Influence of bran on bioavailability of chloramphenicol administered orally to pigs

1984 ◽  
Vol 62 (2) ◽  
pp. 208-211 ◽  
Author(s):  
L. Buéno ◽  
J. Fioramonti ◽  
M. Alvinerie ◽  
T. Bardon
Keyword(s):  
Plasma Concentration ◽  
Intestinal Absorption ◽  
Intravenous Administration ◽  
Pancreatic Lipase ◽  
Lipase Activity ◽  
Maximal Plasma Concentration ◽  
Transit Times ◽  
Rate Of Absorption ◽  
Maximal Plasma

The present study was undertaken to determine if bran added to a fiber-free diet (milk) would modify the absorption of orally administered chloramphenicol (cmp) compared with that observed on a standard concentrates diet in pig. The plasma chloramphenicol level was maximal (0.47 ± 0.26 μg/mL), 3.5 h after a meal of concentrates containing 8 g of chloramphenicol palmitate; this highest concentration represented only 30% of that observed 12 h after a meal of substituted milk and 14% of the maximal plasma concentration of chloramphenicol detected 14 h after a milk meal when supplemented with bran (100 g). Over 24 h, the plasma availability of chloramphenicol with the three tested diets represented, respectively, 11.4% (concentrates), 17.2% (milk), and 74.1% (milk + bran) of that obtained for intravenous administration; similar oral–caecal transit times were observed for these three diets. It was concluded that the presence of bran in the regimen strongly increases the intestinal absorption of chloramphenicol palmitate, with the lowest rate of absorption on standard concentrates, and it is tempting to speculate that this increase is due to a more rapid intestinal hydrolysis by an increased pancreatic lipase activity on bran.

scholarly journals Effects of Vitamin D Plus Calcium Supplements on Pharmacokinetics of Isoflavones in Thai Postmenopausal Women

2011 ◽  
Vol 2011 ◽  
pp. 1-7 ◽  
Author(s):  
Supanimit Teekachunhatean ◽  
Paveena Pongnad ◽  
Noppamas Rojanasthein ◽  
Maleeya Manorot ◽  
Chaichan Sangdee
Keyword(s):  
Vitamin D ◽  
Single Dose ◽  
Plasma Concentration ◽  
Postmenopausal Women ◽  
Plasma Concentrations ◽  
Pharmacokinetic Parameters ◽  
Calcium Supplements ◽  
Maximal Plasma Concentration ◽  
Maximal Plasma ◽  
To Receive

The objective of this study was to determine the effects of vitamin D3plus calcium supplements (D3-calcium) on pharmacokinetics of isoflavones in Thai postmenopausal women. This study was an open-labeled, randomized three-phase crossover study. Twelve healthy subjects were randomized to receive one of the following regimens: (a) a single dose of isoflavones, (b) a single dose of isoflavones, and D3-calcium, or (c) continuous D3-calcium for 7 days followed by a single dose of isoflavones on the 8th day. After a washout period, subjects were switched to receive the 2 remaining regimens according to their randomized sequences. Blood samples were collected before dose and at specific time points until 32 hours after isoflavone administration. Plasma was treated with β-glucuronidase/sulfatase to hydrolyze glucuronide and sulfate conjugates of daidzein and genistein. Plasma concentrations of daidzein and genistein were determined by high performance liquid chromatography. The estimated pharmacokinetic parameters of isoflavones were time to maximal plasma concentration (Tmax), maximal plasma concentration (Cmax), half-life (t1/2) and area under the plasma concentration-time curve (AUC).Tmaxof daidzein and genistein after regimen B was significantly longer than that of regimen A. Other pharmacokinetic parameters of daidzein and genistein obtained following the three regimens were not significantly different.

Pharmacokinetics of low-dose and high-dose buprenorphine in cats after rectal administration of different formulations

2018 ◽  
Vol 21 (10) ◽  
pp. 938-943
Author(s):  
Maike Schroers ◽  
Andrea Meyer-Lindenberg ◽  
Sven Reese ◽  
Britta Dobenecker ◽  
Korbinian Pieper
Keyword(s):  
Plasma Concentration ◽  
Low Dose ◽  
Ph Value ◽  
Plasma Concentrations ◽  
Rectal Administration ◽  
High Dose ◽  
Time Curve ◽  
Maximal Plasma Concentration ◽  
Wide Range ◽  
Maximal Plasma

Objectives A prospective experimental study was performed in nine young healthy cats to investigate a pharmacokinetic profile and the clinical relevance of rectally administered buprenorphine. Rectal pH value was measured in all nine cats. Methods Blood was collected 15, 30, 60, 90, 120, 240 and 480 mins and 24 h after the rectal administration of a suppository and a gel at doses between 0.02 mg/kg and 0.1 mg/kg buprenorphine to determine the plasma concentration of buprenorphine. Rectal pH was measured with pH paper. Results Upon pharmacokinetic non-compartment analysis of high-dose buprenorphine (0.1 mg/kg), average maximal plasma concentration was found to be 1.13 ng/ml, time to maximal plasma concentration was 45 mins and area under the plasma concentration–time curve was 94.19 ng*min/ml, representing low but potential bioavailability. Mean residual time was 152.2 mins and the half-life was 92.6 mins. A wide range of plasma concentrations within the cohort was measured and two of the cats had to be excluded from statistical analysis owing to incomplete uptake. Vital parameters of all cats were considered to be normal but three of the cats showed mydriasis up to 8 h after application. After the administration of a low-dose suppository or a rectal gel (0.02 mg/kg) within pilot studies, no buprenorphine was detected in cat plasma. Rectal pH in all cats was between 7.7 and 8. Conclusions and relevance The rectal application of buprenorphine at a dose of 0.1 mg/kg revealed a potential but weak uptake in cats. Regarding effective concentrations in previous pharmacokinetic investigations, rectal administration is currently not recommended for good provision of opioid analgesia in cats. Pharmacological investigations of formulation and galenics in order to improve the rectal bioavailability of buprenorphine remain to be clarified before further dose-finding and pharmacokinetic/pharmacodynamic studies are performed.

scholarly journals Modification of a phospholipid stabilized emulsion interface by bile salt: effect on pancreatic lipase activity

1998 ◽  
Vol 39 (3) ◽  
pp. 623-632 ◽  
Author(s):  
Martin Wickham ◽  
Martin Garrood ◽  
John Leney ◽  
Peter D.G. Wilson ◽  
Annette Fillery-Travis
Keyword(s):  
Bile Salt ◽  
Pancreatic Lipase ◽  
Lipase Activity ◽  
Salt Effect

scholarly journals Studies on the detergent inhibition of pancreatic lipase activity.

1983 ◽  
Vol 24 (10) ◽  
pp. 1336-1342
Author(s):  
Y Gargouri ◽  
R Julien ◽  
A G Bois ◽  
R Verger ◽  
L Sarda
Keyword(s):  
Pancreatic Lipase ◽  
Lipase Activity

scholarly journals Kinetic studies on pancreatic lipase activity in micellar systems. II. Effect of fatty acid chain length of substrates.

1983 ◽  
Vol 31 (12) ◽  
pp. 4213-4219 ◽  
Author(s):  
HIROSHI NAKAHARA ◽  
SATOSHI OKADA ◽  
KENSHU MOCHIDA ◽  
HIDENOBU OHMORI ◽  
MASAICHIRO MASU
Keyword(s):  
Fatty Acid ◽  
Chain Length ◽  
Pancreatic Lipase ◽  
Lipase Activity ◽  
Kinetic Studies ◽  
Fatty Acid Chain Length ◽  
Fatty Acid Chain ◽  
Micellar Systems

Safety, Tolerability and Pharmacokinetics of BIBN 4096 BS, the First Selective Small Molecule Calcitonin Gene-Related Peptide Receptor Antagonist, Following Single Intravenous Administration in Healthy Volunteers

Cephalalgia ◽  
2004 ◽  
Vol 24 (8) ◽  
pp. 645-656 ◽  
Author(s):  
M Iovino ◽  
U Feifel ◽  
C-L Yong ◽  
J-M Wolters ◽  
G Wallenstein
Keyword(s):  
Plasma Concentration ◽  
Receptor Antagonist ◽  
Small Molecule ◽  
Intravenous Administration ◽  
Calcitonin Gene Related Peptide ◽  
Related Peptide ◽  
Concentration Time ◽  
Calcitonin Gene ◽  
Dose Levels ◽  
Single Intravenous Administration

BIBN 4096 BS ([R-(R∗,S∗)]-N-[2-[[5-amino-1-[[4-(4-pyridinyl)-1-piperazinyl]carbonyl] pentyl]amino]-1-[(3,5-dibromo-4-hydroxyphenyl)methyl]-2-oxoethyl]-4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl)-,1-piperidinecarboxamide) is the first selective, highly potent, small molecule, nonpeptide calcitonin gene-related peptide (CGRP) receptor antagonist, which has been developed for the treatment of acute migraine. The objective of this study was to obtain information on the safety, tolerability and pharmacokinetics of BIBN 4096 BS following single intravenous administration of rising doses (0.1, 0.25, 0.5, 1, 2.5, 5 and 10 mg) in 55 healthy male and female volunteers. The study was of single-centre, double-blind (within dose levels), placebo-controlled, randomized, single rising dose design. Blood pressure, pulse rate, respiratory rate, ECG, laboratory tests and forearm blood flow did not reveal any clinically relevant, drug-induced changes. Sixteen adverse events (AEs) were reported by eight of 41 volunteers after BIBN 4096 BS compared to five AEs reported by four of 14 volunteers after placebo. Approximately two-thirds of all AEs related to active treatment occurred at the highest dose of 10 mg. At this dose level, all AEs were confined to the three BIBN 4096 BS-treated females, and consisted mainly of transient and mild paresthesias. Paresthesias were the single most frequent AE, whereas fatigue was the AE which occurred in the highest number of subjects. Only two AEs were of moderate intensity, all remaining AEs were of mild intensity. No serious AEs were reported. The local tolerability after intravenous administration was good. In summary, intravenously administered BIBN 4096 BS revealed a very favourable safety profile over the dose range tested in both genders. Generally well tolerated at all dose levels, it was of satisfactory tolerability in female subjects at the highest dose of 10 mg. The plasma concentration-time courses of BIBN 4096 BS showed multicompartmental disposition characteristics. Mean maximum concentration (Cmax) values appeared to be dose-proportional. Based on the results from the two high dose levels (5 and 10 mg) with sufficient individual subject data, BIBN 4096 BS exhibited a total plasma clearance (CL) of approximately 12 l/h and an apparent volume of distribution at steady state (Vss) of approximately 20 l, resulting in a terminal half-life (t1/2) of approximately 2.5 h. Inter-individual variability was moderate with a coefficient of variation of approximately 45% based on the area under the plasma concentration-time curve (AUC) values. The mean renal clearance (CLR) was approximately 2 l/h, suggesting that renal excretion plays only a minor role in the elimination of unchanged BIBN 4096 BS.

scholarly journals Physiological parameters governing the action of pancreatic lipase

2010 ◽  
Vol 23 (1) ◽  
pp. 146-154 ◽  
Author(s):  
Iain A. Brownlee ◽  
Deborah J. Forster ◽  
Matthew D. Wilcox ◽  
Peter W. Dettmar ◽  
Chris J. Seal ◽  
...  
Keyword(s):  
Weight Management ◽  
Pancreatic Lipase ◽  
Lipase Activity ◽  
Dietary Lipid ◽  
Ion Concentration ◽  
Lipid Absorption ◽  
Energy Yield ◽  
Body Of Knowledge ◽  
Lipid Ester ◽  
Duodenal Lumen

The most widely used pharmacological therapies for obesity and weight management are based on inhibition of gastrointestinal lipases, resulting in a reduced energy yield of ingested foods by reducing dietary lipid absorption. Colipase-dependent pancreatic lipase is believed to be the major gastrointestinal enzyme involved in catalysis of lipid ester bonds. There is scant literature on the action of pancreatic lipase under the range of physiological conditions that occur within the human small intestine, and the literature that does exist is often contradictory. Due to the importance of pancreatic lipase activity to nutrition and weight management, the present review aims to assess the current body of knowledge with regards to the physiology behind the action of this unique gastrointestinal enzyme system. Existing data would suggest that pancreatic lipase activity is affected by intestinal pH, the presence of colipase and bile salts, but not by the physiological range of Ca ion concentration (as is commonly assumed). The control of secretion of pancreatic lipase and its associated factors appears to be driven by gastrointestinal luminal content, particularly the presence of acid or digested proteins and fats in the duodenal lumen. Secretion of colipase, bile acids and pancreatic lipase is driven by cholecystokinin and secretin release.

Studies of the Toxicological Potential of Capsinoids, XI: Pharmacokinetic and Tissue Distribution Study of 14C-Dihydrocapsiate and Metabolites in Rats

2010 ◽  
Vol 29 (2_suppl) ◽  
pp. 3S-14S ◽  
Author(s):  
Bruce K. Bernard ◽  
Kazuyuki Ubukata ◽  
Ryuichi Mihara ◽  
Yoshiaki Sato ◽  
Hiroyuki Nemoto
Keyword(s):  
Body Weight ◽  
Plasma Concentration ◽  
Vanillic Acid ◽  
Male Rats ◽  
Vanillyl Alcohol ◽  
Tissue Concentrations ◽  
Distribution Study ◽  
Maximal Plasma ◽  
Tissue Distribution Study ◽  
Kidney Liver

Pharmacokinetics of a single gavage dose of 14C-labeled dihydrocapsiate (10 mg/kg) were investigated in male rats. Maximal plasma concentration was achieved in 40 minutes and exhibited an apparent half-life of 2.4 hours. Excretion of radioactivity in the urine, feces, and expired air was 78.2%, 19.4%, and 0.5% of the dose, respectively. Highest tissue concentrations were achieved in the kidney, liver, and blood; the data indicate that radioactivity accumulation following daily exposure at a dose of 10 mg/kg body weight is unlikely. Radioactivity in the plasma was associated with metabolites and their conjugates, probably vanillyl alcohol, vanillic acid, glucuronide of vanillyl alcohol, sulphate of vanillyl alcohol, and sulphate of vanillic acid. These results suggest dihydrocapsiate is metabolized by hydrolysis in the gut, or esterase or other enzymes in the blood, and the metabolites were rapidly absorbed and converted to their conjugates in the liver and eliminated by the kidneys into the urine.

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