Nanoemulsion is considered to be a new and exciting field of research that seeks to exploit the attractive properties of components to improve oral delivery of drugs like candesartan cilexetil used in the management of chronic diseases. Candesartan cilexetil is a lipophilic acidic drug with a half-life of about (5-10) hour and absolute bioavailability of (14-40%). For this reason, the study target was to formulate and characterize candesartan cilexetil nanoemulsions that could improve solubility, dissolution and stability of the lipophilic drug candesartan cilexetil. The solubility of candesartan cilexetil was checked in various vehicles in order to choose the best solubilizing components for building up an efficient nanoemulsion based on regulating hydrophilic/lipophilic balance (HLB) value above 10, and then pseudo-ternary phase diagram was used as a useful tool to evaluate the nanoemulsion domain. The nanoemulsion formulations were prepared using various concentrations of cinnamon oil, tween 80 with poloxamer mixture and transcutol HP as oil, surfactant mixture and co-surfactant respectively by aqueous titration method at surfactant/co-surfactant ratios of 3:1 and 4:1 and varying the type of poloxamer in each ratio. The prepared nanoemulsions were tested for nanodispersion stability studies, droplet size distribution, polydispersity index, zeta potential, viscosity, filter paper spreadability, dye miscibility, electroconductivity, pH, percent transmittance, surface tension, refractive index, morphology and drug dissolution. It was found that release rate and extent for all prepared nanoformulations were significantly higher (p < 0.05) than marketed tablet formulation as well as plain drug powder. The results demonstrated that, the potential use of this system is a perfect technique for improving solubility and dissolution of candesartan cilexetil.
Abstract. The aim of the present study was to enhance the dissolution rate of meloxicam (MLX), a practically water-insoluble drug by preparation of solid dispersion using a hydrophilic polymer, poloxamer 188 (PXM). The kneading technique was used to prepare solid dispersions. A 3 2 full factorial design approach was used for optimization wherein the drug, polymer ratio (X 1 ), and the kneading time (X 2 ) were selected as independent variables and the dissolution efficiency at 60 min (%DE 60 ) and yield percent were selected as the dependent variable. Multiple linear regression analysis revealed that for obtaining higher dissolution of MLX from PXM solid dispersions, a high level of X 1 and a high level of X 2 were suitable. The use of a factorial design approach helped in optimization of the preparation and formulation of solid dispersion. The optimized formula was characterized by solubility studies, angle of repose, and contact angle; Fourier transform infrared spectroscopy, differential scanning calorimetry, x-ray diffraction studies, and scanning electron microscopy demonstrated that enhanced dissolution of MLX from solid dispersion might be due to a decrease in the crystallinity of MLX and PXM. Analysis of dissolution data of optimized formula indicated the best fitting with KorsemeyerPeppas model and the drug release kinetics as Fickian diffusion. In conclusion, dissolution enhancement of MLX was obtained by preparing its solid dispersion with PXM using kneading technique.
Key words: wheat flour, whole meal barley, gelatinized corn flour, balady bread, chemical parameters, rheology, quality This study was focused on substituting a part of wheat flour (WF) with whole meal barley (WBF), gelatinized corn flour (GCF) and both of them in balady bread, as an attempt to solve the shortage in wheat production. Chemical, rheological, color and sensory properties were determined. Stalling of balady bread was evaluated. It is found that the incorporation of WBF and GCF into balady bread improved protein, fat, fiber, ash, β-glucan and minerals (Ca, P, K and Fe). Blending WBF or GCF with WF gave higher rheological parameters of dough; meanwhile lightness of the produced breads was reduced. Also, sensory properties of the separation layers and roundness were not affected significantly, but a significant difference was observed in taste, crust colour and odour at replacement level of 30%. Generally, WF supplemented with WBF:GCF (30:15%) did not affected technological quality of balady bread and improved its nutritive values.
late gluten-free bakery products. The gluten-free bakery products available on the market present poor organoleptic quality, not comparable to wheat ones. Research and development is needed to improve the structure, mouth feel, texture, acceptability and shelf-life of these products. Results from a number of recent studies have highlighted the need for an improvement in the quality of cereal based gluten-free products. Reduced volume, tough and/or dense texture, and reduced flavor development are among the problems that gluten-free bakery products are suffering from [Sumnu et al., 2010].Although the tiger nut cultivation dates back to ancient Egypt, where tubers were found in sarcophagi and tombs of the earliest dynasties, it is largely unexploited [Tigernuts Traders, 2013]. Tiger nut (Cyperus esculentus) belongs to the family Cyperaceae and the order, Cyperales. Tiger nut is a tuber that is grown in the soil and is found worldwide in warm and temperate zones, occurring in Southern Europe and Africa. It has a dimension ranging from 6-10 mm and occurs in different varieties. The color is brown and has a sweet flavor when eaten. Tiger nut has been used extensively mainly for human consumption in Spain [Ukwuru et al., 2011; Tigernuts Traders, 2013] and eaten cold as drink. Tiger nut can be extracted into milk like liquid that is treated and bottled. The flour is used to make cakes and biscuits while oil is used for cooking [Wise, 2013].During the last decade, considerable efforts have been directed towards improving the gluten-free product qual- The effect of using tiger nut flour to improve the functional properties of gluten-free biscuit was explored. Corn flour in the biscuit formulation was replaced at three levels, 10, 20, and 30% with tiger nut flour (TNF). Biscuit containing only corn flour was used as control. Prepared biscuits were analyzed for their proximate composition, physical properties, diameter, thickness, color, texture, and were subjected to measurements using differential scanning calorimetery (DSC) and scanning electron microscopy (SEM).Incorporation of tiger nut flour resulted in a significant increase in fibre and ash contents and in a decrease in protein content. The spread ratio of the biscuits increased significantly by increasing TNF content, which is considered a desirable quality attribute. Tiger nut-containing biscuits exhibited lower total color difference ∆E value compared to the control sample.Thermal characteristics of TNF-containing biscuits differed significantly (P≤0.05) from the control where TNF resulted in decreased onset gelatinization temperature (To) and peak temperature (Tp). Furthermore, enthalpies of control biscuits were significantly higher than of those containing TNF; that might be due to partial gelatinization since their enthalpies were smaller than in control biscuits.Measurement of baked biscuits texture showed that hardness and resilience values decreased when TNF content in the biscuit formulation increased. Microscopic observation revealed that TNF-containi...
Candesartan cilexetil is an ester prodrug antagonist to angiotensin II receptor type 1 (AT1) used in management of many cardiovascular diseases. The absolute bioavailability of candesartan cilexetil is about (14-40%). Therefore, the paper aim was to prepare and evaluate solid self-nanoemulsifying drug delivery systems for candesartan cilexetil in order to improve its solubility, dissolution and stability. Solubility study was run in different vehicles to select the best excipients for dissolving candesartan cilexetil. Pseudo-ternary phase diagrams were constructed at 1:1, 2:1, 3:1 and 4:1 ratios and four formulations were prepared using various concentrations of cinnamon oil, tween 80 with poloxamer 407 mixture and transcutol HP as oil, surfactant mixture and co-surfactant, respectively. After this step about (0.2 milliliter) of each formulation was adsorbed on to two different adsorbent mixtures set which were: avicel 101 with aerosil 200 and avicel 101 with dibasic calcium phosphate anhydrous resulted in eight solid nanoformulations. All prepared formulations were evaluated for particle size distribution, polydispersity index, zeta potential, scanning probe microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray powder diffractometry and in vitro drug dissolution. It was found that release rate and extent for all prepared formulations were significantly higher (p < 0.05) than marketed tablet as well as plain drug powder. It could be concluded from the study that self-nanoemulsifying drug delivery system is a promising approach to improve solubility, wettability, dissolution and stability of candesartan cilexetil.
Abstract. Diazepam is one of the most prescribed benzodiazepines. The purpose of the present research was to optimize the formulation of orodispersible tablets of diazepam. Orodispersible tablets of diazepam were prepared using different types of superdisintegrants (Ac-Di-Sol, sodium starch glycolate, and crospovidone (CP)) and different types of subliming agents (camphor and ammonium bicarbonate (AB)) at different concentrations and two methods of tablets preparations (wet granulation and direct compression methods). The formulations were evaluated for flow properties, wetting time, hardness, friability, content uniformity, in vivo disintegration time (DT), release profiles, and buccal absorption tests. All formulations showed satisfactory mechanical strength except formula F5 which contains camphor and formula F9 which is prepared by direct compression method. The results revealed that the tablets containing CP as a superdisintegrant have good dissolution profile with shortest DT. The optimized formula F7 is prepared using 10% CP as a superdisintegrant and 20% AB as a subliming agent by wet granulation method which shows the shortest DT and good dissolution profile with acceptable stability. This study helps in revealing the effect of formulation processing variables on tablet properties. It can be concluded that the orodispersible tablets of diazepam with better biopharmaceutical properties than conventional tablets could be obtained using formula F7.
This study is carried out to evaluate the chemical composition and physicochemical properties of berry leaves, carob and doum tea infusions and their mixtures. Furthermore, the antioxidant activities of these extracts were investigated by scavenging of 1,1 diphenyl-2-picrylehydrozyl (DPPH) radicals. The proliferation inhibition activities on some types of bacteria and yeast were also measured for evaluating the antimicrobial activity of berry leaves, carob and doum tea infusions and their blends. The results showed that carob was characterized by its high protein content. The highest percentage of fi ber was found in doum sample, followed by carob but ash was the highest in berry leaves samples. The levels of most elements were higher in carob sample, when compared with those of berry leaves and doum samples. The highest value of TSS was found in the tea infusions of doum and carob (22.5 Brix), meanwhile, the lowest was observed in the doum tea infusions (10.60 Brix). Acidity of berry leaves, carob and doum tea infusions was higher than that of the berry leaves +doum tea infusions, but lower than that of the berry leaves + carob + doum tea infusions. Total sugars formed the major components in doum and berry leaves + carob tea infusions. Doum and carob tea infusions had signifi cantly higher non-reducing, but lower contents of reducing sugars than the other tested samples. The results indicated that berry leaves + carob + doum tea infusions sample showed higher quality attributes especially color, taste and overall acceptability. The berry leaves and berry leaves + carob tea infusions had a high level of vit. C (11.05 and 10.28 mg/100 g), while it was low in doum tea infusions. Blended samples showed a higher content of total phenol compounds compared to tea infusions of berry leaves, carob and doum. Data indicated that the berry leaves + carob + doum, berry leaves + carob, berry leaves + doum and doum + carob tea infusions samples were good antioxidants with strong DPPH radical-scavenging activity. The results confi rmed that the investigated extracts had good antimicrobial activity, especially against bacteria.
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