Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Tablets”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 1,585 records · Page 88Linked to original sources
PubMed1996

Evaluation of different doses of soluble ibuprofen and ibuprofen tablets in postoperative dental pain.

The object of the study was to assess the comparative efficacy of three single doses (200, 400, 600 mg) of soluble ibuprofen and ibuprofen tablets after third molar surgery in 148 patients and aged 18-40 years. Outcome was measured by overall assessment of pain (AUC360) assessed from serial visual analogue scales, the number of patients taking additional analgesic and by overall assessment of medication evaluated on a five-point categorical scale. Over the 6-hour investigation period all the ibuprofen treatments with the exception of ibuprofen tablets 200 mg resulted in significantly less pain (p < 0.05) than placebo treatment. A large number of patients required additional analgesia during the investigation period, but the time to taking it was significantly earlier in the placebo group. No significant dose response (p > 0.05) was observed for either ibuprofen preparations assessed by the outcome variable of overall pain experience (AUC360) or time to additional analgesia. There was no significant difference in pain scores or time to taking additional analgesics between the respective doses of soluble and tablet formulations of ibuprofen. Both soluble and tablet formulations of ibuprofen provide effective pain control in the early postoperative period after removal of impacted third molars. There is little analgesic advantage in increasing the dose to 600 mg and only minimal benefit from using a soluble formulation of the drug.

Adult↗
PubMed1999

Pharmacokinetic comparison of the buprenorphine sublingual liquid and tablet.

Buprenorphine is a mu opioid partial agonist being developed as a treatment for opioid dependence. Buprenorphine, usually administered as a sublingual liquid, is now being developed as a sublingual tablet for clinical use. The present study compared participants' plasma concentrations after daily maintenance on three buprenorphine liquid doses (2, 4 and 8 mg) and one tablet dose (8 mg). Fourteen opioid-dependent individuals (11 males, three females) participated. Plasma samples were collected over a 24-h period after at least 7 days of maintenance on each dose. Results showed that the liquid doses produced dose-related increases in plasma concentrations. The 8-mg tablet produced mean plasma concentrations significantly lower than those of the 8-mg liquid, although there was substantial individual variability. Thus, the buprenorphine tablet dose might have to be adjusted to produce plasma concentrations equivalent to those of the liquid.

Administration, Sublingual↗
PubMed2000

Tensile strength of tablets containing two materials with a different compaction behaviour.

The tensile strength of tablets compressed from binary mixtures is in general not linearly related to the strength of tablets prepared from single materials; in many cases it shows a decreased tensile strength relative to interpolation. The materials used in this study, sodium chloride and pregelatinised starch, are both plastically deforming materials, but have a different densification and relaxation behaviour. The yield pressure of the binary mixtures shows an almost linear relationship. As an effect of their lower yield pressure, starch particles yield earlier than sodium chloride particles. The following enclosure prevents some sodium chloride particles to yield or crack. The relaxation of the tablets is higher than the relaxation calculated by linear interpolation of the relaxation behaviour of the two pure materials. The difference between the measured porosity expansion and the data obtained by linear interpolation can be considered as a measure for the reduced interparticle bonding. SEM-photographs indicate that the reduced interparticle bonding is caused by the low adhesive forces. The measured decrease of the tensile strength of the tablets is also considered to be the result of reduced interparticle bonding. In this paper it is shown that there exists a similar relationship between the tensile strength reduction and the percentage of starch on the one hand and the extra porosity expansion and the starch percentage on the other hand.

Pressure↗
PubMed2001

Effect of disintegrants with different hygroscopicity on dissolution of Norfloxacin/Pharmatose DCL 11 tablets.

This paper reports the effect of disintegrant hygroscopicity on dissolution of tablets obtained by compression at 85 MPa of mixtures of Norfloxacin and different proportions of a disintegrant (Starch 1500, PVP XL 10 or Croscarmellose sodium) and a diluent (Pharmatose DCL 11). Dissolution behavior was evaluated according to USP 23, apparatus 2 (paddle) at 50 rpm and using 750 ml acetate buffer solution of pH 4, at 37 degrees C, as medium. Norfloxacin added of increasing proportions, in a given range, of each disintegrant or the diluent increased the drug dissolved. Addition of increasing proportions of Pharmatose DCL 11 to Norfloxacin with 5% of the high hygroscopic Starch 1500 reduced the dissolution improvement effect of Pharmatose DCL 11. Addition of 5% Pharmatose DCL 11 to tablets of the middle hygroscopic Croscarmellose sodium and Norfloxacin slightly reduced the Croscarmellose sodium dissolution promoting effect, while addition of 15% Pharmatose DCL 11 to tablets of the low hygroscopic PVP XL 10 and Norfloxacin showed no inhibition but potentiated substantially the dissolution of Norfloxacin. These effects were attributed to competition for the available water in the tablet and to different water consume, for dissolution or hydration, by the diluent and the disintegrants.

Anti-Infective Agents↗
PubMed2001

Citric acid as excipient in multiple-unit enteric-coated tablets for targeting drugs on the colon.

Delivery of drugs to the large bowel has been extensively investigated during the last decade. The aim of this study was to investigate whether enteric-coated tablets could be made from enteric-coated matrix granules and drug release targeted to the colon. Whether in vitro drug release rate and in vivo absorption could be delayed by adding citric acid to the granules and/or to the tablet matrix was also studied. Ibuprofen was used as model drug because it is absorbed throughout the gastrointestinal tract. Eudragit S and Aqoat AS-HF were used as enteric polymers. Drug release rates were studied at different pH levels and drug absorption was studied in bioavailability tests. The conclusion was that citric acid retarded in vitro drug release when used in multiple-unit tablets. In vivo absorption of ibuprofen was markedly delayed when citric acid was included in both granules and tablet matrix. Further studies are needed to determine the optimal amount of citric acid in formulations.

Adult↗
PubMed2002

The effects of pressure and direct compression on tabletting of microsponges.

Microsponges are porous, polymeric microspheres that are used mostly for topical and recently for oral administration. Ketoprofen was used as a model drug for systemic drug delivery of microsponges in the study. Ketoprofen microsponges were prepared by quasi-emulsion solvent diffusion method with Eudragit RS 100 and afterwards tablets of microsponges were prepared by direct compression method. Different pressure values were applied to the tablet powder mass in order to determine the optimum pressure value for compression of the tablets. Results indicated that microsponge compressibility was much improved over the physical mixture of the drug and polymer and owing to the plastic deformation of sponge-like structure, microsponges produce mechanically strong tablets.

Acrylic Resins↗
PubMed2003

Development of oral acetaminophen chewable tablets with inhibited bitter taste.

Various formulations with some matrix bases and corrigents were examined for development of oral chewable tablets which suppressed the bitter taste of acetaminophen, often used as an antipyretic for infants. Corn starch/lactose, cacao butter and hard fat (Witepsol H-15) were used for matrix bases, and sucrose, cocoa powder and commercial bitter-masking powder mixture made from lecithin (Benecoat BMI-40) were used for corrigents against bitter taste. The bitter taste intensity was evaluated using volunteers by comparison of test samples with standard solutions containing quinine at various concentrations. For the tablets made of matrix base and drug, Witepsol H-15 best inhibited the bitter taste of the drug, and the bitter strength tended to be suppressed with increase in the Witepsol H-15 amount. When the inhibitory effect on the bitter taste of acetaminophen solution was compared among the corrigents, each tended to suppress the bitter taste; especially, Benecoat BMI-40 exhibited a more inhibitory effect. Further, chewable tablets were made of one matrix base and one corrigent, and of one matrix base and two kinds of corrigents, their bitter taste intensities after chewing were compared. As a result, the tablets made of Witepsol H-15/Benecoat BMI-40/sucrose, of Witepsol H-15/cocoa powder/sucrose and of Witepsol H-15/sucrose best masked the bitter taste so that they were tolerable enough to chew and swallow. The dosage forms best masking bitter taste showed good release of the drug, indicating little change in bioavailability by masking.

Acetaminophen↗
PubMed2003

Tablet surface characterisation by various imaging techniques.

The aim of this study was to characterise tablet surfaces using different imaging and roughness analytical techniques including optical microscopy, scanning electron microscopy (SEM), laser profilometry and atomic force microscopy (AFM). The test materials compressed were potassium chloride (KCl) and sodium chloride (NaCl). It was found that all methods used suggested that the KCl tablets were smoother than the NaCl tablets and higher compression pressure made the tablets smoother. Imaging methods like optical microscopy and SEM can give useful information about the roughness of the sample surface, but they do not provide quantitative information about surface roughness. Laser profilometry and AFM on the other hand provide quantitative roughness data from two different scales, laser profilometer from 1 mm and atomic force microscope from 90 microm scale. AFM is a powerful technique but other imaging and roughness measuring methods like SEM, optical microscopy and laser profilometry give valuable additional information.

Compressive Strength↗
PubMed1999

Design and characterization of a surfactant-enriched tablet formulation for oral delivery of a poorly water-soluble immunosuppressive agent.

The feasibility of incorporating significant quantities of the anionic surfactant, sodium lauryl sulfate (SDS), into an immediate release tablet formulation of a poorly water-soluble immunosuppressive agent was investigated. Despite the extremely poor compressibility of SDS and poor chemical stability of the drug, a commercializable, direct-compression tablet formulation with satisfactory mechanical properties and acceptable chemical stability was achieved. Optimal in vitro release of the drug from the tablet formulation was achieved by establishing the minimum molar uptake ratio necessary to achieve complete micellar solubilization of the drug, after which formulation studies were conducted to determine the influence of formulation and process variables on the rate and extent of drug release. A model-independent analysis of dissolution results in a reduced volume (250 ml) of modified simulated gastric fluid demonstrated that the rate and extent of drug release was highly dependent on the mean particle size of the bulk drug, but independent of compression force above that required to achieve a compact of acceptable mechanical strength. Employing the Korsmeyer-Peppas model of Fickian and non-Fickian drug release, it was further shown that release of the drug from the dosage form was governed largely by surface erosion of the surfactant-enriched tablet matrix.

Administration, Oral↗
PubMed1999

Selective drug delivery to the colon using pectin:chitosan:hydroxypropyl methylcellulose film coated tablets.

A study has been carried out to assess the potential of pectin:chitosan:hydroxypropyl methylcellulose (HPMC) (P:C:H) films for colonic drug delivery. Radiolabelled (99mTc) tablets were coated with a 3:1:1, P:C:H film and administered to human volunteers. The gastro-intestinal transit of the tablets was assessed by gamma scintigraphy. The results showed that in all cases (n=4), the tablets were able to pass through the stomach and small intestine intact. Break up of the tablets commenced once they were in the colon, due to degradation of the coat by colonic bacteria. The study has highlighted the potential of this coating system for colonic drug delivery.

Adult↗
PubMed2003

A SPME-GC procedure for monitoring peppermint flavor in tablets.

A method was developed using solid-phase microextraction (SPME) and gas chromatography to monitor the peppermint flavor loss in a taste-masked tablet formulation. This was accomplished by headspace sampling of two major components of peppermint: menthone and menthol. It was found that the excipients from the tablet produced an important matrix effect and that standard addition analysis was necessary for improved accuracy of the determination. The method was shown to be specific and precise. Furthermore, the method produced acceptable results with adequate quantitation limits to determine peppermint flavors in taste-masked tablets. The optimized extraction procedure was successfully used to monitor the stability of peppermint flavor in an oral solid formulation. The accelerated stability studies of the tablet showed that the menthone and menthol was lost in an exponential manner and levels off after several days of heat exposure.

Chromatography, Gas↗
PubMed2003

Seizure of illicitly produced para-fluorofentanyl: quantitative analysis of the content of capsules and tablets.

A gas chromatography/mass spectrometry (GC/MS) method for the quantification of para-fluorofentanyl (pFF) in powder and powdered samples was developed and validated. The method was applied on a seizure of capsules and tablets, that had been confiscated at an illicit production site in the Netherlands. The investigated capsules and tablets contained pFF in the range of 33.8-408.7 microg. As caffeine was detected as being an adulterant, a HPLC/UV method for the quantification of caffeine in capsules and tablets was also validated and applied. Caffeine was detected in the range of 25.6-108 mg per capsule or tablet. Based on an extrapolation of pharmacological and toxicological data of fentanyl, it can be argued that the highest detected single dose of pFF could be lethal, when administered orally. However, the large variability of the doses observed for pFF could mislead abusers, potentially leading to multiple doses and thus overdosing.

Caffeine↗
PubMed2003

Determination of content uniformity and distribution characteristics of an investigational drug in its tablets dosage form and granule by ICP-AES.

An investigational drug (A) in its calcium salt form has been developed as the tablet dosage form. Monitoring drug distribution and uniformity in granules and tablets during early stage formulation/process development is critical for drug product quality control and process robustness. In this report, an efficient and reliable analytical method for monitoring drug compound A uniformity and distribution has been developed by analyzing calcium, the counter ion of the drug substance, by Inductively Coupled Plasma Atomic Emission Spectrometer (ICP-AES). In this method, calcium in compound A granule and tablet samples was digested with 1 M hydrochloric acid by heating at 90 degrees C for 2 h. The resulting suspension was centrifuged, and the supernatant was directly aspirated into an ICP-AES. This method has been validated to demonstrate satisfactory precision, accuracy, specificity and sensitivity. Finally, this method has been used to analyze sieve fraction granules and tablets of drug compound A. The data generated were highly comparable to those by validated HPLC methods (UV method can not be applicable due to significant bias). In comparison with HPLC methods, this method demonstrates a significantly improved efficiency with very short analysis time (1 min per sample), and can be used as an excellent alternative for UV and HPLC methods to support formulation screening.

Drugs, Investigational↗
PubMed1999

Monitoring of a film coating process for tablets using near infrared reflectance spectrometry.

A process analytical chemical method using near infrared diffuse reflectance spectrometry was developed for the determination of the amount of tablet coating on single tablets. This method is based on calibration of the spectra versus the added mass of coating solution. The tablet core was composed of two halves of different chemical composition and spectra were recorded from both sides of the tablets. The calibration was carried out using the chemometric methods principal component analysis (PCA), partial least squares (PLS), and multiplicative signal correction (MSC). The PLS-model utilised spectra obtained from both sides, pretreated with MSC, and ordered into one object. This method can be used in process analytical chemistry at-line. Additional characterisation of the measurements was obtained by calibrating the spectra versus coating thicknesses obtained from optical microscopy. Using PCA, it was possible to roughly estimate the maximum depth in the coating material that returns chemical information, the 'information depth', which was 0.1-0.2 mm.

Analysis of Variance↗
PubMed2000

Automated sample preparation of Roxifiban tablets: transfer of a manual method to an automated workstation.

Automation offers obvious advantages for the preparation of tablets prior to analysis by HPLC including unattended operation, minimization of human intervention and an electronic audit trail. However, significant effort has to be put in up front to develop and validate an automated method, particularly if it is required to closely follow an existing manual method. Here, method transfer for Roxifiban, a fibrinogen receptor antagonist, will be discussed. A Zymark tablet processing workstation II (TPWII) was used for all automated sample preparations. Manual methods for composite assay, content uniformity, weight variation and degradation products testing of a tablet formulation were transferred to the TPWII. The method involved weighing of the sample, disintegration of the dosage form by homogenization, extraction of the analyte in the homogenate solution, filtration of the homogenate, dilution of the filtrate and transfer to autosampler vials. Obstacles to a quick transfer included limitations in the volume capabilities of the TPWII, poor analyte solubility and achieving proper conditioning of the transfer lines and filter. After resolving these issues, a validated method was achieved. Spiked recoveries were from 99.4 to 101.1% (RSD's <0.5%). A cross-validation between automated and manual assay methods was compared by Westlake analysis giving a 0.7% calculated interval at the 95% confidence level. Carryover was 0.07% after 20 sample preparations at the highest tablet strength.

Amidines↗
PubMed2002

In situ, real time observation of the disintegration of paracetamol tablets in aqueous solution by magnetic resonance imaging.

The disintegration behavior of paracetamol tablets was studied by magnetic resonance imaging (MRI) using the Snapshot FLASH method. The total time of the single experiment is 425 ms and allows the study of the disintegration process in real time. The study was carried out in vitro under acidic gastric pH conditions and may help to predict the behavior of paracetamol tablets in the stomach after oral administration. It was shown that in spite of identical conditions, the disintegration of the tablets under study was different. The distribution of protons of 4-(N-acetyl)aminophenol within the paracetamol tablet was shown to be homogeneous. The study was carried out in a non-destructive way by the SPI MRI method.

Acetaminophen↗
PubMed2002

Tablet film-coating with amylose-rich maize starch.

The purpose of the present study was to investigate an aqueous-based amylose-rich maize starch (Hylon VII) film-coating process of tablets performed by a side-vented pan coating system. Three formulation or process parameters of potential importance, including the plasticizer concentration (X(1)), the temperature of coating pan (X(2)) and the spray rate of the coating solution (X(3)), were evaluated using a central composite face-centred experimental design. Only a few process-related limitations associated with the aqueous film coating of Hylon VII were observed, and, in general, the coated tablets were of fairly good quality. At low spray rates, the temperature of the coating pan did not affect the roughness of the coated tablets. At higher spray rates, higher temperature gave smoother films. As regards surface quality and smoothness, a plasticizer concentration (i.e., a 1:1 mixture of sorbitol and glycerol) of approximately 65% of the polymer weight, seems to be suitable for the present formulations. The dissolution of all Hylon VII-coated tablets in an acidic medium was rapid, more than 75% of the drug (theophylline) dissolved within 15 min. On the basis of the present results, it can be concluded that amylose-rich maize starch (Hylon VII) may be considered as an aqueous film-coating agent to be used for pharmaceutical purposes and in established film-coating processes.

Amylose↗
PubMed2000

Development of pectin matrix tablets for colonic delivery of model drug ropivacaine.

The objective of this work was to develop pectin-based matrix tablets for colonic delivery of the model drug ropivacaine, with the future perspective of radiolabelling the system by neutron activation technique for a gamma-scintigraphic study. The aim was to investigate some formulation factors that could reduce the release of the drug in the simulated gastric and intestinal fluids, increase the release in the simulated cecal fluid (with pectinolytic enzymes) and improve the poor compactibility of pectins. For dissolution studies, the flow-through apparatus with sequential dissolution liquids simulating the mouth-to-colon conditions was used. The effect of two pectin types, the incorporation of ethylcellulose as a dry matrix-additive and water or ethanol as granulation liquids were investigated in a study designed as a D-optimal mixture. Amidated pectin (Am.P) produced harder tablets than the calcium salt of pectin (Ca.P) and was more susceptible to enzymatic degradation. Addition of ethylcellulose increased the tablet strength and the dissolution rate. Furthermore, directly compressed Am.P tablets were produced by addition of coarse or micronised qualities of ethylcellulose. The latter improved the crushing strength markedly imposing a marginal release-reducing effect. Coating this formulation with Eudragit((R)) L 100 reduced the release in the simulated upper GI conditions without interference with the subsequent enzymatic activity.

Amides↗