Effect of a Lubricant on Wear Rate of Tablets

The rate of wear and hardness of tablets of Emcompress and sodium chloride compressed at various applied pressures in a lubricated and an unlubricated die are compared. The effect of applied pressure and concentration of magnesium stearate blended with several direct compression excipients on the wear rate constant, hardness and tensile strength of a tablet is reported. The data allow a comparison of the methods used to express the mechanical strength of tablets.     

Effect of a Lubricant on Wear Rate of Tablets

Abstract

The rate of wear and hardness of tablets of Emcompress and sodium chloride compressed at various applied pressures in a lubricated and an unlubricated die are compared. The effect of applied pressure and concentration of magnesium stearate blended with several direct compression excipients on the wear rate constant, hardness and tensile strength of a tablet is reported. The data allow a comparison of the methods used to express the mechanical strength of tablets.     

微通道冷凝器空气侧性能的实验研究

对13个微通道冷凝器空气侧性能进行实验研究,分析空气侧换热系数和压降与迎面空气流速、翅片片距、百叶窗翅片开窗数、扁管宽度及扁管高度之间的关系,并将实验值与3个不同的百叶窗翅片换热及压降关联式的预测值进行比较。结果表明：翅片片距和扁管宽度对空气侧性能影响较大,3个关联式中Kim—Bullard关联式预测偏差相对最小,换热系数的预测偏差在0～-30％以内,摩擦系数的偏差在±20％偏差范围内。最后基于已有实验数据,对KimBullard关联式进行重新拟合。     

The effect of ultrasonic vibration on the compaction characteristics of ibuprofen

An ultrasonic (US) compaction rig has been developed, capable of providing compaction pressure together with high-power ultrasonic vibrations of 20 kHz to a powder or granular material in a die. The rig has been used to investigate the effect of ultrasound on the compaction properties of ibuprofen, a drug with poor compaction properties which produces tablets that are weak and frequently exhibit capping. It was found that coherent ibuprofen tablets could be prepared by ultrasound-assisted compaction at pressures as low as 20-30 MPa. Application of ultrasound before and after compaction was found not to be as effective as ultrasound applied during compaction. The breaking forces of the tablets produced with ultrasound applied during compaction were found to be consistently significantly higher than when compaction was performed conventionally, or with ultrasound applied before or after compaction. Application of ultrasound during compaction made it possible to increase tablet mechanical strength, typically by a factor of 2-5. It was concluded that pressure should be applied together with ultrasound in order to achieve a better acoustical contact, which is required to transmit vibrations from the horn to the material, and also to bond the surfaces of the particles.

Ultrasound application during ibuprofen compaction also resulted in an increase in the apparent density, in relation to the apparent density of conventionally prepared tablets, of up to 14.4%. Ultrasound appears to improve particle rearrangement and provides energy for partial melting of particle asperities and subsequent fusion of particle surfaces, so as to increase interparticulate bonding. Solid bridge formation was thought to result in a reduction of void space, which in turn reduced the rate of water penetration into the compacts and consequently increased disintegration and dissolution times.

It was found that the results of ultrasound-assisted compaction are influenced by formulation and US time. When ibuprofen was mixed with a second material, such as dibasic calcium phosphate dihydrate (DCP) or microcrystalline cellulose (MCC), stronger tablets were prepared by ultrasound-assisted compaction compared to the compacts containing no filler. Positive interactions were considered to have occurred due to ultrasound-induced bonding between the two materials. With an increase in DCP and MCC concentration in ibuprofen formulations, disintegration and drug dissolution rates of the tablets produced with ultrasound significantly increased.

Using temperature-sensitive labels it was found that thermal changes occurred in powdered solids undergoing ultrasound-assisted compaction. Increases in the temperature of tablets were related to US amplitude and US time. With an increase in US amplitude from 5 to 13 µm, the temperature of the DCP tablet surface increased from 40 to 99°C. With an increase in US time from 1 to 5 sec, the temperature of the surface of ibuprofen tablets increased from 43 to 60°C. Increased tablet temperature was thought to be due to ultrasonic energy dissipation turned into heat.

X-ray powder diffraction (XRD) studies of ibuprofen tablets prepared by ultrasound-assisted compaction at 32 MPa revealed that no changes in chemical or/and crystalline structure of the material occurred when ultrasound was applied for up to 5 sec (US amplitude 7 µm). An XRD study of DCP tablets produced by ultrasound-assisted compaction at 32 MPa with ultrasound of different amplitudes (5, 7, 13 µm) applied for 2 sec indicated that no material deterioration occurred in all the tested samples.     

An investigation of frequency domain dispersion correction of pressure bar signals

The frequency-domain method has been used for several years for the correction of dispersed experimental pressure bar signals. However, the accuracy of this method has been assessed only against assumed force–time histories of the loading function, not against a priori known loads. Further, this method presently fails to take into account predictions from the Pochammer–Chree theory for both the variation of axial strain over the bar radius, and the relation between axial stress and strain. In the current work, a known force–time history is applied to the impact face of a finite element model of a pressure bar. The dispersed signal is recorded on the bar perimeter some way from the impact face, and the frequency domain correction method applied in an attempt to re-construct the undispersed forcing function. It is demonstrated that, even for signals containing moderately high frequencies, excellent reconstruction of the forcing function can be achieved if the Pochammer–Chree results for strain variation and stress–strain relation are incorporated in the dispersion correction method.     

基于桥梁断面压力分布统计特性的抑流板抑制涡振机理研究

通过测量大比例流线形扁平钢箱梁模型（１：２０）涡激共振时表面压力,研究典型钢箱梁常用设计断面涡激振动、静止、以及安装抑流板后涡激共振性能。综合对比分析三种工况模型表面压力系数均值、根方差、局部气动力与涡激气动力相关系数等时域统计特性;表面压力脉动的功率谱、局部测点气动力与总体断面气动力间的在模型竖弯频率处的相位谱和相干函数等频域统计特性。研究发现：竖弯涡激共振产生原因是流线模型上表面下游的气流再附区域强烈压力脉动以及箱梁下表面与总气动力具有较强相关性的压力脉动,整体断面各测点脉动压力具有相同的卓越频率。针对本项研究试验实例,抑流板措施减弱了箱梁中下游位置压力脉动的分布强度和作用时序的相关性,可以有效地抑制涡振。     

Effects of hydrophilic excipients and compression pressure on physical properties and release behavior of aspirin-tableted microcapsules.

Aspirin ethylcellulose microcapsules were tableted by compression with or without excipients (lactose or polyvinylpyrrolidone [PVP]). The effects of the amount of the excipients and microcapsule size on the crushing strength and release rate of aspirin from tableted microcapsules were investigated. Tablets without excipients had a crushing strength that was independent of the applied pressure and microcapsule size. An increase in compression pressure from 15 to 60 MPa resulted in an increase in the crushing strength of tablets containing 20% or 40% w/w lactose, but the reverse results were obtained for the tableted microcapsules containing 20% or 40% w/w PVP. Results showed that the release rate of aspirin from microcapsules containing lactose or PVP was independent of the compression pressure with the exception of tablets containing 40% w/w lactose. In vitro release profiles of aspirin from tableted microcapsules containing lactose or PVP showed that increasing the concentration of the excipients resulted in an increase in the release rate of aspirin. Values of n were changed by the compression pressure and the added excipients.     

Effect of Some Excipjents and Compression Pressure on the Adhesion of Aqueous-Based Hydroxypropyl Methylcellulose Film Coatings to Tablet Surface

The adhesion between aqueous-based hydroxypropyl methylcellulose (HPMC) films and tablet surface was evaluated using a Lloyd LRX materials testing machine. Special attention was paid to the effects of compression pressure and the excipients (microcrystalline cellulose, lactose and a commercial combination of lactose and cellulose (Cellactose^R)) on the adhesion properties of the film.

The adhesion of HPMC films was the lowest for the tablets containing lactose as a diluent and the highest for the tablets containing microcrystalline cellulose. The adhesion to Cellactose^R-based tablets increased with increasing compression pressure. With microcrystalline cellulose (MCC) and lactose, the effect of compression pressure on film adhesion was not so clear. The increase in concentration of a hydrophopic lubricant, magnesium stearate, decreased the adhesion between the films and tablets cores. The greatest decrease was observed with the MCC tablets.

Furthermore the results showed that, the film coating increased clearly the mechanical strength of the tablets, depending on the excipient, the compression pressure and amount of magnesium stearate.     

Tabletability of Maltodextrins and Acetaminophen Mixtures

Tabletability of five types of maltodextrin, a filler/binder excipient, was studied by testing their loading potentials with acetaminophen. The formulations consisted of excipient and acetaminophen at five different ratios and magnesium stearate at a 0.5% concentration. These mixtures were compacted employing an Integrated Compaction Research System at a constant punch velocity of 100 mm/sec. under varying applied pressures from 50 to 450 MPa. Compaction data were evaluated using the total work of compaction vs applied pressure plots whilst the post-compaction tests included the measurements of crushing force, disintegration time, and friability of the resulting tablets. Both the energy involved during the compaction of a formulation and the crushing force values of the resulting tablets decreased as the amount of the maltodextrin in a formulation was reduced. Maltodextrins exhibited adequate binding potential at acetaminophen drug loading levels of only up to twenty-five percent. The disintegration times of the tablets containing maltodextrins were generally prolonged and this was found to be due to the formation of a “gel” layer around the tablet which formed on immersion into water. The tabletability of maltodextrins were also compared to that of Fast-Flo lactose, and the compactability of these excipients were found to be similar.     

Effects of Hydrophilic Excipients and Compression Pressure on Physical Properties and Release Behavior of Aspirin-Tableted Microcapsules

Aspirin ethylcellulose microcapsules were tableted by compression with or without excipients (lactose or polyvinylpyrrolidone [PVP]). The effects of the amount of the excipients and microcapsule size on the crushing strength and release rate of aspirin from tableted microcapsules were investigated. Tablets without excipients had a crushing strength that was independent of the applied pressure and microcapsule size. An increase in compression pressure from 15 to 60 MPa resulted in an increase in the crushing strength of tablets containing 20% or 40% w/w lactose, but the reverse results were obtained for the tableted microcapsules containing 20% or 40% w/w PVP. Results showed that the release rate of aspirin from microcapsules containing lactose or PVP was independent of the compression pressure with the exception of tablets containing 40% w/w lactose. In vitro release profiles of aspirin from tableted microcapsules containing lactose or PVP showed that increasing the concentration of the excipients resulted in an increase in the release rate of aspirin. Values of n were changed by the compression pressure and the added excipients.     

Formulation and development of tablets based on Ludipress and scale-up from laboratory to production scale

In spite of the wealth of experience available in the pharmaceutical industry, tablet formulations are still largely developed on an empirical basis, and the scale-up from laboratory to production is a time-consuming and costly process. Using Ludipress greatly simplifies formulation development and the manufacturing process because only the active ingredient Ludipress and a lubricant need to be mixed briefly before being compressed into tablets. The studies described here were designed to investigate the scale-up of Ludipress-based formulations from laboratory to production scale, and to predict changes in tablet properties due to changes in format, compaction pressure, and the use of different tablet presses. It was found that the tensile strength of tablets made of Ludipress increased linearly with compaction pressures up to 300 MPa. It was also independent of the geometry of the tablets (diameter, thickness, shape). It is therefore possible to give an equation with which the compaction pressure required to achieve a given hardness can be calculated for a given tablet form. The equation has to be modified slightly to convert from a single-punch press to a rotary tableting machine. Tablets produced in the rotary machine at the same pressure have a slightly higher tensile strength. The rate of increase in pressure, and therefore the throughput, has no effect on the tensile strength of Ludipress tablets. It is thought that a certain minimum dwell time is responsible for this difference. The production of tablets based on Ludipress can be scaled up from one rotary press to another without problem if the powder mixtures are prepared with the same mixing energy. The tensile strength curve determined for tablets made with Ludipress alone can also be applied to tablets with a small quantity (< 10%) of an active ingredient.     

Tabletability of Maltodextrins and Acetaminophen Mixtures

Abstract

Tabletability of five types of maltodextrin, a filler/binder excipient, was studied by testing their loading potentials with acetaminophen. The formulations consisted of excipient and acetaminophen at five different ratios and magnesium stearate at a 0.5% concentration. These mixtures were compacted employing an Integrated Compaction Research System at a constant punch velocity of 100 mm/sec. under varying applied pressures from 50 to 450 MPa. Compaction data were evaluated using the total work of compaction vs applied pressure plots whilst the post-compaction tests included the measurements of crushing force, disintegration time, and friability of the resulting tablets. Both the energy involved during the compaction of a formulation and the crushing force values of the resulting tablets decreased as the amount of the maltodextrin in a formulation was reduced. Maltodextrins exhibited adequate binding potential at acetaminophen drug loading levels of only up to twenty-five percent. The disintegration times of the tablets containing maltodextrins were generally prolonged and this was found to be due to the formation of a “gel” layer around the tablet which formed on immersion into water. The tabletability of maltodextrins were also compared to that of Fast-Flo lactose, and the compactability of these excipients were found to be similar.     

Effect of Some Excipjents and Compression Pressure on the Adhesion of Aqueous-Based Hydroxypropyl Methylcellulose Film Coatings to Tablet Surface

Abstract

The adhesion between aqueous-based hydroxypropyl methylcellulose (HPMC) films and tablet surface was evaluated using a Lloyd LRX materials testing machine. Special attention was paid to the effects of compression pressure and the excipients (microcrystalline cellulose, lactose and a commercial combination of lactose and cellulose (Cellactose^R)) on the adhesion properties of the film.

The adhesion of HPMC films was the lowest for the tablets containing lactose as a diluent and the highest for the tablets containing microcrystalline cellulose. The adhesion to Cellactose^R-based tablets increased with increasing compression pressure. With microcrystalline cellulose (MCC) and lactose, the effect of compression pressure on film adhesion was not so clear. The increase in concentration of a hydrophopic lubricant, magnesium stearate, decreased the adhesion between the films and tablets cores. The greatest decrease was observed with the MCC tablets.

Furthermore the results showed that, the film coating increased clearly the mechanical strength of the tablets, depending on the excipient, the compression pressure and amount of magnesium stearate.     

Dissolution of Directly Compressed Thiamine Hydrochloride Tablets

Abstract

Directly compressed thiamine hydrochloride tablets with varying concentrations of different vehicles as well as their binary blends, were prepared for this investigation. The results showed that, formulated tablets with avicel anhydrous lactose and celutab completely dissolved within short times. First order mechanism was reported for the tablets prepared with single vehicles. The dissolution rate constant “K”, was a function of disintegration constant “D” of the tablets by the relation In K = a + n In D. In addition to that, it is proved that, “K” of produced tablets of short disintegration times was a function of the contributed vehicle concentration “C” by the relation, I/K = A exp. + NC.

On the other hand, (T 50%) of thiamine hydrochloride in a given batch was a function of its disintegration time.     

Effect of Particle Size on Direct Compaction of Urea Fertilizer

The effect of particle size on compaction properties and characteristics of urea tablets manufactured from available urea granules (TG tablets) and ground urea powders (TP tablets) was investigated. The compaction properties, namely, plastic work, elastic work, friction work, and maximum ejection pressure were analyzed from the force-displacement profile of the compaction process. Five applied pressures ranging between 37.67 MPa and 188.35 MPa were used to compact the materials using a universal testing machine. Characteristics of the tablets tested were mechanical strength and the release of ammonium ion through dissolution test. The results demonstrated that TG tablets underwent high plastic work and elastic work but low friction work compared to the TP tablets. TG tablets released lower amount of ammonium ion compared to the TP tablets at almost all applied pressures, except at 75.34 MPa. This study provides a valuable data for evaluating the behavior of urea in the form of granules and powders during the compaction process as well as the suitability in choosing the form of raw material for the production of urea tablets.     

Effect of Tableting Pressure and Geometrical Factor of Tablet on Dehydration Kinetics of Theophyline Monohydrate Tablets

The effect of compression pressure and geometrical factors (thickness and diameter) of tablet on the dehydration kinetics of theophylline monohydrate tablets was studied using an infrared water-content measuring instrument. The dehydration rate of 2 cm diameter tablets decreased with increase in tabletting pressure. The dehydration rates of tablets also depended on tablet shape. The 2 cm diameter tablets (thin tablets) dehydrated faster than 1 cm diameter tablets (thick tablets). Dehydration of the powder bed (loosely packed tablets) and 2 cm tablets compressed at 49 MPa followed the two-dimensional phase boundary equation, and that of 2 cm diameter tablets compressed at 98 MPa and 196 MPa (thin tablets) followed the three-dimensional phase boundary equation. Dehydration of 1 cm diameter tablets compressed at 98 MPa (thick tablets) followed the one-dimensional diffusion equation. It seems that the dehydration of the tablet was controlled by the porosity and the surface area of the tablet. Therefore, tablet thickness and tabletting pressure are important factors affecting the dehydration mechanism.     

Simulation and evaluation of tablet-coating burst based on finite element method

The objective of this study was to simulate and evaluate the burst behavior of coated tablets. Three-dimensional finite element models of tablet-coating were established using software ANSYS. Swelling pressure of cores was measured by a self-made device and applied at the internal surface of the models. Mechanical properties of the polymer film were determined using a texture analyzer and applied as material properties of the models. The resulted finite element models were validated by experimental data. The validated models were used to assess the factors those influenced burst behavior and predict the coating burst behavior. The simulation results of coating burst and failure location were strongly matched with the experimental data. It was found that internal swelling pressure, inside corner radius and corner thickness were three main factors controlling the stress distribution and burst behavior. Based on the linear relationship between the internal pressure and the maximum principle stress on coating, burst pressure of coatings was calculated and used to predict the burst behavior. This study demonstrated that burst behavior of coated tablets could be simulated and evaluated by finite element method.     

Effect of Tableting Pressure and Geometrical Factor of Tablet on Dehydration Kinetics of Theophyline Monohydrate Tablets

Abstract

The effect of compression pressure and geometrical factors (thickness and diameter) of tablet on the dehydration kinetics of theophylline monohydrate tablets was studied using an infrared water-content measuring instrument. The dehydration rate of 2 cm diameter tablets decreased with increase in tabletting pressure. The dehydration rates of tablets also depended on tablet shape. The 2 cm diameter tablets (thin tablets) dehydrated faster than 1 cm diameter tablets (thick tablets). Dehydration of the powder bed (loosely packed tablets) and 2 cm tablets compressed at 49 MPa followed the two-dimensional phase boundary equation, and that of 2 cm diameter tablets compressed at 98 MPa and 196 MPa (thin tablets) followed the three-dimensional phase boundary equation. Dehydration of 1 cm diameter tablets compressed at 98 MPa (thick tablets) followed the one-dimensional diffusion equation. It seems that the dehydration of the tablet was controlled by the porosity and the surface area of the tablet. Therefore, tablet thickness and tabletting pressure are important factors affecting the dehydration mechanism.     

Changes in the specific surface area of tablets composed of pharmaceutical materials with various deformation behaviors

Objective: The aim of this work is to study the effect of compaction on the specific surface area of tablets composed of various pharmaceutical materials (microcrystalline cellulose, lactose, and anhydrous calcium phosphate) compacted under seven degrees of compaction pressure. Methods: In a first part, the influence of the deformation behavior of the compacted materials on the evolution of the specific surface area is observed. In a second part, the brittle and ductile abilities of the materials are calculated using the specific surface area values. The experimental results are used to calculate the number and the force of interparticulate bonds inside the tablet.Results and Discussion: Tablets made of microcrystalline cellulose, which deform plastically, have specific surface areas that fall under pressure. In the case of lactose, the tablet specific surface area first increases to reach a maximum value at a pressure of 150 MPa. At higher pressure, however, the specific surface area decreases. The specific surface area of tablets composed of anhydrous calcium phosphate consistently increases, whatever the compaction pressure applied. Moreover, the evolution of the specific surface area is correlated with the tensile strength of the corresponding tablets. The number and the force of interparticulate bonds make it possible to classify the materials according to their deformation behavior and to quantify their ability to form cohesive tablets.     

Linear and non-linear dynamic response of sandwich panels to blast loading

The problem of the dynamic response of sandwich flat panels exposed to blast loadings is addressed. The sandwich model includes a number of non-classical effects such as the anisotropy and heterogeneity of face sheets, transverse orthotropy of the core layer, the geometrical non-linearities considered in the von Kármán sense, as well as the initial geometric imperfections. As concerns the blast pulses considered in this analysis, these are due to either an underwater/in-air explosion, or are due to a pressure wave traveling across the panel span. Implications of the explosive charge, stand-off distance, directionality property of face sheets material, damping ratio, geometric non-linearity, initial geometric imperfection, and of the characteristics of the blast, on dynamic response and dynamic magnification factor are put into evidence via a parametric study, and pertinent conclusions are outlined.