Rat palatability,pharmacodynamics effect and bioavailability of mefenamic acid formulations utilizing hot-melt extrusion technology

Abstract

Mefenamic acid (MA) has been reported as a weakly soluble drug which presents weak in vivo absorption upon oral administration using conventional formulations. Solid dispersions (SDs) have been investigated extensively in literature for enhancing the solubility and bioavailability of weakly-soluble molecules. Hence, the aim of proposed study was to prepare MA novel formulations in the form of SDs using hot-melt extrusion technology in order to enhance its palatability, bioavailability, and pharmacodynamics effects/anti-inflammatory efficacy. Various SDs of MA were prepared using hot-melt extrusion technology, characterized physically and investigated for dissolution tests. Optimized SD formulations of MA were being subjected to palatability, pharmacodynamics, and pharmacokinetic studies in rats. Optimized SD of MA showed significant rat palatability tastes as compared with pure and marketed MA (p?<?.05). Anti-inflammatory efficacy of 20% SD and 25% SD of MA was found to be 86.44 and 89.83%, respectively, in comparison with 74.57 and 78.24% by pure MA and marketed MA, respectively. The anti-inflammatory efficacy of optimized SD was found to be significant as compared with pure and marketed MA (p?<?.05). The oral absorption of MA from optimized 20% SD was also noted as statistically significant as compared with pure MA (p?<?.05). The relative bioavailability of MA from 20 and 25% SDs was 2.97 and 2.24-folds higher than pure MA. The results of this study suggested that SDs prepared using hot-melt extrusion technology are capable to enhance palatability, anti-inflammatory efficacy, and oral bioavailability of MA in comparison with pure drug.     

Inhibition of Listeria monocytogenes LMG10470 by plantaricin UG1 in vitro and in beef meat

The inhibition of Listeria monocytogenes LMG 10470 occurred due to plantaricin UG1, but not to lactic acid produced by Lactobacillus plantarum UG1 or its negatie variant (BAC). Partially purified plantaricin UG1 had a higher antilisterial activity in vitro and in meat than Lactobacillus plantarum UG1 culture. Plantaricin UG1 activity was higher in brain heart infusion (BHI) broth than in minced meat. The inhibitory effect of plantaricin UG1 against L. monocytogenes LMG10470 was dependent on its concentration. The 22,880 AU/mL appeared to be an ideal meat preservative in this experiment.     

Incidence of Listeria in Egyptian meat and dairy samples

A total of 180 food samples including meat (raw lean beef, frozen lean beef, and frozen chicken) and dairy products (raw milk, Zabady and Kareesh cheese) were analysed for Listeria. Isolates were differentiated using morphological, cultural, and biochemical tests and an API-Listeria kit. Zabady cheese was completely free of Listeria. The highest incidence rate (13.33%) was in frozen lean beef. Raw lean beef and milk products showed an incidence rate of 6.67%. The lowest incidence rate (3.33%) was in Kareesh cheese and frozen chicken meat samples. L. monocytogenes showed the lowest incidence rate (0.55%), isolated from one frozen lean beef sample. L. ivanovii and L. grayi showed the highest incidence rate (2.22%), isolated from 4 samples. L. innocua and L. seeligeri were positive in 3 samples (1.67%), and L. welshimeri in 2 samples (1.11%). L. monocytogenes and L. ivanovii were positive for virulence factors (hemolytic properties, and extracellular enzyme activities).     

Dielectric Response in the First Silicon Phthalocyanine Network Polymer

Unlike the well known silicon phthalocyanine polymers, which are only bridged polymers, the first silicon-phthalocyanine network polymer [PcSiCl₂] _x 6 was prepared from commercially available precursors. Based on previous modeling studies, elemental composition allowed for determination of both the shape and the content of Pc units in the prepared polymer. The two-dimensional network structure was found to offer an extension of the conjugation of the 18-π electron system of the phthalocyanine and facilitate the charge mobility across the material. This was found to enhance the conductivity and dielectric properties of the material, relative to the analogue materials, by supporting the hoping conduction mechanism. Differential scanning calorimetry was used to follow the non-oxidative thermal degradation of the prepared polymeric material. An interesting phenomenon, water effusion, was detected and proved to play a role in the conduction mechanism. Electrical and dielectric measurements were carried out at different frequencies. The polymer has extremely high values of the permittivity ε′ and dielectric loss ε″ at lower frequencies that decrease gradually with increasing frequency. The relaxation peak at lower frequencies showed without doubt that the moisture enhances the conductivity.     

Noninvasive sensing of thermal treatments of Japanese seafood products using imaging spectroscopy

The potential of imaging spectroscopy for noncontact sensing of thermal treatments experienced on Japanese kamaboko was investigated. Samples were thermally treated at 100, 120, 140, 160, 180 and 200 °C to core temperatures of 45, 50, 55, 60, 65, 70, 75 and 80 °C and then promptly cooled and imaged in the short‐wave near infrared spectral range of 900–2500 nm. Partial least square (PLS) regression models were developed using the whole spectral range as well as using the most important wavelengths to predict the core temperature (T_C) and thermal history (TH) yielding a reasonable level of accuracy of ( = 0.86 and RMSEP = 3.9 °C) and ( = 0.83 and RMSEP = 0.29 min), respectively. Moreover, a stepwise linear discriminant analysis (LDA) model was developed for identifying samples whose core temperatures reached a threshold of 65 °C. The LDA model yielded overall classification accuracy of 93.75% in both calibration and validation sets. The resulting discrimination function was then applied in a pixel‐wise manner to produce understandable classification maps to exhibit the difference among samples with high accuracy.     

Robust colour calibration of an imaging system using a colour space transform and advanced regression modelling

A new algorithm for the conversion of device dependent RGB colour data into device independent L*a*b* colour data without introducing noticeable error has been developed. By combining a linear colour space transform and advanced multiple regression methodologies it was possible to predict L*a*b* colour data with less than 2.2 colour units of error (CIE 1976). By transforming the red, green and blue colour components into new variables that better reflect the structure of the L*a*b* colour space, a low colour calibration error was immediately achieved (ΔE(CAL) = 14.1). Application of a range of regression models on the data further reduced the colour calibration error substantially (multilinear regression ΔE(CAL) = 5.4; response surface ΔE(CAL) = 2.9; PLSR ΔE(CAL) = 2.6; LASSO regression ΔE(CAL) = 2.1). Only the PLSR models deteriorated substantially under cross validation. The algorithm is adaptable and can be easily recalibrated to any working computer vision system. The algorithm was tested on a typical working laboratory computer vision system and delivered only a very marginal loss of colour information ΔE(CAL) = 2.35. Colour features derived on this system were able to safely discriminate between three classes of ham with 100% correct classification whereas colour features measured on a conventional colourimeter were not.     

Near-infrared hyperspectral imaging for grading and classification of pork

In this study, a hyperspectral imaging technique was developed to achieve fast, accurate, and objective determination of pork quality grades. Hyperspectral images were acquired in the near-infrared (NIR) range from 900 to 1700 nm for 75 pork cuts of longissimus dorsi muscle from three quality grades (PSE, RFN and DFD). Spectral information was extracted from each sample and six significant wavelengths that explain most of the variation among pork classes were identified from 2nd derivative spectra. There were obvious reflectance differences among the three quality grades mainly at wavelengths 960, 1074, 1124, 1147, 1207 and 1341 nm. Principal component analysis (PCA) was carried out using these particular wavelengths and the results indicated that pork classes could be precisely discriminated with overall accuracy of 96%. Algorithm was developed to produce classification maps of the tested samples based on score images resulting from PCA and the results were compared with the ordinary classification method. Investigation of the misclassified samples was performed and showed that hyperspectral based classification can aid in class determination by showing spatial location of classes within the samples.     

Evaluation of membrane fouling for in-line filtration of oil sands process-affected water: the effects of pretreatment conditions

Membrane filtration is an effective reclamation option for oil sands process-affected water (OSPW). However, fresh OSPWs contain suspended solids and inorganic constituents in suspended and dissolved forms that can severely foul membranes. Pretreatment of OSPW with coagulation-flocculation (CF) was investigated to determine the effects of different coagulant aids (anionic, cationic, and nonionic polymers) on membrane surface properties and fouling. Our results showed that CF pretreatment effectively enhanced nanofiltration (NF) and reverse osmosis (RO) membrane permeate flux and salt rejection ratio through reducing membrane fouling. It was shown that coagulants and coagulant aids applied to OSPW feedwater can affect membrane physicochemical properties (surface hydrophilicity, zeta potential, and morphology), membrane performance, and the fouling indexes. Membrane rejection of ionic species increased significantly with the inclusion of an anionic coagulant aid and slightly with a cationic coagulant aid. Among three coagulant aids tested, anionic coagulant aids led to the most enhanced membrane performance through increasing membrane surface negativity and decreasing the formation of a fouling layer. Conversely, although cationic coagulant aids were the most effective in reducing OSPW turbidity, the application of cationic coagulant aids promoted the adsorption of foulants on membrane surfaces.     

Quality parameters and RAPD-PCR differentiation of commercial baker's yeast and hybrid strains

Baker's yeast, Saccharomyces cerevisiae, is a key component in bread baking. Total of 12 commercial baker's yeast and 2 hybrid strains were compared using traditional quality parameters. Total of 5 strains with high leavening power and the 2 hybrid strains were selected and evaluated for their alpha-amylase, maltase, glucoamylase enzymes, and compared using random amplified polymorphic DNA (RAPD). The results revealed that all selected yeast strains have a low level of alpha-amylase and a high level of maltase and glucoamylase enzymes. Meanwhile, the Egyptian yeast strain (EY) had the highest content of alpha-amylase and maltase enzymes followed by the hybrid YH strain. The EY and YH strains have the highest content of glucoamylase enzyme almost with the same level. The RAPD banding patterns showed a wide variation among commercial yeast and hybrid strains. The closely related Egyptian yeast strains (EY and AL) demonstrated close similarity of their genotypes. The 2 hybrid strains were clustered to Turkish and European strains in 1 group. The authors conclude that the identification of strains and hybrids using RAPD technique was useful in determining their genetic relationship. These results can be useful not only for the basic research, but also for the quality control in baking factories.