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Lactose Monohydrate (lactose + monohydrate)
Selected AbstractsCrystallization Kinetics and X-ray Diffraction of Crystals Formed in Amorphous Lactose, Trehalose, and Lactose/Trehalose MixturesJOURNAL OF FOOD SCIENCE, Issue 5 2005Song Miao ABSTRACT: Effects of storage time and relative humidity on crystallization kinetics and crystal forms produced from freeze-dried amorphous lactose, trehalose, and a lactose/trehalose mixture were compared. Samples were exposed to 4 different relative water vapor pressure (RVP) (44.1%, 54.5%, 65.6%, 76.1%) environments at room temperature. Crystallization was observed from time-dependent loss of sorbed water and increasing intensities of peaks in X-ray diffraction patterns. The rate of crystallization increased with increasing storage humidity. Lactose crystallized as ,-lactose monohydrate, ,-anhydrous, and anhydrous forms of ,- and ,-lactose in molar ratios of 5:3 and 4:1 in lactose and lactose/trehalose systems. Trehalose seemed to crystallize as a mixture of trehalose dihydrate and anhydrate in trehalose and lactose/trehalose systems. The crystal forms in a mixture of lactose and trehalose did not seem to be affected by the component sugars, but crystallization of the component sugars was delayed. Time-dependent crystallization of lactose and trehalose in the lactose-trehalose mixture could be modeled using the Avrami equation. The results indicated that crystallization data are important in modeling of crystallization phenomena and predicting stability of lactose and trehalose-containing food and pharmaceutical materials. Keywords: crystallization, lactose, trehalose, crystal form, X-ray diffraction [source] Evaluation of a rotary tablet press simulator as a tool for the characterization of compaction properties of pharmaceutical productsJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 6 2010F. Michaut Abstract The Stylcam 100R, a rotary press simulator, was designed to simulate speed profiles of rotary tablet presses. Such a simulator was qualified by numerous laboratories and, actually, its ability to be used for studying the behaviour of powders under pressure should be examined. Then, the purpose of this work was to investigate the performances of the Stylcam 100R for characterizing the compaction behaviour and the tabletting properties of pharmaceutical powders. The compressibility of three pharmaceutical excipients (microcrystalline cellulose, dicalcium phosphate dihydrate and ,-lactose monohydrate) was studied. Four compression speeds were used on the compaction simulator. Force,displacement cycles were associated with two energy parameters, the specific total energy (Estot) and the specific expansion energy (Esexp). The mean yield pressure was calculated from Heckel's plots obtained with the in-die method. The diametral tensile strength of compacts was measured in order to evaluate mechanical properties. To evaluate the accuracy of all these parameters, a comparative study was carried out on an eccentric instrumented press. The values of energy parameters and tensile strengths of tablets are close between the eccentric press and the compaction simulator, whatever the compression speed on the latter. The mean yield pressure values obtained using the two presses are different. Finally, the Stylcam 100R seems to be a good tool for characterising tabletting properties of powders, except for the Heckel's model probably due to an unadapted equation of deformation and a lack of accuracy of the displacement transducers. Future improvements should allow correcting these two points. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99: 2874,2885, 2010 [source] Wet granulation in a twin-screw extruder: Implications of screw designJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 4 2010M.R. Thompson Abstract Wet granulation in twin-screw extrusion machinery is an attractive technology for the continuous processing of pharmaceuticals. The performance of this machinery is integrally tied to its screw design yet little fundamental knowledge exists in this emerging field for granulation to intelligently create, troubleshoot, and scale-up such processes. This study endeavored to systematically examine the influence of different commercially available screw elements on the flow behavior and granulation mechanics of lactose monohydrate saturated at low concentration (5,12%, w/w) with an aqueous polyvinyl-pyrrolidone binder. The results of the work showed that current screw elements could be successfully incorporated into designs for wet granulation, to tailor the particle size as well as particle shape of an agglomerate product. Conveying elements for cohesive granular flows were shown to perform similar to their use in polymer processing, as effective transport units with low specific mechanical energy input. The conveying zones provided little significant change to the particle size or shape, though the degree of channel fill in these sections had a significant influence on the more energy-intensive mixing elements studied. The standard mixing elements for this machine, kneading blocks and comb mixers, were found to be effective for generating coarser particles, though their mechanisms of granulation differed significantly. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99: 2090,2103, 2010 [source] The rheological properties of modified microcrystalline cellulose containing high levels of model drugsJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 6 2009Paul E. Knight Abstract The rheological properties of different types of microcrystalline cellulose (MCC) mixed with model drugs and water have been evaluated to identify the influence of sodium carboxymethylcellulose (SCMC) added to the cellulose during preparation. A ram extruder was used as a capillary rheometer. The mixtures consisted of 20% spheronizing agent (standard grade MCC or modified types with 6% or 8% of low viscosity grade SCMC) and 80% of ascorbic acid, ibuprofen or lactose monohydrate. The introduction of SCMC changed all rheological parameters assessed. It produced more rigid systems, requiring more stress to induce and maintain flow. Degree of non-Newtonian flow, angle of convergence, extensional viscosity, yield and die land shear stress at zero velocity, and static wall friction were increased, but recoverable shear and compliance were decreased. The presence of SCMC did not remove the influence of the type of drug. The mixture of ibuprofen and standard MCC had the lowest values for shear stress as a function of the rate of shear, extensional viscosity, and angle of convergence, but the highest values for recoverable shear and compliance. The findings indicate that the system has insufficient rigidity to form pellets. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:2160,2169, 2009 [source] A near-infrared spectroscopic investigation of relative density and crushing strength in four-component compactsJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 3 2009Steven M. Short Abstract Near-infrared spectroscopy (NIRS) is commonly employed for the analysis of chemical and physical attributes of intact pharmaceutical compacts. Specifically, NIRS has proven useful in the nondestructive measurement of tablet hardness or crushing strength. Near-infrared (NIR) reflectance and transmittance spectra were acquired for 174 13-mm compacts, which were produced according to a four-constituent mixture design (29 points) composed of anhydrous theophylline, lactose monohydrate, microcrystalline cellulose, and soluble starch. Six compacts were produced for each design point by compacting at multiple pressures. Physical testing and regression analyses were used to model the effect of variation in relative density (and crushing strength) on NIR spectra. Chemometric analyses demonstrated that the overall spectral variance was strongly influenced by anhydrous theophylline as a result of the experimental design and the component's spectroscopic signature. The calibration for crushing strength was more linear than the relative density model, although accuracy was poorer in comparison to the density model due to imprecision of the reference measurements. Based on the consideration of reflectance and transmittance measurements, a revised rationalization for NIR sensitivity to compact hardness is presented. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:1095,1109, 2009 [source] Erratum: Dissolution kinetics of single crystals of ,-lactose monohydrateJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 2 2003S. L. Raghavan No abstract is available for this article. [source] The bulk crystallization of ,-lactose monohydrate from aqueous solutionJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 7 2001S.L. Raghavan Abstract The bulk crystallization of ,-lactose monohydrate from aqueous solution by primary nucleation has been studied under controlled conditions of supersaturation, temperature, and pH. The induction times to nucleation were extremely long compared with those generally observed for other materials, even at the high supersaturations used in the experiment. As a result, it was necessary to stir the supersaturated solution vigorously to induce nucleation in a reasonable but still lengthy working time. Even then, nucleation only occurred to a limited extent, following which growth ceased for 8,10 h before resuming. After this period, growth recommenced but again slowed to a low rate after another 8 h. At this stage, the yield of product was low and in most cases the particles had achieved sizes close to the maximum noted. The yields increased with further crystallization time (22,72 h total from the recommencement of growth) to give, under high initial supersaturation conditions, amounts of product close to the theoretical value. For the most part, however, the particle size did not increase with this later increase in yield, showing only significant changes after the extremely long total crystallization times. It is proposed that these extreme properties result from the formation in solution by mutarotation of the anomer ,-lactose, which inhibits nucleation as well as its previously observed influence on growth. © 2001 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 90:823,832, 2001 [source] Determination of amorphous content in the pharmaceutical process environmentJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 2 2007Marja Savolainen The amorphous state has different chemical and physical properties compared with a crystalline one. Amorphous regions in an otherwise crystalline material can affect the bioavailability and the processability. On the other hand, crystalline material can function as nuclei and decrease the stability of an amorphous system. The aim of this study was to determine amorphous content in a pharmaceutical process environment using near infrared (NIR) and Raman spectroscopic techniques together with multivariate modelling tools. Milling was used as a model system for process-induced amorphization of a crystalline starting material, ,-lactose monohydrate. In addition, the crystallization of amorphous material was studied by storing amorphous material, either amorphous lactose or trehalose, at high relative humidity conditions. The results show that both of the spectroscopic techniques combined with multivariate methods could be applied for quantitation. Preprocessing, as well as the sampling area, was found to affect the performance of the models. Standard normal variate (SNV) transformation was the best preprocessing approach and increasing the sampling area was found to improve the models. The root mean square error of prediction (RMSEP) for quantitation of amorphous lactose using NIR spectroscopy was 2.7%, when a measuring setup with a larger sampling area was used. When the sampling area was smaller, the RMSEPs for lactose and trehalose were 4.3% and 4.2%, respectively. For Raman spectroscopy, the RMSEPs were 2.3% and 2.5% for lactose and trehalose, respectively. However, for the optimal performance of a multivariate model, all the physical forms present, as well as the process environment itself, have to be taken into consideration. [source] Factorial designed experiment to study the effects of excipients on the mechanical properties of pelletsJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 10 2006Abraham B. Bashaiwoldu The aim of this work was to determine the effects of formulation factors on the mechanical properties of pellets produced by the process of extrusion and spheronisation. A range of properties from a simple fracture load to detailed load/displacement curves were used to study the effects of the levels of lactose monohydrate and glyceryl monostearate on the mechanical properties of pellets in terms of their surface tensile strength, pellet deformability and linear strain. A series of independent 22 -factorial designs were employed to establish the relationships between composition of the formulations and pellet properties, whereby the concept of an excess variable was explored. It was found that the spheronisation aid used, microcrystalline cellulose, is the domineering factor in most mechanical properties studied, except for the surface tensile strength, which decreased significantly with an increase in glyceryl monostearate concentration. The change in binder liquid from water to a water/ethanol mixture further changed the behaviour of the systems significantly. The assumption of an excess variable being less critical for the statistical outcome of a factorial experiment has not been found feasible for the systems studied. [source] Analysis of a Simple Test Device for Tribo-Electric Charging of Bulk PowdersPARTICLE & PARTICLE SYSTEMS CHARACTERIZATION, Issue 1-2 2009upuk Abstract We have developed a simple device to characterise the tribo-electric charging propensity of powders. A sample of around one gram of powder is shaken in a container by reciprocal strokes in a horizontal direction. The electric charge on the powder is quantified by a Faraday cup before and after shaking. In this paper, we analyse the operation of this simple test device by investigating the behaviour of ,-lactose monohydrate (,-LM), hydroxy propyl cellulose (HPC) and a 50 : 50 binary mixture (by mass) of these two powders with various container surfaces commonly used in the pharmaceutical industry. The experiments are carried out in controlled environmental conditions and using different shaking times and frequencies of 10, 20 and 30,Hz. The experimental results show that the saturated charge is independent of the shaking frequency. Furthermore adhered particles coating the inner surface of the shaking container decrease the net amount of charge generated by up to 50,%. [source] | ||||||||||