Pharmacokinetic Study and Toxicity of Leukovir: A New Combined Drug for the Treatment of Multiple Sclerosis
Show Abstract
Abstract
Leukovir, an enteric-coated tablet, is the original drug product for internal
use. The well-known nucleosides cladribine and ribavirin are the active ingredients of the drug product leukovir. Pharmacokinetic parameters of the
drug product for the internal use of leukovir active ingredients have been established. The cladribine half-absorption period was t1/2a = 49.5 h, C0 = 276.4
μg/ml, Cmax = 6.0 μg/ml. Distribution and accumulation parameters (Vd, Vss
and AUC) have indicated that the drug distribution between the blood cells
and blood plasma takes place in the same way, irrespective of the dosage
form. Cladribine half-life period is t1/2e = 0.62 hours. The molecule total
clearance and average lifetime in the body in the case of subcutaneous drug
administration are approximately the same. Ribavirin is characterized by a
half-absorption period of t1/2a = 0.71 h, C0 = 115.6 μg/ml and Cmax = 75.5
μg/ml. Ribavirin total volume of distribution (Vd = 1.3 l/kg) and stationary
volume of distribution (Vss = 1.64 l/kg) were practically similar to leukovir
when administered subcutaneously. The AUC value = 504.2 μg h/ml, which is
2.5 times less than that in the case of drug form administration. Leukovir was
regarded as slightly toxic in an acute toxicity study. The risk of cumulation
for this drug product is low.
|
Elena N. Kalinichenko,
Irina V. Ponteleeva,
Marina B. Golubeva,
|
0 |
Download Full Paper |
0 |
Safety and Efficacy of a Proprietary Undenatured Beta-Glucan on Different Human Populations
Show Abstract
Abstract
After proving safety in animal and human models, a series of clinical trials were conducted to examine the administration of 1 mg/mL bid of an undenatured beta-glucan on the immune system; and on self-perceived effects on
subjects’ quality of life (QoL) using a Visual Analogue Scale (VAS). In one study, a subject population that was self-perceived to be fatigued was administered an undetaured beta-glucan, to determine if this supplementation affected their quality-of-life as a result of an increased immune system response. 44 subjects were administered 1 mg/mL bid of the undenatured beta-glucan (Lentinex®) for four weeks. Prior to the beginning of the administration, and following the four-week administration period, the subjects were asked to fill out a quality-of-life VAS questionnaire. The changes in the two questionnaires revealed differences that occurred as a result of the beta-glucan administration. More than 75% of the subjects scored “better” (more than 1cm on the VAS) with regard to feeling in a good mood, and feeling rested.
More than 60% increased their energy and reduced their tiredness and exhaustion, and 70% felt less stressed. In a second study, subjects aged 40 years and older, believed to be in good general health, seeking therapy for tiredness/exhaustion/fatigue or similar conditions (neurasthenia) which were administered 1 mg/mL bid Lentinex®. The overall results indicated that the subjects felt significantly better (mean VAS = 5.91) after the last week of the study compared to how they felt initially (VAS = 4.73) (p < 0.0001). A statistically significant (p < 0.0001) change in distribution favoring a better situation after 4 weeks intake of supplement, with a remarkable fall in number of subjects scoring below normal (from 61.4% to 18.2%) accompanied by a significant shift in subjects feeling above normal, from 9.2% to 50.0%. These clinical studies, and others, showed that Lentinex® administration improved the perceived quality-of-life of subjects whose immune system was probably not functioning at optimal levels.
|
Bjørn Kristiansen,
Ronald J. Amen,
|
2022 |
Download Full Paper |
0 |
Stability Monomolecular Properties of Archaeal Tetraether Lipids Layers onto Solid Substrates
Show Abstract
Abstract
This paper reports the recent findings related to the stability properties of tetraether lipid layers. Organizations moleculars of chemical structure modified of Langmuir-Blodgett layers of archael tetraether lipids from the archebacterium Sulfolobus acidocaldarius on the wafer silicon substrates are investigated stable and organized. The behavior of Langmuir-Blodgett layers of chemical structure modified of archaeal tetraether lipids on the wafer silicon
substrates is characterization using Differential Scanning Calorimetry (DSC) and Atomic Force Microscopy (AFM). The thermodynamics behavior and stability of Langmuir-Blodgett layers of archael tetraether lipids on the wafer silicon substrates are shown. Stability of the lipid membranes is of great importance to a number of biomedical applications, including intravenous drug delivery, biomaterials, and biosensors.
|
Sri Vidawati,
Udo Bakowsky,
|
2022 |
Download Full Paper |
0 |
Vitamin D and Parathyroid Hormone Profiles in Living Kidney Failure Patients in Côte d’Ivoire
Show Abstract
Abstract
Introduction: Abnormalities in mineral and bone metabolism, particularly phosphocalcic metabolism, are common in renal failure and are associated with a significant morbidity and mortality. The regulation of phosphocalcic metabolism is subject to a particularly precise and complex control of parathormone (PTH) and vitamin D. Assessment of vitamin D and parathyroid hormone concentrations would help to improve the medical management of patients with chronic kidney disease and ensure a better quality of life. Methods: The study population consisted of 138 individuals including 46 non dialysis renal failure patients, 46 chronic hemodialysis patients and 46 nonrenal failure volunteers to serve as controls. Serum Parathyroid hormone and Vitamin D concentrations were measured using the Vidas automated system.Results: 25-hydroxyvitamin D concentrations in controls (65 ± 2.41 nmol/L) and dialysis patients (70 ± 3.03 nmol/L) were significantly higher than those in CKD patients (48 ± 3.34 nmol/L). On the other hand, the mean values of
Parathyroid hormone in dialysis patients (312 ± 36.22 pg/mL) and CKD patients (117 ± 10.68 pg/mL) were very high compared to that in controls (25 ± 2.34 pg/mL). Conclusion: Secondary hyperparathyroidism is common in renal failure. Parathyroid hormone and 25-hydroxyvitamin D assays would be adequate for better management of chronic renal failure.
|
Lydie Boyvin,
Gnogbo Alexis Bahi,
Cackouoh Carole Constance Koudou,
Souleymane Méité,
Maxime Roméo Kouadio,
Assieoussou Jean-Luc N’Guessan,
Allico Joseph Djaman,
|
2022 |
Download Full Paper |
0 |
Aqueous Extract of Erythrina senegalensis Exhibits Dose-Dependent Hepatoprotective Activity on Paracetamol-Induced Liver Damage in Wistar Rats
Show Abstract
Abstract
Erythrina senegalensis is utilized in the treatment of liver diseases in folklore medicine in most of northern Nigeria, but sufficient pharmacological-based and peer-reviewed scientific literature is not available to authenticate its use
in the treatment of liver ailments. This research is aimed at assessing the hepatoprotective effects of Erythrina senegalensis against paracetamol-induced (PCM-induced) hepatotoxicity in wistar albino rats. This was evaluated by estimating the activities of alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP) as compared with the control group. The extract was concentrated and then desired concentrations of extracts were made by dissolving in normal saline. Four different doses of aqueous extracts Erythrina senegalensis (200, 300, 400 and 500 mg/kg) were administered orally for 6 consecutive days after the 72 hrs administration of paracetamol (1500 mg/kg) per body weight. Paracetamol significantly induced oxidative stress in the liver, ultimately leading to increased serum levels of liver enzyme markers like alanine aminotransferase, aspartate aminotransferase and alkaline phosphatase. Administration of the extracts showed significant (p < 0.05) and dose-dependent hepatoprotective activity resulting in decrease in the activity of ALT, AST and ALP. These data revealed that Erythrina senegalensis aqueous extracts possess significant hepatoprotective activity against PCM-induced toxicity attributable to its constituent phytochemicals.The mechanism of hepatoprotection seems to be through the modulation of antioxidant enzyme systems.
|
Patience Chwe Igeh,
Elkanah Ishaku,
Solomon Choji,
Francis Obiora Okonkwo,
Jacob Gungsat Nangbes,
|
2022 |
Download Full Paper |
0 |