Formulation studies for mirtazapine orally disintegrating tablets

Abstract

Objective: Orally disintegrating tablets (ODTs) recently have gained much attention to fulfill the needs for pediatric, geriatric, and psychiatric patients with dysphagia. Aim of this study was to develop new ODT formulations containing mirtazapine, an antidepressant drug molecule having bitter taste, by using simple and inexpensive preparation methods such as coacervation, direct compression and to compare their characteristics with those of reference product (Remereon SolTab).

Materials and methods: Coacervation method was chosen for taste masking of mirtazapine. In vitro characterization studies such as diameter and thickness, weight variation, tablet hardness, tablet friability and disintegration time were performed on tablet formulations. Wetting time and in vitro dissolution tests of developed ODTs also studied using 900?mL 0.1?N HCl medium, 900?mL pH 6.8 phosphate buffer or 900?mL pH 4.5 acetate buffer at 37?±?0.2?°C as dissolution medium.

Results: Ratio of Eudragit® E-100 was chosen as 6% (w/w) since the dissolution profile of A1 (6% Eudragit® E-100) was found closer to the reference product than A2 (4% Eudragit® E-100) and A3 (8% Eudragit® E-100). Group D, E and F formulations were presented better results in terms of disintegration time. Dissolution results indicated that Group E and F formulations showed optimum properties in all three dissolution media.

Discussion: Formulations D1, D4, D5, E3, E4, F1 and F5 found suitable as ODT formulations due to their favorable disintegration times and dissolution profiles.

Conclusion: Developed mirtazapine ODTs were found promising in terms of showing the similar characteristics to the original formulation.     

Novel superabsorbent materials from bacterial cellulose

A novel process for the production of superabsorbent materials (hydrogels) from bacterial cellulose (BC) was developed. Prior to crosslinking with a water‐soluble polyethylene glycol diacrylate (PEGDA), BC was first carboxymethylated and functionalized with glycidyl methacrylate. The degree of crosslinking influenced the swelling properties of the hydrogels. The use of greater amounts of PEGDA enhanced the formation of a thicker macromolecular network containing fewer capillary spaces in the crosslinked gel. The maximum water retention value of the hydrogels containing 2.5–3.5 mmol of carboxyl groups per gram of gel reached 125 g g^?1 in distilled water, and 29 g g^?1 in saline (0.9% NaCl solution). The highly porous hydrogel architecture with a pore size of 350–600 µm created a high specific surface area. This enables rapid mass penetration in superabsorbent applications. The superabsorbent hydrogels reached 80% of their maximum water absorption capacity in 30 min. © 2018 Society of Chemical Industry     

Graphene‐based ternary composites for supercapacitors

The research on electrode materials for supercapacitor application continues to evolve as the request of high‐energy storage system has increased globally due to the demand for energy consumption. Over the past decades, various types of carbon‐based materials have been employed as electrode materials for high‐performance supercapacitor application. Among them, graphene is 1 of the most widely used carbon‐based materials due to its excellent properties including high surface area and excellent conductivity. To exploit more of its interesting properties, graphene is tailored to produce graphene oxide and reduced graphene oxide to improve the dispersibility in water and easy to be incorporated with other materials to form binary composites or even ternary composites. Nowadays, ternary composites have attracted enormous interest as 2 materials (binary composites) cannot satisfy the requirement of the high‐performance supercapacitor. Thus, many approaches have been employed to fabricate ternary composites by combining 3 different types of electroactive materials for high‐performance supercapacitor application. This review focuses on the supercapacitive performance of graphene‐based ternary composites with different types of active materials, ie, conducting polymers, metal oxide, and other carbon‐based materials.     

Anomaly localization in regular textures based on deep convolutional generative adversarial networks

Applied Intelligence - Pixel-level anomaly localization is a challenging problem due to the lack of abnormal training samples. The existing adversarial network methods attempt to segment anomalies...     

Antioxidant and α-glucosidase inhibitory activities of eight neglected fruit extracts and UHPLC-MS/MS profile of the active extracts

The 70% ethanolic extracts from eight neglected fruits; Muntingia calabura, Leucaena leucocephala, Spondias dulcis, Syzygium jambos, Mangifera caesia, Ardisia elliptica, Cynometra cauliflora and Ficus auriculata were evaluated for their 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging, α-glucosidase inhibitory activities as well as total phenolic content. The results of this study revealed that M. caesia fruit extract demonstrated the most potent radical scavenging activity. Among the fruits examined for α-glucosidase inhibitory activity, M. calabura and F. auriculata exhibited strong activity with no significant difference. The Pearson correlation indicated that the activities of M. caesia and F. auriculata contributed by phenolic compounds. A total of 65 metabolites were tentatively identified by using ultra-high-performance liquid chromatography tandem mass spectrometry (UHLPC-MS/MS). These findings suggested that the possible application of M. caesia and F. auriculata as a functional food with antioxidant and α-glucosidase inhibitory properties.     

Competitiveness analysis of automotive industry in Turkey using Bayesian networks

The purpose of this study is to analyze the relations between the factors that enable national competitive advantage and the establishment of competitive superiority in automotive industry through a comprehensive analytical model. Bayesian networks (BN) are used to investigate the associations of different factors in the automotive industry which lead to competitive advantage. The results of the study focus on building a road map for the automotive sector policy makers in their way to improve the competitiveness through scenario analysis. Using the probabilistic dependency structure of the Bayesian network all of the variables in the model can be estimated. Thus, with the proposed model the automotive industry can be analyzed as a whole system and not only in terms of single variables. Findings of the model indicate that technological developments in automotive industry can alter the nature of competition in this industry.     

Synergistic effect of nanoparticles and Thalassospira sp. isolated from Bahregan area in biodegradation of oil sludge

Oil sludge is obtained from the contaminated site of Bahregan area in the Persian Gulf in Iran. Chemotaxis was used for the isolation of alkane-degrading bacteria from oil sludge and the alk genes were determined with specific primers. bac1 identified in Thalassospira was selected as a powerful strain for biodegradation of oil sludge. Biodegradation of oil sludge by bac1 in the presence of nanoparticles was investigated by GC-MS analysis. Synergistic effect of Fe₂O₃ and Fe₃O₄ nanoparticles on bacteria increases the biodegradation of oil sludge and produces cyclosiloxane compound which is used in the field of medicine; however, the Thalassospira reduced its toxicity in the environment.     

Molecular Characterization of α- and β-Thalassaemia among Malay Patients

Both α- and β-thalassaemia syndromes are public health problems in the multi-ethnic population of Malaysia. To molecularly characterise the α- and β-thalassaemia deletions and mutations among Malays from Penang, Gap-PCR and multiplexed amplification refractory mutation systems were used to study 13 α-thalassaemia determinants and 20 β-thalassaemia mutations in 28 and 40 unrelated Malays, respectively. Four α-thalassaemia deletions and mutations were demonstrated. −−^SEA deletion and α^CSα accounted for more than 70% of the α-thalassaemia alleles. Out of the 20 β-thalassaemia alleles studied, nine different β-thalassaemia mutations were identified of which β^E accounted for more than 40%. We concluded that the highest prevalence of (α- and β-thalassaemia alleles in the Malays from Penang are −−^SEA deletion and β^E mutation, respectively.     

Physicochemical properties of liquid natural rubber bearing fluoro groups for hydrophobic surfaces

The modification of liquid natural rubber (LNR) has attracted interests among chemists as it brings improvements to several of its properties and widens its application to various fields. LNR can be modified into fluorinated LNR (F-LNR) which is of interest to industries due to its remarkable properties, including low surface energies, high thermal stabilities, together with its significant hydrophobic characters. In this work, a new route to prepare fluorinated rubber was presented. Hydroxylated LNR (OH-LNR) was initially synthesized in good yield via oxidation in the presence of tungsten complex catalyst and acetic acid with hydrogen peroxide as an oxidant. The optimum hydroxyl content of 57.0% was obtained within 6 h reaction time at 90 °C. In the second step, the esterification of OH-LNR using pentadecafluorooctanoyl chloride (PDFOC) under mild conditions was conducted, leading to LNR bearing fluoro groups in the side chain of LNR (F-LNR). ATR-FTIR spectroscopy was used to elucidate the structure and determine any changes in the functional groups that may have been induced during the reaction. ¹H NMR spectroscopy was employed to reveal that a high fluorine content of 48.6% was obtained using 3:1 molar ratio of OH-LNR:PDFOC for 8 h at 50 °C. The microstructure of F-LNR was further analyzed using ¹⁹F NMR and ¹³C NMR spectroscopies, and the results confirmed the presence of fluorine in LNR. Thermogravimetric analyses also indicated that the modification improved thermal stability of the LNR. Contact angle measurements were also conducted to verify the hydrophobicity of the fluorinated rubber and the results obtained showed that F-LNR exhibited higher hydrophobicity than LNR.     

Synthesis and application of phenylcarbamodithioate compound for steel protection

Phenyldithiocarbamate compound has been synthesized and studied as corrosion inhibitor for steel. Dithiocarbamate (DTC) compounds with linear alkyl groups are good inhibitors, but their stability is quite low in acidic solutions. It should be noted that long-term stability is important for practical applications, in order to avoid excess use of chemicals. So, we have synthesized phenyl substituted DTC which offers strong inhibition efficiency and extra stability. This new inhibitor is chemically adsorbed on steel through its DTC group, while the aromatic ring provides extra stability and long-term efficiency. For the assessment of corrosion kinetics, we have utilized potentiodynamic and ac impedance studies; also solution assay analysis was realized with atomic absorption spectroscopy. It was revealed that inhibitor exhibits remarkably high efficiency, even under elevated temperature conditions. At 55 °C temperature conditions, i_corr value decreased from 5050 to 154 μA cm^?2, with the addition of 500 ppm inhibitor. The long-term stability of inhibitor was also tested and 85.93% efficiency was obtained after three days of exposure period for 500 ppm concentration.