scholarly journals BIOAVAILABILITY AND DISPOSITION KINETICS OF AMOXICILLIN

2015 ◽  
Vol 22 (01) ◽  
pp. 006-012
Author(s):  
Zulfiqar-Ul- Hassan ◽  
Sualeha Riffat ◽  
Aamir Nazir ◽  
Rahat Naseer ◽  
Anila Asghar ◽  
...  

OBJECTIVE: The study was planned to observe the bioavailability anddisposition kinetics of amoxicillin in adult rabbits (irrespective of sex) under healthy anddehydrated conditions. Design: Comparative. Place and duration of study: The study wasconducted at the department of pharmacology, University of Veterinary and Animal Sciences,Lahore from April 2013 to October 2013. Methodology: Initially all rabbits were weighed andtheir packed cell volume (PCV) and other biochemical parameters were observed under normalconditions. Bioavailability and disposition kinetics of amoxicillin (10mg/kg body weight) werestudied in normal rabbits following oral and intravenous route of drug administration. After 10days washout period, these rabbits were made dehydrated by keeping the animals off waterbut not food. The animals with 10% decrease in body weight were declared dehydrated. Theirparameters were again measured. Treated rabbits were administered amoxicillin orally andintravenously (10mg/kg body weight). Samples were drawn at prescribed time. Amoxicillinwas assessed in plasma by using microbiological assay method. Plasma concentration wasanalyzed using non compartmental method. Results: The water deprived or dehydrated rabbitsshowed a significant increase in the packed cell volume, blood glucose and plasma globulins ascompared to the normal rabbits. However, there was a significant (p<0.05 & p<0.01) decreasein body weight, total proteins, albumins and albumin globulin ratio of the dehydrated rabbits.The peak plasma concentration, volume of distribution and rate constant of elimination waslower in the dehydrated rabbits as compared to the normal rabbits. The plasma concentrationof amoxicillin after intravenous administration in dehydrated rabbits had a significant (p<0.05& p<0.01) larger area under curve, area under 1st moment curve, a longer half life and a largermean residence time. Conclusions: The study in the dehydrated rabbits indicated the need ofmodification of dosage regimen.

2000 ◽  
Vol 92 (2) ◽  
pp. 376-376 ◽  
Author(s):  
Lynne M. Reynolds ◽  
Andrew Infosino ◽  
Ronald Brown ◽  
Jim Hsu ◽  
Dennis M. Fisher

Background A nondepolarizing muscle relaxant with an onset and offset profile similar to succinylcholine is desirable for pediatric anesthesia. The onset and offset of rapacuronium are rapid in children. In the current study, the authors determined its pharmacokinetic characteristics in children. In addition to administering rapacuronium by the usual intravenous route, the authors also gave rapacuronium intramuscularly to determine uptake characteristics and bioavailability. Methods Forty unpremedicated patients aged 2 months to 3 yr were anesthetized with halothane, 0.82-1.0% end-tidal concentration. When anesthetic conditions were stable, rapacuronium was injected either into a peripheral vein (2 mg/kg for infants, 3 mg/kg for children) or a deltoid muscle (2.8 mg/kg for infants, 4.8 mg/kg for children). Four venous plasma samples were obtained from each subject 2-240 min after rapacuronium administration. A mixed-effects population pharmacokinetic analysis was applied to these values to determine bioavailability, absorption rate constant, and time to peak plasma concentration with intramuscular administration. Results Plasma clearance was 4.77 ml x kg(-1) x min(-1) + 8.48 ml/min. Intramuscular bioavailability averaged 56%. Absorption from the intramuscular depot had two rate constants: 0.0491 min(-1) (72.4% of absorbed drug) and 0.0110 min(-1) (27.6% of the absorbed drug). Simulation indicated that plasma concentration peaks 4.0 and 5.0 min after intramuscular rapacuronium in infants and children, respectively, and that, at 30 min, less than 25% of the administered dose remains to be absorbed from the intramuscular depot. Conclusions In infants and children, rapacuronium's clearance and steady state distribution volume are less than in adults. After intramuscular administration, bioavailability is 56%, and plasma rapacuronium concentrations peak within 4 or 5 min.


2010 ◽  
Vol 2010 ◽  
pp. 1-6 ◽  
Author(s):  
Ayman Goudah ◽  
Sherifa Hasabelnaby

The present study was planned to investigate the disposition kinetics of levofloxacin in plasma of female native Barky breed sheep after single intravenous (IV) and intramuscular (IM) administration of 4 mg/kg body weight. The concentrations of levofloxacin in the plasma were measured using high-performance liquid chromatography (HPLC) with a UV detector on samples collected at 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 4, 6, 8, 10, 12, 18, 24, 32, and 48 h after treatment. Following intravenous injection, the decline in plasma drug concentration was biexponential with half-lives of  h and  h for distribution and elimination phases, respectively. The volume of distribution at steady state was  l/kg. After intramuscular administration of levofloxacin at the same dose, the peak plasma concentration was  g/mL and was obtained at  h , the elimination half-life was  h, and AUC was  g.h/mL. The systemic bioavailability was %.In vitroplasma protein binding was 23.74%. When approved therapy fails, levofloxacin may be used in some countries for therapy of food animals, however, that is not true in the US.


Author(s):  
I. Iwanegbe ◽  
M. Suleiman ◽  
A. Jimah

Aims: To investigate the effect of food blends (plantain, soybean and ginger) on the blood glucose, lipid profile and haematological indices on streptozotocin induced diabetic rats. Methodology: A total of 35 rats of mean body weight 219.07 g separated into7 groups (5 per group) where induced by a single intraperitoneal (I.P) injection of streptozotocin (0.1 g dissolved in 5 ml of freshly prepared sodium citrate buffer 0.1 M, pH 4.5) at a dose of 40 mg/kg body weight after fasting for 12 hours and fed with flours/blends. The flours were produced from plant materials for different treatments/blends (blend A=100% unripe plantain, B=80% unripe plantain, 14% soybean, 6% ginger, C=70% unripe plantain, 26% soybean, 4% ginger, D= 60% unripe plantain, 38% soybean, 2% ginger, E= 50% unripe plantain, 50% soybean) and the phytochemicals and minerals content were determined. Blood glucose was determined at 5 days interval for 25 days. Diabetes was confirmed in rats with blood glucose concentrations >200 mg/dl. After 25 days rats were anaesthetized with chloroform vapour and blood samples collected by cardiac puncture for haematology and lipid profile determination. Results: The results showed that unripe plantain, soya beans and ginger in adequate proportion(C=70% unripe plantain, 26% soybean, 4% ginger or D= 60% unripe plantain, 38% soybean, 2% ginger) could help to reduce blood glucose, improve haematological parameters and lipid profile. Significant reduction was observed in the blood glucose level of rats fed blends C and D from 286 to 85 mg/dl and 307 to 90 mg/dl respectively at the end of experiment. These results also demonstrated that the inclusion of ginger at 6% causes rise in blood glucose level. Total cholesterol (TC) increased in all the blends. However, the lowest concentration of TC was observed in blends C and D. The highest packed cell volume (60%) and Haemoglobin (20 g/dl) level observed in rats fed blend C was significantly higher than the normal control fed conventional feeds. The increase in packed cell volume (PCV) (50%) and Hb (17 g/dl) in diabetic rats demonstrated that the formulated blend C was able to raise PCV and Hb above 50% and 17 g/dl (Normal control NC) respectively. Significant increase (P<0.05) in low density lipoprotein cholesterol (LDLc) was also observed in all the blends with blend C having the least (4.0 mg/dl) close to NC (2.0 mg/dl). Conclusion: From the results it is evident that blend C will manage and improve the health status of diabetic patients.


Parasitology ◽  
2018 ◽  
Vol 145 (9) ◽  
pp. 1235-1242 ◽  
Author(s):  
Christine M. Kamidi ◽  
Joanna Auma ◽  
Paul O. Mireji ◽  
Kariuki Ndungu ◽  
Rosemary Bateta ◽  
...  

AbstractThis study assessed the virulence of Trypanosoma evansi, the causative agent of camel trypanosomiasis (surra), affecting mainly camels among other hosts in Africa, Asia and South America, with high mortality and morbidity. Using Swiss white mice, we assessed virulence of 17 T. evansi isolates collected from surra endemic countries. We determined parasitaemia, live body weight, packed cell volume (PCV) and survivorship in mice, for a period of 60 days’ post infection. Based on survivorship, the 17 isolates were classified into three virulence categories; low (31–60 days), moderate (11–30 days) and high (0–10 days). Differences in survivorship, PCV and bodyweights between categories were significant and correlated (P < 0.05). Of the 10 Kenyan isolates, four were of low, five moderate and one (Type B) of high virulence. These findings suggest differential virulence between T. evansi isolates. In conclusion, these results show that the virulence of T. evansi may be region specific, the phenotype of the circulating parasite should be considered in the management of surra. There is also need to collect more isolates from other surra endemic regions to confirm this observation.


2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Satoshi Nakano ◽  
Shuhei Osaka ◽  
Yusuke Sabu ◽  
Kei Minowa ◽  
Saeko Hirai ◽  
...  

AbstractProgressive familial intrahepatic cholestasis (PFIC), a rare inherited disorder, progresses to liver failure in childhood. We have shown that sodium 4-phenylbutyrate (NaPB), a drug approved for urea cycle disorders (UCDs), has beneficial effects in PFIC. However, there is little evidence to determine an optimal regimen for NaPB therapy. Herein, a multicenter, open-label, single-dose study was performed to investigate the influence of meal timing on the pharmacokinetics of NaPB. NaPB (150 mg/kg) was administered orally 30 min before, just before, and just after breakfast following overnight fasting. Seven pediatric PFIC patients were enrolled and six completed the study. Compared with postprandial administration, an approved regimen for UCDs, preprandial administration significantly increased the peak plasma concentration and area under the plasma concentration-time curve of 4-phenylbutyrate by 2.5-fold (95% confidential interval (CI), 2.0–3.0;P = 0.003) and 2.4-fold (95% CI, 1.7–3.2;P = 0.005). The observational study over 3 years in two PFIC patients showed that preprandial, but not prandial or postprandial, oral treatment with 500 mg/kg/day NaPB improved liver function tests and clinical symptoms and suppressed the fibrosis progression. No adverse events were observed. Preprandial oral administration of NaPB was needed to maximize its potency in PFIC patients.


Cephalalgia ◽  
1997 ◽  
Vol 17 (4) ◽  
pp. 541-550 ◽  
Author(s):  
KHP Moore ◽  
EK Hussey ◽  
S Shaw ◽  
E Fuseau ◽  
C Duquesnoy ◽  
...  

The delivery of sumatriptan doses intranasally could add greater flexibility in the treatment of migraine than is possible with the currently available subcutaneous and oral sumatriptan preparations. Two independent double-blind, randomized, placebo-controlled clinical studies were conducted to evaluate the safety, tolerability and pharmacokinetics of intranasally administered sumatriptan following ascending single doses (three different dose levels) and multiple doses. In the four-way crossover, ascending-dose study, 20 healthy female subjects were randomized to receive on separate occasions single intranasal spray doses of 5, 10, or 20 mg sumatriptan (as the hemisulphate salt) or placebo into one nostril. Adverse events were mild and consisted mainly of bitter taste at the back of the throat and events typical of sumatriptan administered by other routes (headache, lightheadedness and tingling). Area under the plasma sumatriptan concentration versus time curve (AUC) and peak plasma concentration (Cmax) increased with the dose. Dose proportionality was demonstrated between 5 and 10 mg but not across the dose range 5–20 mg. Time to maximum plasma concentration (tmax) was variable due to multiple peaking. The elimination half-life (t1/2), approximately 2 h, was unaffected by the magnitude of dose. In the two-period, multiple-dose, crossover study, 12 healthy adult male and female subjects were randomized to receive either sumatriptan hemisulphate 20 mg or placebo, administered intranasally as a spray three times a day for 4 days, The two dosing periods were separated by 3 to 14 days. Multiple doses of sumatriptan were well tolerated, with no serious adverse events occurring or withdrawals due to adverse events. All patients reported a mild to moderate drug-related disturbance of taste. Nasal examinations remained normal, and olfactory function was unaffected. The AUC over the first 8 h following dosing (AUC8) and fraction of the dose excreted in the urine (fe; 6.2% vs 3.6%) were similar on Days 1 and 4. Day 4 values were significantly higher (p0.05) for Cmax (16.9 ng/ml vs 13.1 ng/ml), renal clearance (Clr; 19.0 l/h vs 14.2 l/h), and t1/2 (2.18 h vs 1.93 h), and shorter for tmax (0.88 h vs 1.75 h). Some accumulation (22%) occurred over the 4 days of dosing. Serum concentrations of the pharmacologically inactive indole acetic acid metabolite of sumatriptan were fourfold to fivefold higher than corresponding sumatriptan concentrations. Overall, these studies show the sumatriptan intranasal spray formulation is well tolerated, allows rapid absorption of sumatriptan, and results in only a clinically insignificant degree of sumatriptan accumulation upon repeated dosing.


2011 ◽  
Vol 10 (1) ◽  
pp. 59
Author(s):  
S. A. H. AL-Moramadhi

This study was conducted on broiler chickens to investigate the effect of Marticaria chamomilla flowers extract on some physiological properties. One day age Fawbro birds (Average weight 55g) were used in this study, they fed ad libtum until 7weeks age. (60 chickes) were divided into three groups (each group has 20 birds ).1-treatment one: administrated orally the aqueous extract of Marticaria chamomilla flowers at concentration 50mg /kg body weight .2-treatment two: administrated orally the aqueous extract of Marticaria chamomilla flowers at concentration 100mg /kg body weight3-control group: administrated distilled water .At the end of experiment blood samples were taken from brachial vein for ten birds of each group for hematological and bio chemical examination ,the following parameters are used:- serum glucose concentration, serum cholesterol concentration ,hemoglobin concentration ,packed cell volume ,body weight and food intake. Results showed significant decrease (p<0.05) in glucose concentration in treatments groups compared with control, and significant decrease (p<0.05) in cholesterol concentration in treatments groups compared with the control. While there was no significant effect on hemoglobin concentration, packed cell volume, body weight and food intake in treatments groups compared with the control


Sign in / Sign up

Export Citation Format

Share Document