bluuebunny/crossref_metadata_2025_split huggingface dataset:
Repurposable Drug Candidates are Potential Therapeutic Target against Global SARS-CoV-2 Crisis
Authors: Rahman Md. Siddikur , Mina Fahmida Begum , Das Sabuj , Billah Mutasim , Sumon Karmakar Sumon Karmakar , Khan Alam , Akhtar Sharmin , Acharjee Uzzal Kumar , Hasan Md. Faruk 
Published: October 2020

This review provides a pharmacological approach to combat Severe Acute Respiratory Syndrome Corona Virus-2 (SARS-CoV-2) based on two comprehensive denominations which could be specifically intended for viral replication process by either inhibiting essential genomic viral enzymes or preventing viral entry to human cells. These denominations focused on immune therapies either to improve innate antiviral immune responses or to reduce impairment triggered by underactive inflammatory reactions. A variety of drug candidates are available which can inhibit SARS-CoV-2 infection and replication, comprising serine protease inhibitors: Transmembrane Orotease/Serine Subfamily member 2 (TMPRSS2), camostat mesylate, nafamostat mesylate, and angiotensin-converting enzyme inhibitors. This review is also concerned with identifying drugs and ongoing clinical trials with their mechanisms of action against SARS-CoV-2. Chloroquine and hydroxychloroquine, monoclonal antibody, off-label antiviral drugs, nucleotide analog remdesivir and broad-spectrum antiviral drugs also could be used as inhibitors of SARS-CoV-2. Moreover, non-steroidal anti-inflammatory drugs (NSAIDs), dexamethasone, and antiviral phytochemicals that are currently reachable, can prevent SARS-CoV-2 pandemic morbidity and mortality.
Keywords: COVID-19; Antiviral drugs; NSAIDs; ACE2; Clinical trials
Optimization of Process Parameters for Formulation of Fluvastatin Tablet by Using Dry Granulation Method
Authors: Shete Nikhil Arun , Swami Vishwajeet , Kulkarni Vaibhav , Paratkar Gajanan , Mohan Rahul 
Published: October 2020

The manufacturing process of the tablet is a very complex process; it can be affected by the several process parameters or variables. The aim of this study was to understand and optimize the process parameters such as mixing, granulation, lubrication and tablets compression processes using quality by design (QbD) approach for a model Anti- Hyperlipidemic drug Fluvastatin sodium. During the processes there are several parameters which may influence or affect product quality. So the main objective of present work was to identify various process parameters and optimize this parameter, for the formulation of good quality product which needs to optimize Blending time, Roller force, Compression force and machine speed. A scale up batch was taken to evaluate and optimize the parameters. Critical quality attributes (CQA) such as flow behavior, granules parameters, Blend uniformity, tablet appearance, effect on tablet quality like physical appearance (surface, weight etc.) and tablet dissolution time as well as drug release. The test results of following parameters at various in-process phases are complies with the specified limits and finished product sample results were found to be within specified limits. This study results assures the manufacturing process is reproducible, robust and will yield consistent product, which meets specification.
Keywords: Process Parameters, Quality by Design, Fluvastatin, Granulation, Blending, Compression etc,.
Pharmacology, Pharmaceutics and Clinical Use of Aspirin: A Narrative Review
Authors: Alegbeleye Bamidele Johnson , Akpoveso Oke-Oghene Philomena , Mohammed Rana Kahdim , Asare Bernard Yeboah-Asiamah 
Published: October 2020

Background: Aspirin is one of the most frequently used and cheapest drugs in medicine. Since its first synthesis in 1897, several medicinal roles and mechanisms of action of Aspirin have become apparent, the latest among these being its role in cancer prevention and treatment.
Objective: We present a review of Aspirin's biochemistry and pharmacology, as well as the clinical use of Aspirin. The communiqué also suggests possible strategies for maximizing the gain of Aspirin as a wonder-drug of the future.
Methods: The literature search strategy covered printed and online sources, including manual library search (PubMed), Embase, Medline, and Cochrane Library. For papers written in English and published in the last ten years. A systematic analysis of available data was subsequently performed based on the review questions. An estimated 155 articles were found online, and twenty-eight articles utilized in the final analysis.
Discussion: Aspirin belongs to the non-steroidal anti-inflammatory drugs with a wide range of pharmacological activities, including analgesic, antipyretic, and antiplatelet properties. Discovery of antiplatelet effects led to the increasing use of Aspirin as an anti-thrombotic agent in the prevention of cardiovascular diseases from the 1980s, and firm evidence supporting its usefulness has continued to accumulate. Aspirin irreversibly inhibits platelet function by acetylating cyclooxygenase (COX), which is involved in the production of a potent platelet stimulator, thromboxane A2. The inhibition of COX-2 by Aspirin forms the basis of its anticipated role in preventing colorectal cancer and Alzheimer's disease and the inhibition of the progression of these diseases. It has been pointed out that the incidence of cardiovascular events tends to be high among patients who are Aspirin resistant, but the reason for this increased incidence remains unclear.
Conclusion: The emerging future interest is to accrue evidence in favor of Aspirin as the novel therapeutic drug for combating severe acute inflammation and thrombosis associated with the cytokine storm in COVID-19 patients. Notably, a randomized clinical trial, to test a range of potential treatments for COVID-19, includes low-dose Aspirin as anti-inflammatory and antiplatelet treatment.
Keywords: Aspirin; Anti-platelet; Nonsteroidal Anti-inflammatory Drug; Pharmaceutic; Pharmacodynamic; Pharmacokinetic.
A Prospective Observational Studies on Drug Utilization Evaluation and Rational Use of Corticosteroids in Tertiary Care Hospital
Authors: Unissa Syeda Masarrath , Kareem Sana , Ahmed Sumaiya Faheem , Ul Haq Syed Imran , Quadri S Ahmedullah Hussaini 
Published: October 2020

Background: Corticosteroids are widely prescribed Drugs in Hospitals, forming a part of standard treatment of modern medicine for a wide range of diseases, associated with inflammation and immune activation. Apart from beneficial effects they also produce number of adverse effects. In the present study, Prospective Observational studies on DUE (Drug utilization evaluation) and rationality of Corticosteroids has been Performed.
Objectives: To Investigate the Drug utilization evaluation, Prescription pattern and Rationality of corticosteroids in various department of tertiary care teaching hospital.
Methodology: A prospective observational study was conducted on 100 patients receiving corticosteroids in the various departments of Osmania general Hospital, Hyderabad. Patients prescribed corticosteroids therapy was included in the study. Exclusion of those patients with age less than 18, psychiatric disease, pregnant women and patients not willing to sign on consent form.
Result: This study included 100 Patients out of which 68 were Male and 32 were female. In Age wise distribution, 15 Patients prescribed with corticosteroid in age group 18-28 years, 20 patients in 29- 38 years, 12 in 32-48 years, 16 in 49-58 years, 22 in 59-68 years, 11 in 69-78 years and 4 in above 80 years. This data showed that commonly male populations are more prone to diseases. As per the demographic data our finding shows that Budesonide was the most frequent prescribed corticosteroid (31.75%) followed by Hydrocortisone (26.19%), Dexamethasone (15.08%), Prednisolone 13.49%, Betamethasone (7.94%), Methyl prednisolone (5.56%).
Out of 100 prescriptions total 10 ADRs and 25 Drug interactions were detected in this study. The majority of drug interactions were minor 24 followed by major 1.
Conclusion: The Prescription pattern of corticosteroids was found to be rational as there is no Major drug interaction. Commonly geriatric population was more prone to diseases, for which steroids were used. Hence close observation is required to ensure safety, effectiveness and well-balanced therapeutic management with corticosteroids, both patients and prescribers should be more aware of the appropriate dose, dosage regimen, Drug - Drug interactions, ADRs and overall guidelines for corticosteroids prescribing.
Keywords: Corticosteroids, Drug utilization evaluation, Prescription pattern.
Histo-Epidemiological Profile of Endometrial Cancer in the Oran Region
Authors: FIZAZI Anissa , BOUZOUINA Imene , BOUZIANI Assala Nesrine , BELHADJ Amina , SEDDIKI Sonia , SAHRAOUI Tewfik 
Published: October 2020

Objective: The aim of the present study is to describe the epidemiological, histopathological and therapeutic profile of endometrial cancers in the region of Oran.
Methods: We conducted a retrospective study by exploring the medical files of 25 female patients diagnosed of endometrial cancer and treated at the level of the EHU November 1, 1954’s medical oncology department in Oran during the period from January 2015 to December 2019.
For data collection, we used a structured exploitation sheet to obtain necessary information. Variables were analyzed using SPSS Software Version 20.0.
Results: The median age of patients was 59 years with extremes ranging from 42 to 83 years. More than 56% of our patients were over 50 years old, 40% of the patients were nulliparous and 80% postmenopausal. The average age of menarche was 14.09 ± 1.44 years with extremes ranging from 12 to 17 years. The indication for anatomopathological examination was dominated by metrorrhagia (80%).
Histopathologically, endometrioid adenocarcinoma was the most common at 75% of cases. We also note that 62.5% were classified in stage I and 37.5% in stage II. Myometrium infiltration was observed in 66.67% of cases. The basic treatment for endometrial cancer remains surgical.
Conclusion: At the end of this work, we concluded that this pathology remains essentially that of postmenopausal women. Endometrioid adenocarcinoma was the most common histologic type. This study also revealed many risk factors for endometrial cancer, such as advanced age, hypertension and nulliparity.
Keywords: Cancer, Endometrium, Epidemiology, Anathomopathology, Risk factors
Inhibitory Effect of Xanthine Oxidase from Tamus communis Roots Extracts/Fraction
Authors: ZERARGUI Fatima , SAFFIDINE Karima , GUEMMAZ Thoraya , BAGHIANI Abderrahmane 
Published: October 2020

In the course of our phytochemical studies of plant Tamus communis L., methanol soluble extract (EMeOH) (138 g) was chromatographed on a silica gel column. The column was eluted with chloroform and then with chloroform /methanol mixtures of increasing polarity. A total of 52 fractions (400 ml each) were collected and grouped according to their TLC behaviour into 6 main fractions (I-VI). Total phenolic and flavonoid contents in these extracts were determined by a colorimetric method. Values varied between 73.143±0.009 and 29.214±0.003 equivalent Gallic acid/g lyophilisate. All the extracts showed inhibitory properties on xanthine oxidase, the IC50 ranges from 0.029±0.017 mg/ml to 0.237±0.026 mg/ml. The extracts exhibited an additional superoxide scavenging capacity by using both enzymatic methods and IC50 values ​​range from 0.039±0.023 mg/ml to 0.141±0.086 mg/ml. These results show that Tamus communis L. extracts have strong anti-oxidant effects and may have some clinical benefits.
Keywords: Xanthine oxidase, Antioxidant, Superoxide scavenger, Tamus communis L.
In-vivo Evaluation and Characterization of Novel In-Situ Gelling System as Controlled Delivery System Containing Ciprofloxacin for Ocular Drug Delivery
Authors: Eram Fatima , Vivek , 
Published: October 2020

Objectives: The purpose of this research was to develop the micro emulsion-based in situ gelling systems containing Ciprofloxacin for prophylaxis and treatment of the posterior segment diseases like endophthalmitis.
Methods: Ciprofloxacin was encapsulated in small droplets owing to form microemulsion, and then the formed droplets were dispersed in a polymer solution that converted into a gel upon triggered by the electrolyte present in the tear fluid.
Results: The formulation approach provides better absorption, penetration, retention, and improves the bioavailability of the drug. The average concentration reached into vitreous humor from topical microemulsion in situ gelling formulation was ~0.4 µg/ml, which is far more than the concentration required for therapeutic effect (i.e. >0.047 µg/ml or >MIC90 for S. Epidermidis, a pathogen commonly responsible to cause endophthalmitis).
Conclusion: Thus, novel micro emulsion-based in situ gelling formulation could be a potential drug delivery system for the treatment of posterior segment diseases like endophthalmitis.
Keywords: Microemulsion, ciprofloxacin, endophthalmitis, ocular, infection, in situ
Sperm Profile of Infertile Men in the Western Region of Algeria: About 320 Cases
Authors: FIZAZI Anissa , BENDAHMANE Malika , SAHRAOUI Tewfik 
Published: October 2020

Objective : The aim of this study is to describe the sperm profile and eventually determine the main spermatic disturbances at the origin of male infertility in western Algeria. Methods: We conducted a cross-sectional study in 320 infertile male patients consulting at the Medically Assisted Procreation Unit (MAP) of Oran, in Western Algeria, in the end of exploring the results of their semen analyses and semen culture. Results: The results of semen analysis revealed that the main spermatic disruption in our study was asthenospermia because at the first hour after emission, 93% of our patients had less mobility than normal. Oligospermia was present in 37% of cases and azoospermia in 14% of cases. That is, a concentration of sperm below normal in 51% of cases. Results of the analysis of the sperm’s morphological characteristics revealed that only 16% of our patients had teratospermia. The semen culture revealed that the main pathogen found in our patients is Staphylococci in nearly 70% of cases. Conclusion: Our study revealed alterations in both quantitative and qualitative semen of patients. This was mainly asthenospermia in 93% of cases followed by oligospermia. Keywords: Male infertility, Semen analysis, Semen culture, Western Algeria.
Co-Trimoxazole Induced Severe Cutaneous Adverse Reaction: A Challenging Diagnosis
Authors: Sreehari M , Sana M M , Tom Cyril 
Published: October 2020

Introduction; Drug Reaction with Eosinophilia and systemic symptoms (DRESS) Syndrome is a life-threatening reaction with a mortality rate of 10-20%. Usual reaction period is 2 to 6 week after the first intake of drug. The present case is an example of late presentation of the symptoms which made the diagnosis difficult.
Clinical case: We describe a case of 51 year old male with known history of Acquired ImmunoDeficiency Syndrome (AIDS) and Tuberculosis (TB) presented with complaints of fever, generalised scaling, oedema, eosinophilia and elevated liver enzymes. The symptoms started 45 days back but was then misdiagnosed and treated as exfoliative dermatitis from a local hospital. The symptoms aggravated since 5 days and were admitted in our hospital. Drug reaction was least suspected as he has been taking the Antiretroviral (ART) and Anti-tubercular (ATT) drugs since 3 to 4 months. But later on culprit drug was identified to be Sulfamethoxazole-Trimethoprim and was soon discontinued. Significant improvement was seen with steroid, antihistamines and other topical agents.
Discussion: Timely recognition of DRESS Syndrome, prompt discontinuation of culprit drug and symptomatic management are imperative in a better prognosis. It must also be noted that the latency period can be as long as 105 days after the first intake of the drug, rather than the usual presentation period of 2-6 week.
Phytochemical and Pharmacological Investigations of Lannea grandis (Dennst.) Engl. Leaves Extracts
Authors: Akhter Sharmin , Shahadat Sarrin , Homa Zilly , Kuddus Md Ruhul , Chowdhury M Mohi Uddin , Ibrahim Mohammed 
Published: October 2020

Medicinal plants can serve as a prominent source of bioactive secondary metabolites which can exert beneficial effects to combat against many human diseases. Lannea grandis (Dennst.) Engl, a member of Anacardiaceae family has several applications in the ethnomedical practices. In this study, the ethanol extract of L. grandis leaf (ELG) along with its petroleum-ether and chloroform fractions were subjected to phytochemical analysis along with the evaluation of antimicrobial, anti-diarrheal, and sedative activities using standard protocols. Phytochemical screening was performed according to common phytochemical tests. Antimicrobial assay was carried out by disc diffusion method where the ethanol extract of L. grandis showed significant activity against tested bacterial species (zone of inhibitions = 10.8±0.85 to 13.8±1.84 mm). The same extract also exhibited the highest antifungal activity against Blastomyces dermatitidis (zone of inhibition = 20.5±0.35 mm). The chloroform fraction of L. grandis at the dose of 400 mg/kg body weight produced a significant (p<0.05) anti-diarrheal effect with 40.69% inhibition of castor oil-induced diarrhea in mice. During sedative activity assay in mice, the plant extract at the dose of 400 mg/kg body weight produced mild reduction in the time of onset of sleep and increased the length of the sleeping time induced by a sedative, phenobarbitone. In conclusion, the plant L. grandis can be considered as a base for the development of new drugs and phytomedicine.
Keywords: Lannea grandis, phytochemical, antimicrobial, anti-diarrheal, sedative activity.
Prescribing Pattern of Drugs Used in Chronic Liver Disease with Co Morbid Conditions and Assessment of Severity using MELD Score: A Prospective Observational Study
Authors: Huma Samreen , Fatima Omer Nishat , Ayesha Ishrath , Moiz Jamal Mohammed , Mohiuddin Shareef Mohammed 
Published: October 2020

Objectives: To study the prescribing pattern of drugs & its use in the treatment of CLD & assess the pattern of co-morbidities associated with CLD. To Study the mortality rate of the patient using MELD score at a department of general medicine at Osmania general Hospital to produce a result which would aid better rational drug use and improve quality of life.
Methodology: A Prospective, observational study was carried out at OGH for a period of 6 months in 100 old patients. Population of either sex or ≥ 18 years of age were included.
Conclusion: There is a considerable scope for improving prescribing pattern in CLD by minimizing the use, reduction of doses of drugs to reduce the consequence of hepatotoxicity and Antibiotic Resistance. The prognostic impact of individual comorbidities, on the other hand, may point to areas where cirrhosis and comorbid diseases interact. Studies of individual comorbidities may therefore improve our understanding of the pathophysiology of cirrhosis. MELD showed that the subjects were less likely to get a Liver transplant.
Keywords: Chronic liver disease (CLD), Model for end stage liver disease (MELD), Diabetes Mellitus (DM), hypertension (HTN)
Therapeutic Efficacy of Ursodeoxycholic Acid (Fortibile® tablet) on Nonsteroidal Anti-Inflammatory Drug (NSAID)-induced Hepatic Dysfunction in Experimental Animals
Authors: Darbar Soumendra , Saha Srimoyee , Chattopadhyay Shyamaprasad 
Published: October 2020

Background: Hepatotoxicity is one of the common side effects of nonsteroidal anti-inflammatory drugs (NSAIDs). Scientific study stated that hepatotoxicity is the most serious adverse effects of Aceclofenac.
Objectives: In this study, our aim was to investigate the use of Fortibile® tablet containing ursodeoxycholic acid (UDCA) in prevention of the hepatotoxic effect and biochemical changes induced by aceclofenac (ACE) in laboratory mice.
Materials and Methods: Swiss albino mice were divided into four groups (control, UDCA (Fortibile® tablet) 20 mg/kg, aceclofenac (ACE) 50mg/kg, UDCA 20 mg/kg + aceclofenac 50 mg/kg).
Results: Administration of aceclofenac (ACE) showed decline body weight, food consumption, water intake and elevated liver weight in mice whereas treatment with UDCA (Fortibile® tablet) normalized the same as compared with untreated animals. Animals treated with aceclofenac caused elevated activities of serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP) as well as total and direct bilirubin level. These elevations in liver enzymes were decreased by combination of aceclofenac with UDCA. On the other hand application of aceclofenac (ACE) on mice caused a significant increase in serum and tissue malondialdehyde (MDA) and nitric oxide (NO) content but significant decrease in glutathione GSH and GPx content. Combine thepary of UDCA and aceclofenac resulted in a significant decrease in MDA, NO content and significantly elevated GSH and GPx content.
Conclusion: It could be concluded that Fortibile® tablet containing Ursodeoxycholic acid acts as an effective hepatoprotective agent against NSAIDs induced liver dysfunction, and this effect might be related to its antioxidant properties. Hepatic functions should be monitored, and the dose should be adjusted during aceclofenac (ACE) therapy.
Keywords: Ursodeoxycholic acid, Aceclofenac, Hepatotoxicity, Liver function test, Oxidative stress,
Solid Lipid Nanoparticle for the Delivery of Docetaxel: A Review
Authors: Agrawal Pranav , Tatode Amol , Umekar Milind 
Published: October 2020

Solid lipid nanoparticles are the forefront of the rapidly developing field of nanotechnology with several potential applications in drug delivery, clinical medicine and research. Due to its solid state it has greater stability than other nanocarrier systems. There are several other advantages like sustained release, improves bioavaibility and delivery of poorly water soluble drugs, helps in control of several pharmacokinetic parameters of drugs due to which use of SLN is increasing day by day. Various techniques can be used for the formulation of SLN i.e. solvent evaporation, microemulsification technique, high pressure homogenization and supercritical fluid method. It has several applications likes it is use in gene transfer therapy, also use in different drug delivery systmer like oral and pulmonary drug delivery system. Due to several advantages SLNs are widely used in chemotherapy for the treatment of the cancer. The use of SLN for the delivery of Docetaxel to tumor site have several benefits likes site specific delivery, less toxic effect, more cell cytotoxicity and more bioavaibility which leads to decrease in the dosing frequency. Docetaxel is an anticancer agent extracted from plant Taxus Baccata which is widely used in chemotherapy to treat cancer. This article contains the detail information of about the advantages, disadvantages, different method of preparation and several SLN loaded with Docetaxel.
Keywords: Solid lipid nanoparticles, drug delivery, clinical medicine, poorly water soluble drugs