Aceclofenac (AC) is an orally active phenyl acetic acid derivative, non-steroidal anti-inflammatory drug with exceptional anti-inflammatory, analgesic and antipyretic properties. It has low aqueous solubility, leading to slow dissolution, low permeability and inadequate bioavailability. The aim of the current study was to prepare and characterize AC-NS-based gel to enhance the dissolution rate and then percutaneous permeability. NS.s were prepared using solvent/antisovent precipitation method at different drug to polymer ratios (1:1, 1:2, and 1:3) using different polymers such as poly vinyl pyrrolidone (PVP-K25), hydroxy propyl methyl cellulose (HPMC-E5) and poloxamer® (388) as stabilizers alone and in combinations of two polymers (1:2 and 1:4 Drug: polymer ratio). Fifteen formulas of AC-NS.s were prepared and characterized for production yield, loading efficiency, particle size, polydispersity index and physical stability. The best formulas of NS were then lyophilized to be characterized by FTIR, DSC, P-XRD and SEM. After that, the best prepared formula of AC-NS regarding the involved characterization methods was incorporated in gel dosage forms using carbopol®940. From this study, we conclude that the dissolution rate and permeability of AC were improved when the particle size was reduced to Nano-scale as compared with pure drug.
Objective: This study involved the synthesis of new Schiff bases and 1,3-oxazepine derivatives from the baclofen drug and study the anticancer activities. Methods: Baclofen was initially reacted with aromatic aldehydes to create Schiff base derivatives (Ia–Ib), which were then closed in the next step using anhydrous acids to form oxazepine derivatives (IIa–IId). Results: The title compounds were synthesized successfully and identified using FT-IR, 1H NMR, and 13C NMR spectroscopy. Additionally, compound (IIc)’s (3-(4-chloro-phenyl)-4-[2-(4nitro-phenyl)-4,7-dioxo-4,7-dihydro-[1,3] oxazepin-3-yl]butyric acid) anticancer activity was assessed using MTT assay against FTC-133 (thyroid cancer) compared with WRL-68 (normal cell line). Discus
... Show MoreSynthesis, Characterization And Biological Evaluation of Schiff Base And Ligand Metal Complexes of Some Drug Substances
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... Show MoreIn this study, new heterocyclic compounds were synthesized through the cyclization reactions of o-phenylenediamine (1) with various organic reagents. Benzodiazepine derivatives (2-4) were obtained by reaction of (1) with ethylacetoacetate, malonic acid and acetyl acetone.Treatment of compound (1) with chloroacetamide, chloroacetic acid, p-bromophenacyl bromide and oxalic acid dihydrate afforded quinoxaline derivatives (5-8), respectively. Reaction of compound (1) with benzoic acid, piperonal, cyclohexanone and carbon disulfide resulted in the formation of compounds (9-12), respectively. Finally, reaction of compound (12) with chloroacetic acid in the presence of potassium hydroxide produced compound (13).
The mixed ligand complexes of Mn(II), Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Hg(II) with alanine and 8-hydroxyqinoline (Oxine) were synthesized and characterized by FT-IR ,spectra electronic, flam-AAS] along with conductivity measurements , solubility , melting point, magnetic susceptipibility.The synthesized complexes were tested in vitro for antimicrobial activity. The results obtained indicated that some of these complexes are more active than with others.
The newly synthesized Schiff base ligand (E)-2-((2-phenylhydrazono)methyl)naphthalen-1-ol (phenyl hydrazine derivative), is allowed to react with each of the next mineral ion: Ni2+, Cu2+, Zn2+andCd2+successfully resulting to obtain new metal complexes with different geometric shape. The formation of Schiff base complexes and also the origin Schiff base is indicated using LC-Mass that manifest the obtained molar mass, FT-IR proved the occurrence of coordination through N of azobenzene and O of OH by observing the shifting in azomethines band and appearing of M-N and N-O bands. Moreover, we can also detect by such apparatus, the presence of aquatic water molecule inside the coordination sphere. UV-Vis spectra of all resultants reveale
... Show MoreA large number of researchers had attempted to identify the pattern of the functional relationship between fertility from a side and economic and social characteristics of the population from another, with the strength of effect of each. So, this research aims to monitor and analyze changes in the level of fertility temporally and spatially in recent decades, in addition to estimating fertility levels in Iraq for the period (1977-2011) and then make forecasting to the level of fertility in Iraq at the national level (except for the Kurdistan region), and for the period of (2012-2031). To achieve this goal has been the use of the Lee-Carter model to estimate fertility rates and predictable as well. As this is the form often has been familiar
... Show MoreWireless sensor networks (WSNs) are emerging in various application like military, area monitoring, health monitoring, industry monitoring and many more. The challenges of the successful WSN application are the energy consumption problem. since the small, portable batteries integrated into the sensor chips cannot be re-charged easily from an economical point of view. This work focusses on prolonging the network lifetime of WSNs by reducing and balancing energy consumption during routing process from hop number point of view. In this paper, performance simulation was done between two types of protocols LEACH that uses single hop path and MODLEACH that uses multi hop path by using Intel Care i3 CPU (2.13GHz) laptop with MATLAB (R2014a). Th
... Show MoreThis research develops a new method based on spectral indices and random forest classifier to detect paddy rice areas and then assess their distributions regarding to urban areas. The classification will be conducted on Landsat OLI images and Landsat OLI/Sentinel 1 SAR data. Consequently, developing a new spectral index by analyzing the relative importance of Landsat bands will be calculated by the random forest. The new spectral index has improved depending on the most three important bands, then two additional indices including the normalized difference vegetation index (NDVI), and standardized difference built-up index (NDBI) have been used to extract paddy rice fields from the data. Several experiments being
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