Improved oral bioavailability of lipophilic substances can be achieved using self-emulsifying drug delivery systems. However, because the properties of self-emulsifying are greatly influenced by surfactant amount and type, type of oil used, droplet size, charge, cosolvents, and physiological variables, the synthesis of self-emulsifying is highly complex; consequently, only a small number of excipient self-emulsifying formulations has been developed so far for clinical use. This study reports a highly effective procedure for developing self-emulsifying formulations using a novel approach based on the hydrophilic-lipophilic difference theory. Microemulsion characteristics, such as the constituents and amounts of oil and surfactant electrolyte concentration and temperature, were optimized to produce high-quality self-emulsifying drug delivery systems. Furthermore, in vitro lipolysis and in vivo bioavailability studies of fenofibrate, a highly lipophilic oral drug, loaded self-emulsifying dosage form were conducted. The self-emulsifying drug delivery system used in this study comprised soybean oil, water with a specific salinity, sodium dioctyl sulphosuccinate as a surfactant, and orlistat as a lipase inhibitor. The hydrophilic-lipophilic difference-based approach involved fewer experiments and allowed for the development of an efficient self-emulsifying dosage form with a relatively low surfactant concentration when compared to previous works. The salinity and equivalent alkane carbon number were optimized, with the proper selection of the type and amount of surfactant, to obtain a bicontinuous microemulsion (Winsor type III) that can be fully diluted with water. In vitro lipolysis was investigated in fasting and feeding settings, which showed a significant dosage form digestion by lipase enzyme; orlistat was successfully used to overcome dosage digestion and drug precipitation problem. In vivo experiments in rats involved oral gavage with a self-emulsifying dosage form containing fenofibrate (20 mg/kg). The pharmacokinetic profile of fenofibric acid showed remarkable enhancement in the bioavailability (F-95%). These findings demonstrate that the hydrophilic-lipophilic difference approach is a practical, scalable, and easy technique for self-emulsifying drug delivery system formulation development. Keywords: HLD theory, fenofibrate, SEDDS, lipolysis
Abstract
The current research aims to identify mental health and its role in promoting self-confidence and positive behavior of female university students. The researcher adopted the descriptive analytical approach in this research. The researcher depended on the availability of sources and references, literature, and previous field studies to analyze and study all aspects related to mental health and its role in promoting self-confidence and positive behavior of university students and then expand its importance and identify the areas of mental health, self-confidence, positive behavior, and university. The second chapter included the concept of mental health, the importance of the study, the most important factors of health and psyc
This paper proposed a new method for network self-fault management (NSFM) based on two technologies: intelligent agent to automate fault management tasks, and Windows Management Instrumentations (WMI) to identify the fault faster when resources are independent (different type of devices). The proposed network self-fault management reduced the load of network traffic by reducing the request and response between the server and client, which achieves less downtime for each node in state of fault occurring in the client. The performance of the proposed system is measured by three measures: efficiency, availability, and reliability. A high efficiency average is obtained depending on the faults occurred in the system which reaches to
... Show MoreBackground: Coronary artery disease (CAD) is one of the leading causes of death worldwide. Clopidogrel, antiplatelet drug, has been widely used for management of CAD. Arylesterase, the activity of Paraoxonase-1 (PON-1), is mainly contributed in the biotransformation of clopidogrel to its active thiol form. The purpose of this study was to investigate the effect of receiving clopidogrel drug on the arylesterase activities in CAD patients. The effect of receiving clopidogrel drug on the antioxidant activity of arylesterase was also monitored by determination of malondialdehyde (MDA) level. Methods: One hundred CAD patients, who were followed-up for 5 days after reciving clopidogrel, and 50 healthy volunteers were included in our study
... Show MoreFor many years it was argued that there may be a gender differences in adverse drug reactions (ADRs). This assumption was based on many possible factors such as hormonal or behavior differences, and it was not clearly identified since the female gender was not preferred to be enrolled in many clinical trials. The primary aim of this study was to assess the extent of possibly relevant gender differences in drug–ADRs regarding causality, severity, preventability, seriousness, expectedness and outcome. While the secondary aim was to assess for which group of drugs and for which ADRs gender differences are identified most often. The study was a retrospective one that depends on processing a specially selected group of data obtained from th
... Show MoreThe present work involved designing and synthesizing of a series of new. compounds which their molecules are composed from two biologically active components namely sulfamethoxazole or β-lactam containing drugs and cyclic imides. The target new compounds were synthesized by two steps in the first one a series of six bis (N-drug phthalamic acid_4-yl) ketone (1-6) were prepared from the reaction of sulfamethoxazole or β-lactam containing drugs with benzophenone 3, 3′, 4, 4′ -tetracarboxylic dianhydride.
In the second step, compounds (1-6) were introduced in dehydration reaction via fusion process producing the target compounds bis (N-drug phthalimidyl-4-yl) ketone (7-12). The antibacterial and antifungal high
... Show MoreThree N-(hydroxylphenyl) dimethylmaleimides were directly prepared in good yields (81-86)% from the reaction of dimethylmaleic anhydride with amino phenols. The prepared imides were esterified to the corresponding benzoates, methacrylates and cinnamates via their reaction with different acid chlorides in the presence of triethylamine. The prepared esters were tested as plasticizers for PVC via preparing of thirty six samples of PVC with the prepared esters in certain weight ratio followed by recording their softening points. Comparison the results with the universal plasticizers for PVC (DOP) and (DBP) indicated that the prepared esters in general have high plasticizing efficiency.
The high carbon dioxide emission levels due to the increased consumption of fossil fuels has led to various environmental problems. Efficient strategies for the capture and storage of greenhouse gases, such as carbon dioxide are crucial in reducing their concentrations in the environment. Considering this, herein, three novel heteroatom-doped porous-organic polymers (POPs) containing phosphate units were synthesized in high yields from the coupling reactions of phosphate esters and 1,4-diaminobenzene (three mole equivalents) in boiling ethanol using a simple, efficient, and general procedure. The structures and physicochemical properties of the synthesized POPs were established using various techniques. Field emission scanning elect
... Show MoreAqueous extract of poppy plant) Papaver nudicaule) with five concentrations (50, 100, 150, 200 and 250) mg/l were used to anesthetize fingerlings of the common carp Cyprinus carpio (Mean total length 8.91 ± 0.31 cm and mean total weight 7.72 ± 1.19 gm) instead of the traditional use of MS-222. Results showed that extracted solution of poppy have partial and overall anesthesia effect on these fishes with inverse relationship between the concentrations used and the time needed to reach partial and overall anesthesia, and also direct relationship between concentrations used and time needed for fish recovery. Best results were obtained by using a concentration of 250 mg/l, where time for partial anesthesia was 8 ± 1.52 m
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