Evaluation of rapidly disintegrating tablets prepared by a direct compression method

To make rapidly disintegrating tablets with sufficient mechanical integrity as well as a pleasant taste, microcrystalline cellulose (MCC), Tablettose (TT), and cross-linked sodium carboxymethyl cellulose (Ac-di-sol) or erythritol (ET) were formulated. Tablets were made by a direct compression method [1]. Tablet properties such as porosity, tensile strength, and disintegration time were determined. The tensile strength and disintegration time were selected as response variables, tablet porosity and parameters representing the characteristics of formulation were selected as controlling factors, and their relation was determined by the polynomial regression method. Response surface plots and contour plots of tablet tensile strength and disintegration time were also constructed. The optimum combination of tablet porosity and formulation was obtained by superimposing the contour diagrams of tablet tensile strength and disintegration time. Rapidly disintegrating tablets with durable structure and desirable taste could be prepared within the obtained optimum region.     

Deformation and Mechanical Characteristics of Compacted Binary Mixtures of Plastic (Microcrystalline Cellulose), Elastic (Sodium Starch Glycolate), and Brittle (Lactose Monohydrate) Pharmaceutical Excipients

This work studies the tensile strength, coherence, elastic, and plastic energy of single and bi-component compacted tablets consisting of (i) microcrystalline cellulose (MCC) PH 102 as a plastic material, (ii) (SSG) as an elastic material, and (iii) alpha lactose monohydrate as a brittle material by direct compression. Compacted tablets were studied with various mass ratios formed at an ultimate compaction stress of 150 MPa. The loading and unloading stages of the compaction process for the single and binary tablets were evaluated based on the energies derived from the force-displacement data obtained. The resulting tablet quality was measured in terms of the tensile strength. Material that exhibit predominantly plastic deformation (MCC) shows a dominant property over elastically deforming sodium starch glycolate (SSG) and brittle (lactose) materials during the loading and unloading stages of the compaction process. In conclusion, the tensile strength of the formed tablets depends directly on the plastic energy and indirectly on the elastic energy and is negatively affected by the presence of a brittle material.     

Effect of repeated compaction of tablets on tablet properties and work of compaction using an instrumented laboratory tablet press

The repeated compaction of Avicel PH101, dicalcium phosphate dihydrate (DCP) powder, 50:50 DCP/Avicel PH101 and Starch 1500 was studied using an instrumented laboratory tablet press which measures upper punch force, punch displacement and ejection force and operates using a V-shaped compression profile. The measurement of work compaction was demonstrated, and the test materials were ranked in order of compaction behaviour Avicel PH101?>?DCP/Avicel PH101?>?Starch?>?DCP. The behaviour of the DCP/Avicel PH101 mixture was distinctly non-linear compared with the pure components. Repeated compaction and precompression had no effect on the tensile fracture strength of Avicel PH101 tablets, although small effects on friability and disintegration time were seen. Repeated compaction and precompression reduced the tensile strength and the increased disintegration time of the DCP tablets, but improved the strength and friability of Starch 1500 tablets. Based on the data reported, routine laboratory measurement of tablet work of compaction may have potential as a critical quality attribute of a powder blend for compression. The instrumented press was suitable for student use with minimal supervisor input.     

Influence of compacted hydrophobic and hydrophilic colloidal silicon dioxide on tableting properties of pharmaceutical excipients

The effect of noncompacted and compacted hydrophilic as well as hydrophobic colloidal silicon dioxide (CSD) on tableting properties of three different pharmaceutical excipients used for direct compression, namely, Avicel® PH 101, Starch 1500®®, and Tablettose® 80, was investigated. Binary powder mixtures containing 0.5% CSD and 99.5% excipient were compressed on an instrumented single-punch tablet press, and the radial tensile strength/compaction load profiles were examined. The Ryshkewitch-Duckworth relationship shows that the influence of CSD on tablet strength was dependent on the hydrophobic and hydrophilic nature of the CSD and on the compaction characteristics of the excipients. Tablets from each excipient with and without CSDs were subjected to different levels of relative humidity at 20°C for 7 days. The sorption isotherms and the radial tensile strengths of the tablets after the storage period showed that neither hydrophilic nor hydrophobic CSD influenced the tablet properties of Avicel® PH 101, Starch 1500®®, and Tablettose® 80. Moreover, ternary powder mixtures containing magnesium stearate as a third component were compressed in order to study the influence of CSD on the deleterious effect of magnesium stearate on the interparticle bonding. The radial tensile strength/compaction load profiles and the residual and ejection forces of tablets made from ternary mixtures showed that CSD eliminated the negative effect of magnesium stearate on interparticle bonding while maintaining the lubrication action, in a manner that was affected by its hydrophobicity/hydrophilicity and by the particle deformation properties of the excipient upon compression.     

Influence of Compacted Hydrophobic and Hydrophilic Colloidal Silicon Dioxide on Tableting Properties of Pharmaceutical Excipients

The effect of noncompacted and compacted hydrophilic as well as hydrophobic colloidal silicon dioxide (CSD) on tableting properties of three different pharmaceutical excipients used for direct compression, namely, Avicel® PH 101, Starch 1500®®, and Tablettose® 80, was investigated. Binary powder mixtures containing 0.5% CSD and 99.5% excipient were compressed on an instrumented single-punch tablet press, and the radial tensile strength/compaction load profiles were examined. The Ryshkewitch-Duckworth relationship shows that the influence of CSD on tablet strength was dependent on the hydrophobic and hydrophilic nature of the CSD and on the compaction characteristics of the excipients. Tablets from each excipient with and without CSDs were subjected to different levels of relative humidity at 20°C for 7 days. The sorption isotherms and the radial tensile strengths of the tablets after the storage period showed that neither hydrophilic nor hydrophobic CSD influenced the tablet properties of Avicel® PH 101, Starch 1500®®, and Tablettose® 80. Moreover, ternary powder mixtures containing magnesium stearate as a third component were compressed in order to study the influence of CSD on the deleterious effect of magnesium stearate on the interparticle bonding. The radial tensile strength/compaction load profiles and the residual and ejection forces of tablets made from ternary mixtures showed that CSD eliminated the negative effect of magnesium stearate on interparticle bonding while maintaining the lubrication action, in a manner that was affected by its hydrophobicity/hydrophilicity and by the particle deformation properties of the excipient upon compression.     

Effect of some commercial grades of microcrystalline cellulose on flowability, compressibility, and dissolution profile of piroxicam liquisolid compacts

The technique of liquisolid compacts is a promising method toward enhancing the dissolution of poorly soluble drugs. Lower flowability and compressibility is one of the limitations of this technique. The evaluation of effects of different grades of microcrystalline cellulose (MCC) on flowability, compressibility, and dissolution of liquisolid systems were the aims of this study. For this means, several formulations were prepared using various grades of MCC as carrier. Propylene glycol (PG), silica, and sodium starch glycolate were used as nonvolatile solvent, coating material, and disintegrant, respectively. Then flowability, friability hardness, and dissolution rate of prepared formulations were studied. The effect of tablet aging on mentioned properties was also investigated. The results showed that among the evaluated different grades of MCC, compacts containing MCC PH 101 and 102 showed better dissolution profiles. Harder compacts were obtained using MCC PH 101 and 200 as carriers. Better flowability was observed in compacts containing MCC PH 101. Also, these compacts demonstrated acceptable friability. Aging had no effect on hardness and dissolution profile of liquisolid tablets. It could be concluded that MCC PH 101 is a suitable carrier for preparing liquisolid systems for having acceptable flowability, friability, hardness, and dissolution profile.     

A Hybrid Model Using Bio-Inspired Metaheuristic Algorithms for Network Intrusion Detection System

Network Intrusion Detection System (IDS) aims to maintain computer network security by detecting several forms of attacks and unauthorized uses of applications which often can not be detected by firewalls. The features selection approach plays an important role in constructing effective network IDS. Various bio-inspired metaheuristic algorithms used to reduce features to classify network traffic as abnormal or normal traffic within a shorter duration and showing more accuracy. Therefore, this paper aims to propose a hybrid model for network IDS based on hybridization bio-inspired metaheuristic algorithms to detect the generic attack. The proposed model has two objectives; The first one is to reduce the number of selected features for Network IDS. This objective was met through the hybridization of bio-inspired metaheuristic algorithms with each other in a hybrid model. The algorithms used in this paper are particle swarm optimization (PSO), multi-verse optimizer (MVO), grey wolf optimizer (GWO), moth-flame optimization (MFO), whale optimization algorithm (WOA), firefly algorithm (FFA), and bat algorithm (BAT). The second objective is to detect the generic attack using machine learning classifiers. This objective was met through employing the support vector machine (SVM), C4.5 (J48) decision tree, and random forest (RF) classifiers. UNSW-NB15 dataset used for assessing the effectiveness of the proposed hybrid model. UNSW-NB15 dataset has nine attacks type. The generic attack is the highest among them. Therefore, the proposed model aims to identify generic attacks. My data showed that J48 is the best classifier compared to SVM and RF for the time needed to build the model. In terms of features reduction for the classification, my data show that the MFO-WOA and FFA-GWO models reduce the features to 15 features with close accuracy, sensitivity and F-measure of all features, whereas MVO-BAT model reduces features to 24 features with the same accuracy, sensitivity and F-measure of all features for all classifiers.     

基于遗传算法的碳纤维增强树脂复合材料层合板单搭胶接结构的多目标优化

基于遗传算法对碳纤维增强树脂复合材料(CFRP)层合板单搭胶接结构进行了多目标优化,以提高其结构性能.首先,通过三维Hashin准则和三角形内聚力模型建立三维有限元模型来预测CFRP层内损伤过程、层间失效和胶层损伤过程,并通过试验验证其有效性.其次,利用拉丁超立方抽样(LHS)方法和二次多项式响应面法(RSM),基于搭...     

Evaluation of critical binder properties affecting the compactibility of binary mixtures

The aim of this study was to identify essential physical and mechanical properties of various binders and to investigate their influence on the tensile strength and porosity of tablets made from binary mixtures with sodium bicarbonate. The binders were characterized according to axial and radial tensile strength after compression into tablets, yield pressure and minimum porosity during compression, and elastic recovery after compression. The addition of a binder generally resulted in an increase in the tensile strength and a decrease in the porosity of the sodium bicarbonate tablets. The location of the binder in the voids between the sodium bicarbonate particles thus decreasing the porosity of the tablet seemed to be an important consideration. Consequently, the addition of binders with a low yield pressure value and a relatively small elastic recovery value (e.g., polyethylene glycol 3000 and polyvinylpyrrolidone) resulted in tablets of low porosity and high tensile strength, especially in the axial direction. The tensile strength of the pure binder also seemed to be important, especially for binders with a lower degree of deformability (e.g., microcrystalline cellulose and pregelatinised starch). The results also indicated the value of using both axial and radial tensile strength measurements in assessing the effect of a dry binder and showed that the importance of different binder properties varied according to the direction of the tablet strength measurements. The results demonstrated that the applied characteristics of the binders used in this study may serve as a useful tool in evaluating the effectiveness of binders.     

Influence of granulating method on physical and mechanical properties, compression behavior, and compactibility of lactose and microcrystalline cellulose granules

The physical and mechanical properties of lactose (LC) and microcrystalline cellulose (MCC) granules prepared by various granulating methods were determined, and their effects on the compression and strength of the tablets were examined. From the force-displacement curve obtained in a crushing test on a single granule, all LC granules appeared brittle, and MCC granules were somewhat plastically deformable. Intergranular porosity ε_inter clearly decreased with greater spherical granule shape for both materials. Decrease in intragranular porosity ε_intra enhanced the crushing force of a single granule F_g. Agitating granulation brought about the most compactness and hardness of granules. In granule compression tests, the initial slope of Heckel plots K₁ appeared closely related to ease of filling voids in a granule bed by the slippage or rolling of granules. The reciprocal of the slope in the succeeding step 1/K₂ in compression of MCC granules indicated positive correlation to F_g, while in LC granules, no such obvious relation was evident. 1/K₂ differed only slightly among granulating methods. Tensile strength of tablets T_t obtained by compression of various LC granules was low as a whole and was little influenced by granulating method. For MCC granules, which are plastically deformable, tablet strength greatly depended on granulation. Granules prepared by extruding or dry granulation gave strong tablets. Tablets prepared from granules made by the agitating method showed particularly low T_t. From stereomicroscopic observation, the contact area between granule particles in a tablet appeared smaller; this would explain the decrease in intergranular bond formation.     

Evaluation of Critical Binder Properties Affecting the Compactibility of Binary Mixtures

The aim of this study was to identify essential physical and mechanical properties of various binders and to investigate their influence on the tensile strength and porosity of tablets made from binary mixtures with sodium bicarbonate. The binders were characterized according to axial and radial tensile strength after compression into tablets, yield pressure and minimum porosity during compression, and elastic recovery after compression. The addition of a binder generally resulted in an increase in the tensile strength and a decrease in the porosity of the sodium bicarbonate tablets. The location of the binder in the voids between the sodium bicarbonate particles thus decreasing the porosity of the tablet seemed to be an important consideration. Consequently, the addition of binders with a low yield pressure value and a relatively small elastic recovery value (e.g., polyethylene glycol 3000 and polyvinylpyrrolidone) resulted in tablets of low porosity and high tensile strength, especially in the axial direction. The tensile strength of the pure binder also seemed to be important, especially for binders with a lower degree of deformability (e.g., microcrystalline cellulose and pregelatinised starch). The results also indicated the value of using both axial and radial tensile strength measurements in assessing the effect of a dry binder and showed that the importance of different binder properties varied according to the direction of the tablet strength measurements. The results demonstrated that the applied characteristics of the binders used in this study may serve as a useful tool in evaluating the effectiveness of binders.     

Effect of polymer,plasticizer and filler on orally disintegrating film

Context: Difficulty in swallowing tablets or capsules has been identified as one of the contributing factors to non-compliance of geriatric patients. Although orally disintegrating tablet was designed for fast disintegration in mouth, the fear of taking solid tablets and the risk of choking for certain patient populations still exist.

Objective: The objective of this study was to develop and characterize orally disintegrating film (ODF), which was prepared using different combinations of polymers, plasticizers and fillers.

Materials and methods: Effects of hydroxypropyl methylcellulose (HPMC), polyethylene glycol 400 (PEG 400), glycerin, polyvinyl pyrrolidone (PVP), mannitol and microcrystalline cellulose (MCC) on physical property of ODF formed were studied. The ODF was prepared using the solvent casting method.

Results: Increase in HPMC concentration formed ODF with greater tensile strength. Incorporation of plasticizer (PEG 400 and glycerin) reduced tensile strength but increased elasticity of the ODF formed. PVP increased both tensile strength and elasticity of the ODF. Increase in MCC:mannitol ratio reduced the tensile strength and elasticity of the ODF. Disintegration time of film decreased corresponding to decrease in tensile strength of the film. Formulation R with the optimum tensile strength (13.10?N/mm²), bending flexibility (40 times) and disintegration time (41.50?s) was chosen as final formulation. A total of 80% of the drug was released within five minutes and the ODF was stable at least for one year actual condition.

Conclusion: An ODF containing donepezil HCl was developed and characterized. The donepezil HCl ODF has the potential to improve the compliance of Alzheimer disease patients.     

The Compressional Properties of Dextrose Monohydrate and Anhydrous Dextrose of Varying Water Contents

The effect of moisture on the compressional properties of anhydrous dextrose and dextrose monohydrate was examined. Relationships between moisture content and both tablet tensile strength and tablet toughness were evaluated. An increase in the moisture content of anhydrous dextrose produced a corresponding increase in both strength parameters up to the 8.9% moisture level, possibly due to a recrystallising effect. However any further increase in moisture content beyond this point produced a marked reduction in both tablet tensile strength and tablet toughness. For dextrose monohydrate, any increase in moisture content obtained by exposure to elevated humidities led to a reduction in both tensile strength and toughness.

The consolidation of both anhydrous dextrose and dextrose monohydrate was improved with increasing moisture content, presumably due to a lubrication effect, The yield forces and percentage porosity obtained under compression for anhydrous dextrose were observed to decrease with increasing moisture content up to a level of 9.20%.     

The Compressional Properties of Dextrose Monohydrate and Anhydrous Dextrose of Varying Water Contents

The effect of moisture on the compressional properties of anhydrous dextrose and dextrose monohydrate was examined. Relationships between moisture content and both tablet tensile strength and tablet toughness were evaluated. An increase in the moisture content of anhydrous dextrose produced a corresponding increase in both strength parameters up to the 8.9% moisture level, possibly due to a recrystallising effect. However any further increase in moisture content beyond this point produced a marked reduction in both tablet tensile strength and tablet toughness. For dextrose monohydrate, any increase in moisture content obtained by exposure to elevated humidities led to a reduction in both tensile strength and toughness.

The consolidation of both anhydrous dextrose and dextrose monohydrate was improved with increasing moisture content, presumably due to a lubrication effect, The yield forces and percentage porosity obtained under compression for anhydrous dextrose were observed to decrease with increasing moisture content up to a level of 9.20%.     

Compaction Behaviour of Musol, A New Direct Compression Vehicle

The compaction characteristics of Musol, a new autocompressible vehicle derived through chemical modification of mucuna gum was investigated. Avicel PH 101, Zeparox and Encompress were used as reference tablet vehicles. Values of the mean yield stress derived from the analysis of Heckel plots indicate that Musol consolidates principally by plastic deformation, The effect of lubrication and recompression on friability, tensile strength and re-working potential of the tablets prepared with the vehicles were determined. While Avicel PH 101 yielded the strongest tablets, Musol showed the highest re-working potential for lubricated and un-lubricated slugs. On the basis of friability, tensile Values of strength and re-working potential, Musol than the grades of Zeparpx or Encompress performed better used in the study.     

Effect of Aqueous Film Coating Conditions on Water Removal Efficiency and Physical Properties of Coated Tablet Cores Containing Superdisintegrants

Few studies have examined the effect of aqueous film coating process conditions on the physical integrity of the final coated product. Characterization of the aqueous film coating process was previously carried out by selecting water removal efficiency as the response variable to detect and monitor moisture accumulation in the tablet bed [1]. In this study, regression techniques were utilized to obtain the relationship between some physical characteristics of aqueous film coated tablet cores that contained superdisintegrant and several process parameters such as inlet air temperature, spray rate, and pan speed. Tablet response variables measured included residual moisture content, tensile strength and percent porosity. Predicted values of these properties were plotted as a function of the inlet air temperature and the coating solution spray rate. The correlations between the coated tablet response variables and the water removal efficiency of the coating process indicated that coated tablet properties such as residual moisture content, tensile strength, and porosity were linearly correlated with the water removal efficiency of the coating process, which is indicative of the environmental coating conditions present in the coating pan.     

Compaction Behaviour of Musol,A New Direct Compression Vehicle

Abstract

The compaction characteristics of Musol, a new autocompressible vehicle derived through chemical modification of mucuna gum was investigated. Avicel PH 101, Zeparox and Encompress were used as reference tablet vehicles. Values of the mean yield stress derived from the analysis of Heckel plots indicate that Musol consolidates principally by plastic deformation, The effect of lubrication and recompression on friability, tensile strength and re-working potential of the tablets prepared with the vehicles were determined. While Avicel PH 101 yielded the strongest tablets, Musol showed the highest re-working potential for lubricated and un-lubricated slugs. On the basis of friability, tensile Values of strength and re-working potential, Musol than the grades of Zeparpx or Encompress performed better used in the study.     

Bio-inspired Hybrid Feature Selection Model for Intrusion Detection

Intrusion detection is a serious and complex problem. Undoubtedly due to a large number of attacks around the world, the concept of intrusion detection has become very important. This research proposes a multilayer bio-inspired feature selection model for intrusion detection using an optimized genetic algorithm. Furthermore, the proposed multilayer model consists of two layers (layers 1 and 2). At layer 1, three algorithms are used for the feature selection. The algorithms used are Particle Swarm Optimization (PSO), Grey Wolf Optimization (GWO), and Firefly Optimization Algorithm (FFA). At the end of layer 1, a priority value will be assigned for each feature set. At layer 2 of the proposed model, the Optimized Genetic Algorithm (GA) is used to select one feature set based on the priority value. Modifications are done on standard GA to perform optimization and to fit the proposed model. The Optimized GA is used in the training phase to assign a priority value for each feature set. Also, the priority values are categorized into three categories: high, medium, and low. Besides, the Optimized GA is used in the testing phase to select a feature set based on its priority. The feature set with a high priority will be given a high priority to be selected. At the end of phase 2, an update for feature set priority may occur based on the selected features priority and the calculated F-Measures. The proposed model can learn and modify feature sets priority, which will be reflected in selecting features. For evaluation purposes, two well-known datasets are used in these experiments. The first dataset is UNSW-NB15, the other dataset is the NSL-KDD. Several evaluation criteria are used, such as precision, recall, and F-Measure. The experiments in this research suggest that the proposed model has a powerful and promising mechanism for the intrusion detection system.     

The effects of fabrication atmosphere condition on the microstructural and mechanical properties of laser direct manufactured stainless steel 17-4 PH

The effects of atmosphere conditions on microstructural and mechanical properties of stainless steel 17-4PH components fabricated by laser direct manufacturing (LDM) were investigated through measurements on phase constitution, porosity, tensile strength, fracture morphology, hardness and evolution of substrate temperature. Results showed that the samples produced in air atmosphere condition possessed higher tensile strength and hardness for both as-deposited and heat-treated states than that in Ar chamber condition, due to dispersion strengthening effect of amorphous oxide particles and nitrogen solution strengthening as a result of higher content of oxygen and nitrogen. The temperature of substrate heat accumulation was higher in Ar chamber condition, leading to dramatically lower porosity and more reverse austenite, which also contributed to the lower strength and hardness.