Assessment of Heavy Metals Pollution In Euphrates River Water, Amiriyah Fallujah, Iraq.

The concentrations of heavy metals (Cd, Cr, Fe, Ni and Pb) in water samples for the Euphrates River in Amiriyah Fallujah, Iraq were evaluated to assess the pollution level. Ten sites were selected along the study area and sampled during December 2013 to March 2014. The decreasing trend of metals were observed in water as  Pb > Fe > Cr > Cd > Ni. The concentration of the studied metals was higher than the recommended guidelines for drinking and aquatic life, indicated that the water is not safe for drinking and aquatic life uses. There were significant differences in the concentrations of heavy metal  during the sampling period. Heavy pollution index (HPI) results showed that the water was seriously polluted  with Cd, Cr and Pb. According to metal index (MI) results, the water is seriously threatened with metal pollution and unsafe for drinking, irrigation and aquatic life uses. Principal components analysis (PCA) suggests that the Cd, Cr and Pb are derived from anthropogenic sources. Keywords: River pollution; Pollution index, Metal Index; Euphrates; Ira

Trimethoxylated halogenated chalcones as dual inhibitors of mao-b and bace-1 for the treatment of neurodegenerative disorders

Six halogenated trimethoxy chalcone derivatives (CH1–CH6) were synthesized and spec-trally characterized. The compounds were further evaluated for their inhibitory potential against monoamine oxidases (MAOs) and β-secretase (BACE-1). Six compounds inhibited MAO-B more effectively than MAO-A, and the 2′,3′,4′-methoxy moiety in CH4–CH6 was more effective for MAO-B inhibition than the 2′,4′,6′-methoxy moiety in CH1–CH3. Compound CH5 most potently inhibited MAO-B, with an IC50 value of 0.46 µM, followed by CH4 (IC50 = 0.84 µM). In 2′,3′,4′-methoxy derivatives (CH4-CH6), the order of inhibition was –Br in CH5 >-Cl in CH4 >-F in CH6 at the para-position in ring B of chalcone. CH4 and CH5 were selective for MAO-B, with selectivity index (SI) values of 15.1 and 31.3, respectively, over MAO-A. CH4 and CH5 moderately inhibited BACE-1 with IC50 values of 13.6 and 19.8 µM, respectively. When CH4 and CH5 were assessed for their cell viability studies on the normal African Green Monkey kidney cell line (VERO) using MTT assays, it was noted that both compounds were found to be safe, and only a slightly toxic effect was observed in concentrations above 200 µg/mL. CH4 and CH5 decreased reactive oxygen species (ROS) levels of VERO cells treated with H2 O2, indicating both compounds retained protective effects on the cells by antioxidant activities. All compounds showed high blood brain barrier permeabilities analyzed by a parallel artificial membrane permeability assay (PAMPA). Molecular docking and ADME prediction of the lead compounds provided more insights into the rationale behind the binding and the CNS drug likeness. From non-test mutagenicity and cardiotoxicity studies, CH4 and CH5 were non-mutagenic and non-/weak-cardiotoxic. These results suggest that CH4 and CH5 could be considered candidates for the cure of neurological dysfunctions

The CO2-dependence of Brucella ovis and Brucella abortus biovars is caused by defective carbonic anhydrases

Brucella bacteria cause brucellosis, a major zoonosis whose control requires efficient diagnosis and vaccines. Identification of classical Brucella spp. has traditionally relied on phenotypic characterization, including surface antigens and 5¿10% CO2 necessity for growth (CO2-dependence), a trait of Brucella ovis and most Brucella abortus biovars 1¿4 strains. Although molecular tests are replacing phenotypic methods, CO2-dependence remains of interest as it conditions isolation and propagation and reflects Brucella metabolism, an area of active research. Here, we investigated the connection of CO2-dependence and carbonic anhydrases (CA), the enzymes catalyzing the hydration of CO2 to the bicarbonate used by anaplerotic and biosynthetic carboxylases. Based on the previous demonstration that B. suis carries two functional CAs (CAI and CAII), we analyzed the CA sequences of CO2-dependent and -independent brucellae and spontaneous mutants. The comparisons strongly suggested that CAII is not functional in CO2-dependent B. abortus and B. ovis, and that a modified CAII sequence explains the CO2-independent phenotype of spontaneous mutants. Then, by mutagenesis and heterologous plasmid complementation and chromosomal insertion we proved that CAI alone is enough to support CO2-independent growth of B. suis in rich media but not of B. abortus in rich media or B. suis in minimal media. Finally, we also found that insertion of a heterologous active CAII into B. ovis reverted the CO2-dependence but did not alter its virulence in the mouse model. These results allow a better understanding of central aspects of Brucella metabolism and, in the case of B. ovis, provide tools for large-scale production of diagnostic antigens and vaccines

Hexyl alginate derivative, an amphiphilic innovative buccal film-forming material of promising mechanical and release characteristics for the improvement of repaglinide bioavailability

Ahmed Khames1,2 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, College of Pharmacy, Taif University, Taif 21974, Saudi Arabia Background: Association of long hydrocarbon chain with alginate molecule imparts surface active properties and increases chain flexibility. Purpose: This work studied the efficacy of synthesized hexyl alginate derivative as a film-forming material with unique amphiphilic and mechanical properties for the preparation of rapidly disintegrating repaglinide oral films with higher drug release rate and improved bioavailability. Methods: Alginate hexyl amide derivative was prepared and used in the formulation of oral films by solvent casting technique. Using Box–Behnken experimental design, formulations were optimized at different polymer, plasticizer, and disintegrant levels as independent variables for maximum drug release rate, higher tensile strength, and shortest disintegration time as responses. Optimized film formulae were fully evaluated and subjected to further in vivo bioavailability studies in rabbits. Results: Higher dependency of response results on the selected variables was observed. Optimized formula showed satisfactory tensile strength (145.862 g/cm2), rapid disintegration (22.2 seconds), and higher drug release rate (97.799% within 30 minutes). The drug bioavailability was significantly improved in comparison with plain drug and conventional alginate oral films, where the AUC and Cmax values reached 296.072 µg.h/mL and 116.932 µg/mL in comparison with 164.917 µg.h/mL and 56.568 µg/mL for alginate film and 95.368 µg.h/mL and 31.925 µg/mL for plain drug, respectively. Tmax also showed significant reduction to be only 30 minutes in comparison with 60 minutes for other forms. Conclusion: This led to the final conclusion that the synthesized alginate derivative is an innovative promising film-forming material with unique mechanical and drug release properties for application in buccal drug delivery especially of Biopharmaceutics Classification System (BCS) class II drugs to increase solubility and improve bioavailability. Keywords: amphiphilic derivatives of alginate, Box–Behnken, BCS class II drugs, oral films, repaglinide &nbsp

The Effects of Uncontrolled Breeding's on Iraqi Horses Conformation

Due to the great importance of digital measurements of the conformation of the motor system in horses and the lack of a specialty center for higher cases, the purpose of this research was to form a specialized center for the conformation of the motor system in horses and depended on 60 horses of both sexes between the ages of 3 to 4 and a half years were employee for the body measurement in Iraqi equestrians club in Abu Ghraib and Iraqi equestrians Federation in Al Jadriya. The parameter which were used in this project angles measurement both fore and hind limb as well as the joint inclination. Therefore there were significant changes in the thoroughbred and Iraqi horses. To be concluded that angle inclination measurement can be used for horse evaluation

Hydralazine HCl rapidly disintegrating sublingual tablets: simple dosage form of higher bioavailability and enhanced clinical efficacy for potential rapid control on hypertensive preeclampsia

Samar Genedy,1 Ahmed Khames,2,3 Amal Hussein,4 Hatem Sarhan4 1Department of Clinical Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt; 3Department of Pharmaceutics and Pharmacy Technology, College of Pharmacy, Taif University, Taif, Kingdom of Saudi Arabia; 4Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt Background: Hypertensive disorders are the most common complication in pregnancy which can even lead to maternal mortality. Hydralazine hydrochloride (HHC), a direct-acting vasodilator, is intravenously used as the first-line therapy in controlling hypertension in pregnancy (preeclampsia). It suffers poor oral bioavailability (26%–50%) due to first-pass metabolism.Objective: This work aims for the preparation of HHC rapidly disintegrating sublingual tablets of higher absorption rate, short onset of action, and higher bioavailability for rapid control on blood pressure (BP) in hypertensive emergencies especially preeclampsia.Methods: HHC sublingual tablet mixtures were prepared using starch sodium glycolate and Pharmaburst as super disintegrants at three different levels by direct compression and were subjected to full in vitro evaluation; the drug bioavailability from the optimized sublingual tablet formula was assessed in comparison to conventional oral tablets in rabbits, and the clinical efficacy on controlling BP in induced preeclampsia like mouse model was also studied.Results: The results indicated compatibility of the prepared tablet mixtures, good flow, and acceptable mechanical strength. Sublingual tablet formula containing Pharmaburst (7%) that showed fastest disintegration (21 seconds) and 100% drug release within 5 minutes was selected for further bioavailability and pharmacodynamic studies. The drug bioavailability was significantly increased with Cmax = 28.2767±4.61 µg/mL, AUC(0–α) = 52.85±3.18 µg.h/mL, and Tmax = 0.33±0.011 hour in comparison to 18.0633±23.2 µg/mL, 33.18±5.18 µg.h/mL, and 0.75±0.025 hour for conventional oral tablets. Results of pharmacodynamic studies proved significant rapid control on both systolic and diastolic BP to normal values within only 30 minutes without any significant difference from intravenous data.Conclusion: These results confirm the suitability of the prepared HHC sublingual tablets for use in rapid control on hypertensive crisis especially in pregnant women as an alternate to parenteral administration.Keywords: pre-eclampsia like mouse model, absorption from buccal cavity, preeclampsia, sublingual tablets, hypertension, L-NAM

The effects of uncontrolled breeding’s on Iraqi horses conformation

Due to the great importance of digital measurements of the conformation of the motor system in horses and the lack of a specialty center for higher cases, the purpose of this research was to form a specialized center for the conformation of the motor system in horses and depended on 60 horses of both sexes between the ages of 3 to 4 and a half years were employee for the body measurement in Iraqi equestrians club in Abu Ghraib and Iraqi equestrians Federation in Al Jadriya. The parameter which were used in this project angles measurement both fore and hind limb as well as the joint inclination. Therefore there were significant changes in the thoroughbred and Iraqi horses. To be concluded that angle inclination measurement can be used for horse evaluation

Glucosamine-paracetamol spray-dried solid dispersions with maximized intrinsic dissolution rate, bioavailability and decreased levels of in vivo toxic metabolites

Ahmed Mahmoud Abdelhaleem Ali,1,2 Ahmed Khames,1,2 Majed Mansour Alrobaian,1 Mohammad Hamaidi,3 Mohammed AS Abourehab4,5 1Department of Pharmaceutics, Faculty of Pharmacy, Taif University, Taif, Kingdom of Saudi Arabia; 2Department of Pharmaceutics, Beni-Suef University, Beni-Suef, Egypt; 3Department of Clinical Pharmacy, Taif University, Taif, Kingdom of Saudi Arabia; 4Department of Pharmaceutics, Umm Al-Qura University, Makkah, Kingdom of Saudi Arabia; 5Department of Pharmaceutics, Minia University, Minia, Egypt Purpose: This study is aimed at preparing and testing physicochemical, pharmacokinetic and levels of toxic metabolites of paracetamol and glucosamine solid dispersions intended for multiple deliveries via the parenteral or per oral route. Methods: Solid dispersions were prepared using the spray drying technique at different molar ratios of paracetamol and glucosamine. Characterization of the solid dispersions was carried out using differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM), equilibrium solubility and intrinsic dissolution rate. In vivo pharmacokinetics and toxic metabolites of the prepared dispersions were evaluated and compared to those of pure drugs and physical mixtures. Results: Instant water solubility and more than 7-fold increase in dissolution rate led to significantly high plasma drug concentration (>6.5-fold) compared to paracetamol alone. More than 2-fold increase in area under the curve from 0 to 24 h from the dispersions was noticed on the third day of oral dosing to animals. Lower number and concentration followed by the complete disappearance of toxic pathway metabolites were observed on second and third days of dosing with solid dispersions and physical mixtures, respectively. Conclusions: The spray-dried dispersions support safer and more effective delivery of multiple doses of paracetamol, leading to an acceleration of its analgesic actions. Synergism between the analgesic actions of paracetamol and joint protective actions of glucosamine in this combination is expected to facilitate effective treatment of persistent pain-related illnesses such as osteoarthritis. Keywords: glucosamine, paracetamol, pharmacokinetics, reduced hepatotoxicity, solid dispersions, spray dryin