The benzimidazole scaffold is a promising nucleus for developing novel therapeutic agents for ulcer treatment. Its unique chemical structure provides desirable pharmacological properties, such as excellent bioavailability, metabolic stability, and low toxicity, making it an attractive candidate for ulcer treatment. Several benzimidazole derivatives have shown significant anti-ulcer activity in preclinical and clinical studies, acting through multiple pathways, including inhibition of gastric acid secretion, suppression of gastric inflammation, and promotion of mucosal protection. Some benzimidazole derivatives have also demonstrated anti-Helicobacter pylori activity, suggesting their potential for eradicating bacteria associated with ulcer formation. However, challenges such as poor solubility and limited selectivity remain. Various approaches, such as prodrug design and formulation optimization, have been explored to overcome these issues and improve the therapeutic profile of benzimidazole derivatives. Overall, the benzimidazole scaffold holds great promise as a nucleus for developing novel anti-ulcer agents. Further research and optimization efforts are needed to harness its full potential and translate it into effective treatments for ulcers. With continued advancements in medicinal chemistry and drug design, benzimidazole-based compounds may offer new therapeutic options for patients suffering from ulcers and related gastrointestinal disorders. Hence, this review highlights the knowledge about benzimidazole scaffold, the mechanism of ulcer formation, and various benzimidazole derivatives with anti-ulcer activity, which can be further studied in pre-clinical and clinical trials.
the potent antitumor activity of benzimidazole analogues as Indolamine 2,3-dioxygenase-1 (IDO1) inhibitors
The present study aims at the development and evaluation of dental gel containing metronidazole non-biodegradable polymers for targeted delivery of drug and thus prolonging the action. Hot Method was used for the preparation of gel. Natural polymers like, Guar gum, Sodium alginate, Chitosan, Xanthan gum, Gellan gum were used in the formulations of gel. Prepared gels were evaluated for pH, rheological study, spreadability study, gelation, and gel melting study. At last Field Emission Scanning Electron Microscopy FESEM, Differential Scanning Calorimetry (DSC), Thermo Gravimetric Analysis (TGA), Texture Profile Analysis (TPA) have been done on an optimized gel formulation. All gels revealed pH ranged between 6.16 to 6.47, spreadability between 28.37 to 45.03 g.cm/sec, drug content between 90.01 to 99.10 % viscosity ranged between 3108.44 cps and 3645.47 cps and formulations F3 and F10 showed gelation temperature 39±0.12OC and 37±0.13OC respectively which is similar to the temperature of the body. Surface of the sample gels showed no drug particles, indicating a homogeneous mixture of polymers of drugs as well as natural agents. Formulation F10 containing Guar gum showed slower degradation in all media as compared to gels made of Sodium alginate, Xanthan gum, Chitosan, Gellan gum. DSC results revealed that the drug has the same state in the optimized formulation. TGA results showed that the formulation was found to have high stability in high-temperature settings. TPA results of optimized F10 revealed the parameters Mucoadhesive strength 92.54 ± 2.65 g, Hardness 25.34 ± 0.01N/mm², Compressibility 57.75 ± 0.40N mm, Adhesiveness−4.56 ± 0.26 N mm, Cohesiveness 0.83 ± 0.06. Hence, it is concluded that Metronidazole gel with gellan gum showed a longer degradation time and guar gum showed slower degradation in all over polymers used in gel formulations.
Central nervous system (CNS) stimulants are drugs, which produce a response that could be used to alleviate a particular medical condition. These are the agents, which speed up to treat conditions characterized by lack of adrenergic stimulation, including narcolepsy and neonatal apnea. The majority of CNS stimulants is chemically similar to the neurohormone norepinephrine and simulates the traditional "fight or flight" syndrome associated with sympathetic nervous system arousal. A small figure of added members of the CNS stimulant class do not fall into definite chemical groups. The review on central nervous system stimulants gives detail study of CNS stimulant drugs, their mechanism of action and in vivo models of CNS stimulants. The brain is a delicate tissue, and advancement built very effective methods to guard it. Unfortunately, the same mechanisms that protect it against intrusive chemicals can also upset therapeutic interventions. Many current medications are rendered unsuccessful in the treatment of cerebral maladies due to our incapability to efficiently deliver and sustain them within the brain. KEYWORDS: CNS Stimulants, Blood brain barrier (BBB), Drug toxicity, Drug Safety
A new approach to zero- order drug delivery that includes geometric factors is described. Systems such asmultilayered tablets and other geometrically altered devices have been created to perform this function. Themulti-layered matrix system overcomes inherent disadvantages of non-linearity associated with diffusioncontrolled matrix devices by providing additional release surface with time to compensate for the decreasingrelease rate. These formulations designed to deliver the drug at predetermined rate, maintain therapeuticallyeffective concentrations in systemic circulation for prolonged period of time. Recently, pharmaceutical researchhas focused on controlled drug delivery offer definite advantages over conventional release formulation of thesame drug. Controlled delivery systems that can provide zero-order drug delivery have the potential formaximizing efficacy while minimizing dose frequency and toxicity. In the present study, guar gum was used ashydrophilic matrix carrier for designing oral controlled drug delivery systems of highly soluble druglamivudine. Three layered matrix tablets of lamivudine prepared by wet granulation technique were subjectedfor various evaluating parameters and optimized.
This work investigates the preparation of Oxytetracycline Hydrochloride loaded alginate beads to take advantage of the swelling properties of alginate beads for improving the oral delivery. Variations in polymer concentration, concentration of cross-linking agent and cross-linking time were examined systemically for their effects on the particle size, entrapment efficiency, percent yield, flow properties and In vitro drug release behavior. Calcium alginate (Ca-alginate) beads of Oxytetracycline hydrochloride were prepared by ionic-gelation method. Shape and surface characteristics were determined by scanning electron microscopy (SEM). Average particle size of drug-loaded beads was determined by sieving method. In vitro drug release behavior from Ca-alginate beads were carried out in simulated gastric fluid (SGF) for first 2 h and simulated intestinal fluid (SIF) for the next 6 h. SEM confirmed spherical shape of beads with rough and porous morphology. The average particle size of the beads was in the range of 470.96 ± 15.22 to 709.33 ± 16.28 µm. Results indicated that the average particle size and flow property of the beads increased with an increase in the concentration of polymer and the cross-linking agent as well as the cross-linking time. The entrapment efficiency and percentage yield was found to be in the range of 52.87 ± 1.56 to 61.76 ± 0.96 % and 69.98 ± 0.33 to 78.94 ± 0.43 % respectively. Concentration of the sodium alginate up to 1.75 % w/v, cross-linker concentration up to 2 % w/v and cross-linking time (30 min) shows highest percent entrapment efficiency (61.76 ± 0.96 %) and % yield (78.94 ± 0.43 %). A decrease in the rate and extent of drug release was observed with relative increase in the polymer concentration, cross- linker concentration and cross-linking time. No significant drug-polymer interaction was observed in DSC study. From this study it can be concluded that the natural polymer sodium alginate can prolong the release of Oxytetracycline Hydrochloride.
Swine flu has been confirmed in a number of countries and it is spreading from human to human, which could lead to what is referred to as a pandemic flu outbreak. Pandemic flu is different from ordinary flu because it’s a new flu virus that appears in humans and spreads very quickly from person to person worldwide. The World Health Organization (WHO) is closely monitoring cases of swine flu globally to see whether this virus develops into a pandemic. Because it’s a new virus, no one will have immunity to it and everyone could be at risk of catching it. This includes healthy adults as well as older people, young children and those with existing medical conditions. Tamiflu (Oseltamivir) and Ralenza (Zanamivir) can treat the H N swine flu strain. 1 1 Swine flu virus is never before super flu virus but whenever three known virus such as a swine flu strain, bird flu strain and human flu virus combine with each other than makes H N swine flu virus which is not danger if 1 1 we take some protect against it such as a wear three layer mask on nose, wash the hands after coming home, not involve at place where big crowd attended.
The Time Machine (TM) is a spike-based computation architecture that represents synaptic weights in time. This choice of weight representation allows the use of virtual synapses, providing an excellent tradeoff in terms of flexibility, arbitrary weight connections and hardware usage compared to dedicated synapse architectures. The TM supports an arbitrary number of synapses and is limited only by the number of simultaneously active synapses to each neuron. SpikeSim, a behavioral hardware simulator for the architecture, is described along with example algorithms for edge detection and objection recognition. The TM can implement traditional spike-based processing as well as recently developed time mode operations where step functions serve as the input and output of each neuron block. A custom hybrid digital/analog implementation and a fully digital realization of the TM are discussed. An analog chip with 32 neurons, 1024 synapses and an address event representation (AER) block has been fabricated in 0.5 μm technology. A fully digital field-programmable gate array (FPGA)-based implementation of the architecture has 6,144 neurons and 100,352 simultaneously active synapses. Both implementations utilize a digital controller for routing spikes that can process up to 34 million synapses per second.
A novel spike-based computation architecture has been developed which represents synaptic weights in time. An analog chip with 32 neurons, 1024 synapses and an AER block has been fabricated in 0.5μm technology. A digital implementation of the architecture having 6,144 neurons and 100,352 synapses on an FPGA is also described. A digital controller for routing spikes can processes up to 34 million synapses per second. The architecture is called the time machine as it operates on timing events and uses time to store weights. The time machine is general enough for implementing many spike-based algorithms yet provides flexibility and configurability.
The aim of the present study was to evaluate the anti-inflammatory and analgesic activity of ethanolic extract of Scindapsus officinalis (EESO) fruit as assessed in the carrageenan-induced rat paw oedema at the doses of 50, 100 and 200 mg/kg, using different animal models. Phytochemical analysis of ethanolic extract of Scindapsus officinalis has indicated the presence of steroid, flavonoid and terpenoid-compounds. Since these compounds are of pharmacological interest, coupled with the use of this plant in traditional medicine, prompted us for its possible analgesic and anti-inflammatory activities. The ethanolic extract of Scindapsus officinalis showed statistically significant (P<0.001) analgesic activity in albino rat in a dose-dependent manner. The extract at 50, 100 and 200 mg/kg body weight reduced significantly, the formation of oedema induced by carrageenan. The analgesic activity of extract was evaluated for their central and peripheral pharmacological actions using tail flick method. It was concluded that apart from the folklore uses of Scindapsus officinalis as antioxidant agents, the ethanolic extract of fruit of the plant Scindapsus officinalis also possess anti-inflammatory and analgesic activities.
5 Abstract: Huntington's disease (HD) is an inherited disease of the central nervous system that usually has its onset between 30 and 50 years of age. The patient has progressive dementia with bizarre involvantary movements of chorea. The disease slowly progresses and death is usually due to an intercurrent infection. Huntington's disease affects someone's ability to think, talk and move by destroying cells in the basal ganglia, the part of the brain that controls these capacities. A patient with Huntington's disease may present with neurological or psychiatric symptoms, or both. The movement disorder may begin with simple twitching or jerking or with clumsiness or coordination problems. Huntington's disease caused by the expansion of the ployglutamine tract in the N-terminus of the HD protein (Huntingtin). Although there is currently no cure for this disease, there are ways to manage symptoms effectively. Symptomatic treatment of Huntington's disease involves use of Dopamine antagonists, presynaptic dopamine depleters, Antidepressants, Tranquillizers, Anxiolytic Benzodiazepines, Anticonvulsants and Antibiotics. Several medications including baclofen, idebenone and vitamin E have studied in clinical trials with limited samples. In the present article, we have concentrated on clinical features, diagnosis, symptomatic approaches and other possible therapies involved in the management of Huntington's disease. The aim of present article is to provide in depth knowledge about symptomatic treatment and other therapies involved in the management of Huntington's disease. This article reviews current therapeutic agents for treatment of the symptoms of Huntington's disease.