Biopharmaceutical characterisation of herbal medicinal products: are in vivo studies necessary?

abstract：:Recent evidences suggest that genetic CYP2C19 polymorphism plays a role in the development of treatment resistance for clopidogrel's antiplatelet therapy. This short communication puts forward some strategies that could be potentially used to overcome the genetic polymorphism associated hurdles. While there is some es...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Srinivas NR

更新日期：2009-07-01 00:00:00

abstract：:Previous studies have indicated that borneol has double side effects on the central nervous system (CNS), but the mechanism is unknown. The aim of this study was to clarify the relationship between excitation ratio [contents of excitatory amino acids (AAs) versus that of inhibitory] and the content of natural borneol ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Li WR,Chen RY,Yang L,Huang TL,Xu QW,Mi SQ,Wang NS

更新日期：2012-03-01 00:00:00

abstract：:The aim of this work was to use radiopharmaceuticals such as technetium (99mTc) and indium (DTPA-Ca111In) to visualize, with a gamma-camera, the disintegration area and time of 3 types of enteric coated hard gelatin capsules (obtained by 3 different preparation processes) and thus, to verify that they are really resis...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Catteau D,Barthélémy C,Deveaux M,Robert H,Trublin F,Marchandise X,Van Drunen H

更新日期：1994-04-01 00:00:00

abstract：:The effects of potassium ethylxanthogenate (PEX) and 2,3-Dimercaptopropane sulphonate sodium (Unithiol) on the pentobarbital (40 mg/kg, body weight i.v.) (PB) sleeping time, pharmacokinetics, and metabolism, were studied in comparative experiments on male albino mice. It was established that the pretreatment of animal...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Yanev S,Janku I,Stoytchev T,Havlik I,Krebs V

更新日期：1982-01-01 00:00:00

abstract：:Binding of cefalotin to human serum albumin was studied in vitro by equilibrium dialysis and the quantitative measurement of cefalotin was made by fluorimetric assay. The binding rate of cefalotin to human serum albumin found to be 61,1%. The determination of drug binding parameters showed a large number of binding si...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Decroix MO,Chaumeil JC,Flouvat B

更新日期：1984-07-01 00:00:00

abstract：:Sertraline potently inhibits cytochrome P450 2B6 (CYP2B6) in vitro. Bupropion is commonly co-prescribed with sertraline and is exclusively metabolized by CYP2B6 to its major active metabolite hydroxybupropion. Putatively the co-administration of bupropion and sertraline could lead to a significant pharmacokinetic drug...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Molnari JC,Hassan HE,Myers AL

更新日期：2012-03-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:The disposition of azithromycin in the human eye following topical administration has not been fully explored. Population pharmacokinetic (PopPK) modeling can allow useful conclusions to be drawn based on limited tear sampling data. The aim of this study was therefore to develop and evaluate a...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Wu F,Zhao X,Li X,Cui Y

更新日期：2019-06-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Ketoprofen, a potent nonsteroidal anti-inflammatory drug, is clinically administered as a racemic mixture. One of the possible metabolism routes of ketoprofen is the inversion of the R- to S-enantiomer in the gastrointestinal tract. Ketoprofen, as a weak acid drug, might undergo recirculation ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Lorier M,Magallanes L,Ibarra M,Guevara N,Vázquez M,Fagiolino P

更新日期：2016-12-01 00:00:00

abstract：:The development of peptide therapeutics has increased enormously in recent decades. Many of the peptide drugs and antibody fragments that lack Fc backbone have a short half-life in circulation. In general, the half-life supports the design of the dosing regimen and frequency of administration, which are key aspects in...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hijazi Y

更新日期：2021-01-01 00:00:00

abstract：:The aim of the study was to accelerate the dissolution of the sustained release dosage forms using both elevated temperature and high rpm rates. Teokap(®) SR 200 mg pellets were tested by in vitro sustained and accelerated dissolution studies using USP XXIII rotating paddle method. Sustained dissolution studies were c...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Ertan G,Karasulu E,Ozgüney I,Karasulu Y,Apaydın S,Kantarcı G,Yurdasiper A,Ege MA

更新日期：2011-12-01 00:00:00

abstract：:The disposition of the gonadotropin-releasing hormone (GnRH) agonist buserelin was studied in male rats under conditions of long-term administration. Rats were continuously infused with about 30 pmole [3H]-buserelin/24 h subcutaneously by osmotic minipumps for 4-7 days. After killing the rats, the 3H-activity of the t...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Heinrich N,Albrecht E,Sandow J,Kertscher U,Lorenz D,Oehlke J,Berger H

更新日期：1996-10-01 00:00:00

abstract：:The aim of this study was to investigate by HPLC the in vivo metabolism of 2-[1'-phenyl-3'-(3-chlorophenyl)-2'-propenylyden]hydrazino-3-methyl-4(3H)-quinazolinone as a substrate, and as a model compound in rats. The substrate was dissolved in DMSO/water (1:4) and administered intraperitoneally at a dose of 100 mg/kg i...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Kaymakçioğlu BK,Aktan Y,Süzen S,Gökhan N,Koyunoğlu S,Erol K,Yeşilada A,Rollas S

更新日期：2005-10-01 00:00:00

abstract：:Cytochrome P450-dependent enzymes from wheat catalyze the oxidation of endogenous compounds (lauric and oleic acids) and of several herbicides (diclofop, chlortoluron, bentazon). Treatment of wheat seedlings with the safener, naphthalic anhydride and with phenobarbital increases dramatically several P450-dependent enz...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Forthoffer N,Helvig C,Dillon N,Benveniste I,Zimmerlin A,Tardif F,Salaün JP

更新日期：2001-01-01 00:00:00

abstract：:The co-administration of lidocaine and propranolol leads to significant drug-drug interactions. Beta-blockers decrease liver perfusion and inhibit the activity of hepatic microsomal lidocaine metabolizing enzymes of the P450_2D subfamily. Hence, there is a resulting reduction in the hepatic breakdown of lidocaine and ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Tesseromatis C,Kotsiou A,Tsagataki M,Tigka E,Vovou J,Alevizou A,Perisanidis C,Saranteas T,Karakitsos D,Karabinis A,Kostopanagiotou G

更新日期：2007-10-01 00:00:00

abstract：:We studied the hepatic handling of bromosulfophthalein in healthy rabbits with hepatic coccidiosis 28 days after an experimental infection with sporulated oocysts of Eimeria stiedai, an experimental model of liver disease histopathologically resembling primary biliary cirrhosis in man. A pharmacokinetic study of the r...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Esteller A,Torres MD,Gomez-Bautista M,Mariño EL,Fernandez-Lastra C,Jimenez R

更新日期：1990-01-01 00:00:00

abstract：:The purpose of this study was to determine the distribution of cyclosporin A (CsA) in various ocular fluids and tissues in the rabbit by two routes of administration. CsA was administered to two groups of two rabbits either by intramuscular route at a dose of 25 mg/kg/day or by local route using eyedrops, at a dose of...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Vernillet L,Lundh RL,Acezat-Mispelter F,Goizel C,Humbert H,Pouliquen Y

更新日期：1991-01-01 00:00:00

abstract：:The in vivo assessment of percutaneous absorption of molecules is a very important step in the evaluation of any transdermal drug delivery system and a key goal in the design and optimization of transdermal dosage forms lies in understanding the factors that determine a good in vivo performance. The objective of the p...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Swain K,Pattnaik S,Yeasmin N,Mallick S

更新日期：2011-12-01 00:00:00

abstract：:This study investigated the effect of a commercial preparation of stevioside and a synthetic compound, sodium salt of monketocholic acid (MKC), administered per os (p.o.) and also adminstered via an osmotic pump, on glycemia in normoglycemic and diabetic Wistar rats. Diabetes was induced with alloxan, 100 mg/kg, i.p. ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Rasković A,Mikov M,Skrbić R,Jakovljević V,Vasović V,Posa M,Kuhajda K,Kevresan S,Tomic Z,Siladji D

更新日期：2008-01-01 00:00:00

abstract：:The influence of phenobarbital pretreatment on liver concentration of digitoxin and its metabolites was studied in guinea-pigs after i.p. administration of the cardiac glycoside. During the first hour an increase in liver uptake was observed in pretreated animals. The differences detected in the hepatic subcellular di...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Carvalhas ML,Figueira MA,Maya MR

更新日期：1982-01-01 00:00:00

abstract：BACKGROUND:MTBH, a novel hesperetin derivative, possesses in vivo hepatoprotective effects against carbon tetrachloride (CCl4)-induced acute liver injury in Institute of Cancer Research (ICR) mice. OBJECTIVES:This study investigated the pharmacokinetics and tissue distribution of MTBH and its conjugated metabolites in...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Shen C,Qian Z,Chen R,Meng X,Hu T,Chen Z,Li Y,Huang C,Hu C,Li J

更新日期：2016-12-01 00:00:00

abstract：:This study examined the effects of the absorption enhancers, acylcarnitines, on efflux transporting systems, including P-glycoprotein (P-gp) and other efflux transporters, and elucidated the importance of acyl chain length and the concentration of acylcarnitine on the activity of efflux transport. The effects of two a...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Tomita M,Doi N,Hayashi M

更新日期：2010-09-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:UPARANT has emerged as a novel therapeutic agent with the potential to treat ocular diseases as assessed by studies in animal models. Since limited information is available on the pharmacokinetics of UPARANT, the aim of this study is to evaluate its pharmacokinetics after single and multiple a...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Ciccone M,D'Alonzo D,Cangiano AM,De Fenza M,Pavone V,Mancinelli A

更新日期：2021-01-01 00:00:00

abstract：:The technique of differential display reverse transcription-polymerase chain reaction (ddRT-PCR) has been used to produce unique profiles of up-regulated and down-regulated gene expression in the liver of male Wistar rats following short term exposure to the non-genotoxic hepatocarcinogens, phenobarbital and WY-14,643...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Rockett JC,Esdaile DJ,Gibson GG

更新日期：1997-10-01 00:00:00

abstract：:The effects of aluminium, manganese, ferrous and ferric iron, cobalt, nickel, copper, zinc, cadmium, barium, mercury and lead ions on the rat hepatic UDPglucuronosyltransferase activity with regard to 4-methylumbelliferone, 4-nitrophenol, bilirubin, and 2-aminophenol were investigated in vitro. Conjugation of bilirubi...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Aitio A,Ahotupa M,Parkki MG

更新日期：1980-01-01 00:00:00

abstract：:Carboxylesterases (CESs) play major roles in catalyzing the hydrolysis of a wide range of ester- and amide-containing compounds. CESs dominate both the biotransformation of numerous therapeutic drugs and the detoxification of environmental toxicants, and the activity alteration of CESs may be a determinant reason for ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Xu Y,Zhang C,He W,Liu D

更新日期：2016-08-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:The antitumor activity and toxicity of doxorubicin are potentiated and attenuated by calcitriol, respectively. Potentially, calcitriol can be combined with doxorubicin for clinical benefit in chemotherapy. To gain insight into the interaction between doxorubicin and calcitriol, proposed for com...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Durna Corum D,Uney K

更新日期：2020-10-01 00:00:00

abstract：:Blood loss during cesarean section was calculated based on post-operative decrement of hemoglobin (Hb) and hematocrit (Hct) level. The model used for pregnant women was previously validated for non-pregnant women who underwent gynecological surgery. 1,068 pregnant women who underwent cesarean section and 517 women who...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Milosevic N,Popovic J,Grujic Z,Rapaic M

更新日期：2011-09-01 00:00:00

abstract：:alpha-D-glucose is a weak inhibitor (Ki = 1.7 mM) of glycogen phosphorylase (GP) and acts as physiological regulator of hepatic glycogen metabolism; it binds to GP at the catalytic site and stabilizes the inactive T state of the enzyme promoting the action of protein phosphatase 1 and stimulating glycogen synthase. Th...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Oikonomakos NG,Kontou M,Zographos SE,Tsitoura HS,Johnson LN,Watson KA,Mitchell EP,Fleet GW,Son JC,Bichard CJ

更新日期：1994-07-01 00:00:00

abstract：:A major biotransformation pathway for many NSAIDs from the group of optically active 2-arylpropionic acids is the conjugation with D-glucuronic acid, forming diastereomers. These conjugates of the S-(+)-and the R-(-)-enantiomers can be separated directly, e.g., by ion-pair chromatography on a C18-column using a mixtur...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Spahn H,Iwakawa S,Bevet LZ,Lin ET

更新日期：1987-10-01 00:00:00

abstract：:Parenteral phenytoin solution (Dilantin) was given rectally three times a day for three days to two beagle dogs. This was well tolerated, with no evidence of mucosal irritation noted either on endoscopic nor on rectal mucosal biopsy. When given in this manner, phenytoin is absorbed to a limited degree in canines. Pare...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Fuerst RH,Graves NM,Kriel RL,Olson R

更新日期：1988-10-01 00:00:00