Biomedical subjects

Osmo Antikainen

Publications and source records attributed to Osmo Antikainen.

9 recordsLinked to original sources

PubMed2005

Physical solid-state properties and dissolution of sustained-release matrices of polyvinylacetate.

Solid-state compatibility and in vitro dissolution of direct-compressed sustained-release matrices of polyvinylacetate (PVAc) and polyvinylpyrrolidone (PVP) containing ibuprofen as a model drug were studied. Polyvinylalcohol (PVA) was used as an alternative water-soluble polymer to PVP. Differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD) were used for characterizing solid-state polymer-polymer and drug-polymer interactions. The mechanical treatment for preparing physical mixtures of polyvinyl polymers and the drug (i.e. simple blending or stressed cogrinding) was shown not to affect the physical state of the drug and the polymers. With the drug-polymer mixtures the endothermic effect due to drug melting was always evident, but a considerable modification of the melting point of the drug in physical binary mixtures (drug:PVP) was observed, suggesting some interaction between the two. On the other hand, the lack of a significant shift of the melting endothermic peak of the drug in physical tertiary drug-polymer mixtures revealed no evidence of solid-state interaction between the drug and the present polymers. Sustained-release dissolution profiles were achieved from the direct-compressed matrices made from powder mixtures of the drug and PVAc combined with PVP, and the proportion of PVAc in the mixture clearly altered the drug release profiles in vitro. The drug release from the present matrix systems is controlled by both diffusion of the drug through the hydrate matrix and the erosion of the matrix itself.

Calorimetry, Differential Scanning↗

PubMed2004

Formation and characterization of three-component-sorbitan monoester surfactant, oil and water-creams.

The effect of molecular structure of four sorbitan monoester surfactants (sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate and sorbitan monooleate) on the formation of simple three-component creams is presented. Interfacial properties of the surfactants were determined using a du Nouy tensiometer and rheological properties of selected creams with oscillation stress sweep, creep recovery and viscosity tests. Depending on the composition, sorbitan monolaurate and sorbitan monooleate formed both o/w creams and w/o creams, while sorbitan monopalmitate and sorbitan monostearate formed only o/w creams. Sorbitan monostearate and sorbitan monopalmitate had the smallest cmc and A(cmc) values and they were the most effective surfactants in lowering the interfacial tension. These surfactants formed the most stable and elastic creams with clear linear viscoelastic regions and small compliance values. Sorbitan monolaurate and sorbitan monooleate formed viscous creams without elastic properties.

Drug Compounding↗

PubMed2004

New perspectives for visual characterization of pharmaceutical solids.

The utilization of descriptive image information in pharmaceutical powder technology is rather limited. Consequently, the development of this discipline is a challenge within physical characterization of pharmaceutical solids. The aim of this study was to develop and evaluate an inventive visual characterization approach for monitoring the granule growth in a fluidized-bed granulation process and to use the generated image information in the prediction of tabletting behavior of granules. Surface images of samples from 34 granulations were continuously captured during the spraying and drying phases of the process and particle size distributions were determined. The gray scale difference matrix (GSDM) was derived from two surface images taken in controlled illumination conditions. The particle size calculation from the surface images was based on a multivariate Partial Least Square (PLS) model between the GSDM and sieve analysis measurements. The image information of the end-point samples was also evaluated with respect to tabletting behavior of the granules produced. Principal component analysis (PCA) was used for data visualization. The introduced approach was suitable in particle size measurements of granules during all process phases and in the monitoring of different kinds of granule growth behavior. The visual inspection of the granule samples was powerful, enabling representational batch-to-batch comparisons. The tabletting behavior of the granules could be predicted directly from particle size information generated from the surface images. PCA as a projection method was efficient in data visualization. Development of process analytical technologies (PAT) aims at improving the efficiency of processes. The presented visual characterization approach can be an effective process analytical tool in particle size analysis also enabling the evaluation of the further product quality in the end of the granulation process. The idea of characterization of bulk surface images opens new perspectives for characterization of pharmaceutical solids.

Particle Size↗

PubMed2003

A new method to predict flowability using a microscale fluid bed.

The purpose of this research was to develop a new method to predict the flow behavior of pharmaceutical powders using a multichamber microscale fluid bed. Different amounts of poorly flowing paracetamol were added to various grades of microcrystalline celluloses and silicified microcrystalline cellulose powders. Magnesium stearate was used as a lubricant. Experimental minimum fluidization velocities (u(mf)) were defined using 2 to 4 g (equal to 10 mL) of material (Video 1). The reference flowability of the powders was determined using a specific flow meter. Also, the weight variation of the compressed powders, using a single-punch press, was measured. When the amount of paracetamol in the excipients was increased, the experimental umf increased and the fluidization behavior grew worse (Video 2). Principal component analysis (PCA) established that the pressure difference over the bed as a function of fluidization velocity could be used to characterize the behavior of powders. The increase in poor fluidization behavior of the powders was in accordance with the increasing amount of paracetamol and with the increasing weight variation of the tablets. Furthermore, the angle of repose and the flow rate of silicified microcrystalline cellulose powders were predicted using a partial least squares (PLS) model. The developed method to predict flowability is a promising approach for use in the preformulation and formulation stages of new drug candidates, for example.

Acetaminophen↗

PubMed2003

Characterization of particle sizes in bulk pharmaceutical solids using digital image information.

The purpose of this study was to demonstrate a novel method of extracting relevant information from undispersed bulk powder surfaces to be used in particle size analysis. A new surface imaging approach for undispersed powders combined with multivariate modeling was used. Digital surface images of various granule batches were captured using an inventive optical setup in controlled illumination conditions. A descriptor, the gray scale difference matrix (GSDM), which describes the particle size of granular material was generated and extracted from the powder surface image information. Partial least squares (PLS) modeling was used to create a model between the GSDM and the particle size distribution of granules measured with sieving. The use of lateral illumination and the combining of information from 2 surface images strengthened the shading effects on the powder surfaces. The shading effects exposed the topography or the visual texture of the powder surfaces. This textural information was efficiently extracted using the GSDM descriptor. The goodness-of-fit (R2) for the created PLS model was 0.91 and the predicted variation (Q2) was 0.87, indicating a good model. The model covered granule sizes in the size range of approximately 20 to 2500 microm. The extracted descriptor was effectively used in particle size measurement. This study confirms that digital images taken from undispersed bulk powder surfaces contain substantial information needed for particle size distribution analysis. The use of the GSDM enabled the utilization of bulk powder surface information and provided a fast method for particle size measurement.

Chemistry, Pharmaceutical↗

PubMed2003

Determining the compression behaviour of pharmaceutical powders from the force-distance compression profile.

The force-displacement curves obtained from an eccentric tablet machine were examined in a new way. The tendency of the material for plastic deformation, fragmentation and elasticity is expressed as numerical values, which are comparable between different materials. The dependence of these numerical values on the compression pressure was modelled. The accuracy of the displacement measurement was improved by filtering out noise from the measurement data by a novel method. The plastic deformation of the material near the force maximum of the compression cycle could be seen accurately from this precise displacement data. The elastic deformation of the tablet machine was also defined very precisely from the running machine. Tablets were made with an eccentric tablet machine using fixed lower and upper punch adjustments. This ensured that the speed of the upper punch and the theoretical height of the tablets were the same for all compactions. Therefore, only the properties of the materials determined the differences in the shape of the compression curves. The test materials used were alpha-lactose monohydrate, two grades of microcrystalline cellulose, maize starch and dicalcium phosphate dihydrate. The results showed that the use of accurate displacement measurement is essential in order, to see the small variations in the shape of the force-displacement curve near the force maximum of the compression cycle, and it made it possible to dynamically calibrate the elastic deformation of the eccentric tablet machine during compression. It turned out that the numerical values obtained with the new method described the plastic, brittle and elastic properties of the tested materials satisfactorily in a wide compression pressure range.

Compressive Strength↗

PubMed2003

A novel amylose corn-starch dispersion as an aqueous film coating for tablets.

A novel aqueous coating dispersion of amylose-rich corn starch (Hylon VII) was evaluated in an aqueous film-coating process of tablets using an instrumented laboratory-scale pan-coating apparatus. The influence of two independent process variables, the coating temperature and the atomizing air pressure, on the properties of the coated tablets were investigated. The preuse stability of aqueous coating dispersion (i.e., amylose corn-starch precipitate) was studied using a powder X-ray diffraction (XRD) technique. The crystallinity of amylose starch in the coating dispersion was found to increase slightly during 9 months of storage (in a refrigerator 6 +/- 2 degrees C). The film coatings of an aqueous amylose-rich starch dispersion were successfully applied onto tablets without any significant drawbacks, such as nozzle blockage or related problems. It was found that the temperature in the coating pan had a significant influence on the film surface roughness, mechanical strength, and drug release in vitro. When the lowest coating temperature (30 degrees C) was used, rougher film coatings were obtained due to overwetting. At higher temperatures (up to 50-60 degrees C), lower surface roughness and higher mechanical strength values for the coated tablets were obtained. With the present amylose starch dispersion, the atomizing air pressure had a minor influence on the quality of the coating. Under appropriate coating conditions, a smooth tablet film coating was produced with this new, natural, and inexpensive amylose starch dispersion.

Amylose↗

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↗

PubMed2002

Does a powder surface contain all necessary information for particle size distribution analysis?

The aim of this study was to utilise a new approach where digital image information is used in the characterisation of particle size distributions of a large set of pharmaceutical powders. A novel optical set-up was employed to create images and calculate a stereometric parameter from the digital images of powder surfaces. Analysis was made of 40 granule batches with varying particle sizes and compositions prepared with fluidised bed granulation. The extracted digital image information was then connected to particle size using multivariate modelling. The modelled particle size distributions were compared to particle size determinations with sieve analysis and laser diffraction. The results revealed that the created models corresponded well with the particle size distributions measured with sieve analysis and laser diffraction. This study shows that digital images taken from powder surfaces contain all necessary data that is needed for particle size distribution analysis. To obtain this information from images careful consideration has to be given on the imaging conditions. In conclusion, the results of this study suggest that the new approach is a powerful means of analysis in particle size determination. The method is fast, the sample size needed is very small and the technique enables non-destructive analysis of samples. The method is suitable in the particle size range of approximately 20-1500 microm. However, further investigations with a broad range of powders have to be made to obtain information of the possibilities and limitations of the introduced method in powder characterisation.

Particle Size↗