PROSPECTS FOR INTRODUCTION OF THE THREE-COMPONENT COORDINATION COMPOUND OF HERMANIUM OXYETHYLIDENED DIPHOSPHONATE WITH NICOTIC ACID IN THE BOUNDARIES WITH IN STUDYING OF THEIR PHARMACOKINETICS

2021 ◽  
Author(s):  
A. G. Vidavskaya ◽  
S. B. Strechen
Keyword(s):  
Coordination Compound ◽  
Intraperitoneal Administration ◽  
The Body ◽  
Biologically Active ◽  
Pharmacokinetic Parameters ◽  
Photometric Method ◽  
Pharmacokinetic Studies ◽  
Experimental Animals ◽  
Elimination Half ◽  
Male Wistar Rats

The purpose of this work is to experimentally study the pharmacokinetics of a three-component coordination compound of germanium oxyethylidene diphosphonate with nicotinic acid (MIGU-4), created on the basis of natural metabolites. The study of the pharmacokinetics of MIGU-4 was carried out for germanium and was based on the extraction-photometric method. The experiment was carried out on male Wistar rats weighing 130-170 g. MIGU-4 was injected intraperitoneally at the rate of 37.5 mg of germanium per 1 kg of body weight. Its amount in tissues was determined photometrically by the light absorption of germanium phenifluoronate. The results of the experimental study were processed statistically. Pharmacokinetic parameters calculated using partial models analyzing the pharmacokinetic parameters, it can be seen that MIGU-4 was rapidly distributed over the organs and tissues of experimental animals. The time of admission to the examined organs was less than 0,25 hours. The studied biologically active substance quickly enters the well-vascularized organs and is evenly distributed in them. The elimination half-life (T1|2) was 5 - 8 h, the largest in the lungs, the smallest in the liver. The average residence time of MIGU-4 in experimental animals ranged from 7 hours to 27 hours. Therefore, with intraperitoneal administration of MIGU-4 is rapidly excreted from the body. The results of pharmacokinetic studies have shown that MIGU-4 is promising for the creation of a safe and effective drug. The dynamics of the therapeutic effect is comparable to the maximum concentration of the substance in the organs and tissues of experimental animals.

scholarly journals  Comparative single intraperitoneal dose pharmacokinetics of aspirin and acetaminophen in chicks

2012 ◽  
Vol 57 (No. 3) ◽  
pp. 121-124 ◽  
Author(s):  
FK Mohammad ◽  
AS Mansoor ◽  
MHI Al-Zubaidy
Keyword(s):  
Intraperitoneal Administration ◽  
Compartmental Analysis ◽  
The Body ◽  
Pharmacokinetic Parameters ◽  
Limited Information ◽  
Spectrophotometric Methods ◽  
Elimination Half ◽  
Toxicological Studies ◽  
Intraperitoneal Dose ◽  
Total Body

Limited information is available on the pharmacokinetics and bioavailability of aspirin and acetaminophen in young chicks. The purpose of the present study was to examine the pharmacokinetics of acetyl salicylic acid (aspirin) and acetaminophen in 12-day old chicks after a single intraperitoneal administration of each drug alone at the dose of 100 mg/kg body weight. Blood samples were collected from chicks (six/each time period) at 10, 20, 30, 60 and 120 min after each drug administration. The concentrations of aspirin and acetaminophen in the plasma were determined by spectrophotometric methods. The pharmacokinetic parameters of the drugs were calculated by a non-compartmental analysis. The elimination half-lives of aspirin and acetaminophen were 1.68 and 1.36 h with steady state volume of distributions 0.079 and 1.11 l/kg and total body clearances of 0.029 and 0.53 l/h/kg, respectively. The mean residence times of the drugs were 2.74 and 2.09 h and their area under the plasma concentration-time curves (0–∞) were 3486 and 188 μg/h/ml, respectively. In conclusion, the data show the pharmacokinetic profiles of single intraperitoneal doses of aspirin and acetaminophen in chicks and suggest that acetaminophen is well distributed in the body of the chicks and eliminated faster from the body compared to aspirin. These parameters should be taken into consideration in further therapeutic and toxicological studies of drugs in chickens.  

scholarly journals Toxicity and Pharmacokinetic Studies of Lidocaine and Its Active Metabolite, Monoethylglycinexylidide, in Goat Kids

Animals ◽  
2018 ◽  
Vol 8 (8) ◽  
pp. 142
Author(s):  
Dinakaran Venkatachalam ◽  
Paul Chambers ◽  
Kavitha Kongara ◽  
Preet Singh
Keyword(s):  
Total Dose ◽  
Plasma Concentrations ◽  
Subcutaneous Administration ◽  
Lidocaine Hydrochloride ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Studies ◽  
Liquid Chromatography Mass Spectrometry ◽  
Elimination Half ◽  
The Mean ◽  
Safe Dose

This study determined the convulsant plasma concentrations and pharmacokinetic parameters following cornual nerve block and compared the results to recommend a safe dose of lidocaine hydrochloride for goat kids. The plasma concentrations of lidocaine and monoethylglycinexylidide (MGX) were quantified using liquid chromatography-mass spectrometry. A total dose of 7 mg/kg body weight (BW) was tolerated and should therefore be safe for local and regional anesthesia in goat kids. The mean plasma concentration and mean total dose that produced convulsions in goat kids were 13.59 ± 2.34 µg/mL and 12.31 ± 1.42 mg/kg BW (mean ± S.D.), respectively. The absorption of lidocaine following subcutaneous administration was rapid with Cmax and Tmax of 2.12 ± 0.81 µg/mL and 0.33 ± 0.11 h, respectively. The elimination half-lives (t½λz) of lidocaine hydrochloride and MGX were 1.71 ± 0.51 h and 3.19 ± 1.21 h, respectively. Injection of 1% lidocaine hydrochloride (0.5 mL/site) was safe and effective in blocking the nerves supplying horn buds in goat kids.

scholarly journals Fruits of plants of Amelanchier genus (Amelanchier Medic) as source of biologically active substances and minerals

2018 ◽  
Vol 26 (2) ◽  
pp. 296-304
Author(s):  
Elena A. Laksaeva
Keyword(s):  
The Body ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Erythrocyte Membranes ◽  
Human Organism ◽  
High Concentration ◽  
Experimental Animals ◽  
Polysaccharide Complex ◽  
Physiological Processes ◽  
Active Substances

An interest in plants of Amelanchier genus is stimulated by the necessity of search for plant sources rich in biologically active substances and possessing the ability to influence different physiological processes in a human organism. The article gives information about places of growth of different species of Amelanchier (Amelanchier Medic) and about the fact that its fruits contain high concentration of free sugars, relatively low level of organic acids, sufficient amounts of various vitamins and provitamins and a complex of mineral substances. Nutritive and biological value of Amelanchier fruits in complex may produce a beneficial effect on different biochemical and physiological processes of normal vital activity of a human organism. The data are given about a positive influence of enteral introduction of polysaccharides isolated from Amelanchier fruits, on different physiological processes that enhance adaptational reserves of an organism of experimental animals. In particular, it was shown that watersoluble polysaccharide complex (WSPC) of Amelanchier fruits activates erythropoiesis increasing the amount of erythrocytes and hemoglobin in blood of experimental animals and raises concentration of iron. WSPC improves physical working capacity and increases the body mass of experimental animals. Addition of watersoluble polysaccharide complex of Amelanchier fruits to blood of a healthy donor increases thermal, osmotic and peroxide resistance of erythrocyte membranes thus protecting cells against damage under action of adverse factors in the experiment. Fruits of plants of Amelanchier genus may be recommended to be used as a food additive or a product in dietary and prophylactic therapy.

scholarly journals Characterization and pharmacokinetic parameters of recombinant soluble interleukin-4 receptor

Blood ◽  
1991 ◽  
Vol 77 (11) ◽  
pp. 2396-2403 ◽  
Author(s):  
CA Jacobs ◽  
DH Lynch ◽  
ER Roux ◽  
R Miller ◽  
B Davis ◽  
...  
Keyword(s):  
Half Life ◽  
Integral Membrane Protein ◽  
Interleukin 4 ◽  
Soluble Form ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Studies ◽  
Cdna Clones ◽  
Elimination Half ◽  
Interleukin 4 Receptor

Abstract The interleukin-4 receptor (IL-4R) is expressed as a 140-Kd membrane glycoprotein that binds IL-4 with high affinity. Recently, cDNA clones for the murine IL-4R have been isolated. One clone encodes an integral membrane protein, while another encodes a protein in which translation is terminated before the transmembrane region, thus producing a soluble form of the IL-4R (sIL-4R). HeLa cell clones overexpressing sIL-4R were isolated using a novel filter-overlay and 125I-IL-4 ligand binding technique. Quantitative analysis demonstrated that the kinetics and affinity of IL-4 binding to the recombinant sIL-4R were similar to the native membrane-bound IL-4R. As low doses of sIL-4R specifically inhibited IL-4-induced proliferative responses in vitro, sIL-4R biodistribution and elimination parameters were evaluated to assess the pharmacokinetic potential of sIL-4R as a therapeutic agent. Pharmacokinetic studies demonstrated that radiolabeled sIL-4R had a distribution half-life of 9 minutes and an elimination half-life of 2.3 hours following intravenous (IV) administration. When administered by intraperitoneal or subcutaneous (SC) injection, the elimination half- lives were prolonged to 4.2 hours and 6.2 hours, respectively. Although the initial blood level of sIL-4R was reduced if administered by SC injection, the bioavailability was comparable with IV administration. The main sites of sIL-4R elimination were the liver and kidney.

scholarly journals PHARMACOKINETIC STUDIES OF A CHRONOTHERAPEUTIC DRUG DELIVERY SYSTEM OF LORNOXICAM BY LC-MS/MS METHOD

2018 ◽  
Vol 10 (6) ◽  
pp. 88
Author(s):  
Sindhu Abraham ◽  
Rajamanickam Deveswaran ◽  
Jayaraman Anbu ◽  
Sharon Furtado ◽  
Bharath Srinivasan
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Maximum Concentration ◽  
Area Under The Curve ◽  
Immediate Release ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Studies ◽  
Elimination Half ◽  
Coated Tablet ◽  
Liquid Chromatography Tandem Mass

Objective: The objective of this study was to investigate differences in pharmacokinetic patterns of immediate release tablet (IR) and compression coated tablet (CCT) of lornoxicam, proposed for the chronotherapeutic treatment of rheumatoid arthritis.Methods: The dosage forms were administered to two groups of white New Zealand rabbits (n=3), and the plasma drug levels were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS). Pharmacokinetic parameters like maximum concentration (Cmax), time is taken to reach maximum concentration (Tmax), area under the curve (AUC), elimination half-life (t1/2) and Mean Residence Time (MRT) were determined.Results: In the case of IR tablets, the drug was detected within 15 min after oral administration and a Cmax of 1269.57±4.04 ng/ml were attained at 2±0.15 h. With CCT, the drug was detected only after 5 h and a Cmax of 1279.24±12.76 ng/ml were attained at 8±0.10 h. The CCT showed maximum drug release at the eighth hour in comparison to IR tablet which showed maximum release at the second hour of study.Conclusion: The predominant lag time prior to drug release from CCT is an indication that it is consistent with the requirements of chronopharmaceutical drug delivery. The results suggest that the compression coated tablet is a promising approach for chronotherapeutic management of rheumatoid arthritis.

Vancomycin Disposition following Intraperitoneal Administration in Children Receiving Peritoneal Dialysis

2007 ◽  
Vol 27 (1) ◽  
pp. 79-85 ◽  
Author(s):  
Douglas L. Blowey ◽  
Bradley A. Warady ◽  
Susan Abdel–Rahman ◽  
Reginald F. Frye ◽  
Harold J. Manley
Keyword(s):  
Peritoneal Dialysis ◽  
Total Body Clearance ◽  
Intraperitoneal Administration ◽  
Primary Objective ◽  
Pharmacokinetic Parameters ◽  
Vancomycin Concentration ◽  
Elimination Half ◽  
Serum Vancomycin ◽  
Total Body ◽  
Body Clearance

Background Little information is available on the disposition of vancomycin during chronic peritoneal dialysis (PD) in children. The primary objective of this study was to investigate the disposition of vancomycin following intraperitoneal (IP) administration in children receiving short-dwell [ e.g., automated PD (APD)] and long-dwell [ e.g., continuous ambulatory PD (CAPD)] PD. Methods A 6-hour exchange containing vancomycin 500 mg/L, using an exchange volume of 1100 mL/m2 body surface area (BSA), was followed by 4-, 6-, and 8-hour antibiotic-free exchanges. The 8-hour exchange was followed by three to four 90-minute antibiotic-free exchanges. Serial blood and dialysis effluent samples were obtained and analyzed for vancomycin concentration by high-pressure liquid chromatography. Pharmacokinetic parameters were computed using noncompartmental methods. Results The bioavailability of vancomycin during a 6-hour IP exchange was 70% ± 5%, resulting in a delivered dose of 12.0 ± 1.8 mg/kg, and a 6-hour serum vancomycin concentration of 23.3 ± 7.2 μg/mL. Total body vancomycin clearance measured 10.72 ± 4.52 mL/minute/1.73 m2 BSA, while clearance attributable to PD measured 2.78 ± 1.08 mL/min/1.73 m2 BSA and accounted for 29% ± 11% of total vancomycin clearance. Dialysis clearance during long-dwell (CAPD) and short-dwell (APD) regimens was similar, measuring 2.46 ± 1.04 and 3.09 ± 1.28 mL/min/1.73 m2 BSA, accounting for 25% ± 13% and 32% ± 12% of total body clearance respectively. Conclusions Intraperitoneal absorption and dialysis clearance of vancomycin in children receiving PD are similar to those reported in adult dialysis patients. In contrast, total body clearance of vancomycin appears to be increased and the elimination half-life decreased in children, due to increased elimination by non-renal nondialysis routes. For intermittent IP vancomycin therapy in children with peritonitis, an IP load containing vancomycin 1000 mg/L (or 30 mg/kg), followed a single full-fill (1100 mL/m2 BSA) daily exchange, containing vancomycin 250 mg/L (or 7.5 mg/kg), from day 2 until the end of treatment will maintain a vancomycin dialysate concentration of >4 μg/mL.

scholarly journals Factors influencing elimination and distribution of fleroxacin: metaanalysis of individual data from 10 pharmacokinetic studies.

1996 ◽  
Vol 40 (3) ◽  
pp. 575-580 ◽  
Author(s):  
B G Reigner ◽  
H A Welker
Keyword(s):  
Body Weight ◽  
Volume Of Distribution ◽  
Linear Increase ◽  
The Body ◽  
Pharmacokinetic Parameters ◽  
Lean Body Weight ◽  
Systemic Availability ◽  
Pharmacokinetic Studies ◽  
Age And Gender ◽  
And Gender

A metaanalysis was conducted on data from 172 subjects (healthy volunteers and uninfected patients) included in 10 pharmacokinetic studies of fleroxacin after oral administration. The objectives of this analysis were (i) to estimate the typical values of two key pharmacokinetic parameters, clearance over systemic availability (CL/F) and volume of distribution over systemic availability (V/F), after the administration of therapeutic doses and (ii) to study qualitatively and quantitatively the factors which influence the elimination and distribution of fleroxacin. The main pharmacokinetic parameters, CL/F and V/F, were analyzed separately by a standard two-stage approach. The covariates investigated were predicted creatinine clearance (CLCR), age, gender, body surface area, body weight, and lean body weight (LBW). The predicted CL/F and V/F were 83.5 ml/min and 101 liters, respectively, for a typical male subject (CLCR, 70 ml/min; LBW, 54 kg; age, 54 years). Modeling of CL/F indicated that this parameter increases linearly with CLCR, decreases linearly with age, and is 10.8 ml/min lower in females than in males. The best model for V/F showed a linear increase with LBW and a linear decrease with age. V/F was found to be 20.4 liters greater in males than in females. In conclusion, this metaanalysis has shown that CLCR, age, and gender influence the elimination of fleroxacin from the body, whereas V/F is influenced by LBW, age, and gender.

Clinical Pharmacokinetics of Chlorpheniramine

1984 ◽  
Vol 18 (9) ◽  
pp. 701-707 ◽  
Author(s):  
Martha M. Rumore
Keyword(s):  
Half Life ◽  
The Body ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Studies ◽  
Elimination Kinetics ◽  
Clinical Pharmacokinetics ◽  
Interindividual Variations ◽  
First Pass ◽  
Dose Levels ◽  
Kinetics Of

The clinical pharmacokinetics of chlorpheniramine are reviewed. Recent studies have established that the half-life of chlorpheniramine is longer than previously reported. Chlorpheniramine has a serum half-life of ∼20 hours in adults, and elimination from the body is primarily by metabolism to monodesmethyl and didesmethyl compounds. The half-life is increased in the presence of renal dysfunction and decreased in children. The exact mechanism of the presystemic first-pass elimination and the effects of dose levels on the process presently are unclear. Biopharmaceutical and pharmacokinetic studies after single or multiple doses in humans reveal wide interindividual variations in pharmacokinetics. Age, dialysis, urinary pH and flow influence the elimination kinetics of chlorpheniramine. Attention is brought to major issues that need further clarification to optimize drug therapy with this antihistamine. The use of pharmacokinetic parameters of chlorpheniramine for clinical application is discussed.

scholarly journals Influence of Nanovulin-VRKh on cattle thermoregulation and chemical composition of milk

2020 ◽  
Vol 10 (1) ◽  
pp. 139-144
Author(s):  
M. S. Gruntkoskyi ◽  
V. M. Kondtratiuk ◽  
S. M. Gryshchenko ◽  
N. P. Hryshchenko ◽  
I. S. Mytyay
Keyword(s):  
Dairy Products ◽  
The Body ◽  
Biologically Active ◽  
Cow Milk ◽  
Control Groups ◽  
Experimental Animals ◽  
Nonfat Milk ◽  
Prolonged Effect ◽  
Solids Content ◽  
Milk Solids

The current research described the effect of neurotropic and metabolic non-hormonal biologically active medicine Nanovulin-VRKh © on the milk yield amount and the milk quality. Two cow groups were under study: the experimental and the control groups, each including four cows. The results showed that two of the neurotropic and metabolic Nanovulin-VRKh injections made 12 and 24 hours after the insemination did not effect the body thermoregulation of cows. Administration of the Nanovulin-VRKh contributes to stable fat formation in cow milk. Increased content of protein, nonfat milk solids, stable fat formation in milk were due to Nanovulin-VRKh administration. It was also established that, in the milk of experimental animals were administered the Nanovulin-VRKh, the pronounced effect of the drug on the protein, fat and nonfat milk solids content was observed, and the prolonged effect on these indices was reported during the fourth milking. Introduction of Cuprum aqua-chelate into the drug did not has toxic effect on the animal body and therefore would not effect the human health through the dairy products.

scholarly journals A Deeper Insight into Pharmacokinetics of Drugs Following one Compartment Model

2017 ◽  
Vol II (I) ◽  
pp. 25-33
Author(s):  
Syeda Komal Fatima ◽  
Ayesha Sabir ◽  
Fahad Pervai
Keyword(s):  
Mathematical Model ◽  
Clinical Trials ◽  
Half Life ◽  
Compartment Model ◽  
Drug Clearance ◽  
The Body ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Models ◽  
Elimination Half ◽  
Insight Into

This article discusses the mathematical pharmacokinetic models with reference to one open compartment model in detail. Four types of models, IV, bolus, extravascular 1st and 0 order, have been studied. Mathematical approaches to predict the pharmacokinetic parameters, including elimination half-life, rate constant and drug clearance, have been included. This article focuses on the significance of one open compartment model to study the distribution and elimination of drugs in the body beforehand, to determine whether the drugs under study should proceed to clinical trials or not. Thus, the prediction of the pharmacokinetics of the drug at an earlier stage with the help of this mathematical model saves time and cost during drug and discovery and drug development.

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