition of the glass-ceramic coating were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). The coating composed of amorphous phase and crystalline phase Na2Ca2Si3O9, with the thickness of ∼1.0 μm, exhibited a uniform and crack-free surface morphology. The corrosion behavior of the uncoated and coated Mg alloy substrates was investigated by the electrochemical measurements and immersion tests in simulated body fluid (SBF). Potentiodynamic polarization tests recorded an increase of potential (Ecorr) form -1.60 V to -1.48 V, and a reduction of corrosion current density (icorr) from 4.48 μA cm-2 to 0.16 μA cm-2, due to the protection provided by the glass-ceramic coating. Immersion tests also showed the markedly improved corrosion resistance of the coated sample over the immersion period of 7 days. Moreover, after 14 days of immersion in SBF, the corrosion resistance of the coated sample declined due to the cracking of the glass-ceramic coating, which was confirmed by electrochemical impedance spectroscopy (EIS) analysis. The results suggested that the 45S5 glass-ceramic coated Mg alloy could provide a suitable corrosion behavior for use as degradable implants.

Development and optimization of enteric coated mucoadhesive microspheres of duloxetine hydrochloride using 3(2) full factorial design.

Science.gov (United States)

Setia, Anupama; Kansal, Sahil; Goyal, Naveen

2013-07-01

Microspheres constitute an important part of oral drug delivery system by virtue of their small size and efficient carrier capacity. However, the success of these microspheres is limited due to their short residence time at the site of absorption. The objective of the present study was to formulate and systematically evaluate in vitro performance of enteric coated mucoadhesive microspheres of duloxetine hydrochloride (DLX), an acid labile drug. DLX microspheres were prepared by simple emulsification phase separation technique using chitosan as carrier and glutaraldehyde as a cross-linking agent. Microspheres prepared were coated with eudragit L-100 using an oil-in-oil solvent evaporation method. Eudragit L-100was used as enteric coating polymer with the aim to release the drug in small intestine The microspheres prepared were characterized by particle size, entrapment efficiency, swelling index (SI), mucoadhesion time, in vitro drug release and surface morphology. A 3(2) full factorial design was employed to study the effect of independent variables polymer-to-drug ratio (X1) and stirring speed (X2) on dependent variables, particle size, entrapment efficiency, SI, in vitro mucoadhesion and drug release up to 24 h (t24). Microspheres formed were discrete, spherical and free flowing. The microspheres exhibited good mucoadhesive property and also showed high percentage entrapment efficiency. The microspheres were able to sustain the drug release up to 24 h. Thus, the prepared enteric coated mucoadhesive microspheres may prove to be a potential controlled release formulation of DLX for oral administration.

Bioequivalence of generic alendronate sodium tablets (70 mg to Fosamax® tablets (70 mg in fasting, healthy volunteers: a randomized, open-label, three-way, reference-replicated crossover study

Directory of Open Access Journals (Sweden)

Zhang Y

2017-07-01

Full Text Available Yifan Zhang,1 Xiaoyan Chen,1 Yunbiao Tang,2 Youming Lu,1 Lixia Guo,1 Dafang Zhong1 1State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 2Department of Pharmacy, The General Hospital of Shenyang Military Region, Shenyang, People’s Republic of China Purpose: The aim of this study was to evaluate the bioequivalence of a generic product 70 mg alendronate sodium tablets with the reference product Fosamax® 70 mg tablet. Materials and methods: A single-center, open-label, randomized, three-period, three-sequence, reference-replicated crossover study was performed in 36 healthy Chinese male volunteers under fasting conditions. In each study period, the volunteers received a single oral dose of the generic or reference product (70 mg. Blood samples were collected at pre-dose and up to 8 h after administration. The bioequivalence of the generic product to the reference product was assessed using the US Food and Drug Administration (FDA and European Medicines Agency (EMA reference-scaled average bioequivalence (RSABE methods. Results: The average maximum concentrations (Cmax of alendronic acid were 64.78±43.76, 56.62±31.95, and 60.15±37.12 ng/mL after the single dose of the generic product and the first and second doses of the reference product, respectively. The areas under the plasma concentration–time curves from time 0 to the last timepoint (AUC0–t were 150.36±82.90, 148.15±85.97, and 167.11±110.87 h·ng/mL, respectively. Reference scaling was used because the within-subject standard deviations of the reference product (sWR for Cmax and AUC0–t were all higher than the cutoff value of 0.294. The 95% upper confidence bounds were -0.16 and -0.17 for Cmax and AUC0–t, respectively, and the point estimates for the generic/reference product ratio were 1.08 and 1.00, which satisfied the RSABE acceptance criteria of the FDA. The 90% CIs for Cmax and AUC0–t were 90.35%–129

In vitro and in vivo corrosion, mechanical properties and biocompatibility evaluation of MgF2-coated Mg-Zn-Zr alloy as cancellous screws.

Science.gov (United States)

Li, Zhen; Shizhao, Sun; Chen, Minfang; Fahlman, Bradley Dean; Debao Liu; Bi, Hongwei

2017-06-01

Magnesium (Mg) and its alloys as biodegradable materials have received much attention in the orthopedics applications; however, the corrosion behavior of these metals in vivo remains challenging. In this work, a dense and nanoscale magnesium fluoride (MgF 2 ) coating was deposited on the surface of Mg-Zn-Zr (MZZ) alloy cancellous screw. The MZZ cancellous screw with MgF 2 coating maintained an integrated shape and high yield tensile stress after 30days immersion in SBF, comparing with the bare screw. Hydrogen releasing rate of the MZZ samples was suppressed at a lower level at the initial stage, which is in favour of the adhesion of the cells. And in vivo experiments indicated that MgF 2 -coated MZZ screws presented advantages in cytocompatibility, osteoconductivity and osteogenesis of cancellous bone in rabbits. Corrosion rate in vivo perfusion environment increased very slowly with time in long-term study, which was an opposite trend in vitro static immersion test. Moreover, maximum corrosion rate (CR max ), a critical calculation method of corrosion rate was introduced to predict fracture regions of the sample. The MZZ alloy with MgF 2 coating possesses a great potential for clinical applications for internal fracture fixation repair. Copyright © 2017 Elsevier B.V. All rights reserved.

Behaviour of CaO coating of gas atomized Mg powders using mechanical milling process

International Nuclear Information System (INIS)

Kim, Sun-Mi; Kim, Yong Hwan; Kim, Young Do; Kim, Taek-Soo

2011-01-01

Highlights: → This work is very new, since behaviour of CaO coating with milling time as desulfurizer is not frequently reported. → The manuscript reports the new manner of Mg powders desulfurizer development by the innovative process. - Abstract: In order to synthesize a thermally stable Mg powder as a desulfurizer of iron, pure Mg was gas atomized to powders and coated by CaO powders, to produce a thermally stable desulfurizer using a mechanical milling process. Since the effect of desulfurization is dependent on the degree of surface modification, coating behaviours such as the size, morphology and layer thickness were investigated as a function of milling condition. As the milling conducted from 10 min to 30 min, 1 h, 3 h, 6 h, 12 h, CaO particles began to stick on the surface of Mg powders. The layer of CaO formed from 1 h milling was about 17 μm thick and gradually thickened to be 28 μm, 32 μm and 37 μm with increasing the milling time to 3 h, 6 h and 12 h, respectively. The shape of coated powder became more spherical after 1 h milling, being mostly spherical after 6 h. Desulfurization rate and uniformity were evaluated for the various thickness of the coating layer.

Interchangeability and comparative effectiveness between generic and brand montelukast immediate release tablets after a single oral administration in healthy volunteers.

Science.gov (United States)

Zaid, Abdel Naser; Mousa, Ayman; Ghazal, Nadia; Bustami, Rana

2015-01-01

Montelukast is a leukotriene receptor antagonist. The release of leukotrienes causes narrowing and constricting in the respiratory airways. Blocking the action of these leukotrienes, montelukast can be used for the prophylaxis and treatment of chronic asthma. The aim of this study was to evaluate the interchangeability and comparative effectiveness between a generic and a brand montelukast 10 mg immediate release tablets (Broncast(®) and Singulair(®), respectively) after a single oral dose among Arab Mediterranean volunteers. An open-label, randomized two-period crossover bioequivalence design was conducted in 31 healthy male volunteers with a 1 week washout between each study period and under fasting conditions. The plasma drug concentration was assessed by using a previously validated LC MS/MS method. The ratio between the generic and brand of geometric least squares means was reported for both generic and brand products. Moreover, an in vitro dissolution study was conducted on generic and brand tablets using three different pH media, and similarity and non-similarity factors (f2 and f1) were calculated. The used bioanalytical method was found to be linear within the range 6.098-365.855 ng/mL. The correlation coefficient was close to 0.999 during the course of the study validation. Statistical comparison of the main pharmacokinetic parameters showed the inexistence of any significant difference between generic and the brand. The point estimates (ratios of geometric means) were 111.939, 111.711, and 112.169 % for AUC0-24, AUC0-∞, and Cmax, respectively. The 90 % confidence intervals (CIs) were within the pre-defined limits of 80.00-125.00 % as specified by the FDA and EMA for bioequivalence studies. F2 and f1 were higher than 50 and lower than 15, respectively in all selected pH media. Broncast(®) immediate release film coated tablets (10 mg/tablet) are bioequivalent to Singulair(®) immediate release film coated tablets (10 mg/tablet), with a

Variability in the 3,4-methylenedioxymethamphetamine content of 'ecstasy' tablets in the UK.

Science.gov (United States)

Wood, David Michael; Stribley, Vasoulla; Dargan, Paul Ivor; Davies, Susannah; Holt, David W; Ramsey, John

2011-09-01

Toxicity, such as hyperpyrexia, associated with the use of 3,4-methylenedioxymethamphetamine (MDMA; 'ecstasy') appears to be related to serum MDMA concentrations. However, there does not appear to be a similar association with the number of tablets ingested, suggesting variation in the tablet content of MDMA. Although work has shown this variation in other areas of the world, no studies have reported on the variation of MDMA content in UK ecstasy tablets. Ecstasy tablets seized from individuals attending nightclubs were analysed qualitatively to determine if they contained MDMA and quantitatively to determine the MDMA content per tablet. The mean amount of MDMA hydrochloride in 101 seized ecstasy tablets was 58.7±22.9 mg per tablet, with a range of 20 mg to 131 mg per tablet. The majority (96.0%) of tablets contained less than 100 mg MDMA per tablet. There appeared to be a bimodal distribution of MDMA content at approximately 20-40 mg per tablet and 60-80 mg per tablet. There is variability in the MDMA content of ecstasy tablets in the UK. This variability could potentially put users at increased risk of acute harm due to inadvertent excess ingestion of MDMA, as they are unaware of the differences in the MDMA content. Repeat sampling and quantification of MDMA content of ecstasy tablets in the UK will allow better education of users about the potential harms associated with the variability in the MDMA content. In addition, it will provide information to allow the monitoring of changes in not only the MDMA content, but also other adulterants, in ecstasy tablets.

Studies on portal systemic circulation by oral administration of /sup 201/Tl enclosed enteric coated capsule

Energy Technology Data Exchange (ETDEWEB)

Tonami, Norihisa; Nakajima, Kenichi; Watanabe, Naoto and others

1986-03-01

Thallium-201 enclosed enteric coated capsule was prepared and administered orally to evaluate portal systemic circulation in 11 control subjects and 31 patients with various liver diseases by investigating scintigraphic appearance and the heart-to-liver uptake ratio (H/L ratio). In 10 patients with liver cirrhosis and one with chronic hepatitis, the results of H/L ratio were compared to those obtained by /sup 201/Tl per-rectal administration. 1. It was fundamentally confirmed that /sup 201/Tl enclosed enteric coated capsule was not broken down in the artificial gastric juice, but nearly completely melted 15 minutes after soaking in the artificial intestinal juice. 2. Clinical study was successfully completed in 36 out of 42 cases (86 %). Unsuccessful cases were found in 2 with capsule collapse in the stomach and 4 with its poor moving to the duodenum. 3. In control subjects the liver was clearly visualized and the mean value of H/L ratio was 0.32 which is lower than that of /sup 201/Tl per-rectal administration previously reported. H/L ratio in patients with chronic and acute hepatitis was nearly equal to that in control subjects. H/L ratio in patients with liver cirrhosis was slightly higher than that in control subjects, but there was no significant difference between them. In cases with esophageal varices, H/L ratio was not so high compared to that in control subjects. Out of 7 patients showing high H/L ratio more than 0.8 in /sup 201/Tl per-rectal administration, only one showed similar high ratio (1.07) in oral administration of /sup 201/Tl enclosed enteric coated capsule. In this case the shunting from superior mesenteric vein to inferior vena cava connection was confirmed. From these results, it was considered that the shunting volume of superior mesenteric vein through esophageal varices is small. 4. A possibility of a new administration of radioisotope with enteric coated capsule was emphasized.

Formulation and evaluation of sustained release matrix tablet of rabeprazole using wet granulation technique

Directory of Open Access Journals (Sweden)

Ruqaiyah Khan

2014-01-01

Full Text Available Introduction: Rabeprazole, a member of substituted benzimidazoles, inhibits the final step in gastric acid secretions. This drug claims to cause fastest acid separation (due to higher pKa, and more rapidly converts to the active species to aid gastric mucin synthesis. The most significant pharmacological action of Rabeprazole is dose dependent suppression of gastric acid secretion; without anticholinergic or H2-blocking action. It completely abolishes the hydrochloric acid secretion as it is powerful inhibitor of gastric acid. Rabeprazole is acid labile and hence commonly formulated as an enteric coated tablet. The absorption of rabeprazole occurs rapidly as soon as tablet leaves the stomach. Aim: In the present study an attempt was made to formulate and evaluate Rabeprazole sustained release matrix tablet using wet granulation technique incorporating various polymers like HPMC-E15, Carbopol934, and sodium carboxymethyl cellulose (CMC. Materials and Methods: The Formulated tablets were evaluated for different physicochemical properties like rheological properties, weight variation, thickness, hardness, % friability, in vitro release studies and drug content. Results: Studies revealed that all the physicochemical parameters comply with the official standards. The in vitro release studies exhibits the release up to 90%, over a prolonged period of time which confirms the extended release profile of formulation, having better bioavailability as well as decreased dosing frequency with reduced doses. Conclusion: The sustained release matrix tablets of rabiprazole shown better bioavailability, efficacy and potency, when compared with official standards.

Effect of Coating Solvent Ratio on the Drug Release Lag Time of ...

African Journals Online (AJOL)

Erah

Research Article ... Lag Time of Coated Theophylline Osmotic Tablets ... Key words: Coating solvent, Drug release, Lag time, Osmotic tablet, HPMC, .... following composition (w/w): theophylline ... tablets was measured by UV absorption.

Structure and properties of a duplex coating combining micro-arc oxidation and baking layer on AZ91D Mg alloy

Energy Technology Data Exchange (ETDEWEB)

Cui, Xue-Jun; Li, Ming-Tian; Yang, Rui-Song; Yu, Zu-Xiao [Material Corrosion and Protection Key Laboratory of Sichuan province, Sichuan University of Science and Engineering, Zigong 643000 (China); College of Materials and Chemical Engineering, Sichuan University of Science and Engineering, Zigong 643000 (China)

2016-02-15

Graphical abstract: - Highlights: • A duplex coating was fabricated through combining MAO and baking layer. • A baking coating with a thickness of 92 μm was created on MAO-coated Mg alloy. • The duplex coating noticeably improved the corrosion resistance of Mg alloy. • The related corrosion and wear mechanisms were investigated. - Abstract: A duplex coating (called MAOB coating) was fabricated on AZ91D Mg alloy by combining the process of micro-arc oxidation (MAO) with baking coating (B-coating). The structure, composition, corrosion resistance, and tribological behaviour of the coatings were investigated using scanning electron microscopy (SEM), energy dispersive spectroscopy (EDS), electrochemical and long-term immersion test, and ball-on-disc friction test. The results show that a dense 92 μm thick B-coating was tightly deposited onto the MAO-coated Mg alloy and exhibited a good mechanical interlock along the rough interface. Compared with the MAO-coated sample, the corrosion current density of the MAOB-coated Mg alloy decreased by two or three orders of magnitude and no corrosion phenomenon was observed during a long-term immersion test of about 500 h (severe corrosion pits were found for MAO-treated samples after about 168 h of immersion). The frictional coefficient values of the MAOB coating were similar to those of the MAO coating using dry sliding tests, while the B-coating on the MAO-coated surface significantly improved the wear resistance of the AZ91D Mg alloy. All of these results indicate that a B-coating can be used to further protect Mg alloys from corrosion and wear by providing a thick, dense barrier.

Magnesium substituted hydroxyapatite formation on (Ti,Mg)N coatings produced by cathodic arc PVD technique.

Science.gov (United States)

Onder, Sakip; Kok, Fatma Nese; Kazmanli, Kursat; Urgen, Mustafa

2013-10-01

In this study, formation of magnesium substituted hydroxyapatite (Ca10-xMgx(PO4)6(OH)2) on (Ti,Mg)N and TiN coating surfaces were investigated. The (Ti1-x,Mgx)N (x=0.064) coatings were deposited on titanium substrates by using cathodic arc physical vapor deposition technique. TiN coated grade 2 titanium substrates were used as reference to understand the role of magnesium on hydroxyapatite (HA) formation. The HA formation experiments was carried out in simulated body fluids (SBF) with three different concentrations (1X SBF, 5X SBF and 5X SBF without magnesium ions) at 37 °C. The coatings and hydroxyapatite films formed were characterized by scanning electron microscope (SEM), X-ray diffraction (XRD) and FTIR Spectroscopy techniques. The energy dispersive X-ray spectroscopy (EDS) analyses and XRD investigations of the coatings indicated that magnesium was incorporated in the TiN structure rather than forming a separate phase. The comparison between the TiN and (Ti, Mg)N coatings showed that the presence of magnesium in TiN structure facilitated magnesium substituted HA formation on the surface. The (Ti,Mg)N coatings can potentially be used to accelerate the HA formation in vivo conditions without any prior hydroxyapatite coating procedure. © 2013.

In vivo assessment of a new multifunctional coating architecture for improved Mg alloy biocompatibility.

Science.gov (United States)

Gomes, Pedro S; Zomorodian, Amir; Kwiatkowski, Lech; Lutze, Rafal; Balkowiec, Alicja; Colaço, Bruno; Pinheiro, Vitor; Fernandes, João C S; Montemor, Maria F; Fernandes, Maria H

2016-08-10

Magnesium alloys are regarded as potential biodegradable load-bearing biomaterials for orthopedic applications due to their physico-chemical and biomechanical properties. However, their clinical applicability is restricted by their high degradation rate, which limits the physiological reconstruction of the neighbouring tissues. In this work, a multifunctional coating architecture was developed on an AZ31 alloy by conjoining an anodization process with the deposition of a polymeric-based layer consisting of polyether imine reinforced with hydroxyapatite nanoparticles, aiming at improved control of the corrosion activity and biological performance of the Mg substrate. Anodization and coating protocols were evaluated either independently or combined for corrosion resistance and biological behaviour, i.e. the irritation potential and angiogenic capability within a chicken chorioallantoic membrane assay, and bone tissue response following tibia implantation within a rabbit model. Electrochemical impedance spectroscopy (EIS) analysis showed that coated Mg constructs, particularly anodized plus coated with AZ31, exhibited excellent stability compared to the anodized alloy and, particularly, to the bare AZ31. Microtomographic evaluation of the implanted samples correlated with these degradation results. Mg constructs displayed a non-irritating behaviour, and were associated with high levels of vascular ingrowth. Bone ingrowth neighbouring the implanted constructs was observed for all samples, with coated and anodized plus coated samples presenting the highest bone formation. Gene expression analysis suggested that the enhanced bone tissue formation was associated with the boost in osteogenic activity through Runx2 upregulation, following the activation of PGC-1α/ERRα signaling. Overall, the developed multifunctional coatings appear to be a promising strategy to obtain safe and bioactive biodegradable Mg-based implants with potential applications within bone tissue.

Mini-tablets versus pellets as promising multiparticulate modified release delivery systems for highly soluble drugs.

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Gaber, Dina M; Nafee, Noha; Abdallah, Osama Y

2015-07-05

Whether mini-tablets (tablets, diameters ≤6mm) belong to single- or multiple-unit dosage forms is still questionable. Accordingly, Pharmacopoeial evaluation procedures for mini-tablets are lacking. In this study, the aforementioned points were discussed. Moreover, their potential for oral controlled delivery was assessed. The antidepressant venlafaxine hydrochloride (Vx), a highly soluble drug undergoing first pass effect, low bioavailability and short half-life was selected as a challenging payload. In an attempt to weigh up mini-tablets versus pellets as multiparticulate carriers, Vx-loaded mini-tablets were compared to formulated pellets of the same composition and the innovator Effexor(®)XR pellets. Formulations were prepared using various polymer hydrogels in the core and ethyl cellulose film coating with increasing thickness. Mini-tablets (diameter 2mm) showed extended Vx release (<60%, 8h). Indeed, release profiles comparable to Effexor(®)XR pellets were obtained. Remarkably higher coating thickness was required for pellets to provide equivalent retardation. Ethyl cellulose in the core ensured faster release due to polymer migration to the surface and pore formation in the coat. mini-tablets showed higher stability to pellets upon storage. Industrially speaking, mini-tablets proved to be superior to pellets in terms of manufacturing, product quality and economical aspects. Results point out the urgent need for standardized evaluation procedures for mini-tablets. Copyright © 2015. Published by Elsevier B.V.

Alendronate Sodium as Enteric Coated Solid Lipid Nanoparticles; Preparation, Optimization, and In Vivo Evaluation to Enhance Its Oral Bioavailability.

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Khaled Mohamed Hosny

Full Text Available Treatment of osteoporosis with alendronate sodium has several challenges. The first challenge is the low bioavailability. The second main challenge is side effects, which include oesophageal ulceration. The aim of this research was to reformulate alendronate sodium as enteric coated solid lipid nanoparticles in order to enhance its bioavailability, and preventing the free alendronate sodium from coming into direct contact with the gastrointestinal mucosa, and thereby reducing the possibility of side effects. Enteric coated solid lipid nanoparticles were prepared according to the Box-Behnken design employing Design expert® software, and characterized for size, morphology, and entrapment efficiency. The optimized formula was coated with an Eudragit S100 and evaluated for drug release in acidic and basic media, stability studies and pharmacokinetic evaluations on rabbits. The results indicated that, using Derringer's desirability functional tool for optimization, the highest entrapment efficiency value of 74.3% and the smallest size value of 98 nm were predicted under optimum conditions with a desirability value of 0.917. The optimized nanoparticles released alendronate sodium only at an alkaline pH. The pharmacokinetic evaluation revealed that alendronate sodium bioavailability was enhanced by more than 7.4-fold in rabbits. In conclusion, enteric coated solid lipid nanoparticles is a promising formula for the delivery of alendronate sodium, eliminating its oesophageal side effects and enhancing its bioavailability.

Evaluations of MgB2 Coatings on 2'' Copper Discs for Superconducting Radio Frequency Applications

Science.gov (United States)

Withanage, Wenura; Tan, Teng; Lee, Namhoon; Banjade, Huta; Eremeev, Grigory; Welander, Paul; Valente-Feliciano, Anne-Marie; Kustom, Robert; Wolak, Matthäus; Nassiri, Alireza; Xi, Xiaoxing

We propose that coating the inner walls of copper RF cavities with superconducting MgB2 (Tc = 39 K) can result in a viable alternative to the already established niobium-based SRF technology. This approach improves the thermal conductivity, allows for operation at higher temperatures, and reduces the need for large helium refrigeration, thereby resulting in lower operational costs. For our studies, we grew MgB2 films via hybrid physical chemical vapor deposition (HPCVD) on 2'' Cu substrates. Since Mg and Cu readily form an alloy at higher temperatures, the HPCVD setup was modified in order to achieve lower deposition temperatures, minimize alloy formation, and provide high quality MgB2 films. This method yielded MgB2 coatings on 2'' Cu discs with transition temperatures around 38 K. The samples were characterized with regards to their RF attributes and showed similar performance in comparison to Nb reference samples. The presented results show that MgB2 coated copper can be a suitable alternative for use in SRF cavities.

Calcium phosphate/chitosan composite coating: Effect of different concentrations of Mg2+ in the m-SBF on its bioactivity

International Nuclear Information System (INIS)

Zhang, Jie; Dai, Changsong; Wei, Jie; Wen, Zhaohui; Zhang, Shujuan; Lin, Lemin

2013-01-01

The purpose of this study was to investigate the effect of different concentration of Mg 2+ in a modified simulated body fluid (m-SBF) on the bioactivity of calcium phosphate/chitosan composite coating. Calcium phosphate/chitosan composite coating was prepared on graphite substrate via electrophoretic deposition (EPD) followed by conversion in a phosphate buffer solution (PBS). The obtained samples were soaked in the m-SBF containing different concentration of Mg 2+ for different times. And then, the composite coatings were assessed using X-ray diffractometer (XRD), Fourier-transformed infrared spectroscopy (FTIR), Raman spectra, and scanning electron microscope (SEM) with an energy dispersive spectrometer (EDS). The soaking solution was evaluated by inductively coupled plasma optical emission spectrometer (ICP-OES) test. The analytical results showed that hydroxyapatite (HA) and bone-like apatite (HCA) grew on the surface of calcium phosphate/chitosan composite coating after incubation in different m-SBF. With Mg 2+ concentration in m-SBF increased from 1× Mg to 10× Mg, HA in the composite coating first presented a dissolving process and then a precipitating one slowly, while HCA presented a growing trend, continuously. The increasing of Mg 2+ concentration in the m-SBF inhibited the total growing process of HA and HCA as a whole. The structure of the composite coating changed from spherical into irregular morphology with the concentration of Mg 2+ increasing from 1× Mg to 10× Mg. Over all, with the Mg 2+ concentration increasing, the bioactivity of calcium phosphate/chitosan composite coating tended to decrease.

Calcium phosphate/chitosan composite coating: Effect of different concentrations of Mg2+ in the m-SBF on its bioactivity

Science.gov (United States)

Zhang, Jie; Dai, Changsong; Wei, Jie; Wen, Zhaohui; Zhang, Shujuan; Lin, Lemin

2013-09-01

The purpose of this study was to investigate the effect of different concentration of Mg2+ in a modified simulated body fluid (m-SBF) on the bioactivity of calcium phosphate/chitosan composite coating. Calcium phosphate/chitosan composite coating was prepared on graphite substrate via electrophoretic deposition (EPD) followed by conversion in a phosphate buffer solution (PBS). The obtained samples were soaked in the m-SBF containing different concentration of Mg2+ for different times. And then, the composite coatings were assessed using X-ray diffractometer (XRD), Fourier-transformed infrared spectroscopy (FTIR), Raman spectra, and scanning electron microscope (SEM) with an energy dispersive spectrometer (EDS). The soaking solution was evaluated by inductively coupled plasma optical emission spectrometer (ICP-OES) test. The analytical results showed that hydroxyapatite (HA) and bone-like apatite (HCA) grew on the surface of calcium phosphate/chitosan composite coating after incubation in different m-SBF. With Mg2+ concentration in m-SBF increased from 1× Mg to 10× Mg, HA in the composite coating first presented a dissolving process and then a precipitating one slowly, while HCA presented a growing trend, continuously. The increasing of Mg2+ concentration in the m-SBF inhibited the total growing process of HA and HCA as a whole. The structure of the composite coating changed from spherical into irregular morphology with the concentration of Mg2+ increasing from 1× Mg to 10× Mg. Over all, with the Mg2+ concentration increasing, the bioactivity of calcium phosphate/chitosan composite coating tended to decrease.

Structure and properties of a duplex coating combining micro-arc oxidation and baking layer on AZ91D Mg alloy

Science.gov (United States)

Cui, Xue-Jun; Li, Ming-Tian; Yang, Rui-Song; Yu, Zu-Xiao

2016-02-01

A duplex coating (called MAOB coating) was fabricated on AZ91D Mg alloy by combining the process of micro-arc oxidation (MAO) with baking coating (B-coating). The structure, composition, corrosion resistance, and tribological behaviour of the coatings were investigated using scanning electron microscopy (SEM), energy dispersive spectroscopy (EDS), electrochemical and long-term immersion test, and ball-on-disc friction test. The results show that a dense 92 μm thick B-coating was tightly deposited onto the MAO-coated Mg alloy and exhibited a good mechanical interlock along the rough interface. Compared with the MAO-coated sample, the corrosion current density of the MAOB-coated Mg alloy decreased by two or three orders of magnitude and no corrosion phenomenon was observed during a long-term immersion test of about 500 h (severe corrosion pits were found for MAO-treated samples after about 168 h of immersion). The frictional coefficient values of the MAOB coating were similar to those of the MAO coating using dry sliding tests, while the B-coating on the MAO-coated surface significantly improved the wear resistance of the AZ91D Mg alloy. All of these results indicate that a B-coating can be used to further protect Mg alloys from corrosion and wear by providing a thick, dense barrier.

The formation of FHA coating on biodegradable Mg-Zn-Zr alloy using a two-step chemical treatment method

International Nuclear Information System (INIS)

Jiang, S.T.; Zhang, J.; Shun, S.Z.; Chen, M.F.

2016-01-01

Highlights: • Use a two-step chemical treatment method for formation of FHA coating on biodegradable Mg-Zn-Zr alloy;. • We reported the formation mechanism of FHA coating on Mg-Zn-Zr alloy and achieved optimum properties;. • The MgF_2 coating and FHA coating provide effective protection for the Mg alloy substrate and the FHA coating showed better corrosion resistance. - Abstract: To improve the corrosion resistance of the biomedical magnesium alloy, a two-step chemical treatment method has been employed to prepare an FHA coating on the alloy surface. Prior to forming an FHA layer, the samples of Mg-3 wt% Zn-0.5 wt% Zr alloy were soaked in HF with concentration of 20% (v/v) at 37 °C temperature for 2 h, and were then placed into an aqueous solution with 0.1 mol/L Ca(NO_3).4H_2O and 0.06 mol/L NH_4H_2PO_4 at 90 °C to prepare the Ca-P coating. The concentrations of Mg"2"+, F"− ions, and pH variation with immersing time in the solution were investigated to explore the growth mechanism of FHA. The surface morphologies and compositions of the coatings were characterized by X-ray diffraction, scanning electron microscopy, and energy dispersive spectroscopy. The results showed that the alloy surface treated with acid formed a layer of MgF_2 nanoparticles with a thickness of 0.7 μm. The corrosion resistance of coatings in SBF solution was evaluated by electrochemical impedance spectroscopy (EIS) and potentiodynamic polarization. The results showed that the substrate with FHA coating had good corrosion resistance. After immersing into the calcium phosphate solution, some small spherical particles were first formed on the surface; these then cover the surface completely after 20 min. Some clusters consisting of needle-like crystal were observed in the spherical particles covering the surface, and the Ca/P ratio of the needle-like crystal was 1.46, clearly growing along the c axis preferred orientation growth. After immersion for 60 min, the FHA coating with

Double-layer Tablets of Lornoxicam: Validation of Quantification ...

African Journals Online (AJOL)

Double-layer Tablets of Lornoxicam: Validation of Quantification Method, In vitro Dissolution and Kinetic Modelling. ... Satisfactory results were obtained from all the tablet formulations met compendial requirements. The slowest drug release rate was obtained with tablet cores based on PVP K90 (1.21 mg%.h-1).

Effect Of Formulating Additives On The Properties Of Ibuprofen Tablets

African Journals Online (AJOL)

A study of the comparative effects of different formulating additives and film coating on the properties of ibuprofen tablets was made. The tested properties were hardeness (H), friability (F), the disintegration time (D) and dissolution characteristics of ibuprofen tablets. The hardeness, friability, the hardeness friability ratio ...

Enteric coated HPMC capsules plugged with 5-FU loaded microsponges: a potential approach for treatment of colon cancer

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Ankita Gupta

2015-09-01

Full Text Available The work was aimed at developing novel enteric coated HPMC capsules (ECHC plugged with 5 Florouracil (5-FU loaded Microsponges in combination with calcium pectinate beads. Modified quasi-emulsion solvent diffusion method was used to formulate microsponges based on 32 factorial design and the effects of independent variables (volume of organic solvent and Eudragit RS100 content on the dependent variables (Particle size, %EE & % CDR were determined. The optimized microsponges (F4 were characterized by SEM, PXRD, TGA and were plugged along with calcium pectinate beads in HPMC capsules and the HPMC capsules were further coated with enteric polymer Eudragit L 100 (Ed-L100 and/ or Eudrgit S 100 (Ed-S 100 in different proportions. In vitro release study of ECHC was performed in various release media sequentially SGF for 2 h, followed by SIF for the next 6 h and then in SCF (in the presence and absence of pectinase enzyme for further 16 h. Drug release was retarded on coating with EdS-100 in comparison to blend of EdS-100: EdL-100 coating. The percentage of 5-FU released at the end of 24 h from ECHC 3 was 97.83 ± 0.12% in the presence of pectinase whereas in control study it was 40.08 ± 0.02% drug. The optimized formulation was subjected to in vivo Roentgenographic studies in New Zealand white rabbits to analyze the in vivo behavior of the developed colon targeted capsules. Pharmacokinetic studies in New Zealand white rabbits were conducted to determine the extent of systemic exposure provided by the developed formulation in comparison to 5-FU aqueous solutions. Thus, enteric coated HPMC capsules plugged with 5-FU loaded microsponges and calcium pectinate beads proved to be promising dosage form for colon targeted drug delivery to treat colorectal cancer.

Esophageal transit and in vivo disintegration of branded risedronate sodium tablets and two generic formulations of alendronic acid tablets: a single-center, single-blind, six-period crossover study in healthy female subjects.

Science.gov (United States)

Perkins, Alan C; Blackshaw, P Elaine; Hay, Peter D; Lawes, Simon C; Atherton, Clare T; Dansereau, Richard J; Wagner, Leigh K; Schnell, Dan J; Spiller, Robin C

2008-05-01

Delayed esophageal transit or disintegration of oral bisphosphonate tablets before they enter the stomach may be of concern with respect to iatrogenic complications among patients receiving longterm treatment. Different formulations of generic bisphosphonate tablets meeting regulatory requirements may have substantial differences in pharmaceutical attributes from the branded product that may result in different characteristics during esophageal transit. The primary objective of this study was to evaluate and compare esophageal transit times and in vivo disintegration of 3 bisphosphonate formulations, one branded and the others generic, that are commercially available in Canada and the United Kingdom. This was a single-center, randomized, singleblind, 6-period crossover study in healthy postmenopausal women aged >50 years. Each subject received a single oral dose of a branded risedronate sodium 35-mg tablet and 2 generic formulations of alendronic acid 70-mg tablets (Novopharm Limited, Toronto, Canada, and Teva UK Limited, Morley, United Kingdom) in both the erect and semisupine (45 degrees ) positions. Although the products are labeled to be taken in the erect position, the semisupine position was included to simulate dosing in bedridden patients. Subjects took tablets with 30 mL of water in the morning after an overnight fast. The tablets were radiolabeled with technetium-99m ion-exchange resins to enable visualization and measurement of esophageal transit time and disintegration using a gamma camera. Dynamic scintigraphic images were obtained for a total of 10 minutes: 2 images per second for the first 30 seconds and 1 image every 15 seconds for 9.5 minutes. This was a mechanistic study and tolerability was not assessed. The study was conducted in 20 healthy white female subjects with a mean age of 62 years (range, 51-77 years). The effect of body position was statistically significant (P = 0.043), with the estimated hazard ratio (HR) of 0.74 indicating longer

Influence of compression forces on tablets disintegration by AC Biosusceptometry.

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Corá, Luciana A; Fonseca, Paulo R; Américo, Madileine F; Oliveira, Ricardo B; Baffa, Oswaldo; Miranda, José Ricardo A

2008-05-01

Analysis of physical phenomena that occurs during tablet disintegration has been studied by several experimental approaches; however none of them satisfactorily describe this process. The aim of this study was to investigate the influence of compression force on the tablets by associating the AC Biosusceptometry with consolidated methods in order to validate the biomagnetic technique as a tool for quality control in pharmaceutical processes. Tablets obtained at five compression levels were submitted to mechanical properties tests. For uncoated tablets, water uptake and disintegration force measurements were performed in order to compare with magnetic data. For coated tablets, magnetic measurements were carried out to establish a relationship between physical parameters of the disintegration process. According to the results, differences between the compression levels were found for water uptake, force development and magnetic area variation measurements. ACB method was able to estimate the disintegration properties as well as the kinetics of disintegration process for uncoated and coated tablets. This study provided a new approach for in vitro investigation and validated this biomagnetic technique as a tool for quality control for pharmaceutical industry. Moreover, using ACB will also be possible to test these parameters in humans allowing to establish an in vitro/in vivo correlation (IVIVC).

Effect of Electrochemically Deposited MgO Coating on Printable Perovskite Solar Cell Performance

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T.A. Nirmal Peiris

2017-02-01

Full Text Available Herein, we studied the effect of MgO coating thickness on the performance of printable perovskite solar cells (PSCs by varying the electrodeposition time of Mg(OH2 on the fluorine-doped tin oxide (FTO/TiO2 electrode. Electrodeposited Mg(OH2 in the electrode was confirmed by energy dispersive X-ray (EDX analysis and scanning electron microscopic (SEM images. The performance of printable PSC structures on different deposition times of Mg(OH2 was evaluated on the basis of their photocurrent density-voltage characteristics. The overall results confirmed that the insulating MgO coating has an adverse effect on the photovoltaic performance of the solid state printable PSCs. However, a marginal improvement in the device efficiency was obtained for the device made with the 30 s electrodeposited TiO2 electrode. We believe that this undesirable effect on the photovoltaic performance of the printable PSCs is due to the higher coverage of TiO2 by the insulating MgO layer attained by the electrodeposition technique.

The Effectiveness of Al-Si Coatings for Preventing Interfacial Reaction in Al-Mg Dissimilar Metal Welding

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Wang, Yin; Al-Zubaidy, Basem; Prangnell, Philip B.

2018-01-01

The dissimilar welding of aluminum to magnesium is challenging because of the rapid formation of brittle intermetallic compounds (IMC) at the weld interface. An Al-Si coating interlayer was selected to address this problem, based on thermodynamic calculations which predicted that silicon would change the reaction path to avoid formation of the normally observed binary Al-Mg IMC phases ( β-Al3Mg2 and γ-Al12Mg17). Long-term static heat treatments confirmed that a Si-rich coating will preferentially produce the Mg2Si phase in competition with the less stable, β-Al3Mg2 and γ-Al12Mg17 binary IMC phases, and this reduced the overall reaction layer thickness. However, when an Al-Si clad sheet was tested in a real welding scenario, using the Refill™ friction stir spot welding (FSSW) technique, Mg2Si was only produced in very small amounts owing to the much shorter reaction time. Surprisingly, the coating still led to a significant reduction in the IMC reaction layer thickness and the welds exhibited enhanced mechanical performance, with improved strength and fracture energy. This beneficial behavior has been attributed to the softer coating material both reducing the welding temperature and giving rise to the incorporation of Si particles into the reaction layer, which toughened the brittle interfacial IMC phases during crack propagation.

21 CFR 520.1720a - Phenylbutazone tablets and boluses.

Science.gov (United States)

2010-04-01

... Section 520.1720a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES...-mg or 1-g tablets, or 2- or 4-g boluses, in dogs and horses. (2) Nos. 000010 and 059130 for use of 100- or 200-mg or 1-g tablets in dogs and horses. (3) Nos. 000856 and 061623 for use of 100-mg or 1-g...

Paracetamol 325 mg/tramadol 37.5 mg effect on pain during needle electromyography: a double-blind crossover clinical trial.

Science.gov (United States)

Kalantar, Seyed Sadeq; Abbasi, Mehrshad; Faghihi-Kashani, Sara; Majedi, Hossein; Ahmadi, Mona; Agah, Elmira; Tafakhori, Abbas

2016-12-01

Needle insertion during electromyography (EMG) may cause varying levels of pain that could lead to inaccurate assessment and premature termination of the procedure. The aim of this study is to compare paracetamol 325 mg/tramadol 37.5 mg with placebo in relieving pain before EMG. This is a randomized, crossover, placebo-controlled, double-blind clinical trial; forty-four healthy individuals, including 27 males with a mean age of 35.3 years (range 18-59 years), entered this study. The needles were inserted unilaterally 2 h after administration of two analgesic tablets of paracetamol 325 mg/tramadol 37.5 mg or two placebo tablets. The pain was scored through a 100-mm visual analog scale (VAS) immediately and 2 h after the procedure. The side effects were also recorded. Within a week, the procedure was repeated on the other upper limb, changing the treatment and placebo. The immediate and 2-h VAS scores were notably lower after administration of treatment compared to placebo (immediate pain: 17.5 ± 12.8 vs. 32.1 ± 16.0, P pain: 1.6 ± 5.6 vs. 5.8 ± 7.9, P = 0. 002). There was a higher prevalence of side effects when treatment was used (48 vs. 9 %, P pain. Further application of this medication in patients with neuromuscular disorders would warrant additional clinical trials, particularly considering the adverse events.

Design of tablets for the delayed and complete release of poorly water-soluble weak base drugs using SBE7M-β-CD as a solubilizing agent.

Science.gov (United States)

Rao, Venkatramana M; Zannou, Erika A; Stella, Valentino J

2011-04-01

The challenge of designing a delayed-release oral dosage form is significantly increased when the drug substance is poorly water soluble. This manuscript describes the design and characterization of a novel controlled-release film-coated tablet for the pH-triggered delayed and complete release of poorly water-soluble weak base drugs. Delivery of weak bases is specifically highlighted with the use of dipyridamole and prazosin as model compounds. Tailored delayed release is achieved with a combination of an insoluble but semipermeable polymer and an enteric polymer, such as cellulose acetate and hydroxypropyl cellulose phthalate, respectively, as coatings. The extent of the time lag prior to complete release depends on the film-coating composition and thickness. Complete release is achieved by the addition of a cyclodextrin, namely SBE7M-β-CD with or without a pH modifier added to the tablet core to ensure complete solubilization and release of the drug substance. The film-coating properties allow the complex formation/solubilization to occur in situ. Additionally, the drug release rate can be modulated on the basis of the cyclodextrin to drug molar ratio. This approach offers a platform technology for delayed release of potent but poorly soluble drugs and the release can be modulated by adjusting the film-coating composition and thickness and/or the cyclodextrin and pH modifier, if necessary. Copyright © 2010 Wiley-Liss, Inc.

Compounded Apixaban Suspensions for Enteral Feeding Tubes.

Science.gov (United States)

Caraballo, Maria L; Donmez, Seda; Nathan, Kobi; Zhao, Fang

2017-07-01

Objective: There is limited information on compounded apixaban formulations for administration via enteral feeding tubes. This study was designed to identify a suitable apixaban suspension formulation that is easy to prepare in a pharmacy setting, is compatible with commonly used feeding tubes, and has a beyond-use date of 7 days. Methods: Apixaban suspensions were prepared from commercially available 5-mg Eliquis tablets. Several vehicles and compounding methods were screened for ease of preparation, dosage accuracy, and tube compatibility. Two tubing types, polyurethane and polyvinyl chloride, with varying lengths and diameters, were included in the study. They were mounted on a peg board during evaluation to mimic the patient body position. A 7-day stability study of the selected formulation was also conducted. Results: Vehicles containing 40% to 60% Ora-Plus in water all exhibited satisfactory flowability through the tubes. The mortar/pestle compounding method was found to produce more accurate and consistent apixaban suspensions than the pill crusher or crushing syringe method. The selected formulation, 0.25 mg/mL apixaban in 50:50 Ora-Plus:water, was compatible with both tubing types, retaining >98% drug in posttube samples. The stability study also confirmed that this formulation was stable physically and chemically over 7 days of storage at room temperature. Conclusions: A suitable apixaban suspension formulation was identified for administration via enteral feeding tubes. The formulation consisted of 0.25 mg/mL apixaban in 50:50 Ora-Plus:water. The stability study results supported a beyond-use date of 7 days at room temperature.

Using a single tablet daily to treat latent tuberculosis infection in Brazil: bioequivalence of two different isoniazid formulations (300 mg and 100 mg) demonstrated by a sensitive and rapid high-performance liquid chromatography-tandem mass spectrometry method in a randomised, crossover study.

Science.gov (United States)

Daher, André; Pitta, Luciana; Santos, Tereza; Barreira, Draurio; Pinto, Douglas

2015-06-01

The recommended treatment for latent tuberculosis (TB) infection in adults is a daily dose of isoniazid (INH) 300 mg for six months. In Brazil, INH was formulated as 100 mg tablets. The treatment duration and the high pill burden compromised patient adherence to the treatment. The Brazilian National Programme for Tuberculosis requested a new 300 mg INH formulation. The aim of our study was to compare the bioavailability of the new INH 300 mg formulation and three 100 mg tablets of the reference formulation. We conducted a randomised, single dose, open label, two-phase crossover bioequivalence study in 28 healthy human volunteers. The 90% confidence interval for the INH maximum concentration of drug observed in plasma and area under the plasma concentration vs. time curve from time zero to the last measurable concentration "time t" was 89.61-115.92 and 94.82-119.44, respectively. The main limitation of our study was that neither adherence nor the safety profile of multiple doses was evaluated. To determine the level of INH in human plasma, we developed and validated a sensitive, simple and rapid high-performance liquid chromatography-tandem mass spectrometry method. Our results showed that the new formulation was bioequivalent to the 100 mg reference product. This finding supports the use of a single 300 mg tablet daily strategy to treat latent TB. This new formulation may increase patients' adherence to the treatment and quality of life.

Using a single tablet daily to treat latent tuberculosis infection in Brazil: bioequivalence of two different isoniazid formulations (300 mg and 100 mg demonstrated by a sensitive and rapid high-performance liquid chromatography-tandem mass spectrometry method in a randomised, crossover study

Directory of Open Access Journals (Sweden)

André Daher

2015-06-01

Full Text Available The recommended treatment for latent tuberculosis (TB infection in adults is a daily dose of isoniazid (INH 300 mg for six months. In Brazil, INH was formulated as 100 mg tablets. The treatment duration and the high pill burden compromised patient adherence to the treatment. The Brazilian National Programme for Tuberculosis requested a new 300 mg INH formulation. The aim of our study was to compare the bioavailability of the new INH 300 mg formulation and three 100 mg tablets of the reference formulation. We conducted a randomised, single dose, open label, two-phase crossover bioequivalence study in 28 healthy human volunteers. The 90% confidence interval for the INH maximum concentration of drug observed in plasma and area under the plasma concentration vs. time curve from time zero to the last measurable concentration “time t” was 89.61-115.92 and 94.82-119.44, respectively. The main limitation of our study was that neither adherence nor the safety profile of multiple doses was evaluated. To determine the level of INH in human plasma, we developed and validated a sensitive, simple and rapid high-performance liquid chromatography-tandem mass spectrometry method. Our results showed that the new formulation was bioequivalent to the 100 mg reference product. This finding supports the use of a single 300 mg tablet daily strategy to treat latent TB. This new formulation may increase patients’ adherence to the treatment and quality of life.

The formation of FHA coating on biodegradable Mg-Zn-Zr alloy using a two-step chemical treatment method

Energy Technology Data Exchange (ETDEWEB)

Jiang, S.T.; Zhang, J.; Shun, S.Z. [School of Materials Science and Engineering, Tianjin University of Technology, Tianjin (China); Chen, M.F., E-mail: mfchentj@126.com [School of Materials Science and Engineering, Tianjin University of Technology, Tianjin (China); Tianjin Key Laboratory of Display Materials and Photoelectric Device, Tianjin University of Technology , Tianjin (China)

2016-12-01

Highlights: • Use a two-step chemical treatment method for formation of FHA coating on biodegradable Mg-Zn-Zr alloy;. • We reported the formation mechanism of FHA coating on Mg-Zn-Zr alloy and achieved optimum properties;. • The MgF{sub 2} coating and FHA coating provide effective protection for the Mg alloy substrate and the FHA coating showed better corrosion resistance. - Abstract: To improve the corrosion resistance of the biomedical magnesium alloy, a two-step chemical treatment method has been employed to prepare an FHA coating on the alloy surface. Prior to forming an FHA layer, the samples of Mg-3 wt% Zn-0.5 wt% Zr alloy were soaked in HF with concentration of 20% (v/v) at 37 °C temperature for 2 h, and were then placed into an aqueous solution with 0.1 mol/L Ca(NO{sub 3}).4H{sub 2}O and 0.06 mol/L NH{sub 4}H{sub 2}PO{sub 4} at 90 °C to prepare the Ca-P coating. The concentrations of Mg{sup 2+}, F{sup −} ions, and pH variation with immersing time in the solution were investigated to explore the growth mechanism of FHA. The surface morphologies and compositions of the coatings were characterized by X-ray diffraction, scanning electron microscopy, and energy dispersive spectroscopy. The results showed that the alloy surface treated with acid formed a layer of MgF{sub 2} nanoparticles with a thickness of 0.7 μm. The corrosion resistance of coatings in SBF solution was evaluated by electrochemical impedance spectroscopy (EIS) and potentiodynamic polarization. The results showed that the substrate with FHA coating had good corrosion resistance. After immersing into the calcium phosphate solution, some small spherical particles were first formed on the surface; these then cover the surface completely after 20 min. Some clusters consisting of needle-like crystal were observed in the spherical particles covering the surface, and the Ca/P ratio of the needle-like crystal was 1.46, clearly growing along the c axis preferred orientation growth. After

Hybrid epoxy–silane coatings for improved corrosion protection of Mg alloy

International Nuclear Information System (INIS)

Brusciotti, Fabiola; Snihirova, Darya V.; Xue, Huibin; Montemor, M. Fatima; Lamaka, Svetlana V.; Ferreira, Mario G.S.

2013-01-01

Highlights: ► Hybrid epoxy–silane coatings for corrosion protection of Mg alloy AZ31. ► Electrochemical impedance spectroscopy to study the corrosion behavior. ► Very good corrosion protection after 1 month immersion in 0.05 M NaCl. ► Surface and chemical characterization to understand corrosion processes. ► Influence of organic structure in coatings corrosion performance. - Abstract: New hybrid epoxy–silane coatings, with added functionalities for improved performance and durability, were designed to increase the corrosion protection of magnesium alloys. The corrosion behavior of the coated AZ31 was studied through electrochemical impedance spectroscopy (EIS) in 0.05 M NaCl. The morphology and surface chemistry of the samples were also investigated through scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FT-IR) before and after immersion in the electrolyte. The new hybrid silane coatings showed a high resistance to corrosion that persisted throughout one-month immersion in a pH-neutral NaCl solution.

Calcium phosphate/chitosan composite coating: Effect of different concentrations of Mg{sup 2+} in the m-SBF on its bioactivity

Energy Technology Data Exchange (ETDEWEB)

Zhang, Jie [School of Chemistry Engineering and Technology, Harbin Institute of Technology, Harbin 150001 (China); Pharmacy College, Jiamusi University, Jiamusi 154007 (China); Dai, Changsong, E-mail: changsd@hit.edu.cn [School of Chemistry Engineering and Technology, Harbin Institute of Technology, Harbin 150001 (China); Wei, Jie [School of Chemistry Engineering and Technology, Harbin Institute of Technology, Harbin 150001 (China); School of Chemistry and Bioengineering, Suzhou Science Technology University, Suzhou 215009 (China); Wen, Zhaohui, E-mail: wenzhaohui1968@163.com [Department of neuro intern, First Affiliated Hospital of Harbin Medical University, Harbin 150001 (China); Zhang, Shujuan; Lin, Lemin [Department of neuro intern, First Affiliated Hospital of Harbin Medical University, Harbin 150001 (China)

2013-09-01

The purpose of this study was to investigate the effect of different concentration of Mg{sup 2+} in a modified simulated body fluid (m-SBF) on the bioactivity of calcium phosphate/chitosan composite coating. Calcium phosphate/chitosan composite coating was prepared on graphite substrate via electrophoretic deposition (EPD) followed by conversion in a phosphate buffer solution (PBS). The obtained samples were soaked in the m-SBF containing different concentration of Mg{sup 2+} for different times. And then, the composite coatings were assessed using X-ray diffractometer (XRD), Fourier-transformed infrared spectroscopy (FTIR), Raman spectra, and scanning electron microscope (SEM) with an energy dispersive spectrometer (EDS). The soaking solution was evaluated by inductively coupled plasma optical emission spectrometer (ICP-OES) test. The analytical results showed that hydroxyapatite (HA) and bone-like apatite (HCA) grew on the surface of calcium phosphate/chitosan composite coating after incubation in different m-SBF. With Mg{sup 2+} concentration in m-SBF increased from 1× Mg to 10× Mg, HA in the composite coating first presented a dissolving process and then a precipitating one slowly, while HCA presented a growing trend, continuously. The increasing of Mg{sup 2+} concentration in the m-SBF inhibited the total growing process of HA and HCA as a whole. The structure of the composite coating changed from spherical into irregular morphology with the concentration of Mg{sup 2+} increasing from 1× Mg to 10× Mg. Over all, with the Mg{sup 2+} concentration increasing, the bioactivity of calcium phosphate/chitosan composite coating tended to decrease.

Comparative effects of aspirin and enteric-coated aspirin on loss of chromium 51-labeled erythrocytes from the gastrointestinal tract

International Nuclear Information System (INIS)

Robbins, D.C.; Schwartz, R.S.; Kutny, K.; Vallejo, G.; Horton, E.S.; Cotter, J.M.

1984-01-01

Sodium chromate Cr 51 was used to label red blood cells of 19 healthy male volunteers, whose stools were collected for four days before and four days during oral administration of either uncoated (N . 9) or enteric-coated (N . 10) aspirin. Each subject received 2.925 gm/day of aspirin, in three equal doses separated by eight-hour intervals, for a total of seven days. During drug use, stools were collected on days 4 through 7. Fecal blood content, estimated by measuring radioactivity in the stools, was significantly higher (P less than 0.001) during use of either type of aspirin than at baseline, but losses measured during use of the coated aspirin (mean, 1.54 ml/day) were significantly lower (P less than 0.001) than those measured during use of the uncoated aspirin (mean, 4.33 ml/day). The two types of aspirin produced equivalent serum concentrations of salicylates. We conclude that enteric-coated aspirin reduces gastrointestinal blood loss

21 CFR 520.1200 - Ivermectin, fenbendazole, and praziquantel tablets.

Science.gov (United States)

2010-04-01

... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ivermectin, fenbendazole, and praziquantel tablets... Ivermectin, fenbendazole, and praziquantel tablets. (a) Specifications. Each chewable tablet contains either: (1) 68 micrograms (µg) ivermectin, 1.134 grams fenbendazole, and 57 milligrams (mg) praziquantel; or...

Adjustment of the ratio of Ca/P in the ceramic coating on Mg alloy by plasma electrolytic oxidation

International Nuclear Information System (INIS)

Yao Zhongping; Li Liangliang; Jiang Zhaohua

2009-01-01

The ceramic coatings containing Ca and P were prepared on AZ91D Mg alloy by plasma electrolytic oxidation technique in NaOH system and Na 2 SiO 3 system, respectively. The phase composition, morphology and the element distribution of the coatings was studied by X-ray diffraction, scanning electron microscopy and energy dispersive spectroscopy. The corrosion resistance of the coatings was examined by polarizing curve methods in a 0.9% NaCl solution. In NaOH system, there were a large number of micro-holes distributing evenly on the surface of the coating, and the coating was mainly composed of Mg, Al, P and Ca. In Na 2 SiO 3 system, the micro-holes in the coatings were reduced greatly in number and the distribution of the micro-holes was uneven, and the coating was mainly composed of Mg, Al, Si, P and Ca. The ratio of Ca/P in the coating can be controlled by the adjustment of the technique parameters to a certain extent. The adjustment of the concentration of Ca 2+ in the electrolyte was an effective method to change the ratio of Ca/P in the coating in both systems; the reaction time and the working voltage for the adjustment of the ratio of Ca/P in the coating was more suitable for the NaSi 2 O 3 system than the NaOH system. The polarizing curve tests showed the coatings improved the corrosion resistance of the AZ91D Mg alloy in 0.9% NaCl solution by nearly two orders of magnitude.

Enhanced biocorrosion resistance and biocompatibility of degradable Mg-Nd-Zn-Zr alloy by brushite coating.

Science.gov (United States)

Niu, Jialin; Yuan, Guangyin; Liao, Yi; Mao, Lin; Zhang, Jian; Wang, Yongping; Huang, Feng; Jiang, Yao; He, Yaohua; Ding, Wenjiang

2013-12-01

To further improve the corrosion resistance and biocompatibility of Mg-Nd-Zn-Zr alloy (JDBM), a biodegradable calcium phosphate coating (Ca-P coating) with high bonding strength was developed using a novel chemical deposition method. The main composition of the Ca-P coating was brushite (CaHPO4·2H2O). The bonding strength between the coating and the JDBM substrate was measured to be over 10 MPa, and the thickness of the coating layer was about 10-30 μm. The in vitro corrosion tests indicated that the Ca-P treatment improved the corrosion resistance of JDBM alloy in Hank's solution. Ca-P treatment significantly reduced the hemolysis rate of JDBM alloy from 48% to 0.68%, and induced no toxicity to MC3T3-E1 cells. The in vivo implantation experiment in New Zealand's rabbit tibia showed that the degradation rate was reduced obviously by the Ca-P treatment and less gas was produced from Ca-P treated JDBM bone plates and screws in early stage of the implantation, and at least 10weeks degradation time can be prolonged by the present coating techniques. Both Ca-P treated and untreated JDBM Mg alloy induced bone growth. The primary results indicate that the present Ca-P treatment is a promising technique for the degradable Mg-based biomaterials for orthopedic applications. © 2013.

Industrial production of MgH2 and its application

International Nuclear Information System (INIS)

Uesugi, H.; Sugiyama, T.; Nii, H.; Ito, T.; Nakatsugawa, I.

2011-01-01

Research highlights: → Tablet and powder Mg were hydrogenated in a 50 kg batch furnace based on thermal equilibrium method. → Compression of Mg tablet improved the hydrogenation yield. → Hydrolysis of MgH 2 using citric acid generated hydrogen under 373 K. → A MgH 2 -hydrogen reactor utilizing hydraulic head pressure was developed. → - Abstract: A process for the industrial production of magnesium hydride (MgH 2 ) based on a thermal equilibrium method and its application to portable hydrogen sources is proposed. Mg powders and tablets compressed with mechanically ground Mg ribbons were successfully hydrogenated in a 50-kg-batch furnace. The resultant MgH 2 showed a hydrogen yield of around 96% with good reproducibility. The compression ratio of Mg tablets was found to be an important factor in the hydrogenation yield. A hydrolysis technique using citric acid as an additive was employed to generate hydrogen under 373 K. Increasing the concentration of citric acid and the temperature accelerated the hydrolysis reactivity. A hydrogen reactor utilizing hydraulic head pressure was developed. It generated hydrogen continuously for 1 h at a flow rate of 100 ml min -1 with hydrolysis of 5 g of tablet-form MgH 2 . The conversion yield was around 70%, regardless of the flow rate.

Bioavailability of syrup and tablet formulations of cefetamet pivoxil.

Science.gov (United States)

Ducharme, M P; Edwards, D J; McNamara, P J; Stoeckel, K

1993-12-01

Two studies examining the bioavailability of cefetamet pivoxil in healthy male subjects were conducted. In the first, the bioavailabilities of the 250-mg (M250) and M500 tablet formulations of cefetamet pivoxil to be marketed were compared with that of a tablet used in clinical trials. All products were given with food at a dose of 500 mg. In the second study, the bioavailability of the syrup formulation was evaluated under both fasting and nonfasting conditions and compared with that of the M500 tablet formulation given with food. The absolute bioavailabilities of the M500 and M250 tablets (55.0% +/- 8.0% and 55.7% +/- 7.0%, respectively) were not significantly different from that of the clinical-trial formulation (49.8% +/- 8.5%). The newer tablet formulations exhibited faster absorption as evidenced by higher peak concentrations (3.8 [M500] and 3.9 [M250] mg/liter compared with 3.2 mg/liter for the clinical-trial formulation), a shorter time to peak concentration, and a shorter mean absorption time. The syrup formulation was found to have significantly lower absolute bioavailability (37.9% +/- 6.0%) compared with that of the M500 tablet (58.4% +/- 9.0%) when both were given with food. Food had no significant effect on the bioavailability of the syrup, which averaged 34.0% +/- 8.6% under fasting conditions, although absorption was delayed by food (mean absorption time increased from 2.2 to 3.9 h). This contrasts with the results of previous studies documenting significant increases in tablet bioavailability with food. Despite the lower bioavailability of the syrup, unbound-cefetamet concentrations are expected to remain above the MICs for 90% of the strains tested for susceptible organisms for approximately 10 h of the usual 12-h dosing interval with both syrup and tablet formulations of cefetamet pivoxil given with food.

The Effectiveness of Al-Si Coatings for Preventing Interfacial Reaction in Al - Mg Dissimilar Metal Welding

OpenAIRE

Wang, Yin; Al-Zubaidy, Basem; Prangnell, Philip

2017-01-01

The dissimilar welding of aluminum to magnesium is challenging because of the rapid formation of brittle intermetallic compounds (IMC) at the weld interface. An Al-Si coating interlayer was selected to address this problem, based on thermodynamic calculations that predicted silicon would change the reaction path to avoid formation of the normally observed binary Al-Mg IMC phases (-Al3Mg2 and -Al12Mg17). Long-term static heat treatments confirmed that a Si-rich coating will preferentially pr...

PREPARATION AND CHARACTERIZATION OF CHITOSAN TABLETS OF ACECLOFENAC FOR COLON TARGETED DRUG DELIVERY

OpenAIRE

UMA DEVI,THIRUGANESH, SURESH

2013-01-01

The present study objective was to develop novel colon specific drug delivery systems for aceclofenac using chitosan as a microbially degradable polymeric carrier and to coat the optimized batches with a pH dependent polymeric coating solution containing Eudragit L 100 and S 100 (1:4). Tablets containing four proportions of chitosan were prepared. The tablets were evaluated for physicochemical properties, drug content, dissolution, water uptake & erosion characteristics, in vitro drug rel...

Brand versus generic dispensing trend for ciprofloxacin 500 mg, levofloxacin 500 mg, and moxifloxacin 400 mg (oral dosage forms) among pharmacies of Karachi, Pakistan.

Science.gov (United States)

Zehra, Fatima; Naqvi, Atta Abbas; Tasneem, Sumbul; Ahmad, Rizwan; Ahmad, Niyaz; Shamsi, Adnan Zia; Asghar, Naqiya Ali; Khan, Ghufran Ullah

2017-01-01

Pakistan spends 0.7% of its gross domestic product on health. The public sector health-care system provides services to 22% of population thus paving the way for a dominant private sector. Patients in Pakistan mostly pay their medical expenses directly, and 64% of the health expenditures are borne by the household. Expenditure on medicine constitutes 43% of the total household expenditure. A quantitative cross-sectional study was conducted in Karachi, Pakistan, for a month. It was aimed at gathering response from different pharmacies to understand the brand versus generic dispensing trend of ciprofloxacin 500 mg, levofloxacin 500 mg, and moxifloxacin 400 mg oral dosage forms. The study employed convenience sampling and used a survey checklist. The data gathered was entered in SPSS version 22. The mean price per tablet for ciprofloxacin brand and generic was reported at Pakistani Rupees (PKR) 48.44 and PKR 26.85, respectively. The trend for dispensing ciprofloxacin highlighted a split in the market between brand (51%) and generic (49%). For levofloxacin brand and generic, the price per tablet was reported at PKR 36.50 and PKR 36.15 respectively, and despite same price, the market was dominated by generic levofloxacin (92%). Due to a price difference between brand and generic moxifloxacin, i.e., PKR 129.44 and PKR 71.91, respectively, the market was mostly occupied by the generic form (75%). Pricing mechanism must be revisited, and the authorities should take stern actions against any illegitimate price hike. The surging burden of drug expenditure on poorer sections of the society must be addressed by the government on an urgent basis.

Cladribine tablets for relapsing-remitting multiple sclerosis

DEFF Research Database (Denmark)

Rammohan, Kottil; Giovannoni, Gavin; Comi, Giancarlo

2012-01-01

BACKGROUND: In the phase III CLARITY study, treatment with cladribine tablets at cumulative doses of 3.5 or 5.25mg/kg over 96 weeks led to significant reductions in annualized relapse rates (ARR) versus placebo in patients with relapsing-remitting multiple sclerosis. Further post hoc analyses...... of CLARITY study data were conducted to determine the efficacy of cladribine tablets across patient subgroups stratified by baseline characteristics. METHODS: Relapse rates over the 96-week CLARITY study were analyzed in cohorts stratified by demographics; disease duration; treatment history and disease...... activity at baseline. RESULTS: In the intent-to-treat population (n=437, 433 and 456 in the placebo, cladribine 3.5 and 5.25mg/kg groups, respectively), treatment with cladribine tablets 3.5 and 5.25mg/kg led to consistent improvements in ARR versus placebo in patients stratified by gender; age (≤40...

A non-destructive method for quality control of the pellet distribution within a MUPS tablet by terahertz pulsed imaging

DEFF Research Database (Denmark)

Novikova, Anna; Markl, Daniel; Axel Zeitler, J

2018-01-01

Terahertz pulsed imaging (TPI) was applied to analyse the inner structure of multiple unit pellet system (MUPS) tablets. MUPS tablets containing different amounts of theophylline pellets coated with Eudragit® NE 30 D and with microcrystalline cellulose (MCC) as cushioning agent were analysed....... The tablets were imaged by TPI and the results were compared to X-ray microtomography. The terahertz pulse beam propagates through the tablets and is back-reflected at the interface between the MCC matrix and the coated pellets within the tablet causing a peak in the terahertz waveform. Cross-section images...... of the tablets were extracted at different depths and parallel to the tablet faces from 3D terahertz data to visualize the surface-near structure of the MUPS tablets. The images of the surface-near structure of the MUPS tablets were compared to X-ray microtomography images at the same depths. The surface...

Physical and Microstructure Properties of MgAl2C2 Matrix Composite Coating on Titanium

Science.gov (United States)

Li, Peng

2014-12-01

This work is based on the dry sliding wear of the MgAl2C2-TiB2-FeSi composite coating deposited on a pure Ti using a laser cladding technique. Scanning electron microscope images indicate that the nanocrystals and amorphous phases are produced in such coating. X-ray diffraction result indicated that such coating mainly consists of MgAl2C2, Ti-B, Ti-Si, Fe-Al, Ti3SiC2, TiC and amorphous phases. The high resolution transmission electron microscope image indicated that the TiB nanorods were produced in the coating, which were surrounded by other fine precipitates, favoring the formation of a fine microstructure. With increase of the laser power from 0.85 kW to 1.00 kW, the micro-hardness decreased from 1350 1450 HV0.2 to 1200 1300 HV0.2. The wear volume loss of the laser clad coating was 1/7 of pure Ti.

Ordinance on distribution of iodine tablets to the population

International Nuclear Information System (INIS)

1992-01-01

This Ordinance provides for the organization of supplies of iodine tablets to the population. The tablets will be held in case of occurrences that might endanger the population following an accident provoking the emission of radioactive iodine. The Federal Health Ministry is responsible for organizing the supply to the appropriate bodies for distribution to the population. The Ordinance entered into force on 1 August 1992. (NEA)

Structural, compositional, mechanical characterization and biological assessment of bovine-derived hydroxyapatite coatings reinforced with MgF_2 or MgO for implants functionalization

International Nuclear Information System (INIS)

Mihailescu, Natalia; Stan, G.E.; Duta, L.; Chifiriuc, Mariana Carmen; Bleotu, Coralia; Sopronyi, M.; Luculescu, C.; Oktar, F.N.; Mihailescu, I.N.

2016-01-01

Hydroxyapatite (HA) is a consecrated biomaterial for bone reconstruction. In the form of thin films deposited by pulsed laser technologies, it can be used to cover metallic implants aiming to increase biocompatibility and osseointegration rate. HA of animal origin (bovine, BHA) reinforced with MgF_2 (2 wt.%) or MgO (5 wt.%) were used for deposition of thin coatings with improved adherence, biocompatibility and antimicrobial activity. For pulsed laser deposition experiments, a KrF* (λ = 248 nm, τ_F_W_H_M ≤ 25 ns) excimer laser source was used. The deposited structures were characterized from a physical–chemical point of view by X-Ray Diffraction, Fourier Transform Infra-Red Spectroscopy, Scanning Electron Microscopy in top- and cross-view modes, Energy Dispersive X-Ray Spectroscopy and Pull-out adherence tests. The microbiological assay using the HEp-2 cell line revealed that all target materials and deposited thin films are non-cytotoxic. We conducted tests on three strains isolated from patients with dental implants failure, i.e. Microccocus sp., Enterobacter sp. and Candida albicans sp. The most significant anti-biofilm effect against Microcococcus sp. strain, at 72 h, was obtained in the presence of BHA:MgO thin films. For Enterobacter sp. strain a superior antimicrobial activity at 72 h was noticed, in respect with simple BHA or Ti control. The enhanced antimicrobial performances, correlated with good cytocompatibility and mechanical properties recommend these biomaterials as an alternative to synthetic HA for the fabrication of reliable implant coatings for dentistry and other applications. - Highlights: • Novel biological derived HA coatings fabricated by pulsed laser deposition. • Renewable resources • Reinforcement with MgF_2 and MgO improves the HA coatings' bonding strength. • Significant anti-biofilm effect obtained for MgO reinforced HA films. • Alternative low cost solutions for a new generation of dental implants.

A Three-Pulse Release Tablet for Amoxicillin: Preparation, Pharmacokinetic Study and Physiologically Based Pharmacokinetic Modeling.

Science.gov (United States)

Li, Jin; Chai, Hongyu; Li, Yang; Chai, Xuyu; Zhao, Yan; Zhao, Yunfan; Tao, Tao; Xiang, Xiaoqiang

2016-01-01

Amoxicillin is a commonly used antibiotic which has a short half-life in human. The frequent administration of amoxicillin is often required to keep the plasma drug level in an effective range. The short dosing interval of amoxicillin could also cause some side effects and drug resistance, and impair its therapeutic efficacy and patients' compliance. Therefore, a three-pulse release tablet of amoxicillin is desired to generate sustained release in vivo, and thus to avoid the above mentioned disadvantages. The pulsatile release tablet consists of three pulsatile components: one immediate-release granule and two delayed release pellets, all containing amoxicillin. The preparation of a pulsatile release tablet of amoxicillin mainly includes wet granulation craft, extrusion/spheronization craft, pellet coating craft, mixing craft, tablet compression craft and film coating craft. Box-Behnken design, Scanning Electron Microscope and in vitro drug release test were used to help the optimization of formulations. A crossover pharmacokinetic study was performed to compare the pharmacokinetic profile of our in-house pulsatile tablet with that of commercial immediate release tablet. The pharmacokinetic profile of this pulse formulation was simulated by physiologically based pharmacokinetic (PBPK) model with the help of Simcyp®. Single factor experiments identify four important factors of the formulation, namely, coating weight of Eudragit L30 D-55 (X1), coating weight of AQOAT AS-HF (X2), the extrusion screen aperture (X3) and compression forces (X4). The interrelations of the four factors were uncovered by a Box-Behnken design to help to determine the optimal formulation. The immediate-release granule, two delayed release pellets, together with other excipients, namely, Avicel PH 102, colloidal silicon dioxide, polyplasdone and magnesium stearate were mixed, and compressed into tablets, which was subsequently coated with Opadry® film to produce pulsatile tablet of

[Effect of food thickener on disintegration and dissolution of magnesium oxide tablets].

Science.gov (United States)

Tomita, Takashi; Goto, Hidekazu; Yoshimura, Yuya; Tsubouchi, Yoshiko; Nakanishi, Rie; Kojima, Chikako; Yoneshima, Mihoko; Yoshida, Tadashi; Tanaka, Katsuya; Sumiya, Kenji; Kohda, Yukinao

2015-01-01

It has been reported that magnesium oxide tablets are excreted in a non-disintegrated state in the stool of patients when the tablets are administered after being immersed in a food thickener. Therefore we examined whether immersion in a food thickener affects the pharmacological effect in patients taking magnesium oxide tablets, and whether immersion affects its disintegration and solubility. The mean dosage (1705 mg/d) was higher for patients who took tablets after immersion in a food thickener than for those who took non-immersed tablets (1380 mg/d). The disintegration time and dissolution rate of the immersed tablets were lower than those of non-immersed tablets in vitro. Furthermore, components that constitute the food thickener and differences in composition concentrations differentially affect the disintegration and solubility of magnesium oxide tablets. This suggests that commercially available food thickeners are likely to be associated with changes in the degradation of magnesium oxide tablets, and they therefore should be carefully used in certain clinical situations.

Characterization of the Micro-Arc Coatings Containing β-Tricalcium Phosphate Particles on Mg-0.8Ca Alloy

Directory of Open Access Journals (Sweden)

Mariya B. Sedelnikova

2018-04-01

Full Text Available The characterization of the microstructure, morphology, topography, composition, and physical and chemical properties of the coatings containing β-tricalcium phosphate (β-TCP particles deposited by the micro-arc oxidation (MAO method on biodegradable Mg-0.8Ca alloy has been performed. The electrolyte for the MAO process included the following components: Na2HPO4·12H2O, NaOH, NaF, and β-Ca3(PO42 (β-TCP. The coating morphology, microstructure, and compositions have been studied using scanning electron microscopy (SEM, transmission electron microscopy (TEM, energy-dispersive X-ray spectroscopy (EDX, and X-ray diffraction (XRD. With increasing of the MAO voltage from 350 to 500 V, the coating thickness and surface average roughness of the coatings increased linearly from 6 to 150 µm and from 2 to 8 µm, respectively. The coating deposited at 350 V had more homogeneous porous morphology with numerous pores similar by sizes (2–3 µm than the coatings formed at 450–500 V. The β-TCP isometric particles were included in the coating surface. The XRD recognized the amorphous-crystalline structure in the coatings with incorporation of the following phases: β-TCP, α-TCP, MgO (periclase and hydroxyapatite (HA. The corrosion experiments showed that the biodegradation rate of the Mg-0.8Ca alloy coated by calcium phosphates is almost 10 times less than that of uncoated alloy.

Formulation and Evaluation of Fast-Disintegrating Sublingual Tablets of Atropine Sulfate: the Effect of Tablet Dimensions and Drug Load on Tablet Characteristics.

Science.gov (United States)

Aodah, Alhussain; Bafail, Rawan S; Rawas-Qalaji, Mutasem

2017-07-01

In this study, we formulated and evaluated the effects of tablet dimensions and drug load on the characteristics of atropine sulfate (AS) fast-disintegrating sublingual tablets (FDSTs). We aim to develop AS FDSTs as an alternative non-invasive and portable dosage form for the emergency treatment of organophosphate (OP) toxicity. AS autoinjector, AtroPen®, is the only self-administered dosage form available as an antidote for-out-of-hospital emergency use, but it is associated with several limitations and drawbacks. Seven FDST formulations of two tablet sizes, 150 mg (A) and 50 mg (B), and of several AS loads, 0 mg (A1, B1), 2 mg (A2, B2), 4 mg (B3), and 8 mg (B4a, B4b), were formulated and manufactured by direct compression. AS FDST characteristics were evaluated using USP and non-USP tests. Results were statistically compared at p < 0.05. All FDSTs passed the USP content uniformity and friability tests, disintegrated and released AS in ≤30 and 60 s. B1 and B2 were significantly harder than A1 and A2. Water uptake of A1 was significantly the highest. However, B1 and B2 had shorter disintegration and wetting times and higher amounts of AS dissolved than did A1 and A2 (p < 0.05). Increasing AS negatively affected FDST tensile strength (p < 0.05 for B4a) and water uptake (p < 0.05 for B3, B4a and B4b), however, without affecting AS dissolution. Formulation of AS up to 16% into smaller FDSTs was successful. Smaller FDSTs were harder and disintegrated more quickly. These AS FDSTS have the potential for further in vivo testing to evaluate their OP antidote potential.

In vitro metal ion release and biocompatibility of amorphous Mg67Zn28Ca5 alloy with/without gelatin coating

International Nuclear Information System (INIS)

Chan, W.Y.; Chian, K.S.; Tan, M.J.

2013-01-01

Amorphous zinc-rich Mg–Zn–Ca alloys have exhibited good tissue compatibility and low hydrogen evolution in vivo. However, suboptimal cell–surface interaction on magnesium alloy surface observed in vitro could lead to reduced integration with host tissue for regenerative purpose. This study aims to improve cell–surface interaction of amorphous Mg 67 Zn 28 Ca 5 alloy by coating a gelatin layer by electrospinning. Coated/uncoated alloys were immersed and extracted for 3 days under different CO 2 . The immersion results showed that pH and metal ion release in the alloy extracts were affected by gelatin coating and CO 2 , suggesting their roles in alloy biocorrosion and a mechanism has been proposed for the alloy–CO 2 system with/without coating. Cytotoxicity results are evident that gelatin-coated alloy with 2-day crosslinking not only exhibited no indirect cytotoxicity, but also supported attachment of L929 and MG63 cell lines around/on the alloy with high viability. Therefore, amorphous Mg 67 Zn 28 Ca 5 alloy coated with gelatin by electrospinning technique provides a useful method to improve alloy biocompatibility. - Highlights: • Electrospinning is a new method to coat amorphous Mg 67 Zn 28 Ca 5 alloy with gelatin. • Gelatin-coated alloy has differential effect on pH and ion release at various CO 2 . • L929 cell proliferation correlates with Mg 2+ level in alloy extracts. • Biomimetic gelatin coating significantly improves cell–surface interaction

Carbon-coated boron using low-cost naphthalene for substantial enhancement of Jc in MgB2 superconductor

Energy Technology Data Exchange (ETDEWEB)

Ranot, Mahipal; Shinde, K. P.; Oh, Y. S.; Kang, S. H.; Jang, S. H.; Hwang, D. Y.; Chung, K. C. [Korea Institute of Materials Science, Changwon (Korea, Republic of)

2017-09-15

Carbon coating approach is used to prepare carbon-doped MgB{sub 2} bulk samples using low-cost naphthalene (C{sub 10}H{sub 8}) as a carbon source. The coating of carbon (C) on boron (B) powders was achieved by direct pyrolysis of naphthalene at 120 degrees C and then the C-coated B powders were mixed well with appropriate amount of Mg by solid state reaction method. X-ray diffraction analysis revealed that there is a noticeable shift in (100) and (110) Bragg reflections towards higher angles, while no shift was observed in (002) reflections for MgB2 doped with carbon. As compared to un-doped MgB{sub 2}, a systematic enhancement in Jc(H) properties with increasing carbon doping level was observed for naphthalene-derived C-doped MgB{sub 2} samples. The substantial enhancement in Jc is most likely due to the incorporation of C into MgB{sub 2} lattice and the reduction in crystallite size, as evidenced by the increase in the FWHM values for doped samples.

Chemoinformetrical evaluation of dissolution property of indomethacin tablets by near-infrared spectroscopy.

Science.gov (United States)

Otsuka, Makoto; Tanabe, Hideaki; Osaki, Kazuo; Otsuka, Kuniko; Ozaki, Yukihiro

2007-04-01

The purpose of this study was to use near-infrared spectrometry (NIR) with chemoinformetrics to predict the change of dissolution properties in indomethacin (IMC) tablets during the manufacturing process. A comparative evaluation of the dissolution properties of the tablets was performed by the diffused reflectance (DRNIR) and transmittance (TNIR) NIR spectroscopic methods. Various kinds of IMC tablets (200 mg) were obtained from a powder (20 mg of IMC, 18 mg of microcrystalline cellulose, 160 mg of lactose, and 2 mg of magnesium stearate) under various compression pressures (60-398 MPa). Dissolution tests were performed in phosphate buffer, and the time required for 75% dissolution (T75) and mean dissolution time (MDT) were calculated. DRNIR and TNIR spectra were recorded, and the both NIR spectra used to establish a calibration model for predicting the dissolution properties by principal component regression analysis (PCR). The T75 and MDT increased as the compression pressure increased, since tablet porosity decreased with increasing pressure. Intensity of the DRNIR spectra of the compressed tablets decreased as the compression pressure increased. However, the intensity of TNIR spectra increased along with the pressure. The calibration models used to evaluate the dissolution properties of tablets were established by using PCR based on both DRNIR and TNIR spectra of the tablets. The multiple correlation coefficients of the relationship between the actual and predictive T75 by the DRNIR and TNIR methods were 0.831 and 0.962, respectively. It is possible to predict the dissolution properties of pharmaceutical preparations using both DRNIR and TNIR chemoinformetric methods. The TNIR method was more accurate for predictions of the dissolution behavior of tablets than the DRNIR method. (c) 2007 Wiley-Liss, Inc.

Corrosion resistance and protection mechanism of hot-dip Zn-Al-Mg alloy coated steel sheet under accelerated corrosion environment; Yoyu Zn-Al-Mg kei gokin mekki koban no sokushin fushoku kankyoka ni okeru taishokusei toi boshoku kiko

Energy Technology Data Exchange (ETDEWEB)

Komatsu, A.; Izutani, H.; Tsujimura, T.; Ando, A.; Kittaka, T. [NKK Corp., Tokyo (Japan)

2000-08-01

Corrosion behavior of hot-dip Zn-6%Al 0-3%Mg alloy coated steel sheets in cyclic corrosion test (CCT) has been investigated. The corrosion resistance was improved with increasing Mg content in the coating layer, and the highest corrosion resistance was observed at 3% Mg. In Zn-6%Al-3%Mg alloy coated steel sheet, the formations of zinc carbonate hydroxide and zinc oxide were suppressed for longer duration compared with Zn-0.2%Al and Zn-4.5%Al-0.l%Mg alloy coated steel sheets. As a result, zinc chloride hydroxide existed stable on the surface of the coating layer. From the polarization behaviors in 5% NaCl aqueous solution after CCT, it was found that the corrosion current density of Zn-6%At-3%Mg alloy coated steel sheet was much smaller than those of Zn-0.2%Al and Zn-4.5%Al-0.1%Mg alloy coated steel sheets. As zinc carbonate hydroxide and zinc oxide had poor adhesion to the coating layer and had porous structures, these corrosion products were considered to have little protective action for the coating layer. Therefore, it was concluded that Mg suppressed the formation of such nonprotective corrosion products. resulting in the remarkable improvement of corrosion resistance. (author)

Synthesis of a carbon-coated NiO/MgO core/shell nanocomposite as a Pd electro-catalyst support for ethanol oxidation

International Nuclear Information System (INIS)

Mahendiran, C.; Maiyalagan, T.; Scott, K.; Gedanken, A.

2011-01-01

Highlights: → Carbon coated on NiO/MgO in a core/shell nanostructure is synthesized by RAPET. → The carbon-coated NiO/MgO is supported by Pd. → The electrocatalytic properties of the Pd/(NiO/MgO-C) catalyst for ethanol oxidation studied. - Abstract: Carbon coated on NiO/MgO in a core/shell nanostructure was synthesized by the single-step RAPET (reaction under autogenic pressure at elevated temperatures) technique, and the obtained formation mechanism of the core/shell nanocomposite was presented. The carbon-coated NiO/MgO and its supported Pd catalyst, Pd/(NiO/MgO-C), were characterized by SEM, HR-TEM, XRD and cyclic voltammetry. The X-ray diffraction patterns confirmed the face-centered cubic crystal structure of NiO/MgO. Raman spectroscopy measurements provided structural evidence for the formation of a NiO/MgO composite and the nature of the coated carbon shell. The high-resolution transmission electron microscopy images showed the core and shell morphologies individually. The electrocatalytic properties of the Pd/(NiO/MgO-C) catalyst for ethanol oxidation were investigated in an alkaline solution. The results indicated that the prepared Pd-NiO/MgO-C catalyst has excellent electrocatalytic activity and stability.

Composite polymer-containing coatings on Mg alloys perspective for industry and implant surgery

Science.gov (United States)

Gnedenkov, S. V.; Sinebryukhov, S. L.; Mashtalyar, D. V.; Imshinetskiy, I. M.; Gnedenkov, A. S.; Minaev, A. N.

2017-09-01

In order to improve the corrosion resistance of magnesium alloys the ways of composite protective coating formation were developed by means of plasma electrolytic oxidation (PEO) as well as electrophoretic deposition methods. Electrochemical, corrosion, tribological, and morphological properties of the MAS magnesium alloy composite coatings were studied. The composite polymer-containing coating decrease the corrosion current density values by three orders of magnitude (Ic = 2.0 . 10-10 A/cm2), in comparison with the base PEO-layer. These polymer-containing layers enable one to expand the practical usage area of Mg alloys. The application of such coatings provides the increasing the bioactivity and regulate the corrosion rate of resorbable magnesium implants.

Structural, compositional, mechanical characterization and biological assessment of bovine-derived hydroxyapatite coatings reinforced with MgF{sub 2} or MgO for implants functionalization

Energy Technology Data Exchange (ETDEWEB)

Mihailescu, Natalia [National Institute for Lasers, Plasma and Radiation Physics, Magurele RO-077125 (Romania); Stan, G.E. [National Institute of Materials Physics, Magurele RO-077125 (Romania); Duta, L. [National Institute for Lasers, Plasma and Radiation Physics, Magurele RO-077125 (Romania); Chifiriuc, Mariana Carmen [Department of Microbiology, Faculty of Biology, Bucharest RO-060101 (Romania); Bleotu, Coralia [Stefan S. Nicolau Institute of Virology, 85 Mihai Bravu Avenue, Bucharest RO-030304 (Romania); Sopronyi, M.; Luculescu, C. [National Institute for Lasers, Plasma and Radiation Physics, Magurele RO-077125 (Romania); Oktar, F.N. [Department of Bioengineering, Faculty of Engineering, Marmara University, Goztepe, Istanbul TR-34722 (Turkey); Advance Nanomaterials Research Laboratory, Marmara University, Goztepe, Istanbul TR-34722 (Turkey); Mihailescu, I.N., E-mail: ion.mihailescu@inflpr.ro [National Institute for Lasers, Plasma and Radiation Physics, Magurele RO-077125 (Romania)

2016-02-01

Hydroxyapatite (HA) is a consecrated biomaterial for bone reconstruction. In the form of thin films deposited by pulsed laser technologies, it can be used to cover metallic implants aiming to increase biocompatibility and osseointegration rate. HA of animal origin (bovine, BHA) reinforced with MgF{sub 2} (2 wt.%) or MgO (5 wt.%) were used for deposition of thin coatings with improved adherence, biocompatibility and antimicrobial activity. For pulsed laser deposition experiments, a KrF* (λ = 248 nm, τ{sub FWHM} ≤ 25 ns) excimer laser source was used. The deposited structures were characterized from a physical–chemical point of view by X-Ray Diffraction, Fourier Transform Infra-Red Spectroscopy, Scanning Electron Microscopy in top- and cross-view modes, Energy Dispersive X-Ray Spectroscopy and Pull-out adherence tests. The microbiological assay using the HEp-2 cell line revealed that all target materials and deposited thin films are non-cytotoxic. We conducted tests on three strains isolated from patients with dental implants failure, i.e. Microccocus sp., Enterobacter sp. and Candida albicans sp. The most significant anti-biofilm effect against Microcococcus sp. strain, at 72 h, was obtained in the presence of BHA:MgO thin films. For Enterobacter sp. strain a superior antimicrobial activity at 72 h was noticed, in respect with simple BHA or Ti control. The enhanced antimicrobial performances, correlated with good cytocompatibility and mechanical properties recommend these biomaterials as an alternative to synthetic HA for the fabrication of reliable implant coatings for dentistry and other applications. - Highlights: • Novel biological derived HA coatings fabricated by pulsed laser deposition. • Renewable resources • Reinforcement with MgF{sub 2} and MgO improves the HA coatings' bonding strength. • Significant anti-biofilm effect obtained for MgO reinforced HA films. • Alternative low cost solutions for a new generation of dental implants.

Atomic layer deposition-A novel method for the ultrathin coating of minitablets.

Science.gov (United States)

Hautala, Jaana; Kääriäinen, Tommi; Hoppu, Pekka; Kemell, Marianna; Heinämäki, Jyrki; Cameron, David; George, Steven; Juppo, Anne Mari

2017-10-05

We introduce atomic layer deposition (ALD) as a novel method for the ultrathin coating (nanolayering) of minitablets. The effects of ALD coating on the tablet characteristics and taste masking were investigated and compared with the established coating method. Minitablets containing bitter tasting denatonium benzoate were coated by ALD using three different TiO 2 nanolayer thicknesses (number of deposition cycles). The established coating of minitablets was performed in a laboratory-scale fluidized-bed apparatus using four concentration levels of aqueous Eudragit ® E coating polymer. The coated minitablets were studied with respect to the surface morphology, taste masking capacity, in vitro disintegration and dissolution, mechanical properties, and uniformity of content. The ALD thin coating resulted in minimal increase in the dimensions and weight of minitablets in comparison to original tablet cores. Surprisingly, ALD coating with TiO 2 nanolayers decreased the mechanical strength, and accelerated the in vitro disintegration of minitablets. Unlike previous studies, the studied levels of TiO 2 nanolayers on tablets were also inadequate for effective taste masking. In summary, ALD permits a simple and rapid method for the ultrathin coating (nanolayering) of minitablets, and provides nanoscale-range TiO 2 coatings on porous minitablets. More research, however, is needed to clarify its potential in tablet taste masking applications. Copyright © 2017 Elsevier B.V. All rights reserved.

Challenges in detecting magnesium stearate distribution in tablets.

Science.gov (United States)

Lakio, Satu; Vajna, Balázs; Farkas, István; Salokangas, Henri; Marosi, György; Yliruusi, Jouko

2013-03-01

Magnesium stearate (MS) is the most commonly used lubricant in pharmaceutical industry. During blending, MS particles form a thin layer on the surfaces of the excipient and drug particles prohibiting the bonding from forming between the particles. This hydrophobic layer decreases the tensile strength of tablets and prevents water from penetrating into the tablet restraining the disintegration and dissolution of the tablets. Although overlubrication of the powder mass during MS blending is a well-known problem, the lubricant distribution in tablets has traditionally been challenging to measure. There is currently no adequate analytical method to investigate this phenomenon. In this study, the distribution of MS in microcrystalline cellulose (MCC) tablets was investigated using three different blending scales. The crushing strength of the tablets was used as a secondary response, as its decrease is known to result from the overlubrication. In addition, coating of the MCC particles by MS in intact tablets was detected using Raman microscopic mapping. MS blending was more efficient in larger scales. Raman imaging was successfully applied to characterize MS distribution in MCC tablets despite low concentration of MS. The Raman method can provide highly valuable visual information about the proceeding of the MS blending process. However, the measuring set-up has to be carefully planned to establish reliable and reproducible results.

A fixed-dose combination tablet of gemigliptin and metformin sustained release has comparable pharmacodynamic, pharmacokinetic, and tolerability profiles to separate tablets in healthy subjects.

Science.gov (United States)

Park, Sang-In; Lee, Howard; Oh, Jaeseong; Lim, Kyoung Soo; Jang, In-Jin; Kim, Jeong-Ae; Jung, Jong Hyuk; Yu, Kyung-Sang

2015-01-01

In type 2 diabetes mellitus, fixed-dose combination (FDC) can provide the complementary benefits of correction of multiple pathophysiologic defects such as dysfunctions in glycemic or metabolic control while improving compliance compared with separate tablets taken together. The objective of the study reported here was to compare the pharmacodynamic (PD), pharmacokinetic (PK), and tolerability profiles of gemigliptin and extended-release metformin (metformin XR) between FDC and separate tablets. A randomized, open-label, single-dose, two-way, two-period, crossover study was conducted in 28 healthy male volunteers. Two FDC tablets of gemigliptin/metformin 25/500 mg or separate tablets of gemigliptin (50 mg ×1) and metformin XR (500 mg ×2) were orally administered in each period. Serial blood samples were collected up to 48 hours post-dose to determine dipeptidyl peptidase 4 (DPP-4) activity using spectrophotometric assay and concentrations of gemigliptin and metformin using tandem mass spectrometry. Geometric mean ratios (GMRs) of FDC to separate tablet formulations and their 90% confidence intervals (CIs) were calculated to compare the PD and PK parameters between the two formulations. Tolerability was assessed throughout the study. The plasma DPP-4 activity-time curves of the FDC and the separate tablets almost overlapped, leading to a GMR (90% CI) of the FDC to separate tablets for the plasma DPP-4 activity and its maximum inhibition of 1.00 (0.97-1.04) and 0.92 (0.82-1.05), respectively. Likewise, all of the GMRs (90% CIs) of FDC to separate tablets for the area under the plasma concentration-time curve and maximum plasma concentration of gemigliptin and metformin fell entirely within the conventional bioequivalence range of 0.80-1.25. Both the FDC and separate tablets were well tolerated. The PD, PK, and tolerability profiles of gemigliptin and metformin XR in FDC and separate tablets were found to be comparable. The FDC tablet of gemigliptin and metformin

Post-heat treatment of arc-sprayed coating prepared by the wires combination of Mg-cathode and Al-anode to form protective intermetallic layers

International Nuclear Information System (INIS)

Xu Rongzheng; Song Gang

2011-01-01

A Mg-Al intermetallic compounds coating was prepared on the surface of Mg-steel lap joint by arc-sprayed Al-Mg composite coating (Mg-cathode and Al-anode) and its post-heat treatment (PHT). The effect of PHT temperature on the phase transition, microstructure and mechanical properties of the coating was investigated by X-ray diffraction, scanning electron microscope, energy dispersive X-ray spectroscopy, optical microscope and microhardness test. The result shows that the intermetallic compounds layer that is mainly composed of Al 3 Mg 2 and Mg 17 Al 12 is formed by the self-diffusion reaction of Mg and Al splats in the coating after PHT for 4 h at 430 deg. C.

Development of midazolam sublingual tablets: in vitro study.

Science.gov (United States)

Odou, P; Barthelemy, C; Robert, H

1998-01-01

Midazolam is a benzodiazepine with short elimination half-life, used as induction or continuous agent for general anesthesia. At present, only injectable solution is available from French hospital pharmacies. The aim of the study is the development of 5 mg midazolam sublingual tablets to realize a short general anesthesia without intravenous or intramuscular injection. Incorporation of citric acid in the tablet formulation leads to an increase of dissolution rates of active drug, but a decrease of diffusion through lipid membranes is observed with 10 mg of citric acid when using the Dibbern's Resomat three phases apparatus. One explanation of this result is that midazolam (pKa = 6.1) in presence of 10 mg of citric acid is ionised. The ionised form, more hydrophilic, cannot cross the artificial lipid membrane and therefore the diffusion decreases. On the other hand, the decrease of diffusion's rate, when pH increases, is explained by the precipitation of midazolam at pH higher than 6. A compromise between dissolution and diffusion results leads us to choose the sublingual formulation containing 5 mg of citric acid per tablet.

Identification and Structural Characterization of Unidentified Impurity in Bisoprolol Film-Coated Tablets

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Ivana Mitrevska

2017-01-01

Full Text Available The aim of this study is the identification, structural characterization, and qualification of a degradation impurity of bisoprolol labeled as Impurity RRT 0.95. This degradation product is considered as a principal thermal degradation impurity identified in bisoprolol film-coated tablets. The impurity has been observed in the stress thermal degradation study of the drug product. Using HPLC/DAD/ESI-MS method, a tentative structure was assigned and afterwards confirmed by detailed structural characterization using NMR spectroscopy. The structure of the target Impurity RRT 0.95 was elucidated as phosphomonoester of bisoprolol, having relative molecular mass of 406 (positive ionization mode. The structural characterization was followed by qualification of Impurity RRT 0.95 using several different in silico methodologies. From the results obtained, it can be concluded that no new structural alerts have been generated for Impurity RRT 0.95 relative to the parent compound bisoprolol. The current study presents an in-depth analysis of the full characterization and qualification of an unidentified impurity in a drug product with the purpose of properly defining the quality specification of the product.

Gastric transit and pharmacodynamics of a two-millimeter enteric-coated pancreatin microsphere preparation in patients with chronic pancreatitis

NARCIS (Netherlands)

Bruno, M. J.; Borm, J. J.; Hoek, F. J.; Delzenne, B.; Hofmann, A. F.; de Goeij, J. J.; van Royen, E. A.; van Leeuwen, D. J.; Tytgat, G. N.

1998-01-01

It has been suggested that enteric-coated pancreatin microsphere (ECPM) preparations with sphere sizes larger than 1.7 mm pass through the stomach at a slower rate than a meal and therefore may be less efficacious in restoring pancreatic enzyme activity than preparations with smaller sphere sizes.

Influence of substrate temperature on properties of MgF2 coatings

International Nuclear Information System (INIS)

Yu Hua; Qi Hongji; Cui Yun; Shen Yanming; Shao Jianda; Fan Zhengxiu

2007-01-01

Thermal boat evaporation was employed to prepare MgF 2 single-layer coatings upon both JGS1 and UBK7 substrates at different substrate temperatures. Microstructure, transmittance and residual stress of these coatings were measured by X-ray diffraction, spectrophotometer, and optical interferometer, respectively. Measurement of laser induced damage threshold (LIDT) of the samples was performed at 355 nm, 8 ns pulses. The results showed that high substrate temperature was beneficial to crystallization of the film. Above 244 deg. C, the refractive index increased gradually with the substrate temperature rising. Whereas, it was exceptional at 210 deg. C that the refractive index was higher than those deposited at 244 and 277 deg. C. The tensile residual stresses were exhibited in all MgF 2 films, but not well correlated with the substrate temperature. In addition, the stresses were comparatively smaller upon JGS1 substrates. A tendency could be seen that the LIDTs reached the highest values at about 244 deg. C, and the films upon JGS1 had higher LIDTs than those upon UBK7 substrates at the same temperature. Meanwhile, the damage morphologies showed that the laser damage of the coating resulted from an absorbing center at the film-substrate interface. The features of the damages were displayed by an absorbing center dominated model. Furthermore, the reason of the difference in LIDT values was discussed in detail

Quality Enhancement by Inclusion Complex Formation of Simvastatin Tablets

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Emőke Rédai

2013-08-01

Full Text Available Introduction: Simvastatin is an inhibitor of hydroxy-methyl-glutaryl-coenzyme A reductase, used in the treatment of hypercholesterolemia. To enhance its bioavailability by inclusion complexation, as host molecule randommethyl-β-cyclodextrin had been used. After evaluating the complexes we chose the kneading product in 1:2 molar ratio for incorporation of 10 mg simvastatin tablets. Materials and methods: We prepared homogenous mixtures of the inclusion complex and some excipients. The tablets were prepared by direct compression. The tablets were evaluated in regard to: weight uniformity, thickness, diameter, hardness, friability, disintegration and dissolution profile. Results: Weights are in the range of 196-208 mg, diameter 6.83-6.86 mm, height 3.86-4.01 mm, hardness 78.3-113.1 N, friability 0.75- 1.19 %, disintegration above 15 minutes. The dissolved amounts of simvastatin from the tablets are higher compared to the dissolution of pure simvastatin, but lower than the dissolution of the complex itself. Excipients, like disintegrants and lubricants greatly influence the dissolution properties of the tablets. Conclusions: According to our results, tablets containing inclusion complex of simvastatin exhibit better solubility, according to the dissolved amount of simvastatin, than pure drug alone. Proper physical parameters of the tablets are obtained by application of 5 % Primellose

Zr-based conversion layer on Zn-Al-Mg alloy coated steel sheets: insights into the formation mechanism

International Nuclear Information System (INIS)

Lostak, Thomas; Maljusch, Artjom; Klink, Björn; Krebs, Stefan; Kimpel, Matthias; Flock, Jörg; Schulz, Stephan; Schuhmann, Wolfgang

2014-01-01

Zr-based conversion layers are considered as environmentally friendly alternatives replacing trication phosphatation in the automotive industry. Based on excellent electronic barrier properties they provide an effective corrosion protection of the metallic substrate. In this work, thin protective layers were grown on novel Zn-Al-Mg alloy coated steel sheets by increasing the local pH-value at the sample surface leading to deposition of a Zr-based conversion layer. For this purpose Zn-Al-Mg alloy (ZM) coated steel sheets were treated in an aqueous model conversion solution containing well-defined amounts of hexafluorozirconic acid (H 2 ZrF 6 ) and characterized after different immersion times with SKPFM and field emission SEM (FE-SEM)/EDX techniques. A deposition mechanism of Zr-based conversion coatings on microstructural heterogeneous Zn-Al-Mg alloy surfaces was proposed

78 FR 69856 - Determination That BANZEL (Rufinamide) Tablet, 100 Milligrams, Was Not Withdrawn From Sale for...

Science.gov (United States)

2013-11-21

...] Determination That BANZEL (Rufinamide) Tablet, 100 Milligrams, Was Not Withdrawn From Sale for Reasons of Safety... Drug Administration (FDA) has determined that BANZEL (rufinamide) tablet, 100 milligrams (mg), was not... abbreviated new drug applications (ANDAs) for rufinamide tablet, 100 mg, if all other legal and regulatory...

Enteric-coated, pH-dependent peppermint oil capsules for the treatment of irritable bowel syndrome in children.

Science.gov (United States)

Kline, R M; Kline, J J; Di Palma J; Barbero, G J

2001-01-01

In a randomized, double-blind controlled trial, 42 children with irritable bowel syndrome (IBS) were given pH-dependent, enteric-coated peppermint oil capsules or placebo. After 2 weeks, 75% of those receiving peppermint oil had reduced severity of pain associated with IBS. Peppermint oil may be used as a therapeutic agent during the symptomatic phase of IBS.

Glucose-coated gold nanoparticles transfer across human brain endothelium and enter astrocytes in vitro.

Directory of Open Access Journals (Sweden)

Radka Gromnicova

Full Text Available The blood-brain barrier prevents the entry of many therapeutic agents into the brain. Various nanocarriers have been developed to help agents to cross this barrier, but they all have limitations, with regard to tissue-selectivity and their ability to cross the endothelium. This study investigated the potential for 4 nm coated gold nanoparticles to act as selective carriers across human brain endothelium and subsequently to enter astrocytes. The transfer rate of glucose-coated gold nanoparticles across primary human brain endothelium was at least three times faster than across non-brain endothelia. Movement of these nanoparticles occurred across the apical and basal plasma membranes via the cytosol with relatively little vesicular or paracellular migration; antibiotics that interfere with vesicular transport did not block migration. The transfer rate was also dependent on the surface coating of the nanoparticle and incubation temperature. Using a novel 3-dimensional co-culture system, which includes primary human astrocytes and a brain endothelial cell line hCMEC/D3, we demonstrated that the glucose-coated nanoparticles traverse the endothelium, move through the extracellular matrix and localize in astrocytes. The movement of the nanoparticles through the matrix was >10 µm/hour and they appeared in the nuclei of the astrocytes in considerable numbers. These nanoparticles have the correct properties for efficient and selective carriers of therapeutic agents across the blood-brain barrier.

Enabling the Tablet Product Development of 5-Fluorocytosine by Conjugate Acid Base Cocrystals.

Science.gov (United States)

Perumalla, Sathyanarayana R; Paul, Shubhajit; Sun, Changquan C

2016-06-01

5-Fluorocytosine (FC) is a high-dose antifungal drug that challenges the development of a tablet product due to poor solid-state stability and tabletability. Using 2 pharmaceutically acceptable conjugate acid base (CAB) cocrystals of FC with HCl and acesulfame, we have developed commercially viable high loading FC tablets. The tablets were prepared by direct compression using nano-coated microcrystalline cellulose Avicel PH105 as a tablet binder, which provided both excellent tabletability and good flowability. Commercial manufacturability of formulations based on both CAB cocrystals was verified on a compaction simulator. The results from an expedited friability study were used to set the compaction force, which yielded tablets with sufficient mechanical strength and rapid tablet disintegration. This work demonstrates the potential value of CAB cocrystals in drug product development. Copyright © 2016 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.

Composite Cu/Fe/MgB{sub 2} superconducting wires and MgB{sub 2}/YSZ/Hastelloy coated conductors for ac and dc applications

Energy Technology Data Exchange (ETDEWEB)

Glowacki, B A [Department of Materials Science and Metallurgy, University of Cambridge, Pembroke Street, Cambridge (United Kingdom); Majoros, M [Interdisciplinary Research Centre in Superconductivity, University of Cambridge, Madingley Road, Cambridge (United Kingdom); Vickers, M [Department of Materials Science and Metallurgy, University of Cambridge, Pembroke Street, Cambridge (United Kingdom); Eisterer, M [Atomic Institute of the Austrian Universities, A-1020 Vienna (Austria); Toenies, S [Atomic Institute of the Austrian Universities, A-1020 Vienna (Austria); Weber, H W [Atomic Institute of the Austrian Universities, A-1020 Vienna (Austria); Fukutomi, M [National Institute for Materials Science, Superconducting Materials Center, 1-2-1, Sengen, Ibaraki (Japan); Komori, K [National Institute for Materials Science, Superconducting Materials Center, 1-2-1, Sengen, Ibaraki (Japan); Togano, K [National Institute for Materials Science, Superconducting Materials Center, 1-2-1, Sengen, Ibaraki (Japan)

2003-02-01

We discuss the results of a study of MgB{sub 2} multifilamentary conductors and coated conductors from the point of view of their future dc and ac applications. The correlation between the slope of the irreversibility line induced by neutron irradiation defects and in situ structural imperfections and the critical temperature and critical current density is discussed with respect to the conductor performance and applicability. We debate the possible origin of the observed anomalous decrease of ac susceptibility at 50 K in copper clad in situ powder-in-tube MgB{sub 2} wires. Different conductor preparation methods and conductor architectures, and attainable critical current densities are presented. Some numerical results on critical currents, thermal stability and ac losses of future MgB{sub 2} multifilamentary and coated conductors with magnetic cladding of their filaments are also discussed.

Highly stable carbon coated Mg2Si intermetallic nanoparticles for lithium-ion battery anode

Science.gov (United States)

Tamirat, Andebet Gedamu; Hou, Mengyan; Liu, Yao; Bin, Duan; Sun, Yunhe; Fan, Long; Wang, Yonggang; Xia, Yongyao

2018-04-01

Silicon is an ideal candidate anode material for Li-ion batteries (LIBs). However, it suffers from rapid capacity fading due to large volume expansion upon lithium insertion. Herein, we design and fabricate highly stable carbon coated porous Mg2Si intermetallic anode material using facile mechano-thermal technique followed by carbon coating using thermal vapour deposition (TVD), toluene as carbon source. The electrode exhibits an excellent first reversible capacity of 726 mAh g-1 at a rate of 100 mA g-1. More importantly, the electrode demonstrates high rate capability (380 mAh g-1 at high rate of 2 A g-1) as well as high cycle stability, with capacity retentions of 65% over 500 cycles. These improvements are attributable to both Mg supporting medium and the uniform carbon coating, which can effectively increase the conductivity and electronic contact of the active material and protects large volume alterations during the electrochemical cycling process.

Development of tablets containing semipurified extract of guaraná (Paullinia cupana

Directory of Open Access Journals (Sweden)

Traudi Klein

2012-12-01

Full Text Available This study evaluated the technological feasibility of producing a semipurified extract of guaraná (Paullinia cupana Kunth, Sapindaceae in tablet form, using a direct-compression process. Maltodextrin and gum arabic were used to produce the extract microparticles, in order to protect the microparticles against such factors as temperature, oxidation, and humidity. Using pharmacopoeial methodologies, technological and physicochemistry tests (determination of residual moisture, of bulk and tapped density, Hausner ratio, compressibility and compactibility index, appearance, mean weight, hardness, friability, disintegration time, determination of EPA amount in tablets and in vitro release profile were conducted. The formulation containing 200 mg of microparticles, 170 mg microcrystalline cellulose, and 10 mg lactose gave the best results in terms of hardness (116 N, friabilility (0.28%, mean weight (0.3821 g, and disintegration time (25 min for a tablet designed for oral administration. The results met pharmacopoeial specifications, and the tablets are suitable for oral administration.

Diseño y evaluación de la formulación de tabletas de pimozida 1 y 4 mg

Directory of Open Access Journals (Sweden)

Beatriz Tamargo Santos

1998-04-01

Full Text Available Se estudiaron diferentes formulaciones de tabletas de pimozida en dosis de 1 y 4 mg, diseñadas con el objetivo de obtener una formulación que cumpla con los parámetros establecidos en la Farmacopea de los Estados Unidos XXII para el control de la calidad del producto terminado, así como los requerimientos necesarios para su revestimiento. Entre las formulaciones establecidas la denominada PP cumplió con los parámetros de calidad establecidos, antes y posterior al revestimiento. Los resultados obtenidos en el estudio de vida en estante de las tabletas revestidas fabricadas a escala semiindustrial demostraron que hasta 1 año posterior a la fabricación, éstas cumplen con las especificaciones establecidas en la Farmacopea, lo cual soporta la factibilidad para su escalado al nivel industrial.Different formulations of Pimozide 1 and 4 mg tablets designed to obtain a formulation that meets the parameters established by the United States Pharmacopeia XXII for controlling the quality of the finished product, as well as the necessary requirement for its coating, were studied. Among these formulations, the so-called PP fulfilled the established quality parameters before and after coating. The results obtained in the shelf life study of the coated tablets made at semiindustrial scale showen that even one year after their making they meet the specifications established by the Pharmacopeia, which supports the feasibility for their scale-up at industrial level.

In vitro study of polycaprolactone/bioactive glass composite coatings on corrosion and bioactivity of pure Mg

Energy Technology Data Exchange (ETDEWEB)

Yang, Yuyun; Michalczyk, Carolin [Institute of Biomaterials, University of Erlangen-Nuremberg, 91058 Erlangen (Germany); Singer, Ferdinand [Institute of Surface Science and Corrosion, University of Erlangen-Nuremberg, 91058 Erlangen (Germany); Virtanen, Sannakaisa, E-mail: virtanen@ww.uni-erlangen.de [Institute of Surface Science and Corrosion, University of Erlangen-Nuremberg, 91058 Erlangen (Germany); Boccaccini, Aldo R., E-mail: aldo.boccaccini@ww.uni-erlangen.de [Institute of Biomaterials, University of Erlangen-Nuremberg, 91058 Erlangen (Germany)

2015-11-15

Highlights: • Bioactive glass nanoparticles (nBG) enhance bioactivity of PCL coatings on Mg. • Barrier properties of PCL can be altered by nBG addition. • Degradation of PCL increased by addition of nBG. - Abstract: The influence of the addition of nano-scaled bioactive glass (nBG) powder into polycaprolactone (PCL) coatings on the biodegradation and bioactivity of pure Mg was investigated in the present work. Scanning electron microscopy (SEM), energy-dispersive X-ray spectrometry (EDS), Fourier transform infrared spectroscopy (FTIR) and electrochemical methods were employed to characterize the morphology, chemical composition and anticorrosion properties of the coatings. The results indicate that nBG addition in PCL increases the degradation of PCL in physiological solution; depending on the amount of nBG in the composite coating, the barrier properties of PCL therefore can be modified. At the same time, the addition of nBG facilitates the formation of hydroxyapatite during 7 days immersion in simulated body fluid (SBF).

Preparation and Evaluation of Enteric-Coated Chitosan Derivative-Based Microparticles Loaded with Salmon Calcitonin as an Oral Delivery System

Directory of Open Access Journals (Sweden)

Hiraku Onishi

2016-09-01

Full Text Available Background: The production of protein drugs has recently increased due to advances in biotechnology, but their clinical use is generally limited to parenteral administration due to low absorption in non-parenteral administration. Therefore, non-parenteral delivery systems allowing sufficient absorption draw much attention. Methods: Microparticles (MP were prepared using chitosan-4-thio-butylamidine conjugate (Ch-TBA, trimethyl-chitosan (TMC, and chitosan (Ch. Using salmon calcitonin (sCT as a model protein drug, Ch-TBA-, Ch-TBA/TMC (4/1-, and Ch-based MP were produced, and their Eudragit L100 (Eud-coated MP, named Ch-TBA-MP/Eud, Ch-TBA/TMC-MP/Eud, and Ch-MP/Eud, respectively, were prepared as oral delivery systems. These enteric-coated microparticles were examined in vitro and in vivo. Results: All microparticles before and after enteric coating had a submicron size (600–800 nm and micrometer size (1300–1500 nm, respectively. In vitro release patterns were similar among all microparticles; release occurred gradually, and the release rate was slower at pH 1.2 than at pH 6.8. In oral ingestion, Ch-TBA-MP/Eud suppressed plasma Ca levels most effectively among the microparticles tested. The relative effectiveness of Ch-TBA-MP/Eud to the intramuscular injection was 8.6%, while the sCT solution showed no effectiveness. Conclusion: The results suggest that Eud-coated Ch-TBA-based microparticles should have potential as an oral delivery system of protein drugs.

Magnesium Diboride thin Films, multilayers, and coatings for SRF cavities

Energy Technology Data Exchange (ETDEWEB)

Xi, Xiaoxing [Temple Univ., Philadelphia, PA (United States)

2017-08-17

Superconducting radio frequency (SRF) cavities currently use low-temperature superconductor niobium, and the Nb SRF cavities have approached the performance levels predicted theoretically. Compared to Nb, MgB₂ becomes superconducting at a much higher temperature and promises a better RF performance in terms of higher quality factor Q and higher acceleration capability. An MgB₂ SRF technology can significantly reduce the operating costs of particle accelerators when these potentials are realized. This project aimed to advance the development of an MgB₂ SRF technology. It had two main objectives: (1) materials issues of MgB₂ thin films and multilayers related to their applications in SRF cavities; and (2) coating single-cell cavities for testing at RF frequencies. The key technical thrust of the project is the deposition of high quality clean MgB₂ films and coatings by the hybrid physical-chemical vapor deposition (HPCVD) technique, which was developed in my group. We have achieved technical progress in each of the two areas. For the first objective, we have confirmed that MgB₂ thin film coatings can be used to effectively enhance the vortex penetration field of an SRF cavity. A vortex is a normal region in the shape of spaghetti that threads through a superconductor. Its existence is due to an applied magnetic field that is greater than a so-called lower critical field, H_c1. Once a vortex enters the superconductor, its movement leads to loss. This has been shown to be the reason for an SRF cavity to break down. Thus, enhancing the magnetic field for a vortex to enter the superconductor that forms the SRF cavity has be a goal of intense research. To this end, Gurevich proposed that a coating of thin superconductor layer can impede the vortex entrance. In this project, we have done two important experiment to test this concept. One, we showed that the enhancement of H_c1 can be

A bioequivalence study of two tamsulosin sustained-release tablets in Indonesian healthy volunteers.

Science.gov (United States)

Prasaja, Budi; Harahap, Yahdiana; Lusthom, Windy; Setiawan, Evy C; Ginting, Mena B; Hardiyanti; Lipin

2011-06-01

The bioavailability of two 0.4 mg tamsulosin sustained-release film-coated tablet formulations was compared; using generic tablets (Prostam(®)) as test formulation and the originator product as reference formulation. Twenty-four subjects were included in this single-dose, open-label, randomized two-way crossover design following an overnight fasting. A one-week wash-out period was applied. Blood samples were drawn up to 72 h following drug administration. Plasma concentration of tamsulosin was determined by liquid chromatography-tandem mass spectrometry method with TurboIonSpray mode. Pharmacokinetic parameters AUC(0-t,) AUC(0-∞), C (max) and t (½) were determined and used for bioequivalence evaluation after log-transformation, whereas t (max) ratios were evaluated non-parametrically. The estimated point and 90% confidence intervals (CI) for AUC(0-t,) AUC(0-∞), C (max) and t (½) were 109.55% (96.41-124.49%), 109.94% (96.85-124.81%), 105.87% (92.88-120.67%) and 100.00% (90.56-110.43%), respectively. These results indicated that the two formulations of tamsulosin were bioequivalent; therefore they may be prescribed interchangeably.

Poly(dimethylsiloxane) coatings for controlled drug release--polymer modifications.

Science.gov (United States)

Schulze Nahrup, J; Gao, Z M; Mark, J E; Sakr, A

2004-02-11

Modifications of endhydroxylated poly(dimethylsiloxane) (PDMS) formulations were studied for their ability to be applied onto tablet cores in a spray-coating process and to control drug release in zero-order fashion. Modifications of the crosslinker from the most commonly used tetraethylorthosilicate (TEOS) to the trifunctional 3-(2,3-epoxypropoxy)propyltrimethoxysilane (SIG) and a 1:1 mixture of the two were undertaken. Addition of methylpolysiloxane-copolymers were studied. Lactose, microcrystalline cellulose (MCC) and polyethylene glycol 8000 (PEG) were the channeling agents applied. The effects on dispersion properties were characterized by particle size distribution and viscosity. Mechanical properties of resulting free films were studied to determine applicability in a pan-coating process. Release of hydrochlorothiazide (marker drug) was studied from tablets coated in a lab-size conventional coating pan. All dispersions were found suitable for a spray-coating process. Preparation of free films showed that copolymer addition was not possible due to great decline in mechanical properties. Tablets coated with formulations containing PEG were most suitable to control drug release, at only 5% coating weight. Constant release rates could be achieved for formulations with up to 25% PEG; higher amounts resulted in a non-linear release pattern. Upon adding 50% PEG, a drug release of 63% over 24 h could be achieved.

Effect of Coating Solvent Ratio on the Drug Release Lag Time of ...

African Journals Online (AJOL)

Purpose: The aim of the study was to investigate the effect of hydro-alcohol coating solvent ratio on the surface texture and lag time of porous theophylline osmotic tablet. Methods: Porous theophylline osmotic pump tablets were formulated by direct compression and coated by spraying with varying ratios of water-alcohol ...

Electrochemical corrosion behaviour of Mg-Al alloys with thermal spray Al/SiCp composite coatings

International Nuclear Information System (INIS)

Pardo, A.; Feliu Jr, S.; Merino, M. C.; Mohedano, M.; Casajus, P.; Arrabal, R.

2010-01-01

The corrosion protection of Mg-Al alloys by flame thermal spraying of Al/SiCp composite coatings was evaluated by electrochemical impedance spectroscopy in 3.5 wt.% NaCl solution. The volume fraction of SiC particles (SiCp) varied between 5 and 30%. The as-sprayed Al/SiCp composite coatings revealed a high number of micro-channels, largely in the vicinity of the SiC particles, that facilitated the penetration of the electrolyte and the subsequent galvanic corrosion of the magnesium substrates. The application of a cold-pressing post-treatment reduced the degree of porosity of the coatings and improved the bonding at the coating/substrate and Al/SiC interfaces. This resulted in improved corrosion resistance of the coated specimens. The effectiveness of the coatings slightly decreased with the addition of 5-30 vol.% SiCp compared with the un reinforced thermal spray aluminium coatings. (Author) 31 refs.

The critical role of NIR spectroscopy and statistical process control (SPC) strategy towards captopril tablets (25 mg) manufacturing process understanding: a case study.

Science.gov (United States)

Curtivo, Cátia Panizzon Dal; Funghi, Nathália Bitencourt; Tavares, Guilherme Diniz; Barbosa, Sávio Fujita; Löbenberg, Raimar; Bou-Chacra, Nádia Araci

2015-05-01

In this work, near-infrared spectroscopy (NIRS) method was used to evaluate the uniformity of dosage units of three captopril 25 mg tablets commercial batches. The performance of the calibration method was assessed by determination of Q value (0.9986), standard error of estimation (C-set SEE = 1.956), standard error of prediction (V-set SEP = 2.076) as well as the consistency (106.1%). These results indicated the adequacy of the selected model. The method validation revealed the agreement of the reference high pressure liquid chromatography (HPLC) and NIRS methods. The process evaluation using the NIRS method showed that the variability was due to common causes and delivered predictable results consistently. Cp and Cpk values were, respectively, 2.05 and 1.80. These results revealed a non-centered process in relation to the average target (100% w/w), in the specified range (85-115%). The probability of failure was 21:100 million tablets of captopril. The NIRS in combination with the method of multivariate calibration, partial least squares (PLS) regression, allowed the development of methodology for the uniformity of dosage units evaluation of captopril tablets 25 mg. The statistical process control strategy associated with NIRS method as PAT played a critical role in understanding of the sources and degree of variation and its impact on the process. This approach led towards a better process understanding and provided the sound scientific basis for its continuous improvement.

Superior critical current density obtained in MgB_2 bulks via employing carbon-coated boron and minor Cu addition

International Nuclear Information System (INIS)

Peng, Junming; Liu, Yongchang; Ma, Zongqing; Shahriar Al Hossain, M.; Xin, Ying; Jin, Jianxun

2016-01-01

Highlights: • Usage of carbon-coated boron leads to high level of homogeneous carbon doping. • Cu addition improves MgB_2 grain connectivity, leading to higher J_c at low fields. • Cu addition reduces MgO impurity, also contributing to the improvement of J_c. - Abstract: High performance Cu doped MgB_2 bulks were prepared by an in-situ method with carbon-coated amorphous boron as precursor. It was found that the usage of carbon-coated boron in present work leads to the formation of uniformly refined MgB_2 grains, as well as a high level of homogeneous carbon doping in the MgB_2 samples, which significantly enhance the J_c in both Cu doped and undoped bulks compared to MgB_2 bulks with normal amorphous boron precursor. Moreover, minor Cu can service as activator, and thus facilitates the growth of MgB_2 grains and improves crystallinity and grain connectivity, which can bring about the excellent critical current density (J_c) at self fields and low fields (the best values are 7 × 10"5 A/cm"2 at self fields, and 1 × 10"5 A/cm"2 at 2 T, 20 K, respectively). Simultaneously, minor Cu addition can reduce the amount of MgO impurity significantly, also contributing to the improvement of J_c at low fields. Our work suggests that Cu-activated sintering combined with employment of carbon-coated amorphous boron as precursor could be a promising technique to produce practical MgB_2 bulks or wires with excellent J_c on an industrial scale.

Clinical study on influences of enteric coated aspirin on blood pressure and blood pressure variability.

Science.gov (United States)

Ji, A-L; Chen, W-W; Huang, W-J

2016-12-01

We investigated the effects of oral administration of enteric coated aspirin (ASA) on blood pressure and blood pressure variability of hypertension patients before sleep. We observed 150 hypertension cases, classified as Grade 1-2, from September 2006 to March 2008. They are divided into a control group with 30 cases, ASA I group with 60 cases and ASA II group with 60 cases randomly. Subjects in the control group had proper diets, were losing weight, exercising and maintaining a healthy mentality and were taking 30 mg Adalat orally once a day. Based on the treatment of control group, patients in ASA I group were administered 0.1 g Bayaspirin (produced by Bayer Company) at drought in the morning. Also, based on the treatment of control group, patients in ASA II group were administered 0.1 g Bayaspirin at draught before sleep. The course of treatment is 3 months and then after the treatment, decreasing blood pressure and blood pressure variability conditions in three groups will be compared. Through the comparison of ASA II group with the control group, they have differences in terms of systolic blood pressure (SBP), diastolic blood pressure (DBP), decreasing range of blood pressure and blood pressure variability (p sleep has synergistic effects on decreasing blood pressure of hypertension patients and improving blood pressure variability.

Studies on the mechanism of printing film-coated tablets containing titanium dioxide in the film by using UV laser irradiation.

Science.gov (United States)

Kato, Yoshiteru; Nakashima, Yasuhiko; Shino, Naoki; Sasaki, Koichi; Hosokawa, Akihiro; Ishihara, Hiroshi

2010-04-01

The purpose of this article is to study a detailed mechanism of printing when film-coated tablets were irradiated by UV laser at a wavelength of 355 nm. Hydroxypropylmethylcellulose (HPMC) film containing titanium dioxide (TiO(2)) and the film not containing TiO(2) and TiO(2) powder were lirradiated by the UV laser and estimated by the morphological observation by zoom stereo microscope, thermogravimetric analysis (TGA), total color difference (dE), X-ray powder diffraction (XRD), and dispersive Raman microscopy. In the case of the film containing TiO(2), the film showed a visible change in its color from white to gray by the UV laser irradiation. By zoom stereo microscope, it was found that the entire UV laser-irradiated area was not grayed uniformly, but many black particles, whose diameter was about 2 microm, were observed on the film. When TiO(2) powder was irradiated by the UV laser, a visible change in its color from white to gray was observed similar to the case of the film containing TiO(2). There were many black particles locally in the UV laser-treated TiO(2) powder by the morphological observation, and these black particles, agglomerates of the grayed oxygen-defected TiO(2), were associated with the visible change of the TiO(2). It was found that the film-coated tablets were printed utilizing the formation of the black particles by the agglomeration of the grayed oxygen-defected TiO(2) by the UV laser irradiation.

Development of the technology of tablets on the basis of ademetionine 1,4-butanedisulfonate

Directory of Open Access Journals (Sweden)

K. S. Burdak

2017-04-01

(resistance to crushing, abrasion, dissolution and disintegration research methods, it was proved that this technology allows to obtain tablets that are fully compliant with specifications for the tablets covered with an enteric coating.

Investigation of washing and storage strategy on aging Of Mg-aminoclay (MgAC) coated nanoscale zero-valent iron (nZVI) particles

DEFF Research Database (Denmark)

Hwang, Yuhoon; Lee, Young-Chul; Mines, Paul D.

2014-01-01

The tendency towards agglomeration and oxidation of nanoscale zero-valent iron (nZVI) particles limits its application for in situ groundwater and soil remediation. Although the effect of surface coatings on nanoparticle stabilization has been commonly practiced, the effect of preparation...... correlations (r2 > 0.95, p one another. Pre-storage washing, followed by addition of MgAC, exhibits high stability as pre-storage washing, as well as high reactivity as post-storage washing. Here, it is found that the proper washing procedure is crucial in coated nZVI preparation...

Dose Uniformity of Scored and Unscored Tablets: Application of the FDA Tablet Scoring Guidance for Industry.

Science.gov (United States)

Ciavarella, Anthony B; Khan, Mansoor A; Gupta, Abhay; Faustino, Patrick J

world. Tablets are often split to modify dose strength, make swallowing easier, and reduce cost to the consumer. To better address product quality for this widely used practice, the U.S. Food and Drug Administration (FDA) published a Guidance for Industry that addresses tablet splitting. The guidance provides testing criteria for scored tablets, which is a part of the FDA review process for drugs. The model drugs selected for this study were amlodipine and gabapentin, which have different sizes, shapes, and tablet scores. Whole and split amlodipine tablets were tested for drug content because of a concern that the low-dose strength may cause greater variability. Whole and split gabapentin tablets were tested for weight variation because of their higher dosage strength of 600 mg. All whole tablets met the acceptance criteria for the Uniformity of Dosage Units based on the guidance recommendations. When unscored amlodipine tablets were split by a splitter, all formulations did not meet the acceptance criteria. When fully scored gabapentin tablets were split by hand and by splitter, they met the acceptance criteria. The findings of this FDA study indicated physical characteristics such as size, shape, and tablet score can affect the uniformity of split tablets. © PDA, Inc. 2016.

Anti-scratch AlMgB14 Gorilla® Glass coating

Science.gov (United States)

Putrolaynen, V. V.; Grishin, A. M.; Rigoev, I. V.

2017-10-01

Hard aluminum-magnesium boride (BAM) films were fabricated onto Corning® Gorilla® Glass by radio-frequency magnetron sputtering of a single stoichiometric AlMgB14 target. BAM films exhibit a Vickers hardness from 10 to 30 GPa and a Young's modulus from 80 to 160 GPa depending on applied loading forces. Deposited hard coating increases the critical load at which glass substrate cracks. The adhesion energy of BAM films on Gorilla® Glass is 6.4 J/m2.

Application of the particle backscattering methods for the study of new oxide protective coatings at the surface of Al and Mg alloys

International Nuclear Information System (INIS)

Apelfeld, A.V.; Bespalova, O.V.; Borisov, A.M.; Dunkin, O.N.; Goryaga, N.G.; Kulikauskas, V.S.; Romanovsky, E.A.; Semenov, S.V.; Souminov, I.V.

2000-01-01

Rutherford (1.5 MeV 4 He + ) and Nuclear (7.7 MeV H + ) Backscattering Spectrometry were used for investigation of oxide protective coatings on the surface of Al and Mg alloys obtained by microarc oxidation (MAO). A model of microarc coating formation is proposed. For Mg alloy, the structure of MAO coating with very high corrosion resistance was determined

Formulation and evaluation of rifampicin sustained release tablets using juice of Citrus limetta as bio-retardant.

Science.gov (United States)

Gaur, K Pawan; Soam, Kulwant; Gupta, S K; Dabral, Prashant

2012-03-01

The advantages of biopolymers over synthetic polymers are low cost, natural origin, free from side effects, biocompatible, bio-acceptable, environmental friendly processing, local availability, better patient tolerance as well as public acceptance. Sustained release tablets containing rifampicin was prepared by adding 100 mg polymer and 50 mg Drug and Granules. Same procedure was followed with 3% and 5% of polymer for preparation of sustained release tablets. Additional Tablets of 100 mg, 200 mg and 400 mg were prepared using 5% of the polymer. The results indicated that the selected biopolymer had a good release retardant property thus it can be concluded that the selected biopolymer can be utilized as low cost natural biocompatible and biodegradable agent.

Formulation and evaluation of rifampicin sustained release tablets using juice of Citrus limetta as bio-retardant

Directory of Open Access Journals (Sweden)

K Pawan Gaur

2012-01-01

Full Text Available The advantages of biopolymers over synthetic polymers are low cost, natural origin, free from side effects, biocompatible, bio-acceptable, environmental friendly processing, local availability, better patient tolerance as well as public acceptance. Sustained release tablets containing rifampicin was prepared by adding 100 mg polymer and 50 mg Drug and Granules. Same procedure was followed with 3% and 5% of polymer for preparation of sustained release tablets. Additional Tablets of 100 mg, 200 mg and 400 mg were prepared using 5% of the polymer. The results indicated that the selected biopolymer had a good release retardant property thus it can be concluded that the selected biopolymer can be utilized as low cost natural biocompatible and biodegradable agent.

The formation of FHA coating on biodegradable Mg-Zn-Zr alloy using a two-step chemical treatment method

Science.gov (United States)

Jiang, S. T.; Zhang, J.; Shun, S. Z.; Chen, M. F.

2016-12-01

To improve the corrosion resistance of the biomedical magnesium alloy, a two-step chemical treatment method has been employed to prepare an FHA coating on the alloy surface. Prior to forming an FHA layer, the samples of Mg-3 wt% Zn-0.5 wt% Zr alloy were soaked in HF with concentration of 20% (v/v) at 37 °C temperature for 2 h, and were then placed into an aqueous solution with 0.1 mol/L Ca(NO3).4H2O and 0.06 mol/L NH4H2PO4 at 90 °C to prepare the Ca-P coating. The concentrations of Mg2+, F- ions, and pH variation with immersing time in the solution were investigated to explore the growth mechanism of FHA. The surface morphologies and compositions of the coatings were characterized by X-ray diffraction, scanning electron microscopy, and energy dispersive spectroscopy. The results showed that the alloy surface treated with acid formed a layer of MgF2 nanoparticles with a thickness of 0.7 μm. The corrosion resistance of coatings in SBF solution was evaluated by electrochemical impedance spectroscopy (EIS) and potentiodynamic polarization. The results showed that the substrate with FHA coating had good corrosion resistance. After immersing into the calcium phosphate solution, some small spherical particles were first formed on the surface; these then cover the surface completely after 20 min. Some clusters consisting of needle-like crystal were observed in the spherical particles covering the surface, and the Ca/P ratio of the needle-like crystal was 1.46, clearly growing along the c axis preferred orientation growth. After immersion for 60 min, the FHA coating with completely uniform growth was obtained on the Mg-Zn-Zr alloy surface with its thickness reaching about 120 μm.

Spectrum of tablet computer use by medical students and residents at an academic medical center.

Science.gov (United States)

Robinson, Robert

2015-01-01

Introduction. The value of tablet computer use in medical education is an area of considerable interest, with preliminary investigations showing that the majority of medical trainees feel that tablet computers added value to the curriculum. This study investigated potential differences in tablet computer use between medical students and resident physicians. Materials & Methods. Data collection for this survey was accomplished with an anonymous online questionnaire shared with the medical students and residents at Southern Illinois University School of Medicine (SIU-SOM) in July and August of 2012. Results. There were 76 medical student responses (26% response rate) and 66 resident/fellow responses to this survey (21% response rate). Residents/fellows were more likely to use tablet computers several times daily than medical students (32% vs. 20%, p = 0.035). The most common reported uses were for accessing medical reference applications (46%), e-Books (45%), and board study (32%). Residents were more likely than students to use a tablet computer to access an electronic medical record (41% vs. 21%, p = 0.010), review radiology images (27% vs. 12%, p = 0.019), and enter patient care orders (26% vs. 3%, p e-Books, and to study for board exams. Residents were more likely to use tablet computers to complete clinical tasks. Conclusions. Tablet computer use among medical students and resident physicians was common in this survey. All learners used tablet computers for point of care references and board study. Resident physicians were more likely to use tablet computers to access the EMR, enter patient care orders, and review radiology studies. This difference is likely due to the differing educational and professional demands placed on resident physicians. Further study is needed better understand how tablet computers and other mobile devices may assist in medical education and patient care.

In vitro metal ion release and biocompatibility of amorphous Mg{sub 67}Zn{sub 28}Ca{sub 5} alloy with/without gelatin coating

Energy Technology Data Exchange (ETDEWEB)

Chan, W.Y., E-mail: chan.wing.yue@sgh.com.sg [School of Mechanical and Aerospace Engineering, Nanyang Technological University (Singapore); Department of Plastic, Reconstructive and Aesthetic Surgery, Singapore General Hospital (Singapore); Chian, K.S.; Tan, M.J. [School of Mechanical and Aerospace Engineering, Nanyang Technological University (Singapore)

2013-12-01

Amorphous zinc-rich Mg–Zn–Ca alloys have exhibited good tissue compatibility and low hydrogen evolution in vivo. However, suboptimal cell–surface interaction on magnesium alloy surface observed in vitro could lead to reduced integration with host tissue for regenerative purpose. This study aims to improve cell–surface interaction of amorphous Mg{sub 67}Zn{sub 28}Ca{sub 5} alloy by coating a gelatin layer by electrospinning. Coated/uncoated alloys were immersed and extracted for 3 days under different CO{sub 2}. The immersion results showed that pH and metal ion release in the alloy extracts were affected by gelatin coating and CO{sub 2}, suggesting their roles in alloy biocorrosion and a mechanism has been proposed for the alloy–CO{sub 2} system with/without coating. Cytotoxicity results are evident that gelatin-coated alloy with 2-day crosslinking not only exhibited no indirect cytotoxicity, but also supported attachment of L929 and MG63 cell lines around/on the alloy with high viability. Therefore, amorphous Mg{sub 67}Zn{sub 28}Ca{sub 5} alloy coated with gelatin by electrospinning technique provides a useful method to improve alloy biocompatibility. - Highlights: • Electrospinning is a new method to coat amorphous Mg{sub 67}Zn{sub 28}Ca{sub 5} alloy with gelatin. • Gelatin-coated alloy has differential effect on pH and ion release at various CO{sub 2}. • L929 cell proliferation correlates with Mg{sup 2+} level in alloy extracts. • Biomimetic gelatin coating significantly improves cell–surface interaction.

Plasma deposited composite coatings to control biological response of osteoblast-like MG-63 cells

Science.gov (United States)

Keremidarska, M.; Radeva, E.; Eleršič, K.; Iglič, A.; Pramatarova, L.; Krasteva, N.

2014-12-01

The successful osseointegration of a bone implant is greatly dependent on its ability to support cellular adhesion and functions. Deposition of thin composite coatings onto the implant surface is a promising approach to improve interactions with cells without compromising implant bulk properties. In this work, we have developed composite coatings, based on hexamethyldisiloxane (HMDS) and detonation nanodiamond (DND) particles and have studied adhesion, growth and function of osteoblast-like MG-63 cells. PPHMDS/DND composites are of interest for orthopedics because they combine superior mechanical properties and good biocompatibility of DND with high adherence of HMDS to different substrata including glass, metals and plastics. We have used two approaches of the implementation of DND particles into a polymer matrix: pre-mixture of both components followed by plasma polymerization and layer-by-layer deposition of HMDS and DND particles and found that the deposition approach affects significantly the surface properties of the resulting layers and cell behaviour. The composite, prepared by subsequent deposition of monomer and DND particles was hydrophilic, with a rougher surface and MG-63 cells demonstrated better spreading, growth and function compared to the other composite which was hydrophobic with a smooth surface similarly to unmodified polymer. Thus, by varying the deposition approach, different PPHMDS/DND composite coatings, enhancing or inhibiting osteoblast adhesion and functions, can be obtained. In addition, the effect of fibronectin pre-adsorption was studied and was found to increase greatly MG-63 cell spreading.

Influence of Applied Voltage and Film-Formation Time on Microstructure and Corrosion Resistance of Coatings Formed on Mg-Zn-Zr-Ca Bio-magnesium Alloy

Science.gov (United States)

Yandong, Yu; Shuzhen, Kuang; Jie, Li

2015-09-01

The influence of applied voltage and film-formation time on the microstructure and corrosion resistance of coatings formed on a Mg-Zn-Zr-Ca novel bio-magnesium alloy has been investigated by micro-arc oxidation (MAO) treatment. Phase composition and microstructure of as-coated samples were analyzed by the x-ray diffraction, energy dispersive x-ray spectroscopy and scanning electron microscopy. And the porosity and average of micro-pore aperture of the surface on ceramic coatings were analyzed by general image software. Corrosion microstructure of as-coated samples was caught by a microscope digital camera. The long-term corrosion resistance of as-coated samples was tested in simulated body fluid for 30 days. The results showed that the milky white smooth ceramic coating formed on the Mg-Zn-Zr-Ca novel bio-magnesium alloy was a compound of MgO, Mg2SiO4 and MgSiO3, and its corrosion resistance was significantly improved compared with that of the magnesium substrate. In addition, when the MAO applied voltage were 450 V and 500 V and film-formation time were 9 min and 11 min, the surface micro-morphology and the corrosion resistance of as-coated samples were relatively improved. The results provided a theoretical foundation for the application of the Mg-Zn-Zr-Ca novel bio-magnesium alloy in biomedicine.

Limited sampling strategies drawn within 3 hours postdose poorly predict mycophenolic acid area-under-the-curve after enteric-coated mycophenolate sodium.

NARCIS (Netherlands)

Winter, B.C. de; Gelder, T. van; Mathôt, R.A.A.; Glander, P.; Tedesco-Silva, H.; Hilbrands, L.B.; Budde, K.; Hest, R.M. van

2009-01-01

Previous studies predicted that limited sampling strategies (LSS) for estimation of mycophenolic acid (MPA) area-under-the-curve (AUC(0-12)) after ingestion of enteric-coated mycophenolate sodium (EC-MPS) using a clinically feasible sampling scheme may have poor predictive performance. Failure of

Long-term corrosion inhibition mechanism of microarc oxidation coated AZ31 Mg alloys for biomedical applications

International Nuclear Information System (INIS)

Gu, Yanhong; Bandopadhyay, Sukumar; Chen, Cheng-fu; Ning, Chengyun; Guo, Yuanjun

2013-01-01

Highlights: ► The corrosion behavior is significantly affected by the long-term immersion. ► The degradation is inhibited due to the corrosion product layer. ► The corrosion resistance is enhanced by optimized MAO electrolyte concentrations. ► The corrosion inhibition mechanism is presented by a Flash animation. - Abstract: This paper addresses the long-term corrosion behavior of microarc oxidation coated Mg alloys immersed in simulated body fluid for 28 days. The coatings on AZ31 Mg alloys were produced in the electrolyte of sodium phosphate (Na 3 PO 4 ) at the concentration of 20 g/L, 30 g/L and 40 g/L, respectively. Scanning electron microscope (SEM) and optical micrograph were used to observe the microstructure of the samples before and after corrosion. The composition of the MAO coating and corrosion products were determined by X-Ray Diffraction (XRD). Corrosion product identification showed that hydroxyapatite (HA) was formed on the surface of the corroded samples. The ratio of Ca/P in HA determined by the X-ray Fluorescence (XRF) technique showed that HA is an acceptable biocompatible implant material. The potentiodynamic polarization and electrochemical impedance spectroscopy (EIS) were employed to characterize the corrosion rate and the electrochemical impedance. The corrosion resistance of the coated Mg alloys can be enhanced by optimizing the electrolyte concentrations for fabricating samples, and is enhanced after immersing the coated samples in simulated body fluid for more than 14 days. The enhanced corrosion resistance after long-term immersion is attributed to a corrosion product layer formed on the sample surface. The inhibition mechanism of the corrosion process is discussed and presented with an animation

Tabletted guar gum microspheres of piroxicam for targeted adjuvant therapy for colonic adenocarcinomas.

Science.gov (United States)

Vats, Anima; Pathak, Kamla

2012-11-01

In recent years, nonsteroidal anti-inflammatory drugs have been found to be cogent as an adjuvant therapeutic agent in mitigating colorectal cancer. Thus, this present investigation was aimed to formulate an oral, targeted tablet of piroxicam microspheres for sustained and targeted adjuvant therapy for colonic adenocarcinomas. Crosslinked guar gum microspheres of piroxicam were directly compressed into matrix tablet and coated with Eudragit S100. The optimized tablet that displayed 0% release in simulated gastric fluid, 15% in simulated intestinal fluid and 97.1% in simulated colonic fluid underwent roentgenographic study in rabbits to check its safe transit to the colon. x-ray images revealed intactness of the tablet until it reached the colon where the tablet matrix eroded. The designed, conceptual formulation emerged as potential carrier for targeted adjuvant therapy of piroxicam.

Spectrum of tablet computer use by medical students and residents at an academic medical center

Directory of Open Access Journals (Sweden)

Robert Robinson

2015-07-01

Full Text Available Introduction. The value of tablet computer use in medical education is an area of considerable interest, with preliminary investigations showing that the majority of medical trainees feel that tablet computers added value to the curriculum. This study investigated potential differences in tablet computer use between medical students and resident physicians.Materials & Methods. Data collection for this survey was accomplished with an anonymous online questionnaire shared with the medical students and residents at Southern Illinois University School of Medicine (SIU-SOM in July and August of 2012.Results. There were 76 medical student responses (26% response rate and 66 resident/fellow responses to this survey (21% response rate. Residents/fellows were more likely to use tablet computers several times daily than medical students (32% vs. 20%, p = 0.035. The most common reported uses were for accessing medical reference applications (46%, e-Books (45%, and board study (32%. Residents were more likely than students to use a tablet computer to access an electronic medical record (41% vs. 21%, p = 0.010, review radiology images (27% vs. 12%, p = 0.019, and enter patient care orders (26% vs. 3%, p < 0.001.Discussion. This study shows a high prevalence and frequency of tablet computer use among physicians in training at this academic medical center. Most residents and students use tablet computers to access medical references, e-Books, and to study for board exams. Residents were more likely to use tablet computers to complete clinical tasks.Conclusions. Tablet computer use among medical students and resident physicians was common in this survey. All learners used tablet computers for point of care references and board study. Resident physicians were more likely to use tablet computers to access the EMR, enter patient care orders, and review radiology studies. This difference is likely due to the differing educational and professional demands placed on

78 FR 66009 - Determination That INVEGA (Paliperidone) Extended-Release Tablet, 12 Milligrams, Was Not...

Science.gov (United States)

2013-11-04

...] Determination That INVEGA (Paliperidone) Extended-Release Tablet, 12 Milligrams, Was Not Withdrawn From Sale for... Food and Drug Administration (FDA) has determined that INVEGA (paliperidone) extended-release tablet...-release tablet, 12 mg, if all other legal and regulatory requirements are met. FOR FURTHER INFORMATION...

The enhanced corrosion resistance of UMAO coatings on Mg by silane treatment

Directory of Open Access Journals (Sweden)

Muqin Li

2014-10-01

Full Text Available The surface silanization was carried out on ultrasonic micro-arc oxidation (UMAO coatings on pure magnesium using KH550 as silane coupling agent (SCA. The surface morphology, chemical bonds and corrosion resistance of the silane films were investigated by scanning electron microscope (SEM, Fourier transform infrared spectroscopy (FTIR and electrochemical workstation, respectively. The results showed that hybrid coatings were successfully prepared on pure magnesium by UMAO-NaOH (1 mol/L, 2 mol/L, 3 mol/L-SCA processing. The organic films with Si–O–Mg bonds are helpful for the reduction of the pores in UMAO coatings. The pores decreased with increasing NaOH concentration. Compared with single UMAO treatment, the corrosion potentials (Ecorr of magnesium plates with UMAO-NaOH (1 mol/L, 2 mol/L, 3 mol/L-SCA treatment increased by 29 mV, 53 mV and 75 mV, respectively, meanwhile the corrosion current density (Icorr reduced one to two orders of magnitude. It indicated that the corrosion resistance of the coatings was improved by silane treatment.

Large-area thin self-supporting carbon foils with MgO coatings

Science.gov (United States)

Stolarz, Anna; Maier-Komor, Peter

2002-03-01

Large area self-supporting carbon foils in the thickness of range of 8-22 μg/cm 2, coated with approximately 4 μg/cm 2 MgO have been prepared by e-gun evaporation. They were mounted on frames with apertures of 130 cm 2. Problems related to the parting agent preparation, floating procedure, and mounting onto frames are discussed. Special precautions necessary to avoid damage during foil drying, storage and transportation are suggested.

High-Throughput Synthetic Chemistry Enabled by Organic Solvent Disintegrating Tablet.

Science.gov (United States)

Li, Tingting; Xu, Lei; Xing, Yanjun; Xu, Bo

2017-01-17

Synthetic chemistry remains a time- and labor-intensive process of inherent hazardous nature. Our organic solvent disintegrating tablet (O-Tab) technology has shown potential to make industrial/synthetic chemistry more efficient. As is the case with pharmaceutical tablets, our reagent-containing O-Tabs are mechanically strong, but disintegrate rapidly when in contact with reaction media (organic solvents). For O-Tabs containing sensitive chemicals, they can be further coated to insulate them from air and moisture. © 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Validación de un método espectrofotométrico para la cuantificación de principio activo en tabletas de nifedipino 10 mg Validation of a spectrophotometric method for quantification of the active principle in 10 mg Nifedipine tablets

Directory of Open Access Journals (Sweden)

Yalexmi Ramos Rodríguez

2008-12-01

Full Text Available Se realizó la validación de una técnica espectrofotométrica para la cuantificación del principio activo en tabletas de nifedipino 10 mg con el empleo de etanol al 96 % como solvente. Se determinaron los parámetros de linealidad, exactitud, precisión intermedia, repetibilidad, especificidad y robustez. Se comprobó que el método es lineal, exacto y preciso en un rango de 85 a 115 %, lo que demuestra la fiabilidad del método y su posibilidad de empleo en el control de la calidad de la forma terminada.The validation of a spectrophotometric method for the determination of active principle in tablets of nifedipine 10 mg is presented in this work. The linearity, precision, exactitude, specificity and robustness of the method were evaluated. The method employed was linear, exact and precise in the interval of 85 % to 115%. This proves that the method can be used in the tablets' quality control.

In vitro degradation and electrochemical corrosion evaluations of microarc oxidized pure Mg, Mg-Ca and Mg-Ca-Zn alloys for biomedical applications.

Science.gov (United States)

Pan, Yaokun; He, Siyu; Wang, Diangang; Huang, Danlan; Zheng, Tingting; Wang, Siqi; Dong, Pan; Chen, Chuanzhong

2015-02-01

Calcium phosphate (CaP) ceramic coatings were fabricated on pure magnesium (Mg) and self-designed Mg-0.6Ca, Mg-0.55Ca-1.74Zn alloys by microarc oxidation (MAO). The coating formation, growth and biomineralization mechanisms were discussed. The coating degradability and bioactivity were evaluated by immersion tests in trishydroxymethyl-aminomethane hydrochloric acid (Tris-HCl) buffer and simulated body fluid (SBF) solutions, respectively. The coatings and corrosion products were characterized by scanning electron microscope (SEM), X-ray diffractometer (XRD), X-ray photoelectron spectrometer (XPS) and fourier transform infrared spectrometer (FT-IR). The electrochemical workstation was used to investigate the electrochemical corrosion behaviors of substrates and coatings. Results showed that Mg-0.55Ca-1.74Zn alloy exhibits the highest mechanical strength and electrochemical corrosion resistance among the three alloys. The MAO-coated Mg-0.55Ca-1.74Zn alloy has the potential to be served as a biodegradable implant. Copyright © 2014 Elsevier B.V. All rights reserved.

In vivo study of nanostructured diopside (CaMgSi2O6) coating on magnesium alloy as biodegradable orthopedic implants

International Nuclear Information System (INIS)

Razavi, Mehdi; Fathi, Mohammadhossein; Savabi, Omid; Razavi, Seyed Mohammad; Heidari, Fariba; Manshaei, Maziar; Vashaee, Daryoosh; Tayebi, Lobat

2014-01-01

Highlights: • In vitro biocompatibility of biodegradable Mg alloy was improved by diopside coating. • In vivo biocompatibility of biodegradable Mg alloy was improved by diopside coating. • Degradation behavior of biodegradable Mg alloy was improved by diopside coating. - Abstract: In order to improve the corrosion resistance and bioactivity of a biodegradable magnesium alloy, we have recently prepared a nanostructured diopside (CaMgSi 2 O 6 ) coating on AZ91 magnesium alloy through a combined micro-arc oxidation (MAO) and electrophoretic deposition (EPD) method (reported elsewhere). In this work, we performed a detailed biocompatibility analysis of the implants made by this material and compared their performance with those of the uncoated and micro arc oxidized magnesium implants. The biocompatibility evaluation of samples was performed by culturing L-929 cells and in vivo animal study, including implantation of samples in greater trochanter of rabbits, radiography and histological examinations. The results from both the in vitro and in vivo studies indicated that the diopside/MAO coated magnesium implant significantly enhanced cell viability, biodegradation resistance and new bone formation compared with both the uncoated and the micro-arc oxidized magnesium implants. Our data provides an example of how the proper surface treatment of magnesium implants can overcome their drawbacks in terms of high degradation rate and gas bubble formation under physiological conditions

Formulation and Evaluation of pH-Responsive Mini-Tablets for Ileo ...

African Journals Online (AJOL)

Tropical Journal of Pharmaceutical Research July 2014; 13 (7): 1021-1029 ... Original Research Article. Formulation and ... in the early morning hours such as joint pain and functional .... along with placebo tablets were coated with the.

An environment-friendly phosphate chemical conversion coating on novel Mg-9Li-7Al-1Sn and Mg-9Li-5Al-3Sn-1Zn alloys with remarkable corrosion protection

Science.gov (United States)

Maurya, Rita; Siddiqui, Abdul Rahim; Balani, Kantesh

2018-06-01

An environment-friendly phosphate chemical conversion (PCC) coating has been deposited on novel LAT971 (Mg-9 wt%Li-7 wt%Al-1 wt%Sn) and LATZ9531 (Mg-9 wt%Li-5 wt%Al-3 wt%Sn-1 wt%Zn) alloys for improving their corrosion resistance. A dense and homogeneous flower like morphology (∼30 μm thick) was observed on the PCC coated Mg-Li based alloys. The presence of calcium hydrogen phosphate hydrate, tricalcium phosphate and trimagnesium phosphate were confirmed from the X-ray diffraction and X-ray photoelectron spectroscopy analysis. A lower corrosion current density of 6.74 × 10-7 mA/cm2 and 5.39 × 10-7 mA/cm2 was obtained for PCC coated alloys in 3.5% NaCl aqueous solution than that of uncoated LAT971 (0.82 mA/cm2) and LATZ9531 (0.34 mA/cm2) alloys, respectively, which offers corrosion protection efficiency of >99%. Electrochemical impedance spectroscopy (EIS) has revealed that the inner PCC coating (at coating/substrate interface) delay the direct contact between electrolyte and substrate, which offered higher charge transfer resistance (>4 orders of magnitude) than that of uncoated alloys. Thus, the PCC coating provides an effective corrosion protection to the ultra-lightweight LAT971 and LATZ9531 alloys surface and may be helpful in proving good anchoring with the top organic coatings or paints.

Preparation and characterization of a calcium-phosphate-silicon coating on a Mg-Zn-Ca alloy via two-step micro-arc oxidation.

Science.gov (United States)

Dou, Jinhe; Chen, Yang; Chi, Yiming; Li, Huancai; Gu, Guochao; Chen, Chuanzhong

2017-06-14

Magnesium alloys are the most promising implant materials due to their excellent biodegradability. However, their high degradation rate limits their practical application. In this study, we produced a calcium-phosphate (Ca-P) coating and a calcium-phosphate-silicon (Ca-P-Si) coating via one-step and two-step micro-arc oxidation processes, respectively. The microstructure and chemical composition of the MAO coatings were characterized using SEM, XRD and EDS. The degradation behaviors of the MAO coatings and the substrate were investigated using electrochemical techniques and immersion tests in simulated body fluid (SBF). The results show that the silicate was successfully incorporated into the Ca-P coating in the second MAO step, and this also increased the thickness of the coating. The Ca-P-Si coatings remarkably reduced the corrosion rate of the Mg alloy and Ca-P coating during 18 days of immersion in SBF. In addition, the bone-like apatite layer on the sample surface demonstrated the good biomineralization ability of the Ca-P-Si coating. Potentiodynamic polarization results showed that the MAO coating could clearly enhance the corrosion resistance of the Mg alloy. Moreover, we propose the growth mechanism of the MAO coating in the second step.

Superior critical current density obtained in MgB{sub 2} bulks via employing carbon-coated boron and minor Cu addition

Energy Technology Data Exchange (ETDEWEB)

Peng, Junming; Liu, Yongchang [State Key Laboratory of Hydraulic Engineering Simulation and Safety, School of Materials Science & Engineering, Tianjin University, Tianjin 300072 (China); Ma, Zongqing, E-mail: mzq0320@163.com [State Key Laboratory of Hydraulic Engineering Simulation and Safety, School of Materials Science & Engineering, Tianjin University, Tianjin 300072 (China); Institute for Superconducting and Electronic Materials, AIIM, University of Wollongong, Squires Way, North Wollongong, NSW 2500 (Australia); Shahriar Al Hossain, M. [Institute for Superconducting and Electronic Materials, AIIM, University of Wollongong, Squires Way, North Wollongong, NSW 2500 (Australia); Xin, Ying; Jin, Jianxun [Tianjin University – Futong Group Research Center of Applied Superconductivity, Tianjin University, Tianjin 300072 (China)

2016-09-15

Highlights: • Usage of carbon-coated boron leads to high level of homogeneous carbon doping. • Cu addition improves MgB{sub 2} grain connectivity, leading to higher J{sub c} at low fields. • Cu addition reduces MgO impurity, also contributing to the improvement of J{sub c}. - Abstract: High performance Cu doped MgB{sub 2} bulks were prepared by an in-situ method with carbon-coated amorphous boron as precursor. It was found that the usage of carbon-coated boron in present work leads to the formation of uniformly refined MgB{sub 2} grains, as well as a high level of homogeneous carbon doping in the MgB{sub 2} samples, which significantly enhance the J{sub c} in both Cu doped and undoped bulks compared to MgB{sub 2} bulks with normal amorphous boron precursor. Moreover, minor Cu can service as activator, and thus facilitates the growth of MgB{sub 2} grains and improves crystallinity and grain connectivity, which can bring about the excellent critical current density (J{sub c}) at self fields and low fields (the best values are 7 × 10{sup 5} A/cm{sup 2} at self fields, and 1 × 10{sup 5} A/cm{sup 2} at 2 T, 20 K, respectively). Simultaneously, minor Cu addition can reduce the amount of MgO impurity significantly, also contributing to the improvement of J{sub c} at low fields. Our work suggests that Cu-activated sintering combined with employment of carbon-coated amorphous boron as precursor could be a promising technique to produce practical MgB{sub 2} bulks or wires with excellent J{sub c} on an industrial scale.

Large-area thin self-supporting carbon foils with MgO coatings

CERN Document Server

Stolarz, A

2002-01-01

Large area self-supporting carbon foils in the thickness of range of 8-22 mu g/cm sup 2 , coated with approximately 4 mu g/cm sup 2 MgO have been prepared by e-gun evaporation. They were mounted on frames with apertures of 130 cm sup 2. Problems related to the parting agent preparation, floating procedure, and mounting onto frames are discussed. Special precautions necessary to avoid damage during foil drying, storage and transportation are suggested.

Large-area thin self-supporting carbon foils with MgO coatings

Energy Technology Data Exchange (ETDEWEB)

Stolarz, Anna E-mail: anna@slcj.uw.edu.pl; Maier-Komor, Peter

2002-03-11

Large area self-supporting carbon foils in the thickness of range of 8-22 {mu}g/cm{sup 2}, coated with approximately 4 {mu}g/cm{sup 2} MgO have been prepared by e-gun evaporation. They were mounted on frames with apertures of 130 cm{sup 2}. Problems related to the parting agent preparation, floating procedure, and mounting onto frames are discussed. Special precautions necessary to avoid damage during foil drying, storage and transportation are suggested.

Modified geometry three-layered tablet as a platform for class II ...

African Journals Online (AJOL)

shape tablet composed of a core layer matrix made mainly of the enteric polymer hydroxypropyl methylcellulose acetate succinate and two barrier layers on either sides made of ethylcellulose. He showed that the system is capable of providing a.

Synthesis and evaluation of MgF2 coatings by chemical conversion on magnesium alloys for producing biodegradable orthopedic implants of temporary use

International Nuclear Information System (INIS)

Casanova, P Y; Jaimes, K J; Parada, N J; Viejo, F; Hernández-Barrios, C A; Aparicio, M; Coy, A E

2013-01-01

The aim of the present work was the synthesis of biodegradable MgF 2 coatings by chemical conversion on the commercial Elektron 21 and AZ91D magnesium alloys, in aqueous HF solutions for different concentrations and temperatures. The chemical composition and morphology of the coatings were analyzed by scanning electron microscopy (SEM-EDX) and X-ray diffraction (XRD). On the other hand, their corrosion behavior was evaluated by gravimetric and electrochemical measurements in Hank's solution at 37°C for different immersion times. The experimental results revealed that chemical conversion in HF produced MgF 2 coatings which corrosion resistance was enhanced by increasing the HF concentration. Further, the microstructure and composition of the base alloy played a key role on the growth and degradation mechanisms of the MgF 2 coatings

Cimetidine Pharmacodynamics and Pharmacokinetics in Healthy Subjects: A Comparison of Tablets and Suspension

Directory of Open Access Journals (Sweden)

ABR Thomson

1994-01-01

Full Text Available The objective of this study was to compare the effect of cimetidine 200 mg tablet with that of cimetidine suspension (200 mg/10 mL, a 20 mL suspension of 800 mg magnesium hydroxide and 912 mg aluminum hydroxide, and matching placebo on intragastric pH of healthy volunteers. There were 13 males and seven females, mean age 23 years (range 20 to 32 and mean weight 72 kg (range 55 to 89. The intragastric pH of each subject was measured over 6 h starting immediately before dosing on each of five study days. Cimetidine plasma levels were measured for 6 h after dosing on each of the cimetidine study days. Cimetidine tablet and suspension were superior to placebo tablet or suspension or to the magnesium hydroxide/aluminum hydroxide suspension in the area under the pH time curve from 0 to 6 h, percentage time pH of at least 3.5, change from pretreatment pH area under the pH time curve (0 to 6 h and maximum increase in pH. Mean plasma cimetidine levels were significantly and positively correlated to mean intragastric pH for both cimetidine tablets and cimetidine suspension. Comparing cimetidine concentration (Cmax and lower percentage time plasma cimetidine concentration was at least 0.5 μg/mL (the minimum therapeutic level. These pharmacokinetic variations between cimetidine suspension and tablets may have partially explained the pharmacodynamic differences of the lower area under the pH time curve (0 to 6 h. The results indicate that both cimetidine tablets and cimetidine suspension significantly increase intragastric pH relative to the magnesium hydroxide/aluminum hydroxide suspension, placebo tablets or placebo suspension. Based on the assumption that elevation of intragastric pH is an important factor for alleviation of the symptoms and for the healing of peptic disorders, the results of this study suggest that both cimetidine tablets and cimetidine suspension should be effective treatment.

Understanding corrosion via corrosion product characterization: II. Role of alloying elements in improving the corrosion resistance of Zn-Al-Mg coatings on steel

International Nuclear Information System (INIS)

Volovitch, P.; Vu, T.N.; Allely, C.; Abdel Aal, A.; Ogle, K.

2011-01-01

Highlights: → Origins of better corrosion resistance of ZnAlMg coatings than galvanized steel. → Comparative study of corrosion products formed on ZnAlMg, ZnMg and Zn coatings. → Modeling of dissolution and precipitation stages of corrosion. → At early stages Mg stabilizes protective zinc basic salts during dry-wet cycling. → At later stages Al dissolves at high pH forming protective layered double hydroxides. - Abstract: Corrosion products are identified on Zn, ZnMg and ZnAlMg coatings in cyclic corrosion tests with NaCl or Na 2 SO 4 containing atmospheres. For Mg-containing alloys the improved corrosion resistance is achieved by stabilization of protective simonkolleite and zinc hydroxysulfate. At later stages, the formation of layered double hydroxides (LDH) is observed for ZnAlMg. According to thermodynamic modeling, Mg 2+ ions bind the excess of carbonate or sulfate anions preventing the formation of soluble or less-protective products. A preferential dissolution of Zn and Mg at initial stages of corrosion is confirmed by in situ dissolution measurement. The physicochemical properties of different corrosion products are compared.

Formation process of micro arc oxidation coatings obtained in a sodium phytate containing solution with and without CaCO{sub 3} on binary Mg-1.0Ca alloy

Energy Technology Data Exchange (ETDEWEB)

Zhang, R.F. [School of Material and Electromechanics, Jiangxi Science and Technology Normal University, Nanchang 330013 (China); Zhang, Y.Q. [Zhejiang DunAn Light Alloy Technology CO,.LTD, Zhuji 311835 (China); Hunan University of Science and Technology, Xiangtan 411201 (China); Zhang, S.F.; Qu, B. [School of Material and Electromechanics, Jiangxi Science and Technology Normal University, Nanchang 330013 (China); Guo, S.B. [Hunan University of Science and Technology, Xiangtan 411201 (China); Xiang, J.H., E-mail: xiangjunhuai@163.com [School of Material and Electromechanics, Jiangxi Science and Technology Normal University, Nanchang 330013 (China)

2015-01-15

Highlights: • Compared to the Mg phase, the area of Mg{sub 2}Ca phase is much smaller. • The coatings are preferentially developed on the area adjacent to Mg{sub 2}Ca phase. • During MAO process, some sodium phytate molecules are hydrolyzed. • Anodic coatings are developed from uneven to uniform. - Abstract: Micro arc oxidation (MAO) is an effective method to improve the corrosion resistance of magnesium alloys. In order to reveal the influence of alloying element Ca and CaCO{sub 3} electrolyte on the formation process and chemical compositions of MAO coatings on binary Mg-1.0Ca alloy, anodic coatings after different anodizing times were prepared on binary Mg-1.0Ca alloy in a base solution containing 3 g/L sodium hydroxide and 15 g/L sodium phytate with and without addition of CaCO{sub 3}. The coating formation was studied by using scanning electron microscope (SEM), energy dispersive X-ray spectroscopy (EDS) and X-ray diffraction (XRD). The results show that Mg-1.0Ca alloy is composed of two phases, the Mg phase and Mg{sub 2}Ca phase. After treating for 5 s, the coating began to develop and was preferentially formed on the area nearby Mg{sub 2}Ca phase, which may be resulted from the intrinsic electronegative potential of the Mg phase than that of Mg{sub 2}Ca phase. Anodic coatings unevenly covered the total surface after 20 s. After 80 s, the coatings were uniformly developed on Mg-1.0Ca alloy with micro pores. During MAO process, some sodium phytate molecules are hydrolyzed into inorganic phosphate. CaCO{sub 3} has minor influence on the calcium content of the obtained MAO coatings.

Relative bioavailability of methadone hydrochloride administered in chewing gum and tablets

DEFF Research Database (Denmark)

Christrup, Lona Louring; Angelo, H.R.; Bonde, J.

1990-01-01

Methadone administered in chewing gum in doses of 16.7-22.6 mg to seven patients in a study using an open balanced cross-over design, was compared with 20 mg of methadone given perorally as tablets. There was no significant difference in the AUC/D obtained after administration of chewing gum...... and tablets (p>0.05). It is concluded that the chewing gum formulation should be considered for further testing with respect to suppression of abstinence syndrome in narcotic addicts....

Relative bioavailability of methadone hydrochloride administered in chewing gum and tablets.

Science.gov (United States)

Christrup, L L; Angelo, H R; Bonde, J; Kristensen, F; Rasmussen, S N

1990-01-01

Methadone administered in chewing gum in doses of 16.7-22.6 mg to seven patients in a study using an open balanced cross-over design, was compared with 20 mg of methadone given perorally as tablets. There was no significant difference in the AUC/D obtained after administration of chewing gum and tablets (p greater than 0.05). It is concluded that the chewing gum formulation should be considered for further testing with respect to suppression of abstinence syndrome in narcotic addicts.

In vitro pharmacokinetics of anti-psoriatic fumaric acid esters

NARCIS (Netherlands)

N.H.R. Litjens (Nicolle); E. van Strijen (Elizabeth); C. van Gulpen (Co); H. Mattie (Herman); J.T. van Dissel (Jaap); H.B. Thio (Bing); P.H. Nibbering (Peter)

2004-01-01

textabstractBackground: Psoriasis is a chronic inflammatory skin disease that can be successfully treated with a mixture of fumaric acid esters (FAE) formulated as enteric-coated tablets for oral use. These tablets consist of dimethylfumarate (DMF) and salts of monoethylfumarate (MEF) and its main

Is online information on ecstasy tablet content safe?

Science.gov (United States)

Vrolijk, Ruben Q; Brunt, Tibor M; Vreeker, Annabel; Niesink, Raymond J M

2017-01-01

In recent years, the prevalence of ecstasy use has increased in most European countries. Users can acquire information on ecstasy tablet composition through the internet. This study compares online information from two websites, Pillreports and Partyflock, to the validated Dutch Drugs Information and Monitoring System (DIMS) database, and aims to measure its accuracy and potential danger or value. The drug-related information posted on Pillreports.net and Partyflock.nl between 1 January 2014 and 31 December 2015 was investigated for accuracy and several information characteristics such as picture inclusion and dose range inclusion. In total, 471 informatory statements on ecstasy tablet content were analysed relative to the Dutch ecstasy market. Informatory statements on the content of specific ecstasy tablets were scored as 'too high' or 'too low' if their concentrations deviated > 10 mg from the entries in the DIMS database within a 12-week time-frame, and scored as 'dangerous' if their concentration was > 40 mg too low. Unreported substances were scored as 'dangerous' if listed as an illegal or dangerous substance in the DIMS database and if present in relevant quantities. Also scored were the report characteristics 'picture inclusion', 'spread inclusion' and 'website source', which were tested for their association with report safety/danger. On average, reports on ecstasy tablets from Pillreports and Partyflock show concentrations which are 10.6 mg too high [95% confidence interval (CI) = 6.7-14.4]. Qualitatively, 39.7% of the reports scored as 'too high' (95% CI = 35.2-44.4), 17.6% scored as 'too low' (95% CI = 14.0-21.2) and 15.5% had 'unreported substances' (95% CI = 12.3-18.9), resulting overall in 15.3% of the reports being scored as 'dangerous' (95% CI = 11.9-18.5). The report characteristic 'spread inclusion' associated inversely with report danger [Exp(b) = 0.511, 95% CI = 0.307-0.850, P = 0.01]. Information from the popular

Three-Year Outcomes in Kidney Transplant Patients Randomized to Steroid-Free Immunosuppression or Steroid Withdrawal, with Enteric-Coated Mycophenolate Sodium and Cyclosporine: The Infinity Study

Directory of Open Access Journals (Sweden)

A. Thierry

2014-01-01

Full Text Available In a six-month, multicenter, open-label trial, de novo kidney transplant recipients at low immunological risk were randomized to steroid avoidance or steroid withdrawal with IL-2 receptor antibody (IL-2RA induction, enteric-coated mycophenolate sodium (EC-MPS: 2160 mg/day to week 6, 1440 mg/day thereafter, and cyclosporine. Results from a 30-month observational follow-up study are presented. Of 166 patients who completed the core study on treatment, 131 entered the follow-up study (70 steroid avoidance, 61 steroid withdrawal. The primary efficacy endpoint of treatment failure (clinical biopsy-proven acute rejection (BPAR graft loss, death, or loss to follow-up occurred in 21.4% (95% CI 11.8–31.0% of steroid avoidance patients and 16.4% (95% CI 7.1–25.7% of steroid withdrawal patients by month 36 (P=0.46. BPAR had occurred in 20.0% and 11.5%, respectively (P=0.19. The incidence of adverse events with a suspected relation to steroids during months 6–36 was 22.9% versus 37.1% (P=0.062. By month 36, 32.4% and 51.7% of patients in the steroid avoidance and steroid withdrawal groups, respectively, were receiving oral steroids. In conclusion, IL-2RA induction with early intensified EC-MPS dosing and CNI therapy in de novo kidney transplant patients at low immunological risk may achieve similar three-year efficacy regardless of whether oral steroids are withheld for at least three months.

The in vitro indirect cytotoxicity test and in vivo interface bioactivity evaluation of biodegradable FHA coated Mg-Zn alloys

Energy Technology Data Exchange (ETDEWEB)

Li Jianan [State Key Laboratory of Metal Matrix Composites, School of Materials Science and Engineering, Shanghai Jiao Tong University, Shanghai 200240 (China); Han Pei, E-mail: hanpei_cn@163.com [Orthopaedic Department of the 6th People' s Hospital, Shanghai Jiao Tong University, Shanghai 200233 (China); Ji Weiping [Orthopaedic Department of the 6th People' s Hospital, Shanghai Jiao Tong University, Shanghai 200233 (China); Song, Yang; Zhang, Shaoxiang; Chen Ying; Zhao Changli; Zhang Fan [State Key Laboratory of Metal Matrix Composites, School of Materials Science and Engineering, Shanghai Jiao Tong University, Shanghai 200240 (China); Zhang Xiaonong, E-mail: xnzhang@sjtu.edu.cn [State Key Laboratory of Metal Matrix Composites, School of Materials Science and Engineering, Shanghai Jiao Tong University, Shanghai 200240 (China); Key Laboratory of Inorganic Coating Materials, Chinese Academy of Sciences, Shanghai 200051 (China); Jiang Yao [Orthopaedic Department of the 6th People' s Hospital, Shanghai Jiao Tong University, Shanghai 200233 (China)

2011-12-15

A kind of biodegradable fluoridated hydroxyapatite (FHA) coating was prepared on Mg-Zn alloy to improve the interface bioactivity in bone healing via electrodeposition method. The in vitro cytotoxicity evaluation of the ions released during degradation was taken. No toxicity was shown and even higher cells' viability appeared on the 7th day compared with the normal culture case (negative control). In vivo implantation was carried out in the femoral condyle of adult New Zealand rabbits. The cross section showed by Micro-CT scan confirmed that the better interface contacts happened in the coated group after one month implantation. Also the coating left can still be normally observed by scanning electron microscope (SEM) with a little degradation. As a result, the FHA coating may be a promising candidate to enhance interface bioactivity for biodegradable Mg alloys in orthopaedics.

Contact Behavior of Composite CrTiSiN Coated Dies in Compressing of Mg Alloy Sheets under High Pressure

Directory of Open Access Journals (Sweden)

T.S. Yang

2018-01-01

Full Text Available Hard coatings have been adopted in cutting and forming applications for nearly two decades. The major purpose of using hard coatings is to reduce the friction coefficient between contact surfaces, to increase strength, toughness and anti-wear performance of working tools and molds, and then to obtain a smooth work surface and an increase in service life of tools and molds. In this report, we deposited a composite CrTiSiN hard coating, and a traditional single-layered TiAlN coating as a reference. Then, the coatings were comparatively studied by a series of tests. A field emission SEM was used to characterize the microstructure. Hardness was measured using a nano-indentation tester. Adhesion of coatings was evaluated using a Rockwell C hardness indentation tester. A pin-on-disk wear tester with WC balls as sliding counterparts was used to determine the wear properties. A self-designed compression and friction tester, by combining a Universal Testing Machine and a wear tester, was used to evaluate the contact behavior of composite CrTiSiN coated dies in compressing of Mg alloy sheets under high pressure. The results indicated that the hardness of composite CrTiSiN coating was lower than that of the TiAlN coating. However, the CrTiSiN coating showed better anti-wear performance. The CrTiSiN coated dies achieved smooth surfaces on the Mg alloy sheet in the compressing test and lower friction coefficient in the friction test, as compared with the TiAlN coating.

Contact Behavior of Composite CrTiSiN Coated Dies in Compressing of Mg Alloy Sheets under High Pressure.

Science.gov (United States)

Yang, T S; Yao, S H; Chang, Y Y; Deng, J H

2018-01-08

Hard coatings have been adopted in cutting and forming applications for nearly two decades. The major purpose of using hard coatings is to reduce the friction coefficient between contact surfaces, to increase strength, toughness and anti-wear performance of working tools and molds, and then to obtain a smooth work surface and an increase in service life of tools and molds. In this report, we deposited a composite CrTiSiN hard coating, and a traditional single-layered TiAlN coating as a reference. Then, the coatings were comparatively studied by a series of tests. A field emission SEM was used to characterize the microstructure. Hardness was measured using a nano-indentation tester. Adhesion of coatings was evaluated using a Rockwell C hardness indentation tester. A pin-on-disk wear tester with WC balls as sliding counterparts was used to determine the wear properties. A self-designed compression and friction tester, by combining a Universal Testing Machine and a wear tester, was used to evaluate the contact behavior of composite CrTiSiN coated dies in compressing of Mg alloy sheets under high pressure. The results indicated that the hardness of composite CrTiSiN coating was lower than that of the TiAlN coating. However, the CrTiSiN coating showed better anti-wear performance. The CrTiSiN coated dies achieved smooth surfaces on the Mg alloy sheet in the compressing test and lower friction coefficient in the friction test, as compared with the TiAlN coating.

Comparison of tadalafil pharmacokinetics after administration of a new orodispersible film versus a film-coated tablet

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Park SI

2018-04-01

Full Text Available Sang-In Park,1,* Su-Hak Heo,2,3,* Gihwan Kim,2 Seokhoon Chang,2 Keon-Hyoung Song,3 Min-Gul Kim,4 Eun-Heui Jin,5 JaeWoo Kim,5 SeungHwan Lee,1 Jang Hee Hong5,6 1Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul, Republic of Korea; 2R&D Center, C.L. Pharm Co., Ltd, Seoul, Republic of Korea; 3Department of Pharmaceutical Engineering, College of Medical Science, Soonchunhyang University, Asan, Republic of Korea; 4Department of Pharmacology, School of Medicine, Chonbuk National University, Jeonju, Republic of Korea; 5Clinical Trials Center, Chungnam National University Hospital, Daejeon, Republic of Korea; 6Department of Pharmacology, College of Medicine, Chungnam National University, Daejeon, Republic of Korea *These authors contributed equally to this work Background: An orodispersible film (ODF of tadalafil may provide increased convenience for erectile dysfunction (ED patients as compared to conventional tablet formulations. In this study, we aimed to compare the pharmacokinetic, safety, and tolerability profiles of a newly developed ODF formulation of tadalafil to those of a film-coated tablet (FCT of tadalafil.Materials and methods: This study was conducted in healthy male subjects using an open-label, randomized sequence, two-period, two-formulation, single-dose, crossover design. The subjects were randomly assigned to one of two sequences of the two formulations: both the test drug (ODF and the reference drug (FCT contained 20 mg of tadalafil. Blood samples were collected up to 72 h after administration. Plasma concentrations of tadalafil were analyzed using liquid chromatography–tandem mass spectrometry. Geometric mean ratios (GMRs of the ODF to FCT formulations and their 90% CIs for the pharmacokinetic parameters were estimated. Safety and tolerability were assessed throughout the study.Results: Forty healthy male subjects were enrolled, and 36 of these completed the

Evaluation of salmon calcitonin (sCT) enteric-coated capsule for enhanced absorption and GI tolerability in rats.

Science.gov (United States)

Wu, Lei; Zhang, Ge; Lu, Qin; Sun, Qian; Wang, Mulan; Li, Na; Gao, Zidong; Sun, Ya; Li, Tingting; Han, Deen; Yu, Xue; Wang, Lei; Sun, Wei; Zhao, Di; Wu, Yaning; Lu, Yang; Chen, Xijing

2010-03-01

Considering the chronic and repeated nature of salmon calcitonin (sCT) therapy, the oral route is a preferred route of administration. But, the oral bioavailability of sCT is very low due to enzymatic degradation and poor permeation across intestinal epithelial cells. It was the aim of this study to investigate the pharmacodynamic (PD), pharmacokinetic (PK), and mucosal injury characteristic of sCT oral delivery system. In this study, PD experiments were performed to find a suitable releasing region of sCT, an effect absorption enhancer, and an optimal mass ratio of sCT/enhancer. In addition, the PK experiments were designed to validate the absorption enhancement of this oral delivery system. Histopathological evaluations on the intestinal mucosa were carried out to assess any potential toxicity of the absorption enhancer. Through the PD research, we determined that oral sCT enteric-coated capsules containing sCT and citric acid (CA) with a ratio of 1:20 may be an adaptable delivery. PK study further proved that the oral absorption of sCT was enhanced from this delivery system. Finally, no damage on intestinal mucosa was observed when rats received the delivery system containing CA for up to 7 days. These results suggested that enteric-coated capsules with a certain amount of CA might give enhanced oral delivery of peptide drugs like sCT.

Bioequivalence of 250 mg lysine clonixinate tablets after a single oral dose in a healthy female Mexican population under fasting conditions.

Science.gov (United States)

Marcelín-Jiménez, G; Angeles, A C P; García, A; Morales, M; Rivera, L; Martín-Del-Campo, A

2010-05-01

To evaluate the bioequivalence between two 250 mg-tablets of lysine clonixinate, Dorixina Forte (Siegfried Rhein, México) as reference product, and Prestodol (Farmaceúticos Rayere, S.A., México) as test formulation. 26 healthy adult female Mexican volunteers received a single oral dose of 250-mg lysine clonixinate under fasting conditions. The drug was administered following a randomized, two-period, two-sequence, cross-over design. Twelve serial blood samples were collected up to 8 h after dosing, and clonixin (CLX) was measured by ultra-performance liquid chromatography (UPLC) coupled with tandem mass spectrometry. Decimal logarithm values of Cmax and area under the curve (AUC) were used to construct a classic confidence interval at 90% (90% CI). Bioequivalence was established if 90% CI of mean ratios (test/reference) fall within the 0.8-1.25 range. Volunteers formed a homogeneous population in terms of age (27.2 +/- 6.3 years), weight (55.9 +/- 6.5 kg), height (1.6 +/- 0.04 m), and body mass index (BMI) (22.91 +/- 2.03 kg/m(2)). Reference formulation exhibited the following pharmacokinetics: C(max) (32.39 +/- 8.32 microg/ml); t(max) (0.64 +/- 0.2 h); AUC0-8h (48.92 +/- 16.51 microg x h/ml); t1/2 (1.3 +/- 0.24 h); CLapp (5.64 +/- 1.99 l/h), and Vdapp (10.22 +/- 2.9 l). Concerning bioequivalence, 90% CI were: C(max) (82.32 - 98.79), AUC0-t (94.59-106.29), and AUC(0-inf) (94.61-106.42), with a statistical power of > 0.90 at every tested interval. This single-dose study found that both 250-mg immediate-release tablets of lysine clonixinate met the Mexican regulatory criteria for bioequivalence in these volunteers.

Characteristics and corrosion studies of vanadate conversion coating formed on Mg-14 wt%Li-1 wt%Al-0.1 wt%Ce alloy

Energy Technology Data Exchange (ETDEWEB)

Ma Yibin [School of Chemical Engineering and Technology, Harbin Institute of Technology, Harbin 150001 (China); Li Ning, E-mail: lininghit@263.net [School of Chemical Engineering and Technology, Harbin Institute of Technology, Harbin 150001 (China); Li Deyu [School of Chemical Engineering and Technology, Harbin Institute of Technology, Harbin 150001 (China); Zhang Milin; Huang Xiaomei [Key Laboratory of Superlight Materials and Surface Technology, Ministry of Education, Harbin Engineering University, Harbin 150001 (China)

2012-11-15

Highlights: Black-Right-Pointing-Pointer Vanadate film forms on the surface of Mg-Li-Al-Ce alloy. Black-Right-Pointing-Pointer Vanadate coating improves the corrosion resistance. Black-Right-Pointing-Pointer Vanadate coating is composed of Mg(OH){sub 2}, Li{sub 2}O and V{sub 2}O{sub 5}. - Abstract: Mg-14Li-1Al-0.1Ce alloy is immersed in NH{sub 4}VO{sub 3} + K{sub 3}(Fe(CN){sub 6}) solutions with different NH{sub 4}VO{sub 3} and/or K{sub 3}(Fe(CN){sub 6}) concentrations, and different immersion time. The surface morphology and composition of the vanadate coating are then characterized by scanning electron microscopy with energy dispersion spectroscopy (SEM-EDS) and X-ray photoelectron spectroscopy (XPS), and the corrosion behavior of the conversion coating is studied by polarization technique and electrochemical impedance spectroscopy (EIS). The experimental results indicate that the vanadate film with better corrosion resistance forms on Mg-Li-Al-Ce surface after the sample is immersed in 30 g L{sup -1} NH{sub 4}VO{sub 3} + 3.75 g L{sup -1} K{sub 3}(Fe(CN){sub 6}) solution at 80 Degree-Sign C for 10 min. The coating consists of V{sub 2}O{sub 5}, Li{sub 2}O and Mg(OH){sub 2}.

Formulation and Study of Some Controlled Release Tablets with Pentoxifylline Based on Hydroxypropylcellulose Matrix Obtained by Wet Granulation Method with PEG 6000

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Gabriel Hancu

2011-01-01

Full Text Available In this work three formulations of modified release tablets
containing pentoxifylline 400 mg/tablet were obtained. Hydroxypropylcellulose (HPC in di®erent ratios was used as hydrophilic matrix agent. The pentoxifylline inclusion in the matrix has been carried out by water granulation, using PEG 6000 as binder. Tablets were obtained with a single station
tablet machine (Korsch, using standard pressure, and obtaining tablets with 13 mm diameter, 800 mg weight and 400 mg pentoxifylline per tablet. The weight uniformity, friability, hardness, thickness and disintegration of tablets were determined according to the stipulations of the 2001 Supplement of the Romanian Pharmacopoeia Xth edition. The experimental formulations with 400 mg pentoxifylline/tablet were studied by comparing them to the industrial reference product, Trental 400 mg (Aventis Pharma and in according
to the stipulations of Romanian Pharmacopoeia Xth edition, USP 27 and European Pharmacopoeia 5th edition. Every determination was performed using 20 tablets. We followed the comparison between dissolution profiles of slow release tablets containing pentoxifylline based on hydrophilic matrix. The dissolution studies were performed using the method from USP 24, using the paddle apparatus, and water as medium of dissolution at 37+/-0,5 Celsius degrees, at a rotation speed of 50 rpm. The determination was performed by spectrofotometric as say in UV at 274 nm. It was noticeable that regarding the weight uniformity, friability, hardness, thickness and disintegration the proposed formulations are comparable with the industrial reference product (Trental, 400 mg and are in agreement with the stipulations of the Romanian Pharmacopoeia Xth edition and European Pharmacopoeia 5th edition. The analysis of dissolution profiles showed that all formulations exhibit slow release.

Relative bioavailability of a newly developed 5-mg levomethadone hydrochloride IR tablet (L-Polamidon® 5 mg tablets) in comparison with the 5-mg levomethadone hydrochloride oral solution (L-Polamidon® solution for substitution) as reference product.

Science.gov (United States)

Blume, Henning H; Wedemeyer, Ralf-Steven; Donath, Frank; Roscher, Katrin; Elvert, Gerd; Wagner, Daniel; Bley, Oliver; Vuia, Alexander; Todorova-Sanjari, Marina; Villalobos, Ramon; Schug, Barbara

2015-04-01

To establish the relative bioavailability (rBA) between two p.o. 5-mg levomethadone hydrochloride formulations, i.e., L-Polamidon® 5 mg tablets (test) vs. L-Polamidon® solution for substitution (reference). To assess the safety and tolerability of both formulations. A total of 33 healthy male subjects, aged 29 ± 6 years (BMI: 23.9 ± 2.5 kg/m2) completed this single center, open-label, randomized, 2-period cross-over study with single dose administrations under fasting conditions and coadministration with naltrexone for safety reasons. Administrations of both investigational products were separated by a washout period of at least 2 weeks, i.e., 13 treatmentfree days. The total dose for each subject was 2 x 5 mg resulting in 10 mg levomethadone hydrochloride. For pharmacokinetic evaluation, blood samples were withdrawn until 72 hours postdose. A validated non-stereoselective liquid chromatography-tandem mass spectroscopy method (LC-MS/MS) was applied for the determination of levomethadone in plasma. The lower limit of quantitation was 0.100 ng/mL. Adverse events were descriptively analyzed in the study population. The geometric means of the parameters related with the extent of total exposure of levomethadone, i.e., AUC(0-tlast) and AUC(0-∞), were 244.422 ng x h/mL and 332.999 ng x h/mL for test and 246.837 ng x h/mL and 329.467 ng×h/mL for reference, respectively. The geometric means of the peak exposure for levomethadone, i.e., Cmax, were 8.923 ng/mL for test and 8.635 ng/mL for reference. The point estimates (PEs) of the Test/Reference (T/R) adjusted geometric mean ratios of AUC(0-last), AUC(0-∞), and C(max) were 99.20%, 101.42%, and 104.11%, respectively, and all of them showed 90%-confidence intervals (CIs) within the range of 80.00 - 125.00% as suggested by regulatory requirements for bioequivalence assessment In total, 21 subjects experienced 55 AEs during the study, the most frequently reported AE, i.e., headache, accounted for 13 out of the total

Structural study of Mg doped cobalt ferrite thin films on ITO coated glass substrate

Science.gov (United States)

Suthar, Mahesh; Bapna, Komal; Kumar, Kishor; Ahuja, B. L.

2018-05-01

We have synthesized thin films of Co1-xMgxFe2O4 (x = 0, 0.4, 0.6, 0.8, 1) on transparent conducting indium tin oxide (ITO) coated glass substrate by pulsed laser deposition method. The structural properties of the grown films were analyzed by the X-ray diffraction and Raman spectroscopy, which suggest the single phase growth of these films. Raman spectra revealed the incorporation of Mg ions into CoFe2O4 lattice and suggest that the Mg ions initially go both to the octahedral and tetrahedral sites upto a certain concentration. For higher concentration, Mg ions prefer to occupy the tetrahedral sites.

Effect of antacids in didanosine tablet on bioavailability of isoniazid.

OpenAIRE

Gallicano, K; Sahai, J; Zaror-Behrens, G; Pakuts, A

1994-01-01

The antacids in two didanosine placebo tablets had no significant effect on the plasma pharmacokinetics of a single oral dose of 300 mg of isoniazid administered to 12 healthy volunteers. These results suggest that isoniazid bioavailability will be unaffected by the antacids in didanosine tablets when the two medications are administered simultaneously to human immunodeficiency virus-seropositive patients.

Effect of antacids in didanosine tablet on bioavailability of isoniazid.

Science.gov (United States)

Gallicano, K; Sahai, J; Zaror-Behrens, G; Pakuts, A

1994-04-01

The antacids in two didanosine placebo tablets had no significant effect on the plasma pharmacokinetics of a single oral dose of 300 mg of isoniazid administered to 12 healthy volunteers. These results suggest that isoniazid bioavailability will be unaffected by the antacids in didanosine tablets when the two medications are administered simultaneously to human immunodeficiency virus-seropositive patients.

The practice and clinical implications of tablet splitting in international health

Science.gov (United States)

Elliott, Ivo; Mayxay, Mayfong; Yeuichaixong, Sengchanh; Lee, Sue J; Newton, Paul N

2014-01-01

Objective Tablet splitting is frequently performed to facilitate correct dosing, but the practice and implications in low-income settings have rarely been discussed. Methods We selected eight drugs, with narrow therapeutic indices or critical dosages, frequently divided in the Lao PDR (Laos). These were split, by common techniques used in Laos, by four nurses and four laypersons. The mean percentage deviation from the theoretical expected weight and weight loss of divided tablets/capsules were recorded. Results Five of eight study drugs failed, on splitting, to meet European Pharmacopoeia recommendations for tablet weight deviation from the expected weight of tablet/capsule halves with 10% deviating by more than 25%. There was a significant difference in splitting accuracy between nurses and laypersons (P = 0.027). Coated and unscored tablets were less accurately split than uncoated (P = 0.03 and 0.0019 for each half) and scored (0.0001 for both halves) tablets. Conclusion These findings have potential clinical implications on treatment outcome and the development of antimicrobial resistance. Investment by drug companies in a wider range of dosage units, particularly for narrow therapeutic index and critical dosage medicines, is strongly recommended. PMID:24702766

Evaluation of Certain Pharmaceutical Quality Attributes of Lisinopril Split Tablets

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Khairi M. S. Fahelelbom

2016-10-01

Full Text Available Tablet splitting is an accepted practice for the administration of drugs for a variety of reasons, including dose adjustment, ease of swallowing and cost savings. The purpose of this study was to evaluate the physical properties of lisinopril tablets as a result of splitting the tablets either by hand or with a splitting device. The impact of the splitting technique of lisinopril (Zestril® tablets, 20 mg on certain physical parameters such as weight variation, friability, disintegration, dissolution and drug content were studied. Splitting the tablets either by hand or with a splitter resulted in a minute but statistically significant average weight loss of <0.25% of the tablet to the surrounding environment. The variability in the weight of the hand-split tablet halves was more pronounced (37 out of 40 tablet halves varied by more than 10% from the mean weight than when using the tablet splitter (3 out of 40 tablet halves. The dissolution and drug content of the hand-split tablets were therefore affected because of weight differences. However, the pharmacopoeia requirements for friability and disintegration time were met. Hand splitting of tablets can result in an inaccurate dose and may present clinical safety issues, especially for drugs with a narrow therapeutic window in which large fluctuations in drug concentrations are undesirable. It is recommended to use tablets with the exact desired dose, but if this is not an option, then a tablet splitter could be used.

Synthesized of PEG-6000 coated MgFe2O4 nanoparticles based on natural iron sand by co-precipitation method

Science.gov (United States)

Setiadi, E. A.; Simbolon, S.; Saputra, A. S. P.; Marlianto, E.; Djuhana; Kurniawan, C.; Yunus, M.; Sebayang, P.

2018-02-01

The polymer coated Magnesium Ferrite nanoparticles (MgFe2O4) based on natural iron sand, Mg(CH3COO)2.4H2O, and PEG-6000 have been successfully prepared by co-precipitation method. The mass variation of PEG-6000 content was from 0 to 12 gram. It was prepared at synthesize temperature of 70°C. The PEG coating reduced the effect of agglomeration, so the coercivity value can be closed to soft magnets. The nanoparticle of synthesized has MgFe2O4 single phase and cubic spinel structure. The bonding of MgFe2O4 and PEG-6000 as a coating material was confirmed by FTIR curve. The MgFe2O4 density decreased with the increasing of PEG 6000 content. On the other hand, the coercivity value was slightly reduced as the addition of PEG-6000, with the lowest value was obtained on 8 gram PEG content. The optimum condition is obtained at addition of 8 gram PEG 6000 to MgFe2O4, with coercivity, saturation, and remanence are 198.41 Oe, 52.53 emu/g, and 8.51 emu/g, respectively. So that, the sample is widely used as absorbance material of heavy metal.

The accuracy, precision and sustainability of different techniques for tablet subdivision: breaking by hand and the use of tablet splitters or a kitchen knife.

Science.gov (United States)

van Riet-Nales, Diana A; Doeve, Myrthe E; Nicia, Agnes E; Teerenstra, Steven; Notenboom, Kim; Hekster, Yechiel A; van den Bemt, Bart J F

2014-05-15

Tablets are frequently subdivided to lower the dose, to facilitate swallowing by e.g. children or older people or to save costs. Splitting devices are commonly used when hand breaking is difficult or painful. Three techniques for tablet subdivision were investigated: hand breaking, tablet splitter, kitchen knife. A best case drug (paracetamol), tablet (round, flat, uncoated, 500 mg) and operator (24-year student) were applied. Hundred tablets were subdivided by hand and by three devices of each of the following types: Fit & Healthy, Health Care Logistics, Lifetime, PillAid, PillTool, Pilomat tablet splitter; Blokker kitchen knife. The intra and inter device accuracy, precision and sustainability were investigated. The compliance to (adapted) regulatory requirements was investigated also. The accuracy and precision of hand broken tablets was 104/97% resp. 2.8/3.2% (one part per tablet considered; parts right/left side operator). The right/left accuracies of the splitting devices varied between 60 and 133%; the precisions 4.0 and 29.6%. The devices did not deteriorate over 100-fold use. Only hand broken tablets complied with all regulatory requirements. Health care professionals should realize that tablet splitting may result in inaccurate dosing. Authorities should undertake appropriate measures to assure good function of tablet splitters and, where feasible, to reduce the need for their use. Copyright © 2014 The Authors. Published by Elsevier B.V. All rights reserved.

Tramadol and acetaminophen tablets for dental pain.

OpenAIRE

Medve, R. A.; Wang, J.; Karim, R.

2001-01-01

The purpose of this work was to compare the efficacy and time to analgesia of a new tramadol/acetaminophen combination tablet to those of tramadol or acetaminophen (APAP) alone. A meta-analysis was performed of 3 separate single-dose, double-blind, parallel-group trials in patients with moderate or severe pain following extraction of 2 or more third molars. Patients in each study were evenly randomized to a single dose of tramadol/APAP (75 mg/650 mg), tramadol 75 mg, APAP 650 mg, ibuprofen 40...

A fixed-dose combination tablet of gemigliptin and metformin sustained release has comparable pharmacodynamic, pharmacokinetic, and tolerability profiles to separate tablets in healthy subjects

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Park SI

2015-02-01

Full Text Available Sang-In Park,1,* Howard Lee,1,2,* Jaeseong Oh,1 Kyoung Soo Lim,3 In-Jin Jang,1 Jeong-Ae Kim,4 Jong Hyuk Jung,4 Kyung-Sang Yu1 1Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul, 2Department of Transdisciplinary Studies, Graduate School of Convergence Science and Technology, Seoul National University, Clinical Trials Center, Seoul National University Hospital, Seoul, 3Department of Clinical Pharmacology and Therapeutics, CHA University School of Medicine and CHA Bundang Medical Center, Seongnam, 4LG Life Sciences, Ltd, Seoul, Republic of Korea *These authors contributed equally to this work Background: In type 2 diabetes mellitus, fixed-dose combination (FDC can provide the complementary benefits of correction of multiple pathophysiologic defects such as dysfunctions in glycemic or metabolic control while improving compliance compared with separate tablets taken together. The objective of the study reported here was to compare the pharmacodynamic (PD, pharmacokinetic (PK, and tolerability profiles of gemigliptin and extended-release metformin (metformin XR between FDC and separate tablets.Methods: A randomized, open-label, single-dose, two-way, two-period, crossover study was conducted in 28 healthy male volunteers. Two FDC tablets of gemigliptin/metformin 25/500 mg or separate tablets of gemigliptin (50 mg ×1 and metformin XR (500 mg ×2 were orally administered in each period. Serial blood samples were collected up to 48 hours post-dose to determine dipeptidyl peptidase 4 (DPP-4 activity using spectrophotometric assay and concentrations of gemigliptin and metformin using tandem mass spectrometry. Geometric mean ratios (GMRs of FDC to separate tablet formulations and their 90% confidence intervals (CIs were calculated to compare the PD and PK parameters between the two formulations. Tolerability was assessed throughout the study.Results: The plasma DPP-4 activity�

Biopharmaceutic Risk Assessment of Brand and Generic Lamotrigine Tablets.

Science.gov (United States)

Vaithianathan, Soundarya; Raman, Siddarth; Jiang, Wenlei; Ting, Tricia Y; Kane, Maureen A; Polli, James E

2015-07-06

The therapeutic equivalence of generic and brand name antiepileptic drugs has been questioned by neurologists and the epilepsy community. A potential contributor to such concerns is pharmaceutical quality. The objective was to assess the biopharmaceutic risk of brand name Lamictal 100 mg tablets and generic lamotrigine 100 mg tablets from several manufacturers. Lamotrigine was characterized in terms of the Biopharmaceutics Classification System (BCS), including aqueous solubility and Caco-2 permeability. A panel of pharmaceutical quality tests was also performed on three batches of Lamictal, three batches of Teva generic, and one batch of each of four other generics: appearance, identity, assay, impurity, uniformity of dosage units, disintegration, dissolution, friability, and loss on drying. These market surveillance results indicate that all brand name and generic lamotrigine 100 mg tablets passed all tests and showed acceptable pharmaceutical quality and low biopharmaceutic risk. Lamotrigine was classified as a BCS class IIb drug, exhibiting pH-dependent aqueous solubility and dissolution. At pH 1.2 and 4.5, lamotrigine exhibited high solubility, whereas lamotrigine exhibited low solubility at pH 6.8, including non-sink dissolution. Lamotrigine showed high Caco-2 permeability. The apparent permeability (Papp) of lamotrigine was (73.7 ± 8.7) × 10(-6) cm/s in the apical-to-basolateral (AP-BL) direction and (41.4 ± 1.6) × 10(-6) cm/s in the BL-AP direction, which were higher than metoprolol's AP-BL Papp of (21.2 ± 0.9) × 10(-6) cm/s and BL-AP Papp of (34.6 ± 4.6) × 10(-6) cm/s. Overall, lamotrigine's favorable biopharmaceutics from a drug substance perspective and favorable quality characteristics from a tablet formulation perspective suggest that multisource lamotrigine tablets exhibit a low biopharmaceutic risk.

Bioequivalence of a fixed-dose repaglinide/metformin combination tablet and equivalent doses of repaglinide and metformin tablets
.

Science.gov (United States)

Cho, Hea-Young; Ngo, Lien; Kim, Sang-Ki; Choi, Yoonho; Lee, Yong-Bok

2018-06-01

This study was conducted to determine whether a fixed-dose combination (FDC) tablet of repaglinide/metformin (2/500 mg) is equivalent to coadministration of equivalent doses of individual (EDI) tablets of repaglinide (2 mg) and metformin (500 mg) in healthy Korean male subjects. This study was conducted as an open-label, randomized, single-dose, two-period, two-sequence crossover design in 50 healthy Korean male subjects who received an FDC tablet or EDI tablets. Plasma concentrations of repaglinide and metformin were determined for up to 24 hours using a validated UPLC-MS/MS method. Bioequivalence was assessed according to current guidelines issued by the U.S. Food and Drug Administration (FDA) and Korean legislation. Tolerability was also evaluated throughout the study via subject interview, vital signs, and blood sampling. Point estimates (90% CIs) for AUC0-t, AUC0-∞, and Cmax based on EDI tablets were 110.07 (102.25 - 118.49), 109.90 (101.70 - 118.39), and 112.60 (101.49 - 124.85), respectively, for repaglinide. They were 95.18 (89.62 - 101.05), 95.00 (89.74 - 100.65), and 98.44 (92.72 - 104.50), respectively, for metformin. These results satisfied the bioequivalence criteria of 80.00 - 125.00% proposed by the FDA and Korean legislation. Results of pharmacokinetic analysis suggested that repaglinide and metformin in FDC tablets were bioequivalent to EDI tablets of repaglinide (2 mg) and metformin (500 mg) in healthy Korean male subjects. Both formulations appeared to be well tolerated.
.

Development and validation of dissolution method for carvedilol compression-coated tablets

Directory of Open Access Journals (Sweden)

Ritesh Shah

2011-12-01

Full Text Available The present study describes the development and validation of a dissolution method for carvedilol compression-coated tablets. Dissolution test was performed using a TDT-06T dissolution apparatus. Based on the physiological conditions of the body, 0.1N hydrochloric acid was used as dissolution medium and release was monitored for 2 hours to verify the immediate release pattern of the drug in acidic pH, followed by pH 6.8 in citric-phosphate buffer for 22 hours, to simulate a sustained release pattern in the intestine. Influences of rotation speed and surfactant concentration in medium were evaluated. Samples were analysed by validated UV visible spectrophotometric method at 286 nm. 1% sodium lauryl sulphate (SLS was found to be optimum for improving carvedilol solubility in pH 6.8 citric-phosphate buffer. Analysis of variance showed no significant difference between the results obtained at 50 and 100 rpm. The discriminating dissolution method was successfully developed for carvedilol compression-coated tablets. The conditions that allowed dissolution determination were USP type I apparatus at 100 rpm, containing 1000 ml of 0.1N HCl for 2 hours, followed by pH 6.8 citric-phosphate buffer with 1% SLS for 22 hours at 37.0 ± 0.5 ºC. Samples were analysed by UV spectrophotometric method and validated as per ICH guidelines.O presente estudo descreve o desenvolvimento e a validação de método de dissolução para comprimidos revestidos de carvedilol. O teste de dissolução foi efetuado utilizando-se o aparelho para dissolução TDT-06T. Com base nas condições fisiológicas do organismo, utilizou-se ácido clorídrico 0,1 N como meio de dissolução e a liberação foi monitorada por 2 horas para se verificar o padrão de liberação imediata do fármaco em condições de pH baixo, seguidas por pH 6,8 em tampão cítrico-fosfato por 22 horas, para simular o padrão de liberação controlada no intestino. Avaliou-se a influência da velocidade de

Gravimetric Analysis of Bismuth in Bismuth Subsalicylate Tablets: A Versatile Quantitative Experiment for Undergraduate Laboratories

Science.gov (United States)

Davis, Eric; Cheung, Ken; Pauls, Steve; Dick, Jonathan; Roth, Elijah; Zalewski, Nicole; Veldhuizen, Christopher; Coeler, Joel

2015-01-01

In this laboratory experiment, lower- and upper-division students dissolved bismuth subsalicylate tablets in acid and precipitated the resultant Bi[superscript 3+] in solution with sodium phosphate for a gravimetric determination of bismuth subsalicylate in the tablets. With a labeled concentration of 262 mg/tablet, the combined data from three…

Comparison of electrochemical corrosion behaviour of MgO and ZrO2 coatings on AM50 magnesium alloy formed by plasma electrolytic oxidation

International Nuclear Information System (INIS)

Liang, J.; Srinivasan, P. Bala; Blawert, C.; Dietzel, W.

2009-01-01

Two types of PEO coatings were produced on AM50 magnesium alloy using pulsed DC plasma electrolytic oxidation process in an alkaline phosphate and acidic fluozirconate electrolytes, respectively. The phase composition and microstructure of these PEO coatings were analyzed by X-ray diffraction (XRD) and scanning electron microscopy (SEM). The corrosion behaviour of the coated samples was evaluated by open circuit potential (OCP) measurements, potentiodynamic polarization tests, and electrochemical impedance spectroscopy (EIS) in neutral 0.1 M NaCl solution. The results showed that PEO coating prepared from alkaline phosphate electrolyte consisted of only MgO and on the other hand the one formed in acidic fluozirconate solution was mainly composed of ZrO 2 , MgF 2 . Electrochemical corrosion tests indicated that the phase composition of PEO coating has a significant effect on the deterioration process of coated magnesium alloy in this corrosive environment. The PEO coating that was composed of only MgO suffered from localized corrosion in the 50 h exposure studies, whereas the PEO coating with ZrO 2 compounds showed a much superior stability during the corrosion tests and provided an efficient corrosion protection. The results showed that the preparation of PEO coating with higher chemical stability compounds offers an opportunity to produce layers that could provide better corrosion protection to magnesium alloys.

Innovative micro-textured hydroxyapatite and poly(l-lactic)-acid polymer composite film as a flexible, corrosion resistant, biocompatible, and bioactive coating for Mg implants.

Science.gov (United States)

Kim, Sae-Mi; Kang, Min-Ho; Kim, Hyoun-Ee; Lim, Ho-Kyung; Byun, Soo-Hwan; Lee, Jong-Ho; Lee, Sung-Mi

2017-12-01

The utility of a novel ceramic/polymer-composite coating with a micro-textured microstructure that would significantly enhance the functions of biodegradable Mg implants is demonstrated here. To accomplish this, bioactive hydroxyapatite (HA) micro-dots can be created by immersing a Mg implant with a micro-patterned photoresist surface in an aqueous solution containing calcium and phosphate ions. The HA micro-dots can then be surrounded by a flexible poly(l-lactic)-acid (PLLA) polymer using spin coating to form a HA/PLLA micro-textured coating layer. The HA/PLLA micro-textured coating layer showed an excellent corrosion resistance when it was immersed in a simulated body fluid (SBF) solution and good biocompatibility, which was assessed by in vitro cell tests. In addition, the HA/PLLA micro-textured coating layer had high deformation ability, where no apparent changes in the coating layer were observed even after a 5% elongation, which would be unobtainable using HA and PLLA coating layers; furthermore, this allowed the mechanically-strained Mg implant with the HA/PLLA micro-textured coating layer to preserve its excellent corrosion resistance and biocompatibility in vitro. Copyright © 2017 Elsevier B.V. All rights reserved.

Colon specific CODES based Piroxicam tablet for colon targeting: statistical optimization, in vivo roentgenography and stability assessment.

Science.gov (United States)

Singh, Amit Kumar; Pathak, Kamla

2015-03-01

This study was aimed to statistically optimize CODES™ based Piroxicam (PXM) tablet for colon targeting. A 3(2) full factorial design was used for preparation of core tablet that was subsequently coated to get CODES™ based tablet. The experimental design of core tablets comprised of two independent variables: amount of lactulose and PEG 6000, each at three different levels and the dependent variable was %CDR at 12 h. The core tablets were evaluated for pharmacopoeial and non-pharmacopoeial test and coated with optimized levels of Eudragit E100 followed by HPMC K15 and finally with Eudragit S100. The in vitro drug release study of F1-F9 was carried out by change over media method (0.1 N HCl buffer, pH 1.2, phosphate buffer, pH 7.4 and phosphate buffer, pH 6.8 with enzyme β-galactosidase 120 IU) to select optimized formulation F9 that was subjected to in vivo roentgenography. Roentgenography study corroborated the in vitro performance, thus providing the proof of concept. The experimental design was validated by extra check point formulation and Diffuse Reflectance Spectroscopy revealed absence of any interaction between drug and formulation excipients. The shelf life of F9 was deduced as 12 months. Conclusively, colon targeted CODES™ technology based PXM tablets were successfully optimized and its potential of colon targeting was validated by roentgenography.

Implantable repository adrenaline tablets for long-term studies in rats

International Nuclear Information System (INIS)

Korsatko, W.; Porta, S.; Sadjak, A.; Supanz, S.

1982-01-01

Implantable coated Eudragit matrix tablets containing adrenaline in various concentrations should overcome the problem of additional handling stress during long-term infusions. The efficiency of those tablets was tested in vitro, as well as in vivo using 14 C-adrenaline. Both in vitro and in vivo testing yielded satisfactorily output rates up to 20 h whereby the liver and serum content of 14 C-fragments served as an additional prove for the postulated mode of action. Good correlation has been found between the mentioned out-put rates and adrenaline serum levels (measured according to Da Prada). (author)

Technological development of 40mg furosemide tablets: equivalence and bioavaibility study in dogs Desenvolvimento tecnológico da furosemida comprimido (40mg: estudo da equivalência e biodisponibilidade em cães

Directory of Open Access Journals (Sweden)

Ednaldo Q. Lima

2007-11-01

Full Text Available Furosemide (40mg was administered to 20 street dogs, 10 males and 10 females, in two different pharmaceutical forms: (1 compressed furosemide 40mg formulated at the Federal University of Pernambuco (UFPE-tablet, and (2 a commercial formulation with equal bioequivalence produced by the Laboratory for Pharmaceutical Technology of Pernambuco State (LAFEPE, the LAFEPE-furosemide. The study aimed to evaluate the kinetics of dissolution of the UFPE-tablet in order to analyze the behavior of bioavailability of the best formulation for veterinary use. The plasmatic concentrations of furosemide for the determination of parameters of pharmacological kinetics were analyzed by high-performance liquid chromatographic method (HPLC. The in vitro study accomplished through physiochemical analyses demonstrated that the formulas of the furosemide tablets attained the pharmaceutical requirements in agreement with USP 23 and the Brazilian Pharmacopoeia. The evaluation accomplished in dogs with UFPE-tablets given in only dose demonstrated uniformity in blood levels indicating stability in maintenance of the pharmaceutical formulation and efficiency in absorption of the active compound. These values are not significantly different in relation to the 5% confidence limit. Regarding maximum concentration (Tmax time and global bioavaibility assessed by AUC means, there were no considerable differences as well. UFPE-furosemide displayed 743.492µg/mL.h as AUC average value whereas LAFEPE-furosemide had an average of 537.284µg/mL.h.Furosemida (40mg foi administrada a 20 cães de rua (cães SRD, 10 machos e 10 fêmeas, em duas formas farmacêuicas distintas: (1 furosemida comprimido 40mg formulada na Universidade Federal de Pernambuco (UFPE-comprimido e (2 uma formulação comercial bioequivalente produzida pelo Laboratório de Tecnologia Farmacêutica do Estado de Pernambuco (LAFEPE-furosemida. O estudo objetivou avaliar a cinética de dissolução do UFPE-comprimido para

Evaluation of two novel tablet formulations of artemether-lumefantrine (Coartem) for bioequivalence in a randomized, open-label, two-period study.

Science.gov (United States)

Lefèvre, Gilbert; Bhad, Prafulla; Jain, Jay Prakash; Kalluri, Sampath; Cheng, Yi; Dave, Hardik; Stein, Daniel S

2013-09-08

Artemether-lumefantrine (Coartem; AL) is a standard of care for malaria treatment as an oral six-dose regimen, given twice daily over three days with one to four tablets (20/120 mg) per dose, depending on patient body weight. In order to reduce the pill burden at each dose and potentially enhance compliance, two novel fixed-dose tablet formulations (80/480 mg and 60/360 mg) have been developed and tested in this study for bioequivalence with their respective number of standard tablets. A randomized, open-label, two-period, single-dose, within formulation crossover bioequivalence study comparing artemether and lumefantrine exposure between the novel 80/480 mg tablet and four standard tablets, and the novel 60/360 mg tablet and three standard tablets, was conducted in 120 healthy subjects under fed conditions. Artemether, dihydroartemisinin, and lumefantrine were measured in plasma by HPLC/UPLC-MS/MS. Pharmacokinetic (PK) parameters were determined by non-compartmental analyses. Adjusted geometric mean AUClast for artemether were 345 and 364 ng·h/mL (geometric mean ratio (GMR) 0.95; 90% CI 0.89-1.01) and for lumefantrine were 219 and 218 μg·h/mL (GMR 1.00; 90% CI 0.93-1.08) for 80/480 mg tablet versus four standard tablets, respectively. Corresponding Cmax for artemether were 96.8 and 99.7 ng/mL (GMR 0.97; 90% CI 0.89-1.06) and for lumefantrine were 8.42 and 8.71 μg/mL (GMR 0.97; 90% CI 0.89-1.05). For the 60/360 mg tablet versus three standard tablets, adjusted geometric mean AUClast for artemether were 235 and 231 ng·h/mL (GMR 1.02; 90% CI 0.94-1.10), and for lumefantrine were 160 and 180 μg·h/mL (GMR 0.89; 90% CI 0.83-0.96), respectively. Corresponding Cmax for artemether were 75.5 and 71.5 ng/mL (GMR 1.06; 90% CI 0.95-1.18), and for lumefantrine were 6.64 and 7.61 μg/mL (GMR 0.87; 90% CI 0.81-0.94), respectively. GMR for Cmax and AUClast for artemether and lumefantrine for all primary comparisons were within the bioequivalence acceptance criteria (0

A randomized, phase I, double-blind, crossover study on pharmacokinetics of peppermint oil capsules in healthy volunteers : Enteric-coating versus colon-targeted-delivery

NARCIS (Netherlands)

Weerts, Z.Z.R.M.; Keszthelyi, D.; Frijlink, H.W.; Brouwers, J.R.B.J.; Vork, L.; Jonkers, D.M.A.E.; Masclee, A.A.M.

2016-01-01

Peppermint oil (PO) has been shown to reduce abdominal pain in patients with Irritable Bowel Syndrome (IBS). Menthol, the main constituent of PO, induces intestinal smooth muscle relaxation and desensitizes nociceptive nerve afferents. Enteric-coated (EC PO) capsules that release PO mainly in the

In vivo study of nanostructured diopside (CaMgSi{sub 2}O{sub 6}) coating on magnesium alloy as biodegradable orthopedic implants

Energy Technology Data Exchange (ETDEWEB)

Razavi, Mehdi, E-mail: mrzavi2659@gmail.com [Biomaterials Research Group, Department of Materials Engineering, Isfahan University of Technology, Isfahan 84156-83111 (Iran, Islamic Republic of); Torabinejad Dental Research Center, School of Dentistry, Isfahan University of Medical Sciences, Isfahan 81746-73461 (Iran, Islamic Republic of); School of Materials Science and Engineering, Helmerich Advanced Technology Research Center, Oklahoma State University, Tulsa, OK 74106 (United States); School of Electrical and Computer Engineering, Helmerich Advanced Technology Research Center, Oklahoma State University, Tulsa, OK 74106 (United States); Fathi, Mohammadhossein [Biomaterials Research Group, Department of Materials Engineering, Isfahan University of Technology, Isfahan 84156-83111 (Iran, Islamic Republic of); Dental Materials Research Center, Isfahan University of Medical Sciences, Isfahan (Iran, Islamic Republic of); Savabi, Omid [Torabinejad Dental Research Center, School of Dentistry, Isfahan University of Medical Sciences, Isfahan 81746-73461 (Iran, Islamic Republic of); Razavi, Seyed Mohammad [School of Dentistry, Isfahan University of Medical Sciences, Isfahan 81746-73461 (Iran, Islamic Republic of); Heidari, Fariba; Manshaei, Maziar [Torabinejad Dental Research Center, School of Dentistry, Isfahan University of Medical Sciences, Isfahan 81746-73461 (Iran, Islamic Republic of); Vashaee, Daryoosh [School of Electrical and Computer Engineering, Helmerich Advanced Technology Research Center, Oklahoma State University, Tulsa, OK 74106 (United States); Tayebi, Lobat, E-mail: lobat.tayebi@okstate.edu [School of Materials Science and Engineering, Helmerich Advanced Technology Research Center, Oklahoma State University, Tulsa, OK 74106 (United States); School of Chemical Engineering, Oklahoma State University, Stillwater, OK 74078 (United States)

2014-09-15

Highlights: • In vitro biocompatibility of biodegradable Mg alloy was improved by diopside coating. • In vivo biocompatibility of biodegradable Mg alloy was improved by diopside coating. • Degradation behavior of biodegradable Mg alloy was improved by diopside coating. - Abstract: In order to improve the corrosion resistance and bioactivity of a biodegradable magnesium alloy, we have recently prepared a nanostructured diopside (CaMgSi{sub 2}O{sub 6}) coating on AZ91 magnesium alloy through a combined micro-arc oxidation (MAO) and electrophoretic deposition (EPD) method (reported elsewhere). In this work, we performed a detailed biocompatibility analysis of the implants made by this material and compared their performance with those of the uncoated and micro arc oxidized magnesium implants. The biocompatibility evaluation of samples was performed by culturing L-929 cells and in vivo animal study, including implantation of samples in greater trochanter of rabbits, radiography and histological examinations. The results from both the in vitro and in vivo studies indicated that the diopside/MAO coated magnesium implant significantly enhanced cell viability, biodegradation resistance and new bone formation compared with both the uncoated and the micro-arc oxidized magnesium implants. Our data provides an example of how the proper surface treatment of magnesium implants can overcome their drawbacks in terms of high degradation rate and gas bubble formation under physiological conditions.

Abrasion resistant low friction and ultra-hard magnetron sputtered AlMgB14 coatings

Science.gov (United States)

Grishin, A. M.

2016-04-01

Hard aluminum magnesium boride films were fabricated by RF magnetron sputtering from a single stoichiometric AlMgB14 ceramic target. X-ray amorphous AlMgB14 films are very smooth. Their roughness does not exceed the roughness of Si wafer and Corning glass used as the substrates. Dispersion of refractive index and extinction coefficient were determined within 300 to 2500 nm range for the film deposited onto Corning glass. Stoichiometric in-depth compositionally homogeneous 2 μm thick films on the Si(100) wafer possess the peak values of nanohardness 88 GPa and Young’s modulus 517 GPa at the penetration depth of 26 nm and, respectively, 35 GPa and 275 GPa at 200 nm depth. Friction coefficient was found to be 0.06. The coating scratch adhesion strength of 14 N was obtained as the first chipping of the coating whereas its spallation failure happened at 21 N. These critical loads and the work of adhesion, estimated as high as 18.4 J m-2, surpass characteristics of diamond like carbon films deposited onto tungsten carbide-cobalt (WC-Co) substrates.

Reductive Degradation of Perfluorinated Compounds in Water using Mg-aminoclay coated Nanoscale Zero Valent Iron

OpenAIRE

Arvaniti, Olga S.; Hwang, Yuhoon; Andersen, Henrik Rasmus; Stasinakis, Athanasios S.; Thomaidis , Nikolaos S.; Aloupi, Maria

2015-01-01

Perfluorinated Compounds (PFCs) are extremely persistent micropollutants that are detected worldwide. We studied the removal of PFCs (perfluorooctanoic acid; PFOA, perfluorononanoic acid; PFNA, perfluorodecanoic acid; PFDA and perfluorooctane sulfonate; PFOS) from water by different types of nanoscale zero-valent iron (nZVI). Batch experiments showed that an iron dose of 1 g•L-1 in the form of Mg-aminoclay (MgAC) coated nZVI, at an initial pH of 3.0 effectively removed 38 % to 96 % of individ...

A newly developed lubricant, chitosan laurate, in the manufacture of acetaminophen tablets.

Science.gov (United States)

Bani-Jaber, Ahmad; Kobayashi, Asuka; Yamada, Kyohei; Haj-Ali, Dana; Uchimoto, Takeaki; Iwao, Yasunori; Noguchi, Shuji; Itai, Shigeru

2015-04-10

To study the usefulness of chitosan laurate (CS-LA), a newly developed chitosan salt, as a lubricant, lubrication properties such as the pressure transmission ratio and ejection force were determined at different concentrations of CS-LA in tableting. In addition, tablet properties such as the tensile strength, disintegration time, and dissolution behavior, were also determined. When CS-LA was mixed at concentrations of 0.1%-3.0%, the pressure transmission ratio was increased in a concentration-dependent manner, and the value at a CS-LA concentration of 3% was equal to that of magnesium stearate (Mg-St), a widely used lubricant. Additionally, a reduction in the ejection force was observed at a concentration from 1%, proving that CS-LA has good lubrication performance. A prolonged disintegration time and decreased tensile strength, which are known disadvantages of Mg-St, were not observed with CS-LA. Furthermore, with CS-LA, retardation of dissolution of the drug from the tablets was not observed. Conjugation of CS with LA was found to be quite important for both lubricant and tablet properties. In conclusion, CS-LA should be useful as an alternative lubricant to Mg-St. Copyright © 2015 Elsevier B.V. All rights reserved.

Enhancement in dye-sensitized solar cells based on MgO-coated TiO2 electrodes by reactive DC magnetron sputtering

International Nuclear Information System (INIS)

Wu Sujuan; Han Hongwei; Tai Qidong; Zhang Jing; Xu Sheng; Zhou Conghua; Yang Ying; Hu Hao; Chen Bolei; Sebo, Bobby; Zhao Xingzhong

2008-01-01

A surface modification method was carried out by reactive DC magnetron sputtering to fabricate TiO 2 electrodes coated with insulating MgO for dye-sensitized solar cells. The MgO-coated TiO 2 electrode had been characterized by x-ray photoelectron spectroscopy (XPS), energy-dispersive x-ray spectroscopy (EDX), scanning electron microscopy (SEM), UV-vis spectrophotometer, cyclic voltammetry (CV) and electrochemical impedance spectroscopy (EIS). The study results revealed that the TiO 2 modification increases dye adsorption, decreases trap states and suppresses interfacial recombination. The effects of sputtering MgO for different times on the performance of DSSCs were investigated. It indicated that sputtering MgO for 3 min on TiO 2 increases all cell parameters, resulting in increasing efficiency from 6.45% to 7.57%

[Effect of Tongluo Xingnao effervescent tablets on learning and memory dysfunction in rats with chronic cerebral ischemia].

Science.gov (United States)

Hu, Yong; Ju, Shao-Hua; Zhang, Yin-Jie; Xiong, Min; Xu, Shi-Jun; Ma, Yun-Tong; Zhong, Zhen-Dong

2014-05-01

To study the effect of Tongluo Xingnao effervescent tablets on learning and memory capacity and expression of Na(+)-K(+)-ATPase in hippocampus of rats with chronic cerebral ischemia-induced learning and memory dysfunction model. The 2-VO method was used to establish sd rat model learning and memory dysfunction induced by chronic cerebral ischemia. The 50 rats in the successfully established model were randomly divided into the model control group, the Dihydroergotoxine Mesylate tablets group (0.7 mg x kg(-1), Tongluo Xingnao effervescent tablets high dose (7.56 g x kg(-1)), middle dose (3.78 g x kg(-1)) and low dose (1.59 g x kg(-1)) groups and the sham operation group (n = 10) as the control group. The groups were orally given 10 ml x kg(-1) x d(-1) drugs for consecutively 90 days. On the 86th day, Morris water maze was adopted for them. On the 90th day, a leaning and memory capacity test was held. The brain tissues were fixed with 10% formaldehyde and observed for pathomorphism after routine slide preparation and staining. The expression of hippocampal Na(+)-K(+)-ATPase was detected with immunohistochemistry and image quantitative analysis. Compared with the model group, all of Tongluo Xingnao effervescent tablets groups showed significant decrease in the escape latency at the 5th day in the Morris water maze, and notable increase in the frequency of the first quadrant dwell, the frequency passing the escape platform and the frequency entering effective area (p tablets can improve the learning and memory capacity, reduce pathological changes of hippocampal tissues of rats with chronic cerebral ischemia-induced learning and memory dysfunction model, and promote the expression of Na(+)-K(+)-ATPase in hippocampus.

Relative bioavailability of rifampicin, isoniazid and ethambutol from a combination tablet vs. concomitant administration of a capsule containing rifampicin and a tablet containing isoniazid and ethambutol.

Science.gov (United States)

Schall, R; Müller, F O; Duursema, L; Groenewoud, G; Hundt, H K; Middle, M V; Mogilnicka, E M; Swart, K J

1995-11-01

Twenty male volunteers who were slow metabolisers of isoniazid, completed this single-blind, single-dose, randomised, cross-over study to compare the bioavailability of rifampicin (CAS 13292-46-1), isoniazid (CAS 54-85-3) and ethambutol (CAS 1070-11-7) from Myrin tablets (test preparation) with the bioavailability of these drugs from a combination of capsules containing rifampicin and tablets containing isoniazid and ethambutol (reference). There were 2 treatment periods and on clinic days volunteers were given either the reference (300 mig rifampicin plus 200 mg isoniazid and 600 mg ethambutol HCl), or the test preparation (300 mg rifampicin, 150 mg isoniazid and 600 mg ethambutol HCl). Serial blood samples were drawn from the volunteers and rifampicin, isoniazid and ethambutol assays were performed. The results of this study indicate that the test preparation is equivalent to the reference with respect to both the rate and the extent of absorption of rifampicin, isoniazid (after adjustment for the different doses of isoniazid and ethambutol).

A quality by design (QbD case study on enteric-coated pellets: Screening of critical variables and establishment of design space at laboratory scale

Directory of Open Access Journals (Sweden)

Shuling Kan

2014-10-01

Full Text Available The study aims to prepare naproxen enteric-coated pellets (NAP-ECPs by fluid-bed coating using QbD principle. Risk assessment was firstly performed by using failure mode and effect analysis (FMEA methodology. A Plackett–Burman design was then used for assessment of the most important variables affecting enteric-coated pellets characteristics. A Box–Behnken design was subsequently used for investigating the main, interactive, and quadratic effects of these variables on the response. By FMEA we discovered that eight factors should be considered to be high/important risk variables as compared with others. The responses of acid resistance and cumulative drug release were taken as critical quality attributes (CQAs. Pareto ranking analyses indicated that the coating weight gain (X7, triethyl citrate percentage (X1 and glycerol monostearate percentage (X2 were the most significant factors affecting the selected responses out of the eight high-risk variables. Optimization with response surface method (RSM further fully clarified the relationship between X7, X1, X2 and CQAs, and design space was established based on the constraints set on the responses. Due to the extreme coincidence of the predicted value generated by model with the observed value, the accuracy and robustness of the model were confirmed. It could be concluded that a promising NAP-ECPs was successfully designed using QbD approach in a laboratory scale.

Post-marketing experience with nevirapine extended release (XR) tablets: effectiveness and tolerability in a population-based cohort in British Columbia, Canada.

Science.gov (United States)

Lepik, Katherine J; Yip, Benita; McGovern, Rachel A; Ding, Erin; Nohpal, Adriana; Watson, Birgit E; Toy, Junine; Akagi, Linda; Harrigan, P Richard; Moore, David M; Hogg, Robert S; Montaner, Julio S G; Barrios, Rolando

2015-01-01

Nevirapine 400 mg extended release tablets (nevirapine-XR) are a once-daily alternative to nevirapine 200 mg immediate release tablets (nevirapine-IR). Study objectives were to describe the effectiveness and tolerability of nevirapine-XR in clinical practice and, for patients who switched from once daily 2×200 mg nevirapine-IR to nevirapine-XR, compare virological suppression and plasma nevirapine concentrations during each treatment period. HIV-1-infected adults entered the study cohort if they initiated nevirapine-XR in British Columbia (BC) Canada between 1 April 2012 and 30 September 2012 and were followed until 30 September 2013. Demographic and clinical variables were abstracted from the BC Centre for Excellence in HIV/AIDS databases. Patients who switched from once daily nevirapine-IR to nevirapine-XR were monitored for 6 months pre- and post-switch with comparison of virological suppression (McNeamer's test) and median random plasma nevirapine concentrations (Wilcoxon-Mann-Whitney test) in each period. The 536 nevirapine-XR-treated patients were 96% male, median (IQR) age 49.9 (44.0-56.9) years. Median follow-up was 15.6 (14.7-16.5) months, with 474/536 (88%) maintaining virological suppression. Emergent drug resistance developed in 5/536 (1%), adverse drug reactions in 17/536 (3%) and, although 31/536 (6%) reported 'whole' tablets in their stools, this was not associated with adverse outcomes. Among the 305 patients who switched from nevirapine-IR to nevirapine-XR, median (IQR) random plasma nevirapine concentration was higher during nevirapine-IR 5,000 (3,690-6,090) ng/ml than nevirapine-XR 3,930 (3,050-5,150) ng/ml (Pmarketing study affirms the effectiveness and tolerability of nevirapine-XR as an alternative to nevirapine-IR in adults.

Study on the bonding strength between calcium phosphate/chitosan composite coatings and a Mg alloy substrate

Science.gov (United States)

Zhang, Jie; Dai, Chang-Song; Wei, Jie; Wen, Zhao-Hui

2012-11-01

In order to improve the bonding strength between calcium phosphate/chitosan composite coatings and a micro-arc oxidized (MAO)-AZ91D Mg alloy, different influencing parameters were investigated in the process of electrophoretic deposition (EPD) followed by conversion in a phosphate buffer solution (PBS). Surface morphology and phase constituents of the as-prepared materials were investigated by using X-ray diffractometer (XRD), Fourier-transformed infrared spectrophotometer (FTIR), Raman spectrometer, scanning electron microscope (SEM) with an energy dispersive spectrometer (EDS), and a thermo gravimetric and differential thermal analyzer (TG-DTA). Scratch tests were carried out to study the bonding properties between the coatings and the substrates. In vitro immersion tests were conducted to determine the corrosion behaviors of samples with and without deposit layers through electrochemical experiments. In the EPD process, the acetic acid content in the electrophoresis suspension and the electrophoretic voltage played important roles in improving the bonding properties, while the contents of chitosan (CS) and nano-hydroxyapatite (nHA, Ca10(PO4)6(OH)2) in the suspension had less significant influences on the mechanical bonding strength. It was observed that the coatings showed the excellent bonding property when an electrophoretic voltage was in a range of 40-110 V with other reagent amounts as follows: acetic acid: 4.5 vol.%, CS ≤ 0.25 g, nHA ≤ 2.0 g in 200 ml of a CS-acetic acid aqueous solution and nHA ≤ 2.5 g in 300 ml of absolute ethanol. The morphology of the composite coating obtained under the above optimal condition had a flake-like crystal structure. The EPD in the nHA/CS-acetic acid/ethanol suspension resulted in hydroxyapatite, chitosan, brushite (DCPD, CaHPO4·2H2O) and Ca(OH)2 in the coatings. After the as-prepared coating materials were immersed into PBS, Ca(OH)2 could be converted into HA and DCPD. The results of the electrochemical tests

(Gynazole-1® Compared to Fluconazole 150 mg Tablets (Diflucan® in the Time to Relief of Symptoms in Patients With Vulvovaginal Candidiasis

Directory of Open Access Journals (Sweden)

Larry S. Seidman

2005-01-01

Full Text Available Background. It is estimated that as many as 13 million cases of vulvovaginal infection occur in the United States annually, the majority of which are the result of Candida albicans infection. The symptoms of vulvovaginal infections are often painful and distressing to the patient. The objective of this study was to compare the time to symptomatic relief of vulvovaginal candidiasis (VVC with butoconazole nitrate 2% Site Release® vaginal cream (Gynazole-1® and oral fluconazole 150 mg tablets (Diflucan®.

Study on the bonding strength between calcium phosphate/chitosan composite coatings and a Mg alloy substrate

Energy Technology Data Exchange (ETDEWEB)

Zhang Jie [School of Chemistry Engineering and Technology, Harbin Institute of Technology, Harbin 150001 (China); Pharmacy College, Jiamusi University, Jiamusi 154007 (China); Dai Changsong, E-mail: changsd@hit.edu.cn [School of Chemistry Engineering and Technology, Harbin Institute of Technology, Harbin 150001 (China); Wei Jie [School of Chemistry Engineering and Technology, Harbin Institute of Technology, Harbin 150001 (China); School of Chemistry and Bioengineering, Suzhou Science Technology University, Suzhou 215009 (China); Wen Zhaohui, E-mail: wenzhaohui1968@163.com [Department of Neuro intern, First Affiliated Hospital of Harbin Medical University, Harbin 150001 (China)

2012-11-15

Highlights: Black-Right-Pointing-Pointer Calcium phosphate/chitosan composite coatings on the MAO-AZ91D alloy were prepared. Black-Right-Pointing-Pointer The bonding force between the coating and the magnesium alloy was optimized. Black-Right-Pointing-Pointer The composite coating slowed down the corrosion rate of magnesium alloy in m-SBF. - Abstract: In order to improve the bonding strength between calcium phosphate/chitosan composite coatings and a micro-arc oxidized (MAO)-AZ91D Mg alloy, different influencing parameters were investigated in the process of electrophoretic deposition (EPD) followed by conversion in a phosphate buffer solution (PBS). Surface morphology and phase constituents of the as-prepared materials were investigated by using X-ray diffractometer (XRD), Fourier-transformed infrared spectrophotometer (FTIR), Raman spectrometer, scanning electron microscope (SEM) with an energy dispersive spectrometer (EDS), and a thermo gravimetric and differential thermal analyzer (TG-DTA). Scratch tests were carried out to study the bonding properties between the coatings and the substrates. In vitro immersion tests were conducted to determine the corrosion behaviors of samples with and without deposit layers through electrochemical experiments. In the EPD process, the acetic acid content in the electrophoresis suspension and the electrophoretic voltage played important roles in improving the bonding properties, while the contents of chitosan (CS) and nano-hydroxyapatite (nHA, Ca{sub 10}(PO{sub 4}){sub 6}(OH){sub 2}) in the suspension had less significant influences on the mechanical bonding strength. It was observed that the coatings showed the excellent bonding property when an electrophoretic voltage was in a range of 40-110 V with other reagent amounts as follows: acetic acid: 4.5 vol.%, CS {<=} 0.25 g, nHA {<=} 2.0 g in 200 ml of a CS-acetic acid aqueous solution and nHA {<=} 2.5 g in 300 ml of absolute ethanol. The morphology of the composite coating

Study on the bonding strength between calcium phosphate/chitosan composite coatings and a Mg alloy substrate

International Nuclear Information System (INIS)

Zhang Jie; Dai Changsong; Wei Jie; Wen Zhaohui

2012-01-01

Highlights: ► Calcium phosphate/chitosan composite coatings on the MAO-AZ91D alloy were prepared. ► The bonding force between the coating and the magnesium alloy was optimized. ► The composite coating slowed down the corrosion rate of magnesium alloy in m-SBF. - Abstract: In order to improve the bonding strength between calcium phosphate/chitosan composite coatings and a micro-arc oxidized (MAO)-AZ91D Mg alloy, different influencing parameters were investigated in the process of electrophoretic deposition (EPD) followed by conversion in a phosphate buffer solution (PBS). Surface morphology and phase constituents of the as-prepared materials were investigated by using X-ray diffractometer (XRD), Fourier-transformed infrared spectrophotometer (FTIR), Raman spectrometer, scanning electron microscope (SEM) with an energy dispersive spectrometer (EDS), and a thermo gravimetric and differential thermal analyzer (TG–DTA). Scratch tests were carried out to study the bonding properties between the coatings and the substrates. In vitro immersion tests were conducted to determine the corrosion behaviors of samples with and without deposit layers through electrochemical experiments. In the EPD process, the acetic acid content in the electrophoresis suspension and the electrophoretic voltage played important roles in improving the bonding properties, while the contents of chitosan (CS) and nano-hydroxyapatite (nHA, Ca 10 (PO 4 ) 6 (OH) 2 ) in the suspension had less significant influences on the mechanical bonding strength. It was observed that the coatings showed the excellent bonding property when an electrophoretic voltage was in a range of 40–110 V with other reagent amounts as follows: acetic acid: 4.5 vol.%, CS ≤ 0.25 g, nHA ≤ 2.0 g in 200 ml of a CS–acetic acid aqueous solution and nHA ≤ 2.5 g in 300 ml of absolute ethanol. The morphology of the composite coating obtained under the above optimal condition had a flake-like crystal structure. The EPD in

Structural evolution, thermomechanical recrystallization and electrochemical corrosion properties of Ni-Cu-Mg amorphous coating on mild steel fabricated by dual-anode electrolytic processing