Search results for: Vilsmeier–Haack formulation

Authors: Amitkumar Barot, Vijaykumar Sinha

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There is growing interest in the development of new materials based on recycled polymers from plastic waste, and also in the field of lubricants much effort has been spent on substitution of petro-based raw materials by natural-based renewable ones. This is due to the facts of depleting fossil fuels and due to strict environmental laws. In relevance to this, new technique for the formulation of grease that combines the chemical recycling of poly (ethylene terephthalate) PET with the use of castor oil (CO) has been developed. Comparison to diols used in chemical recycling of PET, castor oil is renewable, easily available, environmentally friendly, economically cheaper and hence sustainability indeed. The process parameters like CO concentration and temperature were altered, and further, the influences of the process parameters have been studied in order to establish technically and commercially viable process. Further thereby formed depolymerized product find an application as base oil in the formulation of grease. A depolymerized product has been characterized by various chemical and instrumental methods, while formulated greases have been evaluated for its tribological properties. The grease formulated using this new environmentally friendly approach presents applicative properties similar, and in some cases superior, compared to those of a commercial grease obtained from non-renewable resources.

Keywords: castor oil, grease formulation, recycling, sustainability

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Authors: Pooya Niksiar, Ali Ashrafizadeh, Mehrzad Shams, Amir Hossein Madani

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There are many computationally demanding applications in science and engineering which need efficient algorithms implemented on high performance computers. Recently, Graphics Processing Units (GPUs) have drawn much attention as compared to the traditional CPU-based hardware and have opened up new improvement venues in scientific computing. One particular application area is Computational Fluid Dynamics (CFD), in which mature CPU-based codes need to be converted to GPU-based algorithms to take advantage of this new technology. In this paper, numerical solutions of two classes of discrete fluid flow models via both CPU and GPU are discussed and compared. Test problems include an Eulerian model of a two-dimensional incompressible laminar flow case and a Lagrangian model of a two phase flow field. The CUDA programming standard is used to employ an NVIDIA GPU with 480 cores and a C++ serial code is run on a single core Intel quad-core CPU. Up to two orders of magnitude speed up is observed on GPU for a certain range of grid resolution or particle numbers. As expected, Lagrangian formulation is better suited for parallel computations on GPU although Eulerian formulation represents significant speed up too.

Keywords: CFD, Eulerian formulation, graphics processing units, Lagrangian formulation

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Authors: Endang Lukitaningsih, Fathul Jannah, Arief R. Hakim, Ratna D. Puspita, Zullies Ikawati

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Rifampicin is a semisynthetic antibiotic derivative of rifamycin B produced by Streptomyces mediterranei. RIF has been used worldwide as first line drug-prescribed throughout tuberculosis therapy. This study aims to develop and to validate an HPLC method couple with a UV detection for determination of rifampicin in spiked human plasma and its application for bioequivalence study. The chromatographic separation was achieved on an RP-C18 column (LachromHitachi, 250 x 4.6 mm., 5μm), utilizing a mobile phase of phosphate buffer/acetonitrile (55:45, v/v, pH 6.8 ± 0.1) at a flow of 1.5 mL/min. Detection was carried out at 337 nm by using spectrophotometer. The developed method was statistically validated for the linearity, accuracy, limit of detection, limit of quantitation, precise and specifity. The specifity of the method was ascertained by comparing chromatograms of blank plasma and plasma containing rifampicin; the matrix and rifampicin were well separated. The limit of detection and limit of quantification were 0.7 µg/mL and 2.3 µg/mL, respectively. The regression curve of standard was linear (r > 0.999) over a range concentration of 20.0 – 100.0 µg/mL. The mean recovery of the method was 96.68 ± 8.06 %. Both intraday and interday precision data showed reproducibility (R.S.D. 2.98% and 1.13 %, respectively). Therefore, the method can be used for routine analysis of rifampicin in human plasma and in bioequivalence study. The validated method was successfully applied in pharmacokinetic and bioequivalence study of rifampicin tablet in a limited number of subjects (under an Ethical Clearance No. KE/FK/6201/EC/2015). The mean values of Cmax, Tmax, AUC(0-24) and AUC(o-∞) for the test formulation of rifampicin were 5.81 ± 0.88 µg/mL, 1.25 hour, 29.16 ± 4.05 µg/mL. h. and 29.41 ± 4.07 µg/mL. h., respectively. Meanwhile for the reference formulation, the values were 5.04 ± 0.54 µg/mL, 1.31 hour, 27.20 ± 3.98 µg/mL.h. and 27.49 ± 4.01 µg/mL.h. From bioequivalence study, the 90% CIs for the test formulation/reference formulation ratio for the logarithmic transformations of Cmax and AUC(0-24) were 97.96-129.48% and 99.13-120.02%, respectively. According to the bioequivamence test guidelines of the European Commission-European Medicines Agency, it can be concluded that the test formulation of rifampicin is bioequivalence with the reference formulation.

Keywords: validation, HPLC, plasma, bioequivalence

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Authors: Sheimah El Bejjaji, Lara Gorsek, Chandler Quilchez, Joaquim Suñer, Mireia Mallandrich

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Flurbiprofen is an anti-inflammatory drug used in several treatments. The purpose of this study was to compare the permeation of two different formulations of flurbiprofen through the human skin. The first formulation was a solution of flurbiprofen dissolved with polyethylene glycol 3350 (PEG 3350). The second formulation was flurbiprofen encapsulated in poly-ɛ-caprolactone (PɛCL) nanoparticles (NPs), stabilized with poloxamer 188, submitted individually for freeze-drying with PEG 3350 as a cryoprotectant and sterilized by gamma-irradiation. Human skin was obtained from the abdominal region of a healthy patient. The experimental protocol was approved by the Bioethics Committee of Barcelona SCIAS Hospital (Spain), and they obtained the written informed consent forms. After being frozen to -20ºC, the skin samples were cut with a dermatome at 400 µm. The ex vivo permeation study was performed in Franz diffusion cells with a diffusion area of 2.54 cm². Skin samples were placed between two compartment sites, the dermal side in contact with the receptor medium and the epidermis side in contact with the donor chamber to which the formulation was applied. The permeation study was conducted for 24 hours at 32 ± 0.5 °C in accordance with sink conditions. The results were analyzed with an unpaired t-test, and the p-values indicate the formulation with nanoparticles had a higher permeability coefficient, flux, partition parameter, diffusion parameter, and lag time. The applicability of this formulation topically can benefit articulations and ligament inflammation as an alternative to oral drugs.

Keywords: anti-inflammatory drug, flurbiprofen, human skin, nanoparticles, skin permeation

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Authors: Md Abu Saieed

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Crafting and implementing public policy is one of the indispensable works in any form of state and government. But the policy objectives, methods of formulation and tools of implementation might be different based on the ideological nature, historical legacy, structure and capacity of administration and management and other push and factors. Public policy in Islamic economic system needs to be based on the key guidelines of divine scriptures along with other sources of sharia’h. As a representative of Allah (SWT), the governor and other apparatus of the state will formulate and implement public policies which will enable to establish a true welfare state based on justice, equity and equality. The whole life of Prophet Muhammad (pbuh) and his policy in operating state of affairs in Madina is the practical guidelines for the policy actors and professionals in Islamic system of economics. Moreover, policy makers need to be more meticulous in formulating Islamic public policy which meets the needs and demands of contemporary worlds as well.

Keywords: formulation, Islam, public policy, policy factors, Sharia’h

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Authors: D. De-León-Escobedo, D. J. Delgado-Hernández, S. Pérez

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A probabilistic formulation to assess the slopes safety under the hazard of strong storms is presented and illustrated through a slope in Mexico. The formulation is based on the classical safety factor (SF) used in practice to appraise the slope stability, but it is introduced the treatment of uncertainties, and the slope failure probability is calculated as the probability that SF<1. As the main hazard is the rainfall on the area, statistics of rainfall intensity and duration are considered and modeled with an exponential distribution. The expected life-cycle cost is assessed by considering a monetary value on the slope failure consequences. Alternative mitigation measures are simulated, and the formulation is used to get the measures driving to the optimal one (minimum life-cycle costs). For the example, the optimal mitigation measure is the reduction on the slope inclination angle.

Keywords: expected life-cycle cost, failure probability, slopes failure, storms

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Authors: S. L. J. Tan, N. Billa, C. J. Roberts

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Oral delivery of amphotericin B (AmpB) potentially eliminates constraints and side effects associated with intravenous administration, but remains challenging due to the physicochemical properties of the drug such that it results in meagre bioavailability (0.3%). In an advanced formulation, 1) nanostructured lipid carriers (NLC) were formulated as they can accommodate higher levels of cargoes and restrict drug expulsion and 2) a mucoadhesion feature was incorporated so as to impart sluggish transit of the NLC along the gastrointestinal tract and hence, maximize uptake and improve bioavailability of AmpB. The AmpB-loaded NLC formulation was successfully formulated via high shear homogenisation and ultrasonication. A chitosan coating was adsorbed onto the formed NLC. Physical properties of the formulations; particle size, zeta potential, encapsulation efficiency (%EE), aggregation states and mucoadhesion as well as the effect of the variable pH on the integrity of the formulations were examined. The particle size of the freshly prepared AmpB-loaded NLC was 163.1 ± 0.7 nm, with a negative surface charge and remained essentially stable over 120 days. Adsorption of chitosan caused a significant increase in particle size to 348.0 ± 12 nm with the zeta potential change towards positivity. Interestingly, the chitosan-coated AmpB-loaded NLC (ChiAmpB NLC) showed significant decrease in particle size upon storage, suggesting 'anti-Ostwald' ripening effect. AmpB-loaded NLC formulation showed %EE of 94.3 ± 0.02 % and incorporation of chitosan increased the %EE significantly, to 99.3 ± 0.15 %. This suggests that the addition of chitosan renders stability to the NLC formulation, interacting with the anionic segment of the NLC and preventing the drug leakage. AmpB in both NLC and ChiAmpB NLC showed polyaggregation which is the non-toxic conformation. The mucoadhesiveness of the ChiAmpB NLC formulation was observed in both acidic pH (pH 5.8) and near-neutral pH (pH 6.8) conditions as opposed to AmpB-loaded NLC formulation. Hence, the incorporation of chitosan into the NLC formulation did not only impart mucoadhesive property but also protected against the expulsion of AmpB which makes it well-primed as a potential oral delivery system for AmpB.

Keywords: Amphotericin B, mucoadhesion, nanostructured lipid carriers, oral delivery

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Authors: R. O. B. Bitencourt, F. S. Farias, M. C. Freitas, C. J. R. Balduino, E.S. Mesquita, A. R. C. Corval, P. S. Gôlo, E. G. Pontes, V. R. E. P. Bittencourt, I. C. Angelo

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Aedes aegypti larval survival rate was assessed after exposure to blastopores or conidia (mineral oil-in-water formulation or aqueous suspension) of Beauveria bassiana CG 479 propagules (blastospores or conidia). Here, mineral oil was used in the fungal formulation to control Aedes aegypti larvae. 1%, 0.5% or 0.1% mineral oil-in-water solutions were used to evaluate mineral oil toxicity for mosquito larvae. In the oil toxicity test, 0.1% mineral oil solution reduced only 4.5% larval survival; accordingly, this concentration was chosen for fungal oil-in-water formulations. Aqueous suspensions were prepared using 0.01% Tween 80^® in sterile dechlorinated water. A. aegypti larvae (L₂) were exposed in aqueous suspensions or mineral oil-in-water fungal formulations at 1×107 propagules mL^-1; the survival rate (assessed daily, for 7 days) and the median survival time (S₅₀) were calculated. Seven days after the treatment, mosquito larvae survival rates were 8.56%, 16.22%, 58%, and 42.56% after exposure to oil-in-water blastospores, oil-in-water conidia, blastospores aqueous suspension and conidia aqueous suspension (respectively). Larvae exposed to 0.01% Tween 80^® had 100% survival rate and the ones treated with 0.1% mineral oil-in-water had 95.11% survival rate. Larvae treated with conidia (regardless the presence of oil) or treated with blastospores formulation had survival median time (S₅₀) ranging from one to two days. S₅₀ was not determined (ND) when larvae were exposed to blastospores aqueous suspension, 0.01% Tween 80^® (aqueous control) or 0.1% mineral oil-in-water formulation (oil control). B. bassiana conidia and blastospores (mineral oil-in-water formulated or suspended in water) had potential to control A. aegypti mosquito larvae, despite mineral oil-in-water formulation yielded better results in comparison to aqueous suspensions. Here, B. bassiana CG 479 isolate is suggested as a potential biocontrol agent of A. aegypti mosquito larvae.

Keywords: blastospores, formulation, mosquitoes, conidia

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Authors: Gennady M. Kulikov, Svetlana V. Plotnikova

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This paper focuses on implementation of the sampling surfaces (SaS) method for the three-dimensional (3D) stress analysis of functionally graded (FG) laminated elastic and piezoelectric shells. The SaS formulation is based on choosing inside the nth layer In not equally spaced SaS parallel to the middle surface of the shell in order to introduce the electric potentials and displacements of these surfaces as basic shell variables. Such choice of unknowns permits the presentation of the proposed FG piezoelectric shell formulation in a very compact form. The SaS are located inside each layer at Chebyshev polynomial nodes that improves the convergence of the SaS method significantly. As a result, the SaS formulation can be applied efficiently to 3D solutions for FG piezoelectric laminated shells, which asymptotically approach the exact solutions of piezoelectricity as the number of SaS In goes to infinity.

Keywords: electroelasticity, functionally graded material, laminated piezoelectric shell, sampling surfaces method

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Authors: S. Talebnezhad, S. Pourmahdian, D. Soudbar, M. Khosravani, J. Merasi

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Adding toughened polypropylene and plastomer in FFS 3 layered blown film formulation resulted in superior dart impact and MD tear resistance along with acceptable tensile properties in TD and MD. The optimum loading of toughened polypropylene and plastomer in each layer depends on miscibility of polypropylene in polyethylene medium, mechanical properties, welding characteristics in bags top and bottoms and friction coefficient of film surfaces. Film property tests and efficiency of FFS machinery during processing in industrial scale showed that about 4% loading of plastomer and 16% of toughened polypropylene (reactor grade) in middle layer and loading of 0-1% plastomer and 5-19% of toughened polypropylene in other layers results optimum characteristics in the formulation based on 1-butene LLDPE grade with MFR of 0.9 and LDPE grade with MFI of 0.3. Both the plastomer and toughened polypropylene had the MFI of blow 1 and the TiO2 and processing aid masterbatches loading was 2%. The friction coefficient test results also represented the anti-block masterbatch could be omitted from formulation with adding toughened polypropylene due to partial miscibility of PP in PE which makes the surface of films somewhat bristly.

Keywords: FFS 3 layered blown film, toughened polypropylene, plastomer, dart impact, tear resistance

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Authors: T. O. Ikpesu, I. Tongo, A. Ariyo

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This study was conducted to assess the effects of an organophosphate pesticide glyphosate formulation on neurological enzymes in the brain, liver and serum of juvenile Clarias gariepinus, and also to examine the antidotal prospect of Garcinia kola seeds extract. The fish divided into five groups were exposed to different treatments of glyphosate formulation and Garcinia kola seeds extract. Acetyl cholinesterase activities in the brain, liver and serum of the fish were estimated in the experimental and control fishes on day -7, 14, 21 and of 28 by spectrophotometrical methods. The enzyme was significantly (p < 0.05) inhibited in glyphosate formulation test. The inhibition percentages of AChE ranged for the brain, liver and serum between 40.7–59.4%, 50-57% and 27.5–51.3%, respectively. The aberrated parameters were recovered in G. kola seeds extract treated aquaria, and was dose and time dependent. The present study demonstrated that in vivo glyphosate formulation exposure caused AChE inhibition in the brain, liver and the serum. The brain tissue, however, might be suggested as a good indicator tissue for aquatic pollutants exposure in the fish and G. kola seeds extract has shown to be a good remedy for neurology restoration in a noxious circumstance. The findings has shown that xenobiotics could be eliminated from aquatic organisms, especially fish, and could be put into practice in areas at risk of pollutants. This approach can reduce the risks of biomagnification of poison in sea food. Hence, formulation of this plant extracts into capsule should be encouraged and supported.

Keywords: glyphosate, Clarias gariepinus, brain, Garcinia kola, acetyl cholinesterase, enzymes

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Authors: Nazmul Huda, Ashik Mosaddik, Abdul Awal, Shafiqur Rahman, Rukhsana Shaheen, Mustofa Nabi

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Polyherbal formulation Sharbat Deenar is a very popular unani medicine in Bangladesh. It is usually used for different kinds of liver disorders. In absence of reliable and inadequate hepatoprotective agents in conventional medicine, the herbal preparations are preferred for liver diseases. The present study was designed to evaluate the hepatoprotective activity of Sharbat Deenar on carbon tetrachloride (CCl₄) induced hepatotoxicity in male Long-Evans albino rats. Group I served as normal control and received neither formulation nor carbon tetrachloride. Group II received only CCl₄ 1mL/kg body weight of rat intraperitoneally for consecutive 14 days. Group III received CCl₄ 1mL/kg body weight of rat intraperitoneally and Silymarin, in dose 50mg/kg body weight of rat orally. Group IV received CCl₄ 1mL/kg body weight of rat intraperitoneally and Sharbat Deenar 1mL/kg body weight of rat for the same 14 consecutive days. At the end of the study, hepatoprotective activity was evaluated by the levels of total bilirubin, alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP). Histopathological study of rat liver was also carried out. The results showed that polyherbal formulation Sharbat Deenar exhibited a significant hepatoprotective effect. Such an outcome seems to be the synergistic effect of all ingredients of tested herbal formulation. Although this study suggests that Sharbat Deenar may be used to cure or minimize various liver diseases, it needs further study to attain the clarity of mechanism and safety.

Keywords: polyherbal formulation, sharbat deenar, carbon tetrachloride, silymarin, hepatoprotective

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Authors: Swapnila V. Shinde, Hemant P. Joshi, Sumit R. Dhas, Dhananjaysingh B. Rajput

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The objective of the present study is to develop hydro-dynamically balanced system for atenolol, β-blocker as a single unit floating tablet. Atenolol shows pH dependent solubility resulting into a bioavailability of 36%. Thus, site specific oral controlled release floating drug delivery system was developed. Formulation includes novice use of rate controlling polymer such as locust bean gum (LBG) in combination of HPMC K4M and gas generating agent sodium bicarbonate. Tablet was prepared by direct compression method and evaluated for physico-mechanical properties. The statistical method was utilized to optimize the effect of independent variables, namely amount of HPMC K4M, LBG and three dependent responses such as cumulative drug release, floating lag time, floating time. Graphical and mathematical analysis of the results allowed the identification and quantification of the formulation variables influencing the selected responses. To study the gastrointestinal transit of the optimized gastro-retentive formulation, in vivo gamma scintigraphy was carried out in six healthy rabbits, after radio labeling the formulation with 99mTc. The transit profiles demonstrated that the dosage form was retained in the stomach for more than 5 hrs. The study signifies the potential of the developed system for stomach targeted delivery of atenolol with improved bioavailability.

Keywords: floating tablet, factorial design, gamma scintigraphy, antihypertensive model drug, HPMC, locust bean gum

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Authors: Venkat Garigapati

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To date, more than a dozen oligonucleotide products are approved as injectable products for clinical use. However, there is no single oligo nucleotide product approved for clinical use. Oral delivery of oligo nucleotides is patient friendly administration however, many challenges involved in the development of oral formulation. Over the course of last twenty plus years, the research in this space aimed to address these challenges. This paper describes the issues involved in solubility, stability, enzymatic (nuclease) induced degradation, and permeation of nucleotides in the Gastrointestinal (GI) and how to overcome these challenges. Also, the translation of in vitro data to in vivo models hinders the formulation development. This paper describes the challenges involved in the development of Oligo Nucleotide products for oral administration. It also discusses the chemistry and formulation strategies for oral administration of oligonucleotides.

Keywords: oral adminstration, oligo nucleotides, stability, permeation, gastrointestinal tract

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Authors: Phanindra Prasad Thummala, Umran Tezcan Un, Ahmet Ozan Celik

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Removal of CO₂ by MEA (monoethanolamine) in structured packing columns depends highly on the gas-liquid interfacial area and film thickness (liquid load). CFD (computational fluid dynamics) is used to find the interfacial area, film thickness and their impact on mass transfer in gas-liquid flow effectively in any column geometry. In general modeling approaches used in CFD derive mass transfer parameters from standard correlations based on penetration or surface renewal theories. In order to avoid the effect of assumptions involved in deriving the correlations and model the mass transfer based solely on fluid properties, state of art approaches like one fluid formulation is useful. In this work, the one fluid formulation was implemented and evaluated for modeling the physical mass transfer of CO₂ by N₂O analogy in OpenFOAM CFD software. N₂O analogy avoids the effect of chemical reactions on absorption and allows studying the amount of CO₂ physical mass transfer possible in a given geometry. The computational domain in the current study was a flat plate with gas and liquid flowing in the countercurrent direction. The effect of operating parameters such as flow rate, the concentration of MEA and angle of inclination on the physical mass transfer is studied in detail. Liquid side mass transfer coefficients obtained by simulations are compared to the correlations available in the literature and it was found that the one fluid formulation was effectively capturing the effects of interface surface instabilities on mass transfer coefficient with higher accuracy. The high mesh refinement near the interface region was found as a limiting reason for utilizing this approach on large-scale simulations. Overall, the one fluid formulation is found more promising for CFD studies involving the CO₂ mass transfer.

Keywords: one fluid formulation, CO₂ absorption, liquid mass transfer coefficient, OpenFOAM, N₂O analogy

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Authors: Abhishek Pandey

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Capping and lamination are the most common tablet defects with poorly compressible drugs the common example of that Ibuprofen and Acetaminophen. Generally both these drugs are compressed by wet granulation method which is very time consuming process Ibuprofen and Acetaminophen is widely used as prescription & non-prescription medicine. Ibuprofen mainly used in the treatment of mild to moderate pain related to headache, migraine, postoperative condition and in the management of spondylitis, osteoarthritis Acetaminophen used as an analgesic and antipyretic drug. Ibuprofen having high tendency of sticking to punches of tablet punching machine while Acetaminophen is not ordinarily compressible to tablet formulation because Acetaminophen crystals are very hard and brittle in nature and fracture very easily when compressed producing capping and laminating tablet defects therefore wet granulation method is used to make them compressible. The aim of study was to prepare Ibuprofen and Acetaminophen tablets by direct compression technique and their evaluation. In this Investigation tablets were prepared by using directly compressible grade excipients. Dibasic calcium phosphate, lactose anhydrous (DCL21), microcrystalline cellulose (Avicel PH 101). In order to obtain best or optimize formulation nine different formulations were generated among them batch F5, F6, F7 shows good results and within the acceptable limit. Formulation (F7) selected as optimize product on the basis of evaluation parameters.

Keywords: capping, lamination, tablet defects, direct compression

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Authors: Temami Oussama, Bessais Lakhdar, Hamadi Djamal, Abderrahmani Sifeddine

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The analysis of complex structures encourages the engineer to make simplifying assumptions, sometimes attempting the analysis of the whole structure as complex as it is, and it can be done using the finite element method (FEM). In the modeling of complex structures by finite elements, various elements can be used: beam element, membrane element, solid element, plates and shells elements. These elements formulated according to the classical formulation and do not generally share the same nodal degrees of freedom, which complicates the development of a compatible model. The compatibility of the elements with each other is often a difficult problem for modeling complicated structure. This compatibility is necessary to ensure the convergence. To overcome this problem, we have proposed finite elements with a rotational degree of freedom. The study used is based on the strain approach formulation with 2D and 3D formulation with different degrees of freedom at each node. For the comparison and confrontation of results; the finite elements available in ABAQUS/Standard are used.

Keywords: compatibility requirement, complex structures, finite elements, modeling, strain approach

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Authors: Abhay Asthana, Shally Toshkhani, Gyati Shilakari

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The objective of the present research work is to develop a topical biodegradable dermal patch based formulation to aid accelerated wound healing. It is always better for patient compliance to be able to reduce the frequency of dressings with improved drug delivery and overall therapeutic efficacy. In present study optimized formulation using biodegradable components was obtained evaluating polymers and excipients (HPMC K4M, Ethylcellulose, Povidone, Polyethylene glycol and Gelatin) to impart significant folding endurance, elasticity, and strength. Molten gelatin was used to get a mixture using ethylene glycol. Chitosan dissolved in acidic medium was mixed with stirring to Gelatin mixture. With continued stirring to the mixture Curcumin was added with the aid of DCM and Methanol in an optimized ratio of 60:40 to get homogenous dispersion. Polymers were dispersed with stirring in the final formulation. The mixture was sonicated casted to get the film form. All steps were carried out under strict aseptic conditions. The final formulation was a thin uniformly smooth textured film with dark brown-yellow color. The film was found to have folding endurance was around 20 to 21 times without a crack in an optimized formulation at RT (23°C). The drug content was in range 96 to 102% and it passed the content uniform test. The final moisture content of the optimized formulation film was NMT 9.0%. The films passed stability study conducted at refrigerated conditions (4±0.2°C) and at room temperature (23 ± 2°C) for 30 days. Further, the drug content and texture remained undisturbed with stability study conducted at RT 23±2°C for 45 and 90 days. Percentage cumulative drug release was found to be 80% in 12h and matched the biodegradation rate as tested in vivo with correlation factor R2>0.9. In in vivo study administration of one dose in equivalent quantity per 2 days was applied topically. The data demonstrated a significant improvement with percentage wound contraction in contrast to control and plain drug respectively in given period. The film based formulation developed shows promising results in terms of stability and in vivo performance.

Keywords: wound healing, biodegradable, polymers, patch

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Authors: P. C. Ihenacho, M. Burby, G. G. Nasr, G. C. Enyi

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Formulation of a low oil-water ratio drilling mud with vegetable oil continuous phase without adversely affecting the mud rheology and stability has been a major challenge. A low oil-water ratio is beneficial in producing low fluid loss which is essential for wellbore stability. This study examined the possibility of 50/50 oil-water ratio invert emulsion drilling mud using a vegetable oil continuous phase. Jatropha oil was used as continuous phase. 12 ml of egg yolk which was separated from the albumen was added as the primary emulsifier additive. The rheological, stability and filtration properties were examined. The plastic viscosity and yield point were found to be 36cp and 17 Ib/100 ft2 respectively. The electrical stability at 48.9ºC was 353v and the 30 minutes fluid loss was 6ml. The results compared favourably with a similar formulation using 70/30 oil - water ratio giving plastic viscosity of 31cp, yield point of 17 Ib/100 ft2, electrical stability value of 480v and 12ml for the 30 minutes fluid loss. This study indicates that with a good mud composition using guided empiricism, 50/50 oil-water ratio invert emulsion drilling mud is feasible with a vegetable oil continuous phase. The choice of egg yolk as emulsifier additive is for compatibility with the vegetable oil and environmental concern. The high water content with no fluid loss additive will also minimise the cost of mud formulation.

Keywords: environmental compatibility, low cost of mud formulation, low fluid loss, wellbore stability

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Authors: Gajera Lalit, Shah Pranav, Shah Shailesh

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Venlafaxine hydrochloride has a short elimination half-life of 5 ± 2 hr, and absorption window in the upper part of gastrointestinal tract. The conventional tablets need to be administered two to three times a day and possess an oral bioavailability of 45%. The purpose of this study was to formulate gastroretentive effervescent floating tablets of Venlafaxine HCl. Different grades of HPMC namely K15M, K4M, K100M and E15LV were employed as swelling polymers whereas sodium bicarbonate was employed as gas generating agent. The direct compression method was employed for the formulation of tablets. The tablets were evaluated in terms of hardness, friability, weight variation, drug content, water uptake, in-vitro floating behavior and in-vitro drug release study. All the formulations exhibited very short floating lag time of < 1 min and total floating time of 12 hr. Formulation L3 containing 25 mg and 75 mg of HPMC E15 LV and HPMC K15M respectively exhibited complete drug release within 12 hrs.

Keywords: venlafaxine HCl, hydroxyl propyl methylcellulose, floating gastro retentive tablets, in-vitro drug release, non-fickian diffusion

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Authors: U. Umadevi, T. Umakanthan

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Globally, mycotic dermatitis is very common but there is no single proven specific allopathic treatment regimen. In this study, domestic animals with skin diseases of different age and breed from geographically varied regions of Tamil Nadu state, India were employed. Most of them have had previous treatment with native and allopathic medicines without success. Clinically, the skin lesions were found to be mild to severe. The trial animals were treated with poly herbal formulation (ointment) prepared using the indigenous medicinal plants – viz Andrographis paniculata, Lawsonia inermis and Madhuca longifolia. Allopathic antifungal drugs and ointments, povidone iodine and curabless (Terbinafine HCl, Ofloxacin, Ornidazole, Clobetasol propionate) were used in control. Comparatively, trial animals were found to have lesser course of treatment time and higher recovery rate than control. In Ethnoveterinary, this combination was tried for the first time. This herbal formulation is economical and an alternative for skin diseases.

Keywords: allopathic drugs, dermatitis, domestic animals, poly herbal formulation

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Authors: Kazunari Ozaki, Mitsuru Kageyama, Kenki Miyazawa, Yoshio Nakamura

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Background: Kampo (Japanese Traditional medicine) is a medicine traditionally practiced in Japan, based on ancient Chinese medicine. Most Kampo doctors have used decoction of crude drug pieces for treatment. 93% of the Kampo drugs sold in Japan are Kampo products nowadays. Of all Kampo products, 81% of them are Kampo extract formulations for prescription, which is prepared in powdered or granulated form from medicinal crude drug extracts mixed with appropriate excipient. Physicians with medical license for Western medicine prescribe these Kampo extract formulations for prescription in Japan. Objectives: Our study aims at presenting a brief history of Kampo extract formulations for prescription in Japan. Methods: Systematic searches for relevant studies were conducted using not only printed journals but also electronic journals from the bibliographic databases, such as PubMed/Medline, Ichushi-Web, and university/institutional websites, as well as search engines, such as Google and Google Scholar. Results: The first commercialization of Kampo extract formulations for general use (or OTC (over-the-counter) Kampo extract formulation) was achieved after 1957. The number of drugs has been subsequentially increased, reaching 148 Kampo extract formulation for prescription currently. Conclusion: We provide a history of Kampo extract formulations for prescription in Japan. The originality of this research is that it analyzes the background history of Kampo in parallel with relevant transitions in the government and insurance systems.

Keywords: health insurance system, history, Kampo, Kampo extract formulation for prescription, OTC Kampo extract formulation, pattern corresponding prescription (Ho-sho-so-tai) system

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Authors: Yaowaporn Sangsen, Kittisak Likhitwitayawuid, Boonchoo Sritularak, Kamonthip Wiwattanawongsa, Ruedeekorn Wiwattanapatapee

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Novel solid lipid nanoparticles (SLNs) were developed to improve oral bioavailability of oxyresveratrol (OXY). The SLNs were prepared by a high speed homogenization technique, at an effective speed and time, using Compritol® 888 ATO (5% w/w) as the solid lipid. The appropriate weight proportions (0.3% w/w) of OXY affected the physicochemical properties of blank SLNs. The effects of surfactant types on the properties of the formulations such as particle size and entrapment efficacy were also investigated. Conclusively, Tween 80 combined with soy lecithin was the most appropriate surfactant to stabilize OXY-loaded SLNs. The mean particle size of the optimized formulation was 134.40 ± 0.57 nm. In vitro drug release study, the selected S2 formulation showed a retarded release profile for OXY with no initial burst release compared to OXY suspension in the simulated gastrointestinal fluids. Therefore, these SLNs could provide a suitable system to develop for the oral OXY delivery.

Keywords: solid lipid nanoparticles, physicochemical properties, in vitro drug release, oxyresveratrol

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Authors: Santhosh A. K.

Abstract:

This work presents an efficient monolithic finite element strategy for solving thermo-fluid-structure interaction problems involving compressible fluids and linear-elastic structure. This formulation uses displacement variables for structure and velocity variables for the fluid, with no additional variables required to ensure traction, velocity, temperature, and heat flux continuity at the fluid-structure interface. Rate of convergence in each time step is quadratic, which is achieved in this formulation by deriving an exact tangent stiffness matrix. The robustness and good performance of the method is ascertained by applying the proposed strategy on a wide spectrum of problems taken from the literature pertaining to steady, transient, two dimensional, axisymmetric, and three dimensional fluid flow and conjugate heat transfer. It is shown that the current formulation gives excellent results on all the case studies conducted, which includes problems involving compressibility effects as well as problems where fluid can be treated as incompressible.

Keywords: linear thermoelasticity, compressible flow, conjugate heat transfer, monolithic FEM

Procedia PDF Downloads 198

Authors: Navneet Sharma, Himanshu Ojha, Dharam Pal Pathak, Rakesh Kumar Sharma

Abstract:

Radio-nuclides decontamination is an important task because any extra second of deposition leads to deleterious health effects. We had developed and characterise nanoemulsion of p-tertbutylcalix[4]arens using phase inversion temperature (PIT) method and evaluate its decontamination efficacy (DE). The solubility of the drug was determined in various oils and surfactants. Nanoemulsion developed with an HLB value of 11 and different ratios of the surfactants 10% (7:3, w/w), oil (20%, w/w), and double distilled water (70%) were selected. Formulation was characterised by multi-photon spectroscopy and parameters like viscosity, droplet size distribution, zeta potential and stability were optimised. In vitro and Ex vivo decontamination efficacy (DE) was evaluated against Technetium-99m, Iodine-131, and Thallium-201 as radio-contaminants applied over skin of Sprague-Dawley rat and human tissue equivalent model. Contaminants were removed using formulation soaked in cotton swabs at different time intervals and whole body imaging and static counts were recorded using SPECT gamma camera before and after decontamination attempt. Data were analysed using one-way analysis of variance (ANOVA) and was found to be significant (p <0.05). DE of the nanoemulsion loaded with p-tertbutylcalix[4]arens was compared with placebo and recorded to be 88±5%, 90±3% and 89±3% for 99mTc, 131I and 201Tl respectively. Ex-vivo complexation study of p-tertbutylcalix[4]arene nanoemulsion with surrogate nuclides of radioactive thallium and Iodine, were performed on rat skin mounted on Franz diffusion cell using high-resolution sector field inductively coupled plasma mass spectroscopy (HR-SF-ICPMS). More than 90% complexation of the formulation with these nuclides was observed. Results demonstrate that the prepared nanoemulsion formulation was found efficacious for the decontamination of radionuclides from a large contaminated population.

Keywords: p-tertbutylcalix[4]arens, skin decontamination, radiological emergencies, nanoemulsion, iodine-131, thallium-201

Procedia PDF Downloads 399

Authors: Dwarakanadha Reddy Peram, D. Swarnalatha, C. Gopinath

Abstract:

The main aim of this research work was to design and development characterization of Pioglitazone transdermal drug delivery system by using various polymers such as Olibanum with different concentration by solvent evaporation technique. The prepared formulations were evaluated for different physicochemical characteristics like thickness, folding endurance, drug content, percentage moisture absorption, percentage moisture loss, percentage elongation break test and weight uniformity. The diffusion studies were performed by using modified Franz diffusion cells. The result of dissolution studies shows that formulation, F3 (Olibanum with 50 mg) showed maximum release of 99.95 % in 12hrs, whereas F1 (Olibanum and EC backing membrane) showed minimum release of 93.65% in 12 hr. Based on the drug release and physicochemical values obtained the formulation F3 is considered as an optimized formulation which shows higher percentage of drug release of 99.95 % in 12 hr. The developed transdermal patches increase the therapeutic efficacy and reduced toxic effect of pioglitazone.

Keywords: pioglitazone, olibanum, transdermal drug delivery system, drug release percantage

Procedia PDF Downloads 206

Authors: Cagri Mollamahmutoglu, Ali Mercan, Aykut Levent

Abstract:

Studies concerning the microstructures are becoming more important as the utilization of various micro-electro mechanical systems (MEMS) are increasing. Thus in recent years, thermal buckling and vibration analysis of microstructures have been subject to many investigations that are utilizing different numerical methods. In this study, thermal effects on mechanical response of a functionally graded (FG) Timoshenko micro-beam are presented in the framework of a mixed finite element formulation. Size effects are taken into consideration via modified couple stress theory. The mixed formulation is based on a function which in turn is derived via Gateaux Differential scientifically. After the resolution of all field equations of the beam, a potential operator is carefully constructed. Then this operator is used for the manufacturing of the functional. Usual procedures of finite element approximation are utilized for the derivation of the mixed finite element equations once the potential is obtained. Resulting finite element formulation allows usage of C₀ type simple linear shape functions and avoids shear-locking phenomena, which is a common shortcoming of the displacement-based formulations of moderately thick beams. The developed numerical scheme is used to obtain the effects of thermal loads on the static bending, free vibration and buckling of FG Timoshenko micro-beams for different power-law parameters, aspect ratios and boundary conditions. The versatility of the mixed formulation is presented over other numerical methods such as generalized differential quadrature method (GDQM). Another attractive property of the formulation is that it allows direct calculation of the contribution of micro effects on the overall mechanical response.

Keywords: micro-beam, functionally graded materials, thermal effect, mixed finite element method

Procedia PDF Downloads 138

Authors: Abdul Karim Zulkarnain, Marchaban, Subagus Wahyono, Ratna Asmah Susidarti

Abstract:

Mahkota Dewa contains phalerin which has activity as sun screen. In this study, 13 formulations of cream oil in water (o/w) were prepared and tested for their physical characteristics. The physical characteristics were then used for determining the optimum formula. This study aimed to explore the physical stability of optimized formulation of cream, its sun protecting factor (SPF) values using in vitro and in vivo tests. The optimum formula of o/w cream were prepared based on Simplex Lattice Design (LSD) method using software Design Expert®. The formulation of o/w cream were varied based on the proportion of cetyl alcohol, mineral oil and tween 80. The difference of physical characteristic of optimum and predicted formula was tested using t-test with significant level of 95%. The optimum formula of o/w cream was the formula which consists of cetyl alcohol 9.71%, mineral oil, 29%, and tween 80 3.29. Based on t-test, there was no significant difference of physical characteristics of optimum and predicted formulation. Viscosity, spread power, adhesive power, and separation volume ratio of o/w at week 0-4 were relatively stable. The o/w creams were relatively stable at extreme temperature. The o/w creams from mahkota dewa, phalerin, and benzophenone have SPF values of 21.32, 33.12, and 42.49, respectively. The formulas did not irritate the skin based on in vivo test.

Keywords: cream, stability, In vitro, In vivo

Procedia PDF Downloads 227

Authors: Bernt O. Myrvold

Abstract:

Lignosulfonates (LS) find widespread use as dispersants, binders, anti-oxidants, and fillers. In most of these applications LS is used in formulation together with a number of other components. To better understand the interactions between LS and water and possibly other components in a formulation, the Hansen solubility parameters have been determined for some LS. The Hansen solubility parameter splits the total solubility parameter into three components, the dispersive, polar and hydrogen bonding part. The Hansen solubility parameter was determined by comparing the solubility in a number of solvents and solvent mixtures. We have found clear differences in the solubility parameters, with softwood LS being closer to water than hardwood LS.

Keywords: Hansen solubility parameter, lignosulfonate (LS), solubility, solvent

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Authors: Tansel Comoglu

Abstract:

Orally fast disintegrating tablets (FDTs or ODTs) have become popular during the last decade, and manufacturing of ODTs is getting a rapidly growing area in the pharmaceutical industry. The concept of ODTs has emerged from the desire to provide patients with more conventional means of taking their medication. Drugs, that have satisfactory absorption from the oral mucosa or aimed for immediate therapeutic activity can be formulated in ODTs. After placing the ODT into the mouth, these tablets dissolve or disintegrate in the mouth usullay less than a minute, in the absence of additional water. Even though the ODT technology has taken an important path, as proved by a large group of commercial products on the drug market, there are so many problems to be solved in ODT formulations such as; formulation of hydrophobic drugs is stil a challenge, especially when the amount of drug is high. As these tablets dissolve or disintegrate in the mouth without the need of additional water, taste masking of active ingredients becomes essential in these systems because the drug is entirely released in the mouth. In ODT technology, coping with the taste of drugs is still a challenge. Resins or sweeteners or other techniques are also used in the formulation to aid taste-masking of the API. Another important factor to consider is whether they can be manufactured using conventional equipment and processes, as this will have a positive influence on manufacturing costs. Some products, however, may require a more costly, special unitdose packaging if the dosage form is fragile. In this overview, benefits, various formulation technologies, clinical studies and some future research trends of ODTs will be discussed.

Keywords: orally fast disintegrating tablets, benefits, formulation technologies, future research trends

Procedia PDF Downloads 359