Journal of Applied Pharmaceutical Sciences and Research

DISSEMINATED STRONGYLOIDIASIS IN PATIENTS DIAGNOSED WITH COVID-19 TREATED WITH CORTICOIDS

2023-10-13T12:54:29+0530

The arrival of a new epidemic at the end of 2019 occurred with an outbreak of new cases of people with a clinical picture that ranged from a common cold to serious complications, which included severe acute respiratory syndrome (SARS). With the rapid increase in the number of infected cases, new therapeutic strategies were devised. Among them, the use of corticosteroids is highlighted as a potential reducer of the inflammatory processes caused by the disease, particularly its effect on respiration, which proved to be an important part of the pathogenesis of the disease. The use of glucocorticoids in the treatment of COVID-19, while being efficient, presents problems such as the development of severe strongyloidiasis, especially in those patients who live or have lived in endemic areas for the parasitosis, and thus screening for this condition before therapy is the best immunosuppressive procedure. The evolution to disseminated strongyloidiasis or to hyperinfection in patients co-infected with SARS-CoV-2 undergoing treatment with glucocorticoids increases in chronic, asymptomatic carriers without a previous diagnosis of Strongyloides stercoralis, and this is due to the corticosteroid stimulus of the parasite larvae. Corticosteroids are an important risk factor for the development of S. stercoralis hyperinfection, which apparently does not depend on the dosage used or duration of treatment. After diagnostic confirmation or after establishing the risk through epidemiological stratification, these patients can be submitted to prophylactic treatment with ivermectin. Therefore, as many patients with COVID-19 are undergoing glucocorticoid therapy and these medications increase the risk of developing strongyloidiasis (disseminated form and form of hyperinfection), especially in risk patients, this study was carried out in the context of this approach theme of the coexistence of this parasitological infection and viral infection by SARS-CoV-2 in patients using the aforementioned immunosuppressive therapy. This is a literature review based on the main data platforms, through which 36 articles published between the years 2020 and 2022 were included for analysis.

METHOD DEVELOPMENT AND VALIDATION OF DIMETHYL SULPHATE CONTENT IN ESOMEPRAZOLE MAGNESIUM DRUG SUBSTANCE BY GC-MS

2023-10-13T12:54:30+0530

Dimethyl sulfate is universally used as an alkylating, sulfating and sulfonating agent in organic synthesis; hence it is one of the probable impurities during the synthesis of the esomeprazole magnesium. As per ICH M7, it is genotoxic and mutagenic, so it needs to be controlled as per the acceptable intake of dimethyl sulfate and daily sample dosage. This method validation can be achieved by the hyphenated technique of gas chromatography with mass spectroscopy, which is used to develop the dimethyl sulfate impurity in esomeprazole magnesium drug substance containing salt. The method is achieved with a DB-1 column with electron impact ionization source in sim mode ion under electronic pneumatic pressure control and deliberate oven ramp programming temperature was used. A dissolved, extracted and auto-injection sample was implemented for sample introduction in a splitless mode. Dichloromethane and 2N NaOH was used as a diluent. The calibration curve showed good linearity over the 1.69 to 8.40 ppm (limit: 5.56 ppm) and its correlation coefficient was >0.999. A limit of detection 0.50 ppm and limit of quantitation 1.69 ppm was achieved when the samples were prepared at 50 mg/mL. While recovery proved to be 106.8 to 113.5%, hence it signified the matrix effect.

MOLECULAR DOCKING PREDICTION OF CARVONE TOWARDS GABA-ATASE AND SODIUM CHANNEL

2023-10-13T12:54:30+0530

Aim: Modern tool designs frequently employ molecular docking to anticipate small molecules’ binding orientation and better comprehend drug-receptor interactions. Carvone’s molecular docking analysis against sodium channels and GABA-AT is part of this research investigation.

Introduction: Carvone’s molecular docking analysis against sodium channels and GABA-AT is part of this research investigation. The biological significance of carvone has been demonstrated to include anti-epileptic, anti-fungal, anti-inflammatory, anti-cancer, and antioxidant effects. In modern drug design, molecular docking is commonly used to get an understanding of drug-receptor interaction carried out an in-silico evaluation of derivatives of carvone.

Methodology: ChemDraw 2D (15.1) software is used to draw the ligands, ChemDraw-3D is utilized to decrease energy consumption, chimera is used to produce the protein, and Auto Dock 4.0 was used to examine the binding score. To determine whether it would cross to BBB+/BBB- or not, cheminformatics and fingerprint analysis were done using Molinspiration and Adaboost with SVM.

Result: Comparable metrics for newly created carvone derivatives included potential energy, docking score, glide score, and highest docking score. Compounds with docking scores of (-8.39, -5.06, -4.00 kcal/mol). The conformers at the active site are shown and predicted using Discovery Studio Visualizer.

Conclusion: The results of the molecular docking study showed that compound1 has a high affinity for the active pocket and a low binding energy, which made them potentially useful as an anti-convulsant.

PREVALENCE AND ASSOCIATED FACTORS OF PEPTIC ULCER DISEASE AMONG DYSPEPTIC PATIENTS AT ENDOSCOPY UNIT IN KABUL, AFGHANISTAN

2023-10-13T12:54:30+0530

Introduction: Dyspepsia is a medical term utilized to describe a cluster of symptoms related to the digestive system, particularly in the upper gastrointestinal tract. The most prevalent causes of dyspepsia encompass gastro esophageal reflux disease (GERD), peptic ulcer disease (PUD), and non-ulcer dyspepsia (NUD). A peptic ulcer is a sore or erosion that forms in the lining of the stomach, upper part of the small intestine, or lower part esophagus.

Materials and Methods: The study incorporated 500 dyspeptic patients who underwent upper gastrointestinal endoscopic assessments. This hospital-based analytical cross-sectional study was conducted at the endoscopy unit of different hospitals, spanning from January 1, 2023, to September 30, 2023.

Results: The findings revealed that out of 500 dyspeptic patients, 45 (9%) exhibited positive results for peptic ulcer, while 455 (91%) displayed non-peptic ulcer conditions. The correlation between dyspepsia and peptic ulcer was statistically significant (χ2= 73, P= 0.01). Gender-specific prevalence indicated that 17 (37.7%) males and 28 (62.2%) females exhibited peptic ulcers. When stratified by age, the prevalence was 20 (44.4%) for individuals aged 18-40, 10 (22.2%) for those aged 41-52, and 15 (33.3%) for those above 52 years. Notably, significant differences were observed among age groups (χ2= 85, P= 0.04). Peptic ulcer prevalence was 16 (35.55%) for urban residents and 29 (64.44%) for rural residents. In the context of smoking habits, 30 (66.6%) of smokers exhibited peptic ulcers, compared to 15 (33.3%) of non-smokers. The association between smoking and peptic ulcers was statistically significant (χ2= 101, P= 0.02). Additionally, 28 (62.2%) of individuals with H. pylori infections displayed peptic ulcers, in contrast to 17(37.7%) without the infection. The association between H. pylori infection and peptic ulcers was statistically significant (χ2= 85, P= 0.05). Regarding NSAID use, 29 (64.4%) of participants who used NSAIDs and 16 (35.5%) who did not use NSAIDs showed peptic ulcer prevalence. The highest prevalence was among individuals using NSAIDs for pain relief. The association between NSAID use and peptic ulcers was statistically significant (χ2= 100, P= 0.05).

Discussion: These results highlight the significance of addressing these risk factors in the management and prevention of peptic ulcer disease.

DISCOVERY OF NOVEL PHTHALIMIDE ANALOGOUS BASED ANTI-EPILEPTIC BY MOLECULAR DOCKING

2023-10-13T12:54:30+0530

Aim: The development of innovative compounds for managing seizures with greater therapeutic efficacy and fewer side effects by molecular docking.

Introduction: One of the major global problems is epilepsy, a severe brain illness that affects around 1% of people globally. Vigabatrin, sodium valproate, phenytoin, and other strong medications for the treatment of epilepsy causes side effects and patient resistance. Despite the antiepileptic drug development process seems to be successful, more effective and safer, still antiepileptic drugs are needed, especially for the treatment of refractory seizures. The study’s focus was on phthalimide analogs with strong GABA-AT inhibitory effects by molecular docking.

Methodology: Since protein-ligand interactions are important for drug design, The protein data bank was used to retrieve the 3D structures of GABA-AT, and the Chem Office tool was used to dock the 3D structures of Novel Ligand (Chem Draw 16.0).

Result: By using Lipinski’s rule of five on the novel analogs to assess their anti-epileptic activity, and the drug-likeness property was verified. All the compounds had docking energies over 6.11 kcal/mol for the anti-epileptic GABA-AT receptors.

Conclusion: These concluded that novel compounds can be the promising lead for further study as an Anti-Epileptic for the management and prevention of Epilepsy

EXPLORING ANTIDIABETIC POTENTIAL OF GYMNEMA SYLVESTRE

2023-11-03T14:22:28+0530

Context: Gymnema sylvestre (GS) is a plant species that is mostly found in the tropical regions of Asia, Africa and Australia; it is widespread in India and Sri Lanka. According to various scientific studies, GS contains a chemical constituent that is known to suppress the taste for sugar; this kindled our interest to study the various extracts of GS for their antidiabetic potential.

Aim: The current study emphasizes screening the leaves extracts of Gymnema sylvestre using chloroform, ethyl acetate, and water for their phytoconstituents and evaluating their Antidiabetic property. All the individual concentrates were exposed to subjective qualitative examinations for the distinguishing proof of the phytoconstituents, which was followed by evaluating the effect of different extracts of GS on blood glucose level against Streptozotocin induced Diabetic rats as GS had been reported for its antidiabetic activity.

Material and Methods: The plant material Gymnema sylvestre 1.5 kg was macerated with 3.75 liter of chloroform, ethyl acetate and water for comparative antidiabetic activity. A total of 36 male wistar rats were utilized to induce diabetes by means of intraperitoneal injection with 60 mg/kg STZ. The acute toxicity study adhered to the guidelines set by the Organization for Economic Co-operation and Development (OECD 423, 2001). Throughout a period of 21 days, the animals received various treatments. Glucose levels were measured on day 1, which marked the initiation of any treatment, as well as on the 7th, 14th, and 21st days, utilizing a one-touch glucometer. Hematoxylin and eosin staining were employed for histopathological examination of the pancreas. Statistical analysis was conducted using SPSS software, employing one-way ANOVA followed by Dunnet’s multiple comparisons.

Results: Blood glucose levels in streptozotocin induced diabetic rats fed with different GS extracts decreased to normal levels. When the reduced percentage of blood glucose levels of the various extracts was compared with that of glibenclamide (62%), aqueous extract showed maximal (59%) decline, thus confirming the potentiality of the GS as the most significant antidiabetic agent.