This search include the synthesis of some new 1,3-oxazepine derivatives have been prepared, starting from reaction of L-ascorbic acid with dry acetone in presence of dry hydrogen chloride afforded the acetal (I). Treatment of the latter with p-nitrobenzoyl chloride in pyridine yielded the ester (II) which was dissolved in (65%) acetic acid in absolute ethanol yielded the glycol (III). The reaction of the glycol (III) with sodium periodate in distilled water at room temperature produced the aldehyde (IV). The compound (V) [4-(1,3-dioxoisoindolin-2-yl)benzoic acid] was synthesized by reaction p-aminobenzoic acid and phthalic anhydride in presence of (gla. CH3COOH). Reaction of compound (V) with thionyl chloride produced [4-(1,3-dioxoisoindolin-2-yl)benzoyl chloride]. Condensation of acid chloride with hydrazine hydrate afforded 4-(1,3-dioxoisoindolin-2-yl)benzohydrazide (VI). The azomethine (VII) has been synthesized from the reaction between compounds (IV) and (VI). Moreover compounds (VIII-X) were synthesized from the cyclic condensation of Schiff base (VII) with (maleic, phthalic and 3-nitrophthalic) anhydride, the structures of the newly synthesized compounds have been confirmed by physical properties and spectral measurements such as (FTIR and some of them by 1H-NMR and 13C-NMR).
Four batches of sertraline HCl microspheres were prepared using a poly (D-L-lactide-co-glycolide) (PLGA) polymer ( Mw. 9, 27, 30 and 83 KDa) as a delivery system. The microspheres were prepared by a dispersion/solvent extraction-evaporation method and characterized for drug loading by UV, particle size by laser diffractometry and surface morphology by scanning electron microscopy (SEM). The in vitro sertraline HCl release was studied. Spherical microspheres with a mean diameter of 21 to 26 µm loaded with 24.6 – 38.2% were produced. The in vitro drug release was shown to be depend on polymer molecular weight and also on the drug loading. Differential scanning calorimetry (DSC) was employed to investigate the physical state
... Show MoreFelodipine is a calcium-channel blocker with low aqueous solubility and bioavailability. Lipid dosage forms are attractive delivery systems for such hydrophobic drug molecules. Nanoemulsion (NE) is one of the popular methods that has been used to solve the dispersibility problems of many drugs. Felodipine was formulated as a NE utilizing oleic acid as an oil phase, tween 80 and tween 60 as surfactants and ethanol as a co-surfactant. Eight formulas were prepared, and different tests were performed to ensure the stability of the NEs, such as particle size, polydispersity index, zeta potential, dilution test, drug content, viscosity and in-vitro drug release. Result
... Show MoreSelexipag is an orally selective long-acting prostacyclin receptor agonist, which indicated for the treatment of pulmonary arterial hypertension. It is practically insoluble in water ( class II, according to BCS). This work aims to prepare and optimized Selexipag nanosuspensions to achieve an enhancement in the in vitro dissolution rate. The solvent antisolvent precipitation method was used for the production of nanosuspension, and the effect of formulation parameters (stabilizer type, drug: stabilizer ratio, and use of co-stabilizer) and process parameter (stirring speed) on the particle size and polydispersity index were studied. SLPNS prepared with Soluplus® as amain stabilizer (F15) showed the smallest particle size 47nm wi
... Show MoreThis study was carried out to prepare and characterize domperidone nanoparticles to enhance solubility and the release rate. Domperidone is practically insoluble in water and has low and an erratic bioavailability range from 13%-17%. The domperidone nanoparticles were prepared by solvent/antisolvent precipitation method at different polymer:drug ratios of 1:1 and 2:1 using different polymers and grades of poly vinyl pyrolidone, hydroxy propyl methyl cellulose and sodium carboxymethyl cellulose as stabilizers. The effect of polymer type, ratio of polymer:drug, solvent:antisolvent ratio, stirring rate and stirring time on the particle size, were investigated and found to have a significant (p? 0.05) effect on particle size. The best formul
... Show MoreIsradipine belong to dihydropyridine (DHP) class of calcium channel blockers (CCBs). It is used in the treatment of hypertension, angina pectoris, in addition to Parkinson disease. It goes under the BCS class II drug (low solubility-high permeability). The drug will experience extensive first-pass metabolism in liver, therefore, oral bio-availability will be approximately15 to 24 %.
The aim of this study was to formulate and optimize a stable nanoparticles of a highly hydrophobic drug, isradipine by anti-solvent microprecipitation Method to achieve the higher in vitro dissolution rate, so that it will be absorbed by intestinal lymphatic transport in order to avoid hepatic first-pass metabolism&nbs
... Show MoreIn the present research we the study the deposition of radioactive elements naturally and particularly radioactive radon gas in parts of the body of organisms which are of direct relevance to human life in the city of Baghdad as the samples which were collected from the bones and skin of some kinds of birds and chicken based on the principle that radioactive elements are concentrated always on the bones. We use of this as the exercise detector impact nuclear (CR-39), using the technology Cylindrical diffusion , the results indicated that the largest concentration of radon found in the bone bird Seagull tapered as it was (625 ± 37) Bq.cm-3, and less concentration of radon gas in the chicken bones of Al-kafeel as it was (105 ± 10) Bq.c
... Show MoreThe experiments were conducted in laboratory conditions of a temperature of 25± 2C and relative moisture of 40± 5 % to evaluate the effectiveness of the cinnamon, lavender and clove essential oils on some biological life aspects of cowpea beetle, C. maculates. Results of the obligative experiment for the effect of the oils on insect adult killing showed that the concentration of 5% caused a mortality percentage averaged 13.33% of the insect males. The mortality percentage of the insect females was 11.3% for the cinnamon and lavender oils. The lavender oil had the lowest effect on adult killing, not exceeding 0. For the effect of the oils on egg laying, clove oil affected the number of eggs highly at the concentration of 5%, result
... Show MoreThe experiments were conducted in laboratory conditions of a temperature of 25± 2C and relative moisture of 40± 5 % to evaluate the effectiveness of the cinnamon, lavender and clove essential oils on some biological life aspects of cowpea beetle, C. maculates. Results of the obligative experiment for the effect of the oils on insect adult killing showed that the concentration of 5% caused a mortality percentage averaged 13.33% of the insect males. The mortality percentage of the insect females was 11.3% for the cinnamon and lavender oils. The lavender oil had the lowest effect on adult killing, not exceeding 0. For the effect of the oils on egg laying, clove oil affected the number of eggs highly at the concentration of 5%, result
... Show MoreThis research was carried out to determine the impact of heat shock, electric shock and seeds in soaking nitrous acid mutagen solution on three cultivars of faba beans plant (Zaina, Aguadulce and Local) at the year 2012-2013. Factorial experiment was arranged in randomized complete block design (RCBD) with three replicates were used. The results showed that heat shock lead to early plants of 50% in flowering and an increase in the number of branches/plant and the number of seeds/pod compared to other treatments, whereas the seeds soaked in nitrous acid mutagen solution gave the highest plant height, leaf area index, number of pods/plant, seed weight, seed yield kg/ha, and did not differ significantly with treatment of electric shock in the
... Show MoreCadmium has been known to be harmful to human healthy , manily Via contaminated drinking water , food supplies , tobacco and industrial pollutant . The aim of this study was to determine the toxicity of new Cadmium (II) complex ( Bis[ 5- ( P- nitrophenyl ) – ? 4 – Phenyl- 1,2,4- triazole -3- dithiocarbamatohydrazide] cadmium (II) Hydra ( 0.5) and compare it with anticancer drug cyclophosphamide ( CP) in female albino mice . This complex causes to several alterations in Enzymatic activity of Glutamate Pyruvate Transaminase (GPT) and Alkaline Phosphatase (ALP ) in three organs after the treatment of mice with different doses of a new cadmium (II) complex ( 0.09 / 0.25ml , 0.18/ 0.5ml and 0.25mg /0.7 ml /30 gm of mous
... Show More