Liquisolid compact is the most promising technique for increasing dissolution rate and bioavailability of poorly soluble drugs.Clopidogrel bisulfate is an oral antiplatelets used for treatment and prophylaxis of cardiovacular and peripheral vascular diseases related to platelets aggreagation.Clopidogrel has low solubility at high pH media of intestine and low bioavailability of a bout 50% after oral doses.The purpose of this work was to enhance dissolution pattern of clopidogrel through its formulation into liquisolid tablets.A mathematical model was used to calculate the optimum quantities of tween 80 , carrier (Avicel PH 102) and coating material (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures.The liquisolid tablets were evaluated for hardness, percent friability, weight variation, content uniformity , disintegration time and in vitro drug release profile.DSC , FTIR , XRD and SEM were used for assessment of physicochemical properties of drug and compatibility with excipients in the liquisolid compacts.The selected formulation (F2) released 92.2% of its content during first 10 min. compared to 13.6% of directly compressed tablet and 24.2% of marketed tablet. In conclusion the dissolution rate and bioavailability of clopidogrel can be enhanced to a great extent by liquisolid technique.
The purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (5-8). These compounds were characterized spectroscopically by
... Show MoreIn this research, new compounds were synthesized via the reaction of dichloroacetic acid with two moles of piperidine. The novel acid 1 was converted to its ester 2. Acid hydrizide 3 was prepared by the reaction of hydrazine hydrate with new ester 2, which was later used to prepare derivatives of Schiff bases 4-13. In the last step, Schiff bases and thioglycolic acid were reacted to give thiazolidine derivatives 14-23. All these compounds were diagnosed using melting points, FTIR, 1HNMR and mass spectroscopy. Scheme 1 shows all the synthesized compounds' reaction steps and structures. Keywords: Thiazolidine; Schiff bases; biological activity; piperidine; dichloroacetic acid.
The current study performs an explicit nonlinear finite element simulation to predict temperature distribution and consequent stresses during the friction stir welding (FSW) of AA 7075-T651 alloy. The ABAQUS® finite element software was used to model and analyze the process steps that involve plunging, dwelling, and traverse stages. Techniques such as Arbitrary Lagrangian–Eulerian (ALE) formulation, adaptive meshing, and computational feature of mass scaling were utilized to simulate sequence events during the friction stir welding process. The contact between the welding tool and workpiece was modelled through applying Coulomb’s friction model with a nonlinear friction coefficient value. Also, the model considered the effect of nonlin
... Show MoreThe current study performs an explicit nonlinear finite element simulation to predict temperature distribution and consequent stresses during the friction stir welding (FSW) of AA 7075-T651 alloy. The ABAQUS® finite element software was used to model and analyze the process steps that involve plunging, dwelling, and traverse stages. Techniques such as Arbitrary Lagrangian–Eulerian (ALE) formulation, adaptive meshing, and computational feature of mass scaling were utilized to simulate sequence events during the friction stir welding process. The contact between the welding tool and workpiece was modelled through applying Coulomb’s friction model with a nonlinear friction coefficient value. Also, the model considered the effect o
... Show MoreContracting cancer typically induces a state of terror among the individuals who are affected. Exploring how glucose excess, estrogen excess, and anxiety work together to affect the speed at which breast cancer cells multiply and the immune system’s response model is necessary to conceive of ways to stop the spread of cancer. This paper proposes a mathematical model to investigate the impact of psychological panic, glucose excess, and estrogen excess on the interaction of cancer and immunity. The proposed model is precisely described. The focus of the model’s dynamic analysis is to identify the potential equilibrium locations. According to the analysis, it is possible to establish four equilibrium positions. The stability analys
... Show MoreThe purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (
Derivatives of Schiff-bases possess a great importance in pharmaceutical chemistry. They can be used for synthesizing different types of bioactive compounds. In this paper, derivatives of new Schiff bases have been synthesized from several serial steps. The acid (I) was synthesized from the reaction of dichloroethanoic acid with 2 moles of p-aminoacetanilide. New acid (I) converted to its ester (II) via the reaction of (I) with dimethyl sulphate in the present of anhydrous of sodium carbonate and dry acetone. Acid hydrazide (III) has been synthesized by adding 80% of hydrazine hydrate to the new ester using ethanol as a solvent. The last step included the preparation of new Schiff-bases (IV-VIII) by the reaction of acid hydrazide with app
... Show MoreDerivatives of Schiff-bases possess a great importance in pharmaceutical chemistry. They can be used for synthesizing different types of bioactive compounds. In this paper, derivatives of new Schiff bases have been synthesized from several serial steps. The acid (I) was synthesized from the reaction of dichloroethanoic acid with 2 moles of p-aminoacetanilide. New acid (I) converted to its ester (II) via the reaction of (I) with dimethyl sulphate in the present of anhydrous of sodium carbonate and dry acetone. Acid hydrazide (III) has been synthesized by adding 80% of hydrazine hydrate to the new ester using ethanol as a solvent. The last step included the preparation of new Schiff-bases (IV-VIII) by the reaction of acid hydrazide with
... Show MoreThis study aimed to determine the measurements and classification of Schneider membrane thickness correlated to age and sex factors using cone beam computed tomography (CBCT). Methods: The study included CBCT images for 100 maxillary sinuses of 50 consecutive patients, and the thickness of the maxillary sinus membrane (Schneiderian membrane) was measured in coronal view from the lowest point in the floor of the maxillary sinus to the highest point. The thickness of the Schneiderian membrane was classified into 4 types. Results: The study result revealed that out of the total cases, 45% of sinus membranes were classified as type 2, while only 10% were classified as type 4. The most frequent type of membrane thickness diagnosed in the age gro
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