Posted by admin on Jan 31, 2021 in |
The present work evaluates the impact of alterable manufacturing and formulation factors on the physicomechanical properties of Acetaminophen (APAP); a poorly compressible Active Pharmaceutical Ingredient (API). By varying the amount of APAP and particle size of Microcrystalline Cellulose (MCC), six different formulations were prepared. These formulations were compressed into tablets at different compression pressures and speeds. The porosity of the tablets was evaluated through “out-of-die” Heckel analysis. Furthermore, the qualitative and quantitative relationships of (i) Percentage of APAP, (ii) Compression pressures, (iii) Compression speeds, and (iv) Particle size of MCC with tablet porosity were evaluated by principle component analysis (PCA) and principle component regression (PCR). Heckel analysis revealed that increasing the ratio of APAP to MCC in the formulation adds its compressibility when the MCC particle size is similar to that of APAP. While, using large MCC particle size increases the compressibility due to fragmentation of particles, using MCC of small particle size increases the compressibility to a higher extend. The PCA indicated that the percentage of APAP, compression...
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Posted by admin on Jan 31, 2021 in |
The outbreak of a novel coronavirus 2019 was traced back in China in late 2019, followed by their worldwide transmission as a pandemic. From January to August 2020, a total of 1,724 papers were published, where 125 were only published in August 2020, demonstrating the importance and need for current awareness and research to overcome this deleterious virus. This paper briefly highlighted the major characteristics of the SARS-CoV-2 in detail, including; a brief history of coronavirus, various transmission routes, range of mild to severe symptoms, available diagnostic tests, treatment options, measures for infection control and prevention, and particular emphasis on self-acceptance and upholding to face mask-wearing. The impact of the COVID-19 pandemic is limitless and has affected all the nation throughout the horizon; the voyage is indeed hard but not impossible to overcome. However, it is the responsibility of each and every individual to be cautious, know, and understand their role in this difficult situation. To conclude, due to the lack of cohesive data, this review has collated the...
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Posted by admin on Jan 31, 2021 in |
There is a new public health crisis threatening the world with the emergence and spread of the 2019 novel coronavirus (2019-nCoV). Coronavirus disease 2019 (COVID-19) is caused by the Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2), which invades cells through the angiotensin-converting enzyme 2 (ACE2) receptor. SARS-CoV-2 shares 82% genome sequence similarity to SARS-CoV and 50% genome sequence homology to Middle East respiratory syndrome coronavirus (MERS-CoV); all three coronaviruses are known to cause severe respiratory symptoms. Cancer patients are more susceptible to infections than healthy persons because of their systemic immunosuppressive state caused by the malignancy and anticancer treatments, such as chemotherapy or surgery. Therefore, these patients might be at increased risk of COVID-19. The level of ACE2 expression may play a role in the risk of reporting COVID-19 infection and the risk of developing more severe forms of the disease in cancer patients the disease in cancer patients. Treatment is essentially supportive; the role of antiviral agents is yet to be established. Prevention entails home isolation of suspected cases...
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Posted by admin on Jan 31, 2021 in |
Gentisic acid (2, 5-dihydroxybenzoic acid) is a diphenolic compound, present abundantly in natural sources. It possesses several pharmacological activities such as nephroprotective, hepatoprotective, neuroprotective, etc. However, the available literature on oral absorption of gentisic acid is scarce. Thus, the aim of the present study was to determine the pharmacokinetic parameters and bioavailability of gentisic acid. A single dose in-vivo pharmacokinetic study was conducted in rats. Gentisic acid was administered at 50 mg/kg, either orally or by intravenous route. Blood samples were withdrawn at designated time intervals (0.083, 0.25, 0.5, 1, 2, 4, 8, 12, and 24 h post-dose), and plasma was separated. A method for the evaluation of gentisic acid in the plasma was developed and validated. The plasma levels of gentisic acid were determined by HPLC using the validated method. The Cmax for oral administration was 312 µg/mL, and Tmax was at 0.083 h. The plasma exposure AUClast values for oral and i.v route of administration were comparable (Oral: 765 h*µg/mL; I.V.: 770 h*µg/mL), indicating similar bioavailability. The...
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Posted by admin on Jan 31, 2021 in |
Drug resistance mutations M184V and M184I are associated with lamivudine. Y181C and H221Y drug resistance mutations are associated with nevirapine and efavirenz and G190R and M230I drug resistance mutations are associated with efavirenz in the reverse transcriptase gene of HIV-1. In the present study, we attempted to identify the drug resistance mutations and interacting amino acids in the reverse transcriptase gene of HIV-1 through a molecular docking approach. Molecular docking of first-line antiretroviral drugs like lamivudine, nevirapine, and efavirenz with wild and mutant type structures was performed using MTi auto dock to compare the binding behaviour of drugs with amino acids of the reverse transcriptase gene. The receptor structure preparation was performed by the University of California, San Francisco chimera (UCSF Chimera). The Ligplot program was used to plot the 2D interaction diagrams of protein-ligand complexes. The 3D models of the mutant-drugs were generated using PyMOL (PyMOL molecular graphics system). The clear bond interactions were visualized with Discovery Studio 3.5 (BIOVIA, USA). Thus, these findings suggest that mutations in...
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