scholarly journals The Effect of Apigenin on Pharmacokinetics of Imatinib and Its Metabolite N-Desmethyl Imatinib in Rats

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Xian-yun Liu ◽  
Tao Xu ◽  
Wan-shu Li ◽  
Jun Luo ◽  
Pei-wu Geng ◽  
...  
Keyword(s):  
Single Dose ◽  
Pharmacokinetic Parameters ◽  
Control Group ◽  
Term Study ◽  
Long Term Study ◽  
Short Term Study ◽  
Term Administration ◽  
Group A ◽  
Group B

The purpose of this study was to determine the effect of apigenin on the pharmacokinetics of imatinib and N-desmethyl imatinib in rats. Healthy male SD rats were randomly divided into four groups: A group (the control group), B group (the long-term administration of 165 mg/kg apigenin for 15 days), C group (a single dose of 165 mg/kg apigenin), and D group (a single dose of 252 mg/kg apigenin). The serum concentrations of imatinib and N-desmethyl imatinib were measured by HPLC, and pharmacokinetic parameters were calculated using DAS 3.0 software. The parameters ofAUC(0-t),AUC(0−∞),Tmax,Vz/F, andCLz/Ffor imatinib in group B were different from those in group A (P<0.05). Besides,MRT(0−t)andMRT(0−∞)in groups C and D differed distinctly from those in group A as well. The parameters ofAUC(0-t)andCmaxfor N-desmethyl imatinib in group C were significantly lower than those in group A (P<0.05); however, compared with groups B and D, the magnitude of effect was modest. Those results indicated that apigenin in the short-term study inhibited the metabolism of imatinib and its metabolite N-desmethyl imatinib, while in the long-term study the metabolism could be accelerated.

Hematologic and Bone Marrow Changes after Short- and Long-term Administration of Two Recombinant Bovine Granulocyte Colony-stimulating Factors

1992 ◽  
Vol 29 (6) ◽  
pp. 521-527 ◽  
Author(s):  
J. S. Cullor ◽  
W. Smith ◽  
J. G. Zinkl ◽  
J. D. Dellinger ◽  
T. Boone
Keyword(s):  
Bone Marrow ◽  
Specific Response ◽  
Short Term ◽  
Term Study ◽  
Colony Stimulating Factors ◽  
Long Term Study ◽  
Short Term Study ◽  
Term Administration ◽  
A Cell

Colony-stimulating factors are a category of glycoproteins that are instrumental in the regulation of hematopoiesis and inflammation. This investigation documented the clinical bone marrow and peripheral blood responses to short-term and long-term administration of a recombinant bovine granulocyte colony-stimulating factor (rb-GCSF) and an analog, where the cysteine at position 17 was substituted with a serine (rb-GCSF ser17). The colony-stimulating factors produced the expected changes in the hematologic findings of the bovine subjects in the study, and there was a cell-specific response to the compounds. The sustained neutrophilia in the long-term study indicates that the bovine species can tolerate the administration of recombinant forms of bovine GCSF for extended periods of time without detectable adverse side effects. The neutrophils from the short-term study revealed no apparent fluctuation, either as enhanced or reduced capability to reduce nitro blue tetrazolium as compared to pretreatment neutrophils. The administration of both recombinant forms of GCSF produced large increases in the bone marrow myeloid: erythroid (M:E) ratio concomitantly with the neutrophilias. This is the first preliminary report documenting the bone marrow response of cattle to the native and recombinant (rb-GCSF ser17) forms of bovine GCSF.

scholarly journals Pharmacokinetics Interaction between Imatinib and Genistein in Rats

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Zhe Wang ◽  
Li Wang ◽  
Meng-ming Xia ◽  
Wei Sun ◽  
Cheng-ke Huang ◽  
...  
Keyword(s):  
Single Dose ◽  
Multiple Dose ◽  
Pharmacokinetic Parameters ◽  
Control Group ◽  
Sprague Dawley ◽  
Sprague Dawley Rats ◽  
Significant Difference ◽  
Group A ◽  
Group B ◽  
Group Control Group

The objective of this work was to investigate the effect of orally administered genistein on the pharmacokinetics of imatinib and N-desmethyl imatinib in rats. Twenty-five healthy male SD (Sprague-Dawley) rats were randomly divided into five groups: A group (control group), B group (multiple dose of 100 mg/kg genistein for consecutive 15 days), C group (multiple dose of 50 mg/kg genistein for consecutive 15 days), D group (a single dose of 100 mg/kg genistein), and E group (a single dose of 50 mg/kg genistein). A single dose of imatinib is administered orally 30 min after administration of genistein (100 mg/kg or 50 mg/kg). The pharmacokinetic parameters of imatinib and N-desmethyl imatinib were calculated by DAS 3.0 software. The multiple dose of 100 mg/kg or 50 mg/kg genistein significantly (P<0.05) decreased theAUC0-tandCmaxof imatinib.AUC0-tand theCmaxof N-desmethyl imatinib were also increased, but without any significant difference. However, the single dose of 100 mg/kg or 50 mg/kg genistein has no effect on the pharmacokinetics of imatinib and N-desmethyl imatinib. Those results indicated that multiple dose of genistein (100 mg/kg or 50 mg/kg) induces the metabolism of imatinib, while single dose of genistein has no effect.

The effect of different partitions of seaweed Sargassum plagyophylum on depression behavior in mice model of despair

2019 ◽  
Vol 16 (4) ◽  
Author(s):  
Azadeh Mesripour ◽  
Neda Rabian ◽  
Afsaneh Yegdaneh
Keyword(s):  
Single Dose ◽  
Biological Activities ◽  
Food Resource ◽  
Control Group ◽  
Mice Model ◽  
Antidepressant Effects ◽  
Immobility Time ◽  
Term Administration ◽  
Swimming Test

Abstract Background Seaweeds are a famous traditional food resource in some countries containing different types of secondary metabolites. These marine organisms have shown different biological activities. The aim of this study was to investigate the effects of hexane and methanol extracts of Sargassum plagyophylum on depression. Methods Sargassum plagyophylum was collected from Persian Gulf. The plant was extracted by maceration with methanol-ethyl acetate solvent. The extract was evaporated and partitioned by hexane and methanol solvents. The two partitions were administered i.p. to male mice either a single dose or for 7 days. Depression was evaluated by the forced swimming test (FST) which higher immobility time indicates depressive-like behavior. Results The immobility time during FST decreased significantly by all the doses of the hexane partitions (notably 40 mg/kg; 10 s ± 2 vs. 114 s ± 12 control group). However, only the lowest dose (20 mg/kg) of the methanol partition reduced immobility time during FST (23 s ± 8, p<0.001). Following the long term administration both of the partitions reduced the immobility time in FST (hexane 27 s ± 11, methanol 70 s ± 14, p<0.05 vs. control 140 s ± 14). Conclusion The hexane partition showed antidepressant effects not only by long-term administration but also by the single dose during FST. The 7 days therapy with methanol partition also induced antidepressant behavior, but only the lowest single dose reduced immobility in FST. The methanol partitions possibly have certain substance that interfered with behavior in the FST. Therefore, S. plagyophylum should be considered for further antidepressant studies.

Carbamazepine Phakmacokinetics in Obese and Lean Subjects

1995 ◽  
Vol 29 (9) ◽  
pp. 843-847 ◽  
Author(s):  
Yoseph Caraco ◽  
Ester Zylber-Katz ◽  
Elliot M Berry ◽  
Micha Levy
Keyword(s):  
Body Weight ◽  
Single Dose ◽  
Ideal Body Weight ◽  
Obese Group ◽  
University Hospital ◽  
Pharmacokinetic Parameters ◽  
Group A ◽  
Obese Subjects ◽  
Group B ◽  
Lean Group

Objective: To compare carbamazepine pharmacokinetic parameters between obese and lean subjects following the administration of a single 200-mg tablet. Design: Single-dose intervention, open study. Setting: Teaching university hospital. Subjects: Eighteen obese (group A) otherwise healthy subjects, referred to the metabolic outpatient clinic, and 13 healthy lean (group B) volunteers. Inclusion criterion for the obese subjects was a body mass index (BMI = weight/height2) of more than 30 kg/m2. In the obese group, mean ± SD total body weight (TBW), BMI, and percent of ideal body weight (IBW) were 111.4 ± 19.9 kg, 38.8 ± 6.0 kg/m2, and 182.7% ± 30.7%, respectively. These values were significantly greater than the respective values of 63.2 ± 8.3 kg, 22.4 ± 1.6 kg/m2, and 105.8% ± 5.8% obtained in the lean group (p < 0.001). Intervention: Single-dose oral administration of carbamazepine 200-mg tablet (Teril, Taro, Israel). Outcomes: Carbamazepine elimination half-life (t1/2), apparent volume of distribution (Varea/F), and its oral clearance (Clpo/F) were derived from the drug concentration-time curves. Results: Carbamazepine Varea/F and t1/2 were significantly greater in group A than in group B (98.4 ± 26.9 vs. 60.7 ± 8.5 L, respectively, p < 0.001; and 59.4 ± 14.7 vs. 31.0 ± 5.0 h, respectively, p < 0.001), but its Clpo/F was reduced only slightly in obese as compared with lean subjects (19.8 ± 5.2 vs. 23.0 ± 4.6 mL/min, respectively, p = 0.07). Correction for IBW yielded similar results for Varea/F and t1/2, but Clpo/F per kg of IBW was significantly smaller in the obese than in the lean subjects (0.32 ± 0.07 vs. 0.39 ± 0.06 mL/min/kg of IBW, respectively, p < 0.02). Linear correlations were observed between Varea/F and TBW for both group A (r = 0.92, p < 0.001) and group B (r = 0.77, p < 0.002). Conclusions: In comparison with lean subjects, carbamazepine Varea/F is significantly greater in obese subjects and its t1/2 is markedly prolonged. The minor nonsignificant effect of obesity on carbamazepine Clpo/F suggests that in obese subjects the carbamazepine daily dose should be based on IBW, not on TBW.

scholarly journals A Prospective Randomized Trial to Assess the Antireflux Effect of Antireflux Mucosectomy in the Porcine Model

2019 ◽  
Vol 2019 ◽  
pp. 1-6
Author(s):  
Xuan Li ◽  
Weifeng Zhang ◽  
Meihong Chen ◽  
Shuchun Wei ◽  
Xiangyang Zhao ◽  
...  
Keyword(s):  
Gastroesophageal Reflux Disease ◽  
Proton Pump Inhibitor ◽  
Porcine Model ◽  
Gastroesophageal Junction ◽  
Control Group ◽  
Potential Efficacy ◽  
Significant Difference ◽  
Group A ◽  
Group B

Background. Both long-term proton pump inhibitor use and surgical fundoplication have potential drawbacks as treatments for chronic gastroesophageal reflux disease (GERD). Our aim was to investigate the potential efficacy of antireflux mucosectomy (ARMS) in porcine and determine the optimal circumference of resection in relation to gastroesophageal junction (GEJ). Methods. Nine pigs were allocated into the following 3 groups by computerized randomization: group A: control, group B: 1/3 circumference of the esophagus, and group C: 2/3 circumference of the esophagus. We performed mucosectomy with a crescentic mucosal resection at 3 cm above the GEJ and 1 cm below the GEJ. The animals were kept on a liquid diet for 24 h prior to endoscopy. At 6 weeks, animals underwent esophagoscopy, barium radiography, gastric yield pressure (GYP), and gastric yield volume (GYV) determination. Results. The weight of swines has no significant difference, and all pigs had maintained their weight after the procedure. We both found scar formation at the GEJ in group B and C. Compared with group A and B, group C produced significantly higher GYP (24.23±3.42 mmHg, p=0.004) and significantly smaller GYV (2200.0±238.96 mL, p=0.028) after 6 weeks. Barium radiography showed that the width of the cardia was narrower (13.73±1.19 mm, p=0.032) in group C after 6-week postprocedure. Conclusion. Our study demonstrated the potential antireflux effect of ARMS. We also recommend the 2/3 circumference resection of mucosa at 3 cm distance from the GEJ.

Efficacy and Safety of Fenofibrate in Uncomplicated Hyperbilirubinemia in Newborn: A Randomized Trial, with a 6-month Follow-up

2020 ◽  
pp. 37-42
Author(s):  
Jayendra R. Gohil ◽  
Vishal S. Rathod ◽  
Bhoomika D. Rathod
Keyword(s):  
Single Dose ◽  
Serum Bilirubin ◽  
Total Serum Bilirubin ◽  
Total Serum ◽  
Control Group ◽  
Term Neonates ◽  
Significant Difference ◽  
Group A ◽  
Group B

Objective: To study the effect and safety of Fenofibrate in uncomplicated hyperbilirubinemia in newborn with 6-month follow-up. Materials and Methods: This is a randomized controlled clinical trial conducted in 60 normal term neonates admitted for uncomplicated hyperbilirubinemia in NICU at Sir T G Hospital, Bhavnagar from January 2012 to December 2012. The data included: age, sex, total serum bilirubin (TSB), weight and duration of phototherapy. All neonates enrolled in the study received phototherapy. They were divided in two groups of 30 each: control group A and group B receiving Fenofibrate (100 mg/kg single dose). There was statistically insignificant difference between the parameters of age, sex, weight and TSB between the two groups at hospitalization. Data was analyzed by using appropriate statistical methods. Results: Mean values for total serum bilirubin in Fenofibrate group B at 24 and 48 hours after admission were significantly lower than those for control group A (p<0.0001,  p=0.0001). There was no significant difference in fall of TSB between 24 and 48 hours. The mean duration of phototherapy in Fenofibrate group (44.8h: 24-72h) was significantly shorter than that in control group (55.2 h: 24‐96 h) (P=0.02). There were no side effects of the drug observed during the study and during 6 months follow up period. Conclusion: Fenofibrate as a single 100 mg/kg dose in healthy full term neonates, is effective and a safe drug (till six-month follow-up) for neonatal hyperbilirubinemia, that can decrease the time needed for phototherapy and hence hospitalization. Effect of a single dose seems to wane after 24 hours.

scholarly journals Increase in liver nuclear tri-iodothyronine receptors associated with increased deoxyribonucleic acid by long-term administration of tri-iodothyronine in thyroidectomized rats

1979 ◽  
Vol 184 (1) ◽  
pp. 143-148 ◽  
Author(s):  
Hirotoshi Nakamura ◽  
Satoshi Hamada ◽  
Hiroo Imura
Keyword(s):  
Nuclear Receptors ◽  
Binding Capacity ◽  
Relative Increase ◽  
Control Value ◽  
Glycerophosphate Dehydrogenase ◽  
Small Doses ◽  
Term Administration ◽  
Group A ◽  
Group B

The effect of long-term administration of small amounts of tri-iodothyronine was examined on the nuclear tri-iodothyronine receptors in rat liver. The maximal binding capacity (Cmax.) and association constant (Ka) of the receptors were determined in thyroidectomized rats given vehicle alone (group A), 2μg of tri-iodothyronine/100g body wt. (group B) or 7μg of tri-iodothyronine/100g body wt. (group C) for 2 weeks. Scatchard analyses with correction for the amount of endogenous tri-iodothyronine revealed that Cmax. values per g of liver were increased to 1.5 and 2.7 times the control value in groups B and C respectively. Since concentrations of DNA per g of liver were significantly increased in the two groups of hormone-treated rats, Cmax. values per mg of DNA were nearly the same in group B, but still increased significantly in group C compared with group A. Ka values remained unchanged in all three groups of animals. Mitochondrial α-glycerophosphate dehydrogenase activity was 9.6 and 28.7 times as high in groups B and C, respectively, as in group A. Concentrations of endogenous tri-iodothyronine bound to non-histone protein were substantially increased in groups B and C, although concentrations of serum tri-iodothyronine remained rather low. The results obtained indicate that the long-term administration of tri-iodothyronine in small doses induces an increase in the nuclear receptors associated with increased DNA with and without accompanying a relative increase in the receptor concentration in thyroidectomized rats. Also the hormonal effect is closely related to the total number of the nuclear receptors and the concentrations of nuclear tri-iodothyronine bound to the receptors rather than the serum tri-iodothyronine concentrations.

scholarly journals Effect of Single Dose of Pregabalin on Post Tracheal Intubation Sore Throat after General Anesthesia

2019 ◽  
Author(s):  
Hassan Mohammadipour Anvari ◽  
Maarouf Ansari Kazaj ◽  
Khosro Kolahdouzan ◽  
Nasser Ghobanian ◽  
Afsaneh Khobeydeh
Keyword(s):  
Single Dose ◽  
Tracheal Intubation ◽  
General Anesthesia ◽  
Sore Throat ◽  
Control Group ◽  
Case Group ◽  
Double Blind ◽  
Analgesic Effects ◽  
Group A ◽  
Group B

Background: Sore throat is one of the major complications of tracheal intubation after general anesthesia. Pregabalin is an analgesic, the anti neuropathic pain and analgesic effects of which have been demonstrated in various studies. This study examined the effects of single dose pregabalin one hour before tracheal intubation, to prevent sore throat after extubation. Methods: In a double-blind, randomized clinical trial, 60 patients who had undergone general and urologic surgeries at Imam Reza hospital in Tabriz, Iran, since March to July 2015 that required tracheal intubation, were included in the study. The patients were randomly divided into two groups (group A, 30 patients and group B, 30 patients). In the group A, an hour before anesthesia, one pregabalin tablet (300mg) was given to the patients. For the patients of the group B, the placebo was given. After awareness of patients, the severity of sore throat was measured and recorded by VAS scale after 2, 6 and 24 hours of the surgery. Results: Severity and incidence of sore throat after tracheal intubation were not significantly different between two groups. Meanwhile, no side effects of pregabalin were observed in the group A. Conclusion: Administration of pregabalin as a single dose of 300 mg one hour prior to anesthesia and intubation decreased the incidence and severity of sore throat in the case group than the control group, although the amount of this reduction was not statistically significant between the two groups.

Corneal Epithelial Deficiency Induced by the Use of β-Blocker Eye Drops

1997 ◽  
Vol 7 (4) ◽  
pp. 334-339 ◽  
Author(s):  
Y. Haruta ◽  
Y. Ohashi ◽  
S. Matsuda
Keyword(s):  
Wound Healing ◽  
Physiological Saline ◽  
Eye Drops ◽  
Term Study ◽  
Corneal Epithelial ◽  
Long Term Study ◽  
Short Term Study ◽  
Epithelial Wound Healing ◽  
Β Blocker

Two studies were conducted to check the effects of β-blocker eye drops, 2% carteolol (Mikelan®) and 0.5% timolol (Timoptol®), on regeneration of corneal epithelium in rabbit eyes. For the short-term study, epithelial deficiency was artificially induced in the cornea of albino rabbits. One of the β-blocker eye drops or 0.005% benzalkonium chloride was applied in the right eye and physiological saline solution was applied to the left eye four times a day, and wound healing rate was calculated. Two weeks later, images of the surface epithelium were analyzed by scanning electron microscopy and proliferative capacity was studied, using proliferating cell nuclear antigen as a marker. The long-term study was conducted similarly except that the eye drops were applied twice a day and epithelial deficiency was re-induced every two weeks. In the short-term study, epithelial wound healing rate was slowed in β-blocker groups. Significant differences were detected between the Mikelan® and Timoptol® groups, and the benzalkonium and physiological saline groups. The β-blocker groups had severe epithelial cell desquamation, as well as detachment. In the long-term study, the Mikelan® group had significantly delayed wound healing at first induction, the benzalkonium group showed delay up to the third induction and the Timoptol® group up to the fifth induction. These studies indicate that β-blocker eye drops delay corneal epithelial wound healing and supported the concept that corneal epithelial deficiency occurs clinically after the long-term administration of β-blocker eye drops.

Effect of Phosphate Supplements on Soft-Tissue Calcification and Bone Turnover

1972 ◽  
Vol 42 (3) ◽  
pp. 289-299 ◽  
Author(s):  
Jenifer Jowsey ◽  
P. Balasubramaniam
Keyword(s):  
Soft Tissue ◽  
Soft Tissues ◽  
Control Diet ◽  
Control Period ◽  
Control Group ◽  
Soft Tissue Calcification ◽  
Term Study ◽  
Tissue Calcification ◽  
Long Term Study

1. The short- and long-term effects of oral phosphate supplements were studied in two groups of adult rabbits. 2. In the short-term study, compared with control animals, the bones of phosphate-supplemented rabbits showed a greater degree of porosity, and defects in the tibia created at the beginning of the study were replaced with bone tissue containing many areas of resorption. There was an increase in retention of 85Sr in the hard and soft tissues, particularly in the kidney and thoracic aorta. 3. In the long-term study, a second group of rabbits received a low calcium and phosphate intake during the control period; half of this group were then fed a low dosage of supplemental phosphate while the remaining half remained on the control diet. After a period of 6 months the bones of phosphate-supplemented animals showed increased porosity and there was an increase in 85Sr retention by the kidney compared with the control group. 4. Phosphate supplementation appears to result in secondary hyperparathyroidism and to cause soft-tissue calcification.

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