Oblong Tablets Research Articles

Questionnaire Study to Investigate the Preferences of Children, Parents, and Healthcare Professionals for Different Formulations of Oral Medicinal Products.

Since the acceptability of a medicine can significantly impact therapeutic outcomes, this study aimed to determine and compare the preferences of children, parents, and healthcare professionals for the most commonly used pediatric oral medicine formulations (syrup, mini-tablets, oblong tablets, round tablets) addressing all pediatric age groups, 0-<18 years (y). This survey study employed sex-, age-, and participant group-adapted questionnaires for eight cohorts of participants, i.e., children 6-<12 y, adolescents 12-<18 y, parents of children in four age groups (0-<2 y, 2-<6 y, 6-<12 y, and 12-<18 y), nurses, and pediatricians. Descriptive statistics were used for data analysis. In the age groups 0-<2 y and 2-<6 y, mini-tablets were preferred over syrup by all participants. In the age group 6-12 y, solid dosage forms were also preferred over syrup by all participants. In the age group 12-<18 y, healthcare professionals preferred solid dosage forms over syrup. Parents preferred higher amounts of mini-tablets and syrup compared to round and oblong tablets, while adolescents' preferences did not differentiate between these formulations. Based on the study results and in contrast to current practice, it is suggested to consider solid dosage forms for future age-appropriate medicinal products already for younger age groups.

Bioequivalence of Related GelShieldⓇ Sustained-release Formulations of Metformin: A Pooled Pharmacokinetic Analysis

PurposeGlucophageⓇ (Merck Healthcare KGaA, Darmstadt, Germany) is the originator brand of metformin hydrochloride, an oral antidiabetic drug. Metformin is recommended in guidelines as first-line treatment of type 2 diabetes mellitus and increasingly in related insulin-resistant conditions, such as prediabetes and polycystic ovary syndrome. The GelShieldⓇ sustained-release formulation tablet of GlucophageⓇ has been improved from the historic version marketed in 2000. Bioequivalence has been demonstrated stepwise along this evolution; however, a head-to-head evaluation between the initial and the current version is missing. This analysis aims to close this gap and to determine bioequivalence between related originator GelShieldⓇ sustained-release formulations of metformin, GlucophageⓇ (GXR 500 mg), from Europe and the United States. MethodsData from seven randomized crossover bioequivalence studies in 361 healthy participants of Asian and non-Asian ethnicity from Europe, the United States, and Asia were considered. All evaluated a single oral dose of 500 mg of the test and reference formulation in healthy male and female participants in fed and fasted state. Bioequivalence was evaluated by means of a combined bridging analysis of available data on the current round tablet from Europe (rGXR EU) and the historic oblong tablet from the United States (oGXR US) in healthy Asian and non-Asian participants under fed and fasting conditions. Bioequivalence between the two formulations was assessed statistically with a mixed effects model for AUC0-t, Cmax, and AUC0-inf. FindingsIn all studies, bioequivalence between the respective test and reference formulations of GXR was shown. Statistical analysis of pooled pharmacokinetic data of 2 (primary pooling set) or 3 studies (secondary pooling set) demonstrated bioequivalence between rGXR EU and oGXR US via bridging with oGXR EU. The 90% CI for the geometric mean ratio of all pharmacokinetic parameters was within the bioequivalence range of 0.80 to 1.25. In the primary pooling set, geometric least squares mean ratios in the fed group ranged from 0.9931 (90% CI, 0.9151–1.0778) for AUC0-inf to 1.1344 (90% CI, 1.0711–1.2014) for Cmax; results in the fasted group were similar. The secondary pooling set, which added a study in Asians, confirmed these findings. ImplicationsBioequivalence was determined between sustained-release formulations of GlucophageⓇ from Europe and the United States under fasted and fed conditions in healthy men and women, including different ethnicities. The efficacy and safety of GlucophageⓇ XR can be claimed along the evolution from oGXR US, via oGXR EU to rGXR EU, and in several ethnicities and production sites.

Validating a composite endpoint for acceptability evaluation of oral drug formulations in the pediatric population: a randomized, open-label, single dose, cross-over study.

This study aimed to validate the newly developed composite acceptability endpoint to investigate acceptability of oral pediatric drug formulations that integrates swallowability and palatability assessments. In this open-label study acceptability of oral formulations was tested in three age groups (1-<6months, 6-<12years, and 12-<18years) with a 2-way cross-over design in children aged 1-<6months (syrup and mini-tablets), and with an incomplete block design of four sequences with three out of four formulations (syrup, mini-tablets, oblong tablet, and round tablet) each in children aged 6-<18years. The primary endpoint was acceptability derived from the composite acceptability endpoint. Secondary endpoints were palatability and acceptability derived from swallowability. A total of 320 children were stratified into three age groups (80 children aged 1-<6months, 120 children aged 6-<12years, and 120 children aged 12-<18years). All participants completed the study. Age-specific differences were observed in acceptability derived from the composite acceptability endpoint. Mini-tablets had the highest acceptability in participants aged 1-<6months and 6-<12years while the oblong tablet was leading in adolescent participants (12-<18years). This study demonstrated that the composite acceptability endpoint method integrating both swallowability and palatability assessments is a sensitive method to assess acceptability of drug formulations in children of different age. https://drks.de/search/de, identifier DRKS00027948.

The application of Near-Infrared Spatially Resolved Spectroscopy in scope of achieving continuous real-time quality monitoring and control of tablets with challenging dimensions

In scope of achieving real-time release of tablets, quality attributes need to be monitored and controlled through Process Analytical Technology tools such as near-infrared spectroscopy (NIRS). The authors evaluated the suitability of NIR-Spatially Resolved Spectroscopy (NIR-SRS) for continuous real-time monitoring and control of content uniformity, hardness and homogeneity of tablets with challenging dimensions. A novel user-friendly research and development inspection unit was used as standalone equipment for the analysis of small oblong tablets with deep-cut break lines. A total of 66 tablets varying in hardness and Active Pharmaceutical Ingredient (API) content were inspected, with each tablet being analysed five times and measurements repeated on three different days. Partial Least Squares (PLS) models were developed to assess content uniformity and hardness, of which the former showed higher accuracy. The authors attempted to visualize tablet homogeneity through NIR-SRS spectra by regressing all spectra obtained during a single measurement using a content uniformity PLS model. The NIR-SRS probe demonstrated its potential towards real-time release testing through its ability to quickly monitor content uniformity, hardness and visualize homogeneity, even for tablets with challenging dimensions.

Itraconazole Amorphous Solid Dispersion Tablets: Formulation and Compaction Process Optimization Using Quality by Design Principles and Tools.

BCS Class II drugs, such as itraconazole (ITZ), exhibit poor solubility (1-4 ng/mL) and so require solubility enhancement. Therefore, ITZ and Kollidon® VA64 (KOL) amorphous solid dispersions (ASDs) were produced using hot-melt extrusion (HME) to improve ITZ's poor solubility. A novel strategy for tablet formulations using five inorganic salts was investigated (KCl, NaCl, KBr, KHCO3 and KH2PO4). These kosmotopric salts are thought to compete for water hydration near the polymer chain, hence, preventing polymer gelation and, therefore, facilitating disintegration and dissolution. Out of all the formulations, the KCl containing one demonstrated acceptable tensile strength (above 1.7 MPa), whilst providing a quick disintegration time (less than 15 min) and so was selected for further formulation development through a design of the experiment approach. Seven ITZ-KOL-ASD formulations with KCl were compacted using round and oblong punches. Round tablets were found to disintegrate under 20 min, whereas oblong tablets disintegrated within 10 min. The round tablets achieved over 80% ITZ release within 15 min, with six out of seven formulations achieving 100% ITZ release by 30 min. It was found that tablets comprising high levels of Avicel® pH 102 (30%) and low levels of KCl (5%) tend to fail the disintegration target due to the strong bonding capacity of Avicel® pH 102. The disintegration time and tensile strength responses were modeled to obtain design spaces (DSs) relevant to both round and oblong tablets. Within the DS, several formulations can be chosen, which meet the Quality Target Product Profile (QTPP) requirements for immediate-release round and oblong tablets and allow for flexibility to compact in different tablet shape to accommodate patients' needs. It was concluded that the use of inorganic salts, such as KCl, is the key to producing tablets of ITZ ASDs with fast disintegration and enhanced dissolution. Overall, ITZ-KOL-ASD tablet formulations, which meet the QTPP, were achieved in this study with the aid of Quality by Design (QbD) principles for formulation and compaction process development and optimization.

A Composite Endpoint for Acceptability Evaluation of Oral Drug Formulations in the Pediatric Population

IntroductionA medicine’s acceptability is likely to have significant impact on pediatric adherence. The importance is underlined in EMA and FDA guidance on this topic where investigation of acceptability is stated as a regulatory expectation. Demonstrating acceptability can be challenging given there is no globally recognized definition and no standardized testing methodology or assessment criteria. Palatability and swallowability are generally recognized as important elements of acceptability, and this work proposes a definition of acceptability using these elements to give a composite endpoint for acceptability for pediatric subjects across all age ranges.MethodsThis composite acceptability endpoint is based on validated assessment methods for swallowability and palatability in children of different age groups using different galenic placebo formulations, in line with criteria proposed by EMA for assessing acceptability in children from newborn to 18 years of age. Data from two studies investigating mini-tablets, oblong tablets, orodispersible films, and syrup were analyzed to establish the validity, expediency, and applicability of the suggested composite acceptability assessment tool.ResultsThe new composite endpoint is an efficient and suitable way to distinguish preferences of oral formulations: Mini-tablets and oblong tablets had significantly better acceptability than syrups and orodispersible films.ConclusionSince the suggested acceptability criteria takes both swallowability and palatability into account as composite endpoint, it is highly sensitive to detect acceptability differences between oral formulations. It is a well-defined valid approach, which meets regulatory requirements in an appropriate and comprehensive manner and may in future serve as a pragmatic, standardized method to assess and compare acceptability of pediatric formulations with active substances.

Blind-Watermarking-Proof-of-Concept of a Novel Approach to Ensure Batch Traceability for 3D Printed Tablets.

Falsified medicines are a major issue and a threat around the world. Various approaches are currently being investigated to mitigate the threat. In this study, a concept is tested that encodes binary digits (bits) on the surface of Fused Deposition Modelling (FDM) 3D printed geometries. All that is needed is a computer, a FDM 3D printer and a paper scanner for detection. For the experiments, eleven different formulations were tested, covering the most used polymers for 3D printing in pharma: Ethylene-vinyl acetate (EVA), polyvinyl alcohol (PVA), polylactic acid (PLA), Hypromellose (HPMC), ethyl cellulose (EC), basic butylated-methacrylate-copolymer (EPO), and ammonio-methacrylate-copolymer type A (ERL). In addition, the scanning process and printing process were evaluated. It was possible to print up to 32 bits per side on oblong shaped tablets corresponding to the dimensions of market preparations of oblong tablets and capsules. Not all polymers or polymer blends were suitable for this method. Only PVA, PLA, EC, EC+HPMC, and EPO allowed the detection of bits with the scanner. EVA and ERL had too much surface roughness, too low viscosity, and cooled down too slowly preventing the detection of bits. It was observed that the addition of a colorant or active pharmaceutical ingredient (API) could facilitate the detection process. Thus, the process could be transferred for 3D printed pharmaceuticals, but further improvement is necessary to increase robustness and allow use for more materials.

Influence of the geometry of 3D printed solid oral dosage forms on their swallowability

3D printing can be used to realise a wide variety of geometries of oral dosage forms. In this work, the swallowability of 3D-printed dosage forms with comparable size and different shape using fused deposition modelling (FDM) from isomalt was investigated in a controlled, randomised crossover study design. To produce the required number of dosage forms, a commercial 3D printer was modified with regard to product safety and production time. The modifications carried out permit the printing of 4 pharmaceutical forms simultaneously as well as the printing of rigid filaments.Six 3D-printed placebo objects and two compressed placebo reference objects were tested by 12 subjects in a blinded design. A questionnaire was used to assess swallowability, foreign body sensation at the moment of swallowing, persistent foreign body sensation after swallowing and pain after swallowing. Furthermore, the amount of additional water drunk after administration was documented. With the modified printer, the required 576 test objects could be printed within a few days with good reproducibility. In all questions, the best results were obtained for the printed and compressed oblong tablets, followed by the printed and compressed round tablets, the football and the sphere. The worst results were obtained for the pyramid closely followed by the cuboctahedron. The study shows that the variety of shapes of oral dosage forms made possible by 3D printing needs to be tested in swallowability studies, as not every shape is also easy to swallow.

Acceptability of small-sized oblong tablets in comparison to syrup and mini-tablets in infants and toddlers: A randomized controlled trial

ObjectiveThere is limited evidence for the acceptability of various drug formulations holding the potential to improve medicines administration to children. Suitable formulations need to meet the requirements of pediatric patients. Previous studies have demonstrated the acceptance of mini-tablets. Oblong tablets may carry more active ingredient content per unit than mini-tablets and could be an important alternative when the drug substance requires administration of higher doses.The primary objective was to demonstrate non-inferiority of acceptability of oblong tablets in comparison to 3 ml glucose syrup in children aged 1 to 5 years. Secondary objectives were investigation of acceptability, swallowability and palatability of mini-tablets, oblong tablets and glucose syrup in children between 1 and 5 years. MethodsAn open, randomized, single dose two-way cross-over design in two parallel study arms was applied. 280 children were stratified to one of five age groups and randomized to receiving one oblong tablet (2.5 × 6 mm) in comparison either to 3 ml glucose syrup or to three mini-tablets (2 × 2 mm). Acceptability and swallowability were assessed according to pre-defined evaluation criteria. The application of the formulations was video documented to evaluate the palatability. ResultsAs primary objective, non-inferiority was observed regarding acceptability of the oblong tablet compared to syrup in all age groups (84.4% vs 80.1%, difference 4,29% points with 95% CI of −3.00%,11.57%). For swallowability, superiority of the oblong tablet compared to syrup could be shown (74.5% vs. 53.2%, difference 21.26% points, 95% CI of 11.29%, 31.23%). Regarding palatability, <10% of children demonstrated unpleasant reaction after intake of the oblong tablet or mini-tablets as graded by both raters, however, in contrast up to 40% of children after intake of syrup. ConclusionOblong tablets are a promising, safe alternative to liquid drug formulations and administration of multiple mini-tablets in children.

Formulation & assessment of combined antibiotics in a floating oblong tablet for treatment of H. pylori: (A) Radiological imaging to prove the floating of a high-weight oblong tablet

The floating drug delivery system (FDDS) is considered as a renewable technique in the pharmaceutical technology because the dreams of increasing the stomach residence time for local or systemic effect are continuously actual for different purposes. It was studied for small weight tablet, but it is not clearly studied for the high weight tablet which may be essential for high dose drugs or when combined drugs are needed. Sodium bicarbonate was only used as a gas generating agent to give the chance to increase the weight of the drugs. Factorial experimental design was utilized to statistically analyze factors affecting tablet buoyancy. The results showed that, all factors studied and their interactions have significant effect on the buoyancy lag time. The addition method of gas generating agent has the most significant effect on the buoyancy process regardless of concentration of sodium bicarbonate used. That is due to the gas generation process is an in-organic interaction between the moieties of strong acid normally present in the stomach and the base added to the tablet during formulation. F4 is selected as an optimum formula that achieves the lowest floating lag time (7 s) through intragranular addition of gas generating agent at the highest concentration for in-vivo radiological imaging. In-vivo study in mature human gastrointestinal tract shows that the gastric residence time has extended to 4 h after swallowing the optimum floated high weight tablet at 2 h after meal. Therefore, it is advisable that, such tablet formula should be administered after standard calorific meal since such meal delays the stomach evacuation.

MAPPING THE THREE-DIMENSIONAL “X-SHAPED STRUCTURE” IN MODELS OF THE GALACTIC BULGE

Numerical simulations have shown that the X-shaped structure in the Milky Way bulge can naturally arise from the bar instability and buckling instability. To understand the influence of the buckling amplitude on the morphology of the X-shape, we analyze three self-consistent numerical simulations of barred galaxies with different buckling amplitudes (strong, intermediate and weak). We derive the three-dimensional density with an adaptive kernel smoothing technique. The face-on iso-density surfaces are all elliptical, while in the edge-on view, the morphology of buckled bars transitions with increasing radius, from a central boxy core to a peanut bulge and then to an extended thin bar. Based on these iso-density surfaces at different density levels, we find no clear evidence for a well-defined structure shaped like a letter X. The X-shaped structure is more peanut-like, whose visual perception is probably enhanced by the pinched inner concave iso-density contours. The peanut bulge can reproduce qualitatively the observed bimodal distributions which were used as evidence for the discovery of the X-shape. The central boxy core is shaped like an oblong tablet, extending to $\sim$ 500 pc above and below the Galactic plane ($|b| \sim 4^\circ$). From the solar perspective, lines of sight passing through the central boxy core do not show bimodal distributions. This generally agrees with the observations that the double peaks merge at $|b| \sim 4^\circ - 5^\circ$ from the Galactic plane, indicating the presence of a possibly similar structure in the Galactic bulge.

Swallowing Tablets and Capsules Increases the Risk of Penetration and Aspiration in Patients with Stroke-Induced Dysphagia.

We evaluated the prevalence of difficulties swallowing solid dosage forms in patients with stroke-induced dysphagia and whether swallowing tablets/capsules increases their risk of penetration and aspiration. Concurrently, we explored whether routinely performed assessment tests help identify patients at risk. Using video endoscopy, we evaluated how 52 patients swallowed four different placebos (round, oval, and oblong tablets and a capsule) with texture-modified water (TMW, pudding consistency) and milk and rated their swallowing performance according to the Penetration Aspiration Scale (PAS). Additionally, Daniels Test, Bogenhausener Dysphagiescore, Scandinavian Stroke Scale, Barthel Index, and Tinetti's Mobility Test were conducted. A substantial proportion of the patients experienced severe difficulties swallowing solid oral dosage forms (TMW: 40.4 %, milk: 43.5 %). Compared to the administration of TMW/milk alone, the placebos increased the PAS values in the majority of the patients (TMW: median PAS from 1.5 to 2.0; milk: median PAS from 1.5 to 2.5, each p value <0.0001) and residue values were significantly higher (p < 0.05). Whereas video-endoscopic examination reliably identified patients with difficulties swallowing medication, neither patients' self-evaluation nor one of the routinely performed bedside tests did. Therefore, before video-endoscopic evaluation, many drugs were modified unnecessarily and 20.8 % of these were crushed inadequately, although switching to another dosage form or drug would have been possible. Hence, safety and effectiveness of swallowing tablets and capsules should be evaluated routinely in video-endoscopic examinations, tablets/capsules should rather be provided with TMW than with milk, and the appropriateness of "non per os except medication" orders for dysphagic stroke patients should be questioned.

Expectations of medicine adverse effects: Perceptual characteristics of tablets and personality background

The possible roles of perceptual characteristics (colour, shape, size) of tablets and personality characteristics in generating expectations of drug side effects were investigated. Two hundred and thirteen hospitalized patients (mean age 48.9 ± 18.84 years) completed questionnaires (trait anxiety — STAI-T, dispositional optimism — LOT-R, subjective somatic symptoms — PHQ-15, somatosensory amplification — SSAS, previous personal and family-level experiences) and the expected probabilities of nine side effects for six differently looking tablets were estimated. PHQ-15, SSAS and family-level experience scores were significant predictors of the expectations of side effects. Red tablets evoked significantly more stimulating type expectations than did white pills. Expected gastrointestinal side effects were associated with oblong-shaped tablets. Regarding headache, medium-sized round tablet was expected to evoke fewer side effects than the small round and the oblong tablets. Although expectations do not always manifest themselves as actual symptoms, they can reduce the overall effectiveness of a therapy by influencing patient's adherence.

Effect of disintegrants on the properties of multiparticulate tablets comprising starch pellets and excipient granules

A design of experiments (DOE) approach (2-level full factorial design) was used to investigate the effect of several formulation and process variables on the properties of fast disintegrating tablets comprising starch-based pellets and excipient granules and to optimize and validate the design space. The percentage of starch pellets (30–50%, w/w), type of disintegrants (Ac-di-sol, Explotab, Polyplasdone), percentage of external disintegrant (4–8%, w/w) and compression force (5–15 kN) were the evaluated factors (24 runs + 9 centre points = 33 experiments), while tablet hardness, friability and disintegration time were the studied tablet properties (responses). Starch pellets were prepared by extrusion–spheronisation. Excipient granules containing microcrystalline cellulose, lactose, internal disintegrant (8%) and polyvinylpyrrolidone K-30 (4%) were prepared by wet granulation. Pellets, granules (700–1000 μm) and external disintegrant were mixed and compressed into oblong tablets (17.1 mm long, 8.2 mm wide). Evaluation of the effects calculated from the DOE results showed that a lower concentration of starch pellets and higher compression force were required to yield tablets with a high hardness, a low friability (<1%) and short disintegration time (<3 min). Polyplasdone granules had the lowest porosity and friability which was reflected in the DOE study, where the Polyplasdone-containing tablets were harder, less friable and disintegrated faster compared to Ac-di-sol and Explotab-containing tablets. Monte carlo simulations at the optimal factor settings (30% starch pellets, 4% Polyplasdone and 10 kN compression force) indicated that a robust system was formed as the probability to exceed the limits was low for all responses. Validation of the design space (at optimal settings) showed that the results predicted via the DOE models correlated well with the observed experimental data.

Prediction of the Ease of Subdivision of Scored Tablets from Their Physical Parameters

At present, the ease of subdivision of scored tablets is estimated in vivo. In order to replace such in vivo testing and to develop a surrogate test which uses in vitro techniques, the association between physical parameters of scored tablets and their ease of subdivision was studied. The physical properties of 23 brands of scored tablets of which their ease of subdivision in vivo was known were established. Statistical modeling using a logistic regression model was used to fit the data and estimate the contribution of each physical parameter to the goodness of the fit. For scored oblong tablets, the critical parameters for their ease of subdivision are: diameter; diameter/width ratio; depth of score line and resistance to crushing. Criteria for each of these parameters were derived. All criteria need to be complied with to guarantee sufficient ease of subdivision of scored oblong tablets. For scored round tablets the critical parameters, in decreasing order of importance, for their ease of subdivision, are: resistance to crushing, diameter, score mark (one- or two-sided), and shape (flat or biconvex). A five-parameter predictive model was developed, showing excellent discrimination. For development, the proposed surrogate tests are sufficiently reliable. For release testing and stability studies, resistance to crushing of a scored tablet is a reliable predictor of its ease of subdivision.

Expectations evoked by perceptual characteristics of tablets and their personality background

Event Abstract Back to Event Expectations evoked by perceptual characteristics of tablets and their personality background Ferenc Köteles1*, Adrienn Tóth1 and György Bárdos2 1 Eötvös Loránd University, Department of Personality and Health Psychology, Hungary 2 Eötvös Loránd University, Department of Physiology and Neurobiology and Institute of Health Promotion and Sport Sciences, Hungary The possible role of perceptual characteristics (colour, shape, size) of tablets and of some personality characteristics in the generation of expectations of adverse drug side effects were investigated in this questionnaire study. 213 hospitalized patients (mean age 48,9±18,84 ys) completed questionnaires (trait anxiety - STAI-T, dispositional optimism - LOT-R, subjective somatic symptoms - PHQ-15, somatosensory amplification - SSAS, previous personal and family-level experiences with side effects) and estimated the probability of the occurance of nine side effects in the case of six differently looking tablets. As for personality traits, SSAS and family-level experiences proved to be significant predictors of the expectations of side effects in the regression analysis. Red tablets evoked significantly more stimulating expectations (agitation, palpitation, hypertension) than did white tablets. Expectations of gastrointestinal side effects (diarrhea, nausea, heartburn) were associated with oblong shaped tablets. Regarding headache, medium size round tablets were expected to evoke less side effects than the small round or the oblong tablets. We conclude that expectations of adverse drug effects are quantitatively associated with some personality characteristics whereas perceptual characteristics of drugs influence the direction of expectations. Although expectations might or might not manifest themselves as actual symptoms, they can reduce the overall effectiveness of a therapy by influencing patient's adherence. Conference: IBRO International Workshop 2010, Pécs, Hungary, 21 Jan - 23 Jan, 2010. Presentation Type: Poster Presentation Topic: Cognition and behavior Citation: Köteles F, Tóth A and Bárdos G (2010). Expectations evoked by perceptual characteristics of tablets and their personality background. Front. Neurosci. Conference Abstract: IBRO International Workshop 2010. doi: 10.3389/conf.fnins.2010.10.00164 Copyright: The abstracts in this collection have not been subject to any Frontiers peer review or checks, and are not endorsed by Frontiers. They are made available through the Frontiers publishing platform as a service to conference organizers and presenters. The copyright in the individual abstracts is owned by the author of each abstract or his/her employer unless otherwise stated. Each abstract, as well as the collection of abstracts, are published under a Creative Commons CC-BY 4.0 (attribution) licence (https://creativecommons.org/licenses/by/4.0/) and may thus be reproduced, translated, adapted and be the subject of derivative works provided the authors and Frontiers are attributed. For Frontiers’ terms and conditions please see https://www.frontiersin.org/legal/terms-and-conditions. Received: 30 Apr 2010; Published Online: 30 Apr 2010. * Correspondence: Ferenc Köteles, Eötvös Loránd University, Department of Personality and Health Psychology, Budapest, Hungary, fecuska@gmail.com Login Required This action requires you to be registered with Frontiers and logged in. To register or login click here. Abstract Info Abstract The Authors in Frontiers Ferenc Köteles Adrienn Tóth György Bárdos Google Ferenc Köteles Adrienn Tóth György Bárdos Google Scholar Ferenc Köteles Adrienn Tóth György Bárdos PubMed Ferenc Köteles Adrienn Tóth György Bárdos Related Article in Frontiers Google Scholar PubMed Abstract Close Back to top Javascript is disabled. Please enable Javascript in your browser settings in order to see all the content on this page.

Granulation by Roller Compaction and Enteric Coated Tablet Formulation of the Extract of the Seeds of Glinus Lotoides Loaded on Aeroperl® 300 Pharma

The purpose of this research was to improve the hygroscopicity and poor flow properties of the crude dry extract of the seeds of Glinus lotoides and improve the disintegration time of the core-tablets for enteric coated formulation thereof. The liquid crude extract of the plant was adsorbed on granulated colloidal silicon dioxide (Aeroperl 300 Pharma) at 30% w/w and the dry extract preparation (DEP) was dry-granulated with roller-compaction using Micro-Pactor. Hygroscopicity, flow property and disintegration time were improved significantly due to the adsorption and granulation processes. Moreover, the DEP does not become mucilaginous even at higher relative humidity levels (above 65%). Oblong tablets (20 x 8.25 mm) containing 947 mg of the granulated DEP (equivalent to the traditional dose), 363 mg of Avicel PH101 and 90 mg of Ac-di-Sol as disintegrant were formulated using an instrumented eccentric tablet machine at 20 kN. The tablets showed a crushing strength of 195 N, a friability of 0.4% and disintegrated within 9 min. The tablets were then enteric coated using polymethacrylate co-polymers (Eudragit L 100-55 and Kollicoat MAE 100P). The coated tablets resisted disintegration or softening in simulated gastric fluid for a minimum of 2 h and disintegrated within 15 min in intestine simulated fluid at pH 6.8. In addition to controlling the release of the active agents, the enteric coating improved the strength and decreased friability of the core-tablets.

Compressed collagen sponges as gastroretentive dosage forms: In vitro and in vivo studies

The objective of the present investigations was to develop oblong tablets which expand after contact with gastrointestinal fluids within a few minutes to a length of 4–6 cm and which should remain in the stomach for a prolonged period of time due to their size. The tablets were prepared from riboflavin-containing collagen sponges using a computer controlled single punch tablet machine. The collagen material was compressed to oblong tablets with dimensions of 3.5 mm × 9 mm × 18 mm. In vitro investigations were carried out to characterise drug release. The model drug riboflavin was released from the collagen tablets over 12 h. The gastrointestinal retention time of the new dosage form was indirectly estimated by determining the duration of riboflavin excretion after oral intake of the tablet. A crossover in vivo study with 12 healthy male and female subjects was performed. The renal excretion of riboflavin was measured after oral administration of collagen tablets and small sustained release hydrocolloid tablets as reference preparation. The amount of riboflavin excreted into the urine was enhanced after administration of the expanding collagen tablets in comparison with the hydrocolloid tablets. The differences were statistically significant after 5, 6, 8, 9, 10 and 12 h.

A near-infrared reflectance analysis method for the noninvasive identification of film-coated and non-film-coated, blister-packed tablets

A non-invasive near-infrared reflectance analysis (NIRA) method has been developed to confirm the identity of blister-packed, film-coated and non film-coated tablets for clinical trial supplies. NIR spectra of the tablets were measured through the blister pack plastic using a fiber optic probe. The blister packs contained 18 cells which held pink, pentagonal tablets or film-coated, white, oblong tablets. The pink tablets contained about 80% w w of a marketed drug as a clinical comparator or were matching placebos. The white film-coated tablets contained about 60% w w of an experimental drug, about 75% w w of a marketed drug as a clinical comparator, or were matching placebos. Pattern recognition methods were developed to identify tablets in the blister pack by using libraries of second derivative NIR spectra of each tablet-type. Three chemometric methods were used, the wavelength distance method, SIMCA residual variance method, and Mahalanobis distance method. The methods were tested with full spectra (1100–2350 nm) and three subset wavelength ranges. Several of the methods reported here reliably discriminate between film-coated and non film-coated tablets, and between active and placebo tablets. Library validation and test set data are presented along with a discussion of the advantages and disadvantages of selecting subset wavelength regions.

Evaluation of the strength of a scored oblong tablet.

Evaluation of the strength of a scored oblong tablet.