Distribution of Phenylindanedione in Blood and Tissues after Oral and Intravenous Administration

1958 ◽  
Vol 02 (03/04) ◽  
pp. 236-249 ◽  
Author(s):  
G. J Millar ◽  
Mary Ogilvie Mersereau ◽  
J Lowenthal ◽  
L. B Jaques
Keyword(s):  
Absorption Spectrum ◽  
Oral Administration ◽  
Intravenous Injection ◽  
Optical Density ◽  
Intravenous Administration ◽  
Phosphate Buffer ◽  
Red Cells ◽  
Tissue Levels

SummaryThe absorption spectrum and Polarographie behaviour are described for phenylindanedione. The drug may be estimated by measuring the optical density at 338 nιμ or the Polarographie reduction ware in a phosphate buffer at pH 11.8. For the estimation of the drug in tissue and plasma, the substance is extracted with toluene, taken up in alkali and estimated spectrometrically. For red cells, it is necessary to extract with acetone and after evaporation, take up the residue in water and determine the phenylindanedione polarographically. Blood and tissue levels were determined after administration to rabbits and dogs. Phenylindanedione disappeared from the plasma after intravenous injection much more rapidly than dicumarol. Considerable amounts of the drug were detected in liver and intestine one hour later. On oral administration, after 4—6 hours 50°/o was still recovered from the intestine, while 10—20% was found in the liver. Phenylindanedione and / or its metabolic derivative could be detected in the erythrocytes of rabbits but not in those of dogs.

Effect of i. v. and Oral Administration of Heparinoids G31150, G31150-A and of Nitrilotriacetic Acid on Blood Coagulation

1971 ◽  
Vol 25 (01) ◽  
pp. 187-200 ◽  
Author(s):  
C. L Jarrett ◽  
L. B Jaques
Keyword(s):  
Absorption Spectrum ◽  
Oral Administration ◽  
Blood Coagulation ◽  
Intravenous Injection ◽  
Anticoagulant Activity ◽  
Chelating Agent ◽  
Nitrilotriacetic Acid ◽  
Clotting Time ◽  
Coagulation Time

SummaryThe heparinoid G31150-A and nitrilotriacetic acid (NTA) were compared with heparinoid G31150 and heparin. In vitro the anticoagulant activity of NTA was 1/20000, G31150-A 1/8th and G31150, 1/10th of heparin. On intravenous injection in dogs, the degree and duration of hypocoagulability was about the same for the two heparinoids but less than predicted from the effects in vitro. Injection of 25 mg NTA/kg caused a slight increase in coagulation time lasting over 4 hours. When heparinoid G31150-A and NTA were given orally, there was an increase in clotting time of blood and metachromatic activity appeared in the urine. The greatest amount of activity was excreted with the highest dose of NTA alone. Microelectrophoresis of the urinary concentrate indicated the excreted material after NTA was not heparin, but another mucopolysaccharide; after G31150, a heparinoid. These results were confirmed by the resulting absorption spectrum of the dye obtained with added urinary concentrate. It is suggested that the effects produced when a chelating agent is given with oral heparin and heparinoids may be due to the release of a mucopolysaccharide.

UPTAKE OF OXYTOCIN IN TISSUES AFTER INTRAVENOUS ADMINISTRATION OF TRITIATED OXYTOCIN IN RATS

1969 ◽  
Vol 61 (3) ◽  
pp. 432-440 ◽  
Author(s):  
Ingvar Sjöholm ◽  
Gunnar Rydén
Keyword(s):  
Skeletal Muscle ◽  
Distribution Pattern ◽  
Intravenous Injection ◽  
Intravenous Administration ◽  
Time Course ◽  
Tritiated Water ◽  
Preferential Distribution ◽  
Time Period ◽  
Initial Uptake

ABSTRACT The distribution of oxytocin in the kidneys, liver, uterus and skeletal muscle of the rat was followed during 10 min after intravenous injection of tritium labelled oxytocin. Oxytocin was found to be taken up and degraded mainly in the kidneys and the liver. After 150 seconds no intact oxytocin could be detected in these organs. The time course of the distribution of the radioactivity in the liver and the skeletal muscle showed no noteworthy characteristics, whereas a different course was found in the kidneys and in the uterus. In the kidneys, the radioactivity increased continuously from 60 to 200 seconds after the injection, indicating an accumulation of oxytocin or its metabolites in the kidneys. In the uterus a high initial uptake was observed, followed by a decrease of the radioactivity from 60 to 100 seconds after the injection. This distribution pattern was specific to oxytocin, since the uptake of tritiated tyrosine and tritiated water was almost constant during the same time period. These findings may indicate a preferential distribution of oxytocin to the uterus.

Absorption Spectrum of HÆMoglobin in Red Cells

Nature ◽  
1946 ◽  
Vol 158 (4026) ◽  
pp. 952-953 ◽  
Author(s):  
D. L. RUBINSTEIN ◽  
H. M. RAVIKOVICH
Keyword(s):  
Absorption Spectrum ◽  
Red Cells

scholarly journals Effects of Diabetes Mellitus Induced by Alloxan on the Pharmacokinetics of Metformin in Rats: Restoration of Pharmacokinetic Parameters to the Control State by Insulin Treatment

2008 ◽  
Vol 11 (1) ◽  
pp. 88 ◽  
Author(s):  
Myung G. Lee ◽  
Young H Choi ◽  
Inchul Lee
Keyword(s):  
Diabetes Mellitus ◽  
Oral Administration ◽  
Protein Expression ◽  
Intravenous Administration ◽  
Insulin Treatment ◽  
Pharmacokinetic Parameters ◽  
Mrna Levels ◽  
Altered Pharmacokinetic ◽  
Intravenous And Oral Administration ◽  
Control State

To test the effect of insulin treatment on the pharmacokinetics of metformin in rats with diabetes mellitus induced by alloxan (DMIA rats). The following results were reported from other studies. Metformin was metabolized via hepatic CYP2C11, 2D1, and 3A1/2 in rats. In DMIA rats, the protein expression and mRNA levels of hepatic CYP2C11 and 3A1/2 decreased and increased, respectively. In rat model of diabetes mellitus induced by streptozotocin, the protein expression of hepatic CYP2D1 was not changed. The increase in hepatic CYP1A2, 2B1, and 2E1, and decrease in hepatic CYP2C11 in DMIA rats was returned to the controls by insulin treatment. METHODS. Metformin (100 mg/kg) was administered intravenously and orally to the control rats, DMIA rats, and DMIA rats with insulin treatment for 3 weeks (DMIA rats with insulin). RESULTS. After intravenous administration of metformin to the DMIA rats, the CLR and CLNR of the drug were significantly slower than the controls. After oral administration of metformin to the DMIA rats, the AUC of the drug was also significantly greater than the controls. After intravenous administration of metformin to the DMIA rats with insulin, the significantly slower CLNR of the drug in the DMIA rats was returned to the controls. The altered pharmacokinetic indices observed following intravenous and oral administration of metformin to DMIA rats returned to the control values in the DMIA rats with insulin. CONCLUSIONS. The significantly slower CLNR of metformin in the DMIA rats could be due to the decrease in hepatic CYP2C11 than the controls. The comparable CLNR of metformin between the DMIA rats with insulin and the control rats could be due to restoration of hepatic CYP enzyme changes in DMIA rats to the controls.

scholarly journals Physicochemical Effects of the Major Quassinoids in a Standardized Eurycoma longifolia Extract (Fr 2) on the Bioavailability and Pharmacokinetic Properties, and their Implications for Oral Antimalarial Activity

2011 ◽  
Vol 6 (3) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Bin-Seng Low ◽  
Chin-Hoe Teh ◽  
Kah-Hay Yuen ◽  
Kit-Lam Chan
Keyword(s):  
Oral Administration ◽  
Intravenous Administration ◽  
Antimalarial Activity ◽  
Elimination Rate ◽  
Rat Plasma ◽  
Chemical Degradation ◽  
Absolute Bioavailability ◽  
Phytochemical Analysis ◽  
Eurycoma Longifolia ◽  
Pharmacokinetic Properties

A simple validated LC-UV method for the phytochemical analysis of four bioactive quassinoids, 13α(21)-epoxyeurycomanone (EP), eurycomanone (EN), 13α,21-dihydroeurycomanone (ED) and eurycomanol (EL) in rat plasma following oral (200 mg/kg) and intravenous administration (10 mg/kg) of a standardized extract Fr 2 of Eurycoma longifolia Jack was developed for pharmacokinetic and bioavailability studies. The extract Fr 2 contained 4.0%, 18.5%, 0.7% and 9.5% of EP, EN, ED and EL, respectively. Following intravenous administration, EP displayed a relatively longer biological half-life (t½ = 0.75 ± 0.25 h) due primarily to its lower elimination rate constant (ke) of 0.84 ± 0.26 h−1) when compared with the t½ of 0.35 ± 0.04 h and ke of 2.14 ± 0.27 h−1, respectively of EN. Following oral administration, EP showed a higher Cmax of 1.61± 0.41 μg/mL over that of EN (Cmax = 0.53 ± 0.10 μg/mL). The absolute bioavailability of EP was 9.5-fold higher than that of EN, not because of chemical degradation since both quassinoids were stable at the simulated gastric pH of 1. Instead, the higher log Kow value of EP (-0.43) contributed to greater membrane permeability over that of EN (log Kow = −1.46) at pH 1. In contrast, EL, being in higher concentration in the extract than EP, was not detected in the plasma after oral administration because of substantial degradation by the gastric juices after 2 h. Similarly, ED, being unstable at the acidic pH and together with its low concentration in Fr 2, was not detectable in the rat plasma. In conclusion, upon oral administration of the bioactive standardized extract Fr 2, EP and EN may be the only quassinoids contributing to the overall antimalarial activity; this is worthy of further investigation.

Effect of Intravenous Injection of Hypertonic Glucose Solution on External Secretion of the Pancreas

1956 ◽  
Vol 186 (2) ◽  
pp. 187-189 ◽  
Author(s):  
J. O. Crider ◽  
S. S. Conly ◽  
J. E. C. Dorchester ◽  
J. E. Thomas
Keyword(s):  
Hydrochloric Acid ◽  
Specific Gravity ◽  
Intravenous Injection ◽  
Pancreatic Juice ◽  
Intravenous Administration ◽  
Glucose Solution ◽  
Chronic Fistula ◽  
Hypertonic Glucose

Effect of the intravenous administration of hypertonic glucose solution on the specific gravity, volume and amylase content of pancreatic juice collected from unanesthetized, chronic fistula dogs secreting in response to hydrochloric acid in the duodenum was studied. There was an increase in the specific gravity and amylase but no change in volume.

Disruption of Bordetella pertussis in the Ribi Cell Fractionator. 1. Effect of different pressures

1971 ◽  
Vol 17 (9) ◽  
pp. 1169-1174 ◽  
Author(s):  
E. Hollinger ◽  
A. C. Wardlaw
Keyword(s):  
Optical Density ◽  
Bordetella Pertussis ◽  
Phosphate Buffer ◽  
Protective Antigen ◽  
Dry Weight ◽  
Cell Disruption ◽  
Cytoplasmic Fraction ◽  
Cell Envelopes

Exposure of B. pertussis in pH 7.0 phosphate buffer to disruption in the Ribi Cell Fractionator (RCF) at a series of increasing pressures caused progressive lysis as judged by the decrease of optical density and by the release of protein and DNA into the 20 000 g supernatant. A plateau of maximum lysis was reached around 20 000 psi, although DNA continued to be released from the cell residues up to 30 000 psi. The 20 000 g residues (cell envelopes) from 30 000 psi lysates comprised, after pH 7.0 washing, about 30% of the dry weight of the original cells and contained about 30% of the original protein and 14–27% of the original DNA. They contained the greater part (80–90%) of the original lipopolysaccharide (LPS) and between one-half and two-thirds of the histamine-sensitizing factor(HSF)and protective antigen (PA). However, the 20 000 g supernatant fractions also contained HSF and PA. Thus although HSF and PA were not destroyed by RCF treatment, it was not possible to get efficient cell disruption in pH 7.0 phosphate buffer without causing release of one-third or more of the HSF and PA into the cytoplasmic fraction.

scholarly journals STUDIES ON THE CX-REACTIVE PROTEIN

1957 ◽  
Vol 106 (2) ◽  
pp. 315-320 ◽  
Author(s):  
Harrison F. Wood ◽  
Sigfrido Montella
Keyword(s):  
Intravenous Injection ◽  
Acute Phase ◽  
Intravenous Administration ◽  
Inflammatory Reaction ◽  
Reactive Protein

It has been found that normal rabbits respond to the intravenous administration of Cx-reactive protein by producing this acute phase substance. When Cx-reactive protein incorporated in adjuvant is injected intracutaneously, in addition to producing Cx-reactive protein, the recipient animals develop a characteristic inflammatory reaction about the site of injection. This inflammatory reaction can be inhibited by the prior intravenous injection of thorotrast.

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