scholarly journals Pharmacokinetic Studies of 3-Methyl-1-phenyl-2-pyrazolin-5-one(MCI-186) in rats. (2). Blood and Plasma Levels, Distribution, Metabolism, Excretion and Accumulation during and after Repeated Intravenous Administration.

1996 ◽  
Vol 11 (5) ◽  
pp. 481-491
Author(s):  
Teiko KOMATSU ◽  
Hiroshi NAKAI ◽  
Katsuyoshi MASAKI ◽  
Rie OBATA ◽  
Keiko NAKAI ◽  
...  
2020 ◽  
Vol 15 (12) ◽  
pp. 1934578X2098143
Author(s):  
Hui Liu ◽  
Hao Chen ◽  
Xiaoli Qin ◽  
Xue Ma ◽  
Zipeng Gong ◽  
...  

Periploca forrestii Schltr ( P. forrestii) is a herb used in traditional Chinese medicine for its anti-rheumatoid arthritis effect. The aim of this study was to compare the pharmacokinetic properties of the 5 active components of this plant: neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, isochlorogenic acid C, and periplocin between normal rats and adjuvant-induced arthritis model rats. After the intravenous administration (177.78 mg/kg) of P. forrestii extract, samples were analyzed by ultra-performance liquid chromatography-tandem mass spectrometry. Compared with normal rats, the area under the curve [(AUC)(0-t), AUC(0-∞)], mean residence time [(MRT)(0-t), MRT(0-∞)] of neochlorogenic acid-treated rats decreased significantly, and drug clearance (CL) and apparent volume of distribution (V) increased significantly; the V of chlorogenic acid-treated rats decreased significantly, and MRT(0-t) significantly increased; the AUC(0-t) and AUC(0-∞) of cryptochlorogenic acid-treated rats decreased significantly, and CL and V increased significantly; the AUC(0-t) and MRT(0-t) of isochlorogenic acid C-treated rats decreased significantly, and V increased significantly; the AUC(0-t) and AUC(0-∞) of periplocin-treated rats increased significantly, and MRT(0-t), MRT(0-∞), CL, and V decreased significantly in model rats. The disease condition of rheumatoid arthritis in rats had a significant effect on the in vivo pharmacokinetics of P. forrestii after the intravenous administration.


1992 ◽  
Vol 10 (6) ◽  
pp. 1001-1006 ◽  
Author(s):  
V W Rusch ◽  
D Niedzwiecki ◽  
Y Tao ◽  
C Menendez-Botet ◽  
A Dnistrian ◽  
...  

PURPOSE Intrapleural cisplatin-based chemotherapy has been used in the treatment of patients with malignant pleural mesothelioma and malignant pleural effusions, but the pharmacokinetics of this form of chemotherapy have not been previously evaluated. We performed pharmacokinetic studies on 12 patients who received both intrapleural cisplatin and mitomycin immediately following pleurectomy/decortication for malignant pleural mesothelioma. PATIENTS AND METHODS Simultaneous pleural fluid and plasma samples were collected at 15 and 30 minutes, and at 1, 2, 3, 4, and 24 hours after administration of the intrapleural chemotherapy (cisplatin 100 mg/m2 and mitomycin 8 mg/m2), and after cisplatin (total and free) and mitomycin levels were measured. The mean peak levels, the areas under the concentration-time curve (AUC) and the drug half-lives (t1/2s) in plasma and pleural fluid were compared using the paired t test. Differences were considered significant if P less than or equal to .05. RESULTS Systemic absorption was rapid, with peak plasma levels being reached within 1 hour of administration of the intrapleural chemotherapy. Peak plasma levels measured after intrapleural chemotherapy approximated those reportedly attained during systemic administration of these drugs at similar doses. However, the mean peak cisplatin and mitomycin levels, and their mean AUCs, were significantly higher in the pleural fluid than in the plasma. There was a three- to fivefold advantage (on a logarithmic scale) for pleural to plasma AUCs for both cisplatin and mitomycin. The mean t1/2s for cisplatin and mitomycin were significantly longer in the plasma than in the pleural fluid. CONCLUSIONS The pharmacokinetics of intrapleural cisplatin-based chemotherapy are analogous to those of intraperitoneal chemotherapy. Our findings show that intrapleural cisplatin-based chemotherapy has a distinct local pharmacologic advantage, but also produces significant and sustained drug plasma levels.


1976 ◽  
Vol 83 (4) ◽  
pp. 856-864 ◽  
Author(s):  
Pentti Holma ◽  
Herman Adlercreutz

ABSTRACT Plasma levels of testosterone, luteinizing hormone (LH) and follicle-stimulating hormone (FSH) as well as the response of LH and FSH to the intravenous administration of 100 μg of luteinizing hormone releasing hormone (LRH) were measured in 16 well-trained athletes (mean age 30 years) before and after 2 months of daily oral intake of 15 mg of metandienon, an anabolic steroid (Anabolin®, 17α-methyl-17β-hydroxy-1,4-androstadien-3-one, Medica, Finland). All athletes continued to train regularly, just as they had done for several years. During administration of metandienon the mean plasma testosterone level fell 69%, from 29.4 ± 11.6 nmol/l to 9.1 ± 7.5 nmol/l. The mean plasma levels of LH and FSH also fell significantly (P < 0.001 and P < 0.01, respectively), both about 50%. Because LH and FSH levels were low after administration of the steroid the maximum stimulation values after LRH administration were also lower than pre-treatment values although the mean increments did not differ significantly before and after administration of the anabolic steroid. However, after treatment, the FSH response curve had a biphasic pattern in most subjects, with peaks at 10 to 20 and 50 to 60 min after the iv injection of LRH. Administration of LRH after the treatment period had no effect on FSH secretion in two subjects and no effect on LH secretion in one. Our results show that administration of an anabolic steroid causes a pronounced lowering of plasma levels of testosterone, LH and FSH but causes no gross alteration in the response of LH secretion to stimulation by LRH. The reason for the biphasic response pattern of FSH to LRH administration in most subjects is not known.


1974 ◽  
Vol 2 (2) ◽  
pp. 125-131 ◽  
Author(s):  
Hugo Trujillo ◽  
Rafael Manotas ◽  
Cecilia Salazar ◽  
Alfonso Rodriguez ◽  
Alvaro Uribe ◽  
...  

Parenteral administration, intravenous followed by intramuscular, or intramuscular alone, cured thirty children with pneumonia and empyema caused by S. aureus, D. pneumoniae, Klebsiella sp. and other gram-negative bacteria, within one to three weeks. Pathogens disappeared from pleural pus in all empyema cases within the first forty-eight hours of treatment. Following intravenous administration peak plasma levels ( 117 mcg/ml) were obtained in five minutes, and following intramuscular injections peak plasma levels ( 55 mcg/ml) were obtained in one hour. High concentration levels were observed in pleural pus ( 23-37 mcg/ml) in two hours. The drug was very well tolerated both locally and systemically.


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