The present investigation developed the ester prodrugs of Non-steroidal anti inflammatory drugs (NSAIDs), Mefenamic acid and Flurbiprofen by conjugating with the natural antioxidant, 4-methyl umbelliferone that resulted the formation of Mefenamic acid-umbelliferone ester prodrug and Flurbiprofen-umbelliferone ester prodrug .The principal objective this study is the synthesis of the ester prodrugs of NSAIDs with the enhanced therapeutic activity and minimized side effects. Prodrugs were synthesized by coupling method using N,N’- dicyclohexylcarbodiimide/4-dimethylaminopyrimidine, subjected to physical, chemical characterization, spectral characterization (IR, 1H NMR, 13C NMR and Mass spectra),hydro
... Show Moreβ-Adrenergic blocking agents, mostly comprising of β-amino alcohols, are of pharmaceutical significance and have received major attention due to their utility in the management of cardiovascular disorders including hypertension, angina pectoris, cardiac arrhythmias and other disorders related to the sympathetic nervous system. Most compounds available for clinical use belong to the aryloxypropanolamine series, which is considered the second generation of β-blocking agents. The present study includes the synthesis of compounds with an N-substituted oxypropanolamine moiety attached to the 1, 3, 4-thiadiazole derivatives. According to this information, eight compounds were synthesized and characterized by IR spectra and elemental m
... Show MoreBecause pathogenic bacteria have gained resistance, bacterial illnesses are difficult to treat. Every year, a huge number of studies aimed at creating novel antibacterials are released. Shiff bases are an important field in organic synthesis due to their biological activities. Schiff bases also possessing an important range of pharmacological activities. Hybridization-combing two pharmacophores [heterocycle from starting molecule and synthesized hydrazones] to form one molecule-is the important method in designing new drugs. The new compounds [hydrazones] derivatives were created using a multi-step process including synthesis of indomethacin hydrazide by coupling agent reaction (EDC.HCL,HOBt) and then reaction with defferent aldehyde
... Show MoreEpidermal growth factor receptor tyrosine kinase (EGFR-TK) is a vastly fascinating epigenetic target for medicine treatment. EGFR-TK is overexpressed in several diseases, including cancers. In this study, we designed new EGFR-TK inhibitors with the same consists of erlotinib (approved anticancer drug) with longer linker and substituted hydrophobic moiety using Ligand Designer from Glide (Schrodinger LLC). By experimenting with different amide and Schiff base residues, the linker was optimized. Using licensed Schrodinger modeling software, the probable inhibition over EGFR-TK for the best-designed items was virtually assessed. The findings demonstrated that there is a possibility of an acceptable level of fitness interaction between the h
... Show MoreAmong the strong calcium channel blockers, lercanidipine hydrochloride (LER) has been shown to be useful in reducing blood pressure by acting on L-type calcium channels. Nevertheless, the main drawback of lercanidipine is that it is a BCS class II medication with poor solubility and a 10% oral bioavailability because of significant first pass metabolism. The goal of this study is to use the thin film hydration process to generate and assess lercanidipine nanomicelles utilizing soluplus in conjugation with other surfactants/polymers at different ratios in order to boost the solubility of virtually insoluble LER. Six formulations were prepared and analyzed for their micelles size, polydispersity index (PDI), encapsulation efficiency (EE%),
... Show MoreBy producing reactive oxygen species, primarily reactive hydroxyl radicals, iron overload may contribute to cellular damage and change the integrity of essential organelles. Echinacea Purpura; a medical plant with a root liquid extract contains various biologically active phytochemical compounds. This study aimed to evaluate the protective effect of Echinacea Purpura on bone marrow suppression with liver and spleen cells apoptosis induced by iron overload. Fifty albino rats were divided into five groups: Group (I) [negative control] intraperitoneally injection with (0.2 ml) normal saline solution every 3 days; with daily oral gavage of (1 ml) normal saline for 4 weeks. Group (
... Show MoreThe unique opportunity lies in targeting tumor cells through glycolysis, a pathway that compensates for decreased ATP production by increasing sugar consumption. This strategy allows for the development of a novel therapeutic approach, targeting malignant cells with selective pharmacological inhibitors of glycolysis without harming normal cells. In this study, hexokinase, glycolytic enzyme, was targeting to selectively inhibit energy production pathways in cancer cells without harming normal cells. The anticancer mechanisms of 2 Deoxy-D-Glucose (2DG) and Mannoheptulose (MH) in esophagus adenocarcinoma (SK-GT-4) and HBL-100 normal cell lines were investigated using MTT and wound healing assays to assess their cytotoxic effects and cellula
... Show MoreDoxorubicin is a potent anthracycline antibiotic used to treat many types of human neoplasms. The long-term adverse effect is cardiomyopathy, which is primarily caused by the extensive production of reactive oxygen species, which relates to several events related to nucleic acid metabolism and the activation of the immune system. Chromium is a trace element mostly utilized to regulate glucose levels and enhance the body's response to insulin, particularly in people with diabetes. Chromium picolinate often contains Chromium in its trivalent state, coupled with picolinic acid. The current study aims to evaluate the anti-inflammatory effect of chromium picolinate in doxorubicin-induced cardiotoxicity of rats. Twenty eight Wister male rats w
... Show MoreOne of the most potent and effective drugs in the field of chemotherapy is doxorubicin. It has shown remarkable efficacy against multiple cancer targets. Despite the effectiveness of this treatment, an important drawback is the cardiotoxicity caused by doxorubicin. This limitation has led oncologists to explore potential ways to prevent or reduce this toxic side effect. We will investigate in this study whether saxagliptin and telmisartan have any protective effects on heart tissue. We will study their effects on oxidative stress and apoptotic indicators in particular. There were a total of 28 rats, with 7 animals in each of the four groups: First group(control group): seven rats in good health were given distill
... Show MoreA novel glycine-based sulfonamide derivates were synthesized. This study presents the newly synthesized compounds (G1-G6) that exhibit promising DHPS inhibition activities, designed through a molecular docking analysis targeting the Yersinia pestis DHPS protein (PDB ID: 5JQ9). The docked compounds were subsequently subjected to ADME study to evaluate their pharmacokinetic properties. This work started with the synthesis of the glycine methyl ester HCL salt by esterification of the carbonyl group of the carboxylic acid functionality of glycine with thionyl chloride and methanol and the synthesis of 4-acetamidobenzene sulfonyl chloride from acetanilide, the reaction of the latter two intermediates using the TEA as base and neutralizing age
... Show MoreBackground: Paracetamol poisoning is a global issue that results in severe liver failure and permanent liver damage, necessitating the need for liver transplantation. The objective of our study was to assess and compare the preventive effects of Apigenin and vitexin against paracetamol-induced liver damage in rats.
Methods: Rats were divided into four groups and treated for seven consecutive days. Group I received 0.5% DMSO, Group II received a single paracetamol dose, and Groups III-IV received 10 mg/kg Apigenin or 40 mg/kg vitexin i.p for 7 days. On the seventh day, all groups except the Group I received a single oral dosage of 3000 mg/kg paracetamol three hours after their final Apigenin or vitexin dose. After 24 hours of parac
... Show MoreAn intranasal drug delivery system offers a non-invasive, effective, reliable, direct, and alternative route to the CNS via the neural connections between the nasal mucosa and the brain. Paliperidone (PAL) is mainly used to treat schizophrenia and disorder. It’s practically insoluble in water class II with low bioavailability 28%. Therefore the aim of preparation of nano nasal suspension gel is in order to target PAL to brain via neural connections of nasal mucosa and the brain, and then enhance the uptake and bioavailability of the drug near and at the site of action. Different variables were investigated in this study, in order to recognize the best formula that aims the drug
... Show MoreNimodipine (NID) is used for the prevention of ruptured intracranial aneurysms and subarachnoid haemorrhage (SAH). The objective of study using the benefits of a combined approach of polymeric nanoparticles and microneedles to fabricate NID as polymeric nanoparticles (NID-NPs) loaded in a bilayer dissolving microneedle (bDMNs) patch to enhance the delivery of drugs through skin layers as a promising noninvasive and painless delivery system, improving poor solubility and lower oral bioavailability (5–10%) owing to first-pass metabolism, which leads to frequent dosing, inconsistent clinical responses, and poor patient compliance. The NID-NPs formula was fabricated with a (1:8) drug to polymer, Soluplus®, w/w ratio and 0.25% polyvinylpyr
... Show MoreNimodipine is a vasodilator medicinal agent approved for the prevention of cerebral vasospasm, a major risk factor that causes deaths in patients diagnosed with subarachnoid hemorrhage. The current marketed products of this drug are associated with challenges such as frequent dosing orally, or continuous infusion through central vein. Therefore, transdermal delivery of nimodipine via transferosomes can overcome these difficulties. Solvent evaporation-hydration method followed by sonication was applied for the preparation of transferosomes. The aim of present study is to investigate and optimize the processing parameters of this method through the utilization of Design-Expert software. Box-Behnken statistical design was selected for this
... Show MoreThe present work aims to formulate carvedilol as nanomicelle and study variables effect on the particle size of nanomicelle, and on the entrapment efficiency (EE%). The formulations were performed by two methods; thin film hydration method and direct dissolution method using soluplus® and polyvinylpyrrolidone (PVP K-25) as polymers. The results revealed that formulations prepared by direct dissolution method exhibits lower size and higher EE% as compared with thin film hydration method, it was found that soluplus® produces larger size of nanomicelle and lower EE% as compared with PVP K-25, it was found that as the amount of polymer raised, the size of nanomicelle increased in both polymers, the effect of solvent indicates that
... Show MoreAmong the many NSAIDs generated from phenyl acetic acid is Aceclofenac, or ACE. Its antipyretic, analgesic, and anti-inflammatory effects are noteworthy. However, the substance's delayed dissolution, limit permeability, and inadequate bioavailability are caused by its low solubility in water, which hinders its usefulness. Nanosponges (NS) are tiny particles with nanoscale holes and a distinctive three-dimensional nanostructure. The incorporation of both water-soluble and fat-soluble molecules into these hollow spaces enhances the efficacy and safety of medication delivery. This study aims to improve and advance the formulation of ACE-containing nanosponges. The emulsion solvent diffusion procedure is used to prepare the nanosponges that
... Show MoreObjectives. Muslims in the United States exhibit high rates of tobacco use, which make them highly vulnerable to lung cancer. Lung cancer could be avoided by regularly undergoing preventive lung screening. This study investigated the associations between Social Cognitive Theory factors and being interested in preventive lung screening in a sample of adult US Muslims.
Methods. We examined a convenience sample of adult US Muslims. A cross-sectional online survey was used to collect data. Binomial logistic regression analyses were conducted to identify the factors related to interest in preventive lung screening.
Key Findings. Two hundred seventy-one eligible parti
... Show MoreCOVID-19 disease is an acute viral infection illness of the airway system resulting from the SARS-CoV-2 virus. Cranberry is an evergreen group of dwarf shrubs of the Vaccinium Oxycoccus. The most important pharmacological effects of cranberry are related to its composition liking of quercetin, flavonols, and proanthocyanidins. cranberry had numerous pharmacological activities encompassing antioxidant, cardioprotective, antibacterial, anticancer, antiviral, and regulated glucose levels. This research aimed to estimate the potential activity of cranberry to enhance the efficacy of standard therapy for COVID-19 infection. A total of 30 patients with age ≥ 18 years suffering from mild to moderate COVID-19 pneumonia volunteered to do this s
... Show MoreCrohn’s disease is an inflammatory bowel disease that is characterized by chronic inflammation of any part of the gastrointestinal tract, has a progressive and destructive course and is increasing in incidence worldwide. Medical treatment of Crohn’s disease is usually divided into remission induction therapy and remission maintenance therapy. Medication-related burden is a new concept focused on the negative experiences resulting from taking medicines. The aims of the current study were to measure medication-related burden among a sample of Iraqi patients with Crohn’s disease, and to determine any associations between medication-related burden and some patient factors. The present study was cross-sectional conducted at ‟Gastroent
... Show MoreTo test the effect of 4 levels of nitrogen (i.e. 0, 45, 90 and 135 Kg N ha-1) as urea (46% N) and 3 levels of phosphorus (i.e. 0, 17.5 and 35 Kg P ha-1) as triple superphosphate (21.8% P) on yield and concentration of dill (Anethum graveolens L. local cultivar) seed oil this experiment was carried out during winter season of 1999 - 2000 at the experimental field of Agriculture College, Abu-Ghraib.
Both fertilizers were applied in two equal splits, first at seeds sowing and the second was added one month after emergence. Dried and ground seed samples were subjected to water distillation for extraction of volatile oils
Result indicated that fertilization of dill plants with 90 Kg N
... Show MoreDiabetes mellitus (DM) is a metabolic disorder specified by persistent hyperglycemia that occurs when β-cell insulin production became unable to control blood glucose with deterioration of response for insulin. The consequent development of DM complications with increased risk for many diseases caused by damaged variety of biological systems, including blood vessels, eyes, kidneys, heart, and nerves. Carnosine is a natural dipeptide (β-alanyl-L-histidine) expressed in both the central nervous system and periphery, it occurs in several tissues most notably in muscle where they represent an appreciable fraction of the total water-soluble nitrogen-containing compounds. Carnosine is synthesized by a cytosolic amino acid ligase, carnosine s
... Show MoreFrom a large number of bacterial samples collected from different hospital in Iraq in central health laboratory ,only ten isolates were identified primary as Vibrio. A number of morphology and biochemical test were carried out to complete this identification that showed all bacterial isolates were related to Vibrio cholerae .In this study all Vibrio isolates were investigated for Bio typing and the result showed that all (10) isolate were related to (Eltor biotypes) .Also, the susceptibility test towards eight antibiotics were carried out .
Results shows that ciprofloxacin , Norfloxacin, Erythromycin, Ampicillin, ceftriaxone and Amikacin were the most effective
... Show MorePsoriasis is a long-lasting autoimmune disease that is characterized by swollen skin patches. Normally, these skin patches are dark, swollen, itchy and scaly. The single application of the innate TLR7/8 ligand Imiquimod (IMQ) in mice easily induces a dermatitis that closely resembles human psoriasis, critically dependent on the axis of IL-23/IL-17. Artemisia dracunculus prepared as an ointment and has been used topically to mice before imiquimod application. The results of the current study showed that A. dracunculus ointment can significantly reduce psoriasis area and severity index in (A. dracunculus ointment + imiquimod group as compared with both control group and (vehicle ointment + imiquimod) group.
The aim of the present investigation was to develop a microsponge delivery system of acyclovir to control its release when applied topically thereby reducing dosing frequency and enhancement patient compliance. The microsponges were produced by the oil in oil emulsion solvent diffusion method. The effect of different formulation and process variables such as internal phase volume, polymer type, drug-polymer ratio, stirring speed and stirring duration on microsponge production yield, loading efficiency, particle size and in-vitro drug release was evaluated. The result showed that the microsponge F2 prepared from Eudrajet RS polymer had optimum physical properties regarding the loading efficiency of 99.71_+ 0.7% and product
... Show MoreChlopheniramine maleate ( CPM ) , is one of the H- receptor antagonist , widely used in allergic diseases ,like skin rash and pruritis .CPM 3%w/w was successfully loaded in 2%w/w sodium alginate (SA) as a gel base , and to be considered as a selected formula .It was found that the diffusion of CPM through the skin of albino rat was increased as the concentration of CPM increased from 2 %w/w sodium alginate , More
... Show MoreEpilepsy is a common chronic neurological disorder that affects almost 50 million people worldwide. Most patients require long-term, and sometimes lifelong therapy with antiseizure medications (ASMs), our case control study evaluates the long-term effect of carbamazepine (CBZ) and valproate (VPA) on bone mineral density and bone health biochemical markers. 50 patients with newly diagnosed epilepsy who had no history of antiseizure medications (ASMs) intake prior were divided into 2 groups. In the first group, 25 patients started carbamazepine (CBZ) monotherapy, while the second group included 25 patients who started receiving valproate (VPA) monotherapy. Another 25 healthy
... Show MoreWet granulation method was used instead of conventional pan coating or fluidized –bed coating technique to prepare enteric-coated diclofenac sodium granules, using ethanolic solution of EudragitTM L100 as coating, binding and granulating agent .Addition of PEG400 or di-n-butyl phthalate as a plasticizer was found to improve the enteric property of the coat.
Part of the resulted granules was filled in hard gelatin capsules (size 0), while the other part was compressed into tablets with and without disintegrant.
The release profile of these two dosage forms in 0.1N HCl (pH 1.2)for 2 hours, and in phosphate buffer (pH 6.8) for 45 minutes as well as the release kinetic were compared with that of the en
... Show MoreA Modified version of the Generlized standard addition method ( GSAM) was developed. This modified version was used for the quantitative determination of arginine (Arg) and glycine ( Gly) in arginine acetyl salicylate – glycine complex . According to this method two linear equations were solved to obtain the amounts of (Arg) and (Gly). The first equation was obtained by spectrophotometic measurement of the total absorbance of (Arg) and (Gly) colored complex with ninhydrin . The second equation was obtained by measuring the total acid consumed by total amino groups of (Arg) and ( Gly). The titration was carried out in non- aqueous media using perchloric acid in glacial acetic acid as a titrant. The developed metho
... Show MoreThe diabetic neuropathy complication exerts a considerable decline in the level of patient’s well-being. The main approaches to hamper the progression of diabetic complications and improve patient’s life quality are controlling the glycemic levels and amelioration of the hyperglycemia-induced neuroinflammation, oxidative stress and pain. Supplementation of appropriate anti-inflammatory and anti-oxidants such as resveratrol may therefore be effective in the management of diabetic complications. The aim of this trial was to assess resveratrol’s impact on improving life quality of patients with the neuropathic complication of diabetes. Sixty-one patients with diabetic neuropathy were recruited in this double-blinded placebo-controlled
... Show MoreUntil today, one of the leading predominant infections is Urinary tract infection (UTI). It exerts a huge burden on health systems worldwide each year. Treating UTIs empirically with antimicrobials improves morbidity rates. This study aims to assess the prevalence of UTI-associated bacteria in adult patients and to determine their antibiotic susceptibility profile. A retrospective study was conducted for adult outpatients who visited Al-Diwaniya tertiary hospitals from January 2020 till February 2022 to review their medical and lab records in addition to sociodemographic data. A total of 256 patients’ records were included of which 204 (79.7%) belong to females and 52 (20.3%) were males with an average age of 39.22±17.10 years. The pr
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