The bioavailability of oral nifedipine formulations: a statistical and simulation approach.

abstract：:Niosomes (non-ionic surfactant vesicles) prepared from C16G2 (a hexadecyl-diglycerol ether), and loaded with doxorubicin, were administered intraperitoneally to male AKR mice at dose levels of 0, 2.5, 5.0, and 10.0 mg kg-1. Free drug was given at 10.0 mg kg-1 by the intraperitoneal route. At a dose level of 10.0 mg kg...

journal_title：Biopharmaceutics & drug disposition

authors： Uchegbu IF,Turton JA,Double JA,Florence AT

更新日期：1994-11-01 00:00:00

abstract：:The purpose of this study was to formulate a drug-in-adhesive (DIA) transdermal patch containing letrozole, a third generation aromatase inhibitor for the treatment of breast cancer, using pressure-sensitive-adhesives (PSAs) and to evaluate the percutaneous penetration and pharmacokinetics of letrozole after transderm...

journal_title：Biopharmaceutics & drug disposition

authors： Li L,Fang L,Xu X,Liu Y,Sun Y,He Z

更新日期：2010-03-01 00:00:00

abstract：:The pharmacokinetics of verapamil, a calcium channel blocker, were studied in male Sprague-Dawley rats following i.v. administration at a dose of 1 mg kg-1. Both arterial and venous blood were collected and the plasma drug concentrations were determined by reversed-phase high-performance liquid chromatography. Verapam...

journal_title：Biopharmaceutics & drug disposition

authors： Manitpisitkul P,Chiou WL

更新日期：1993-10-01 00:00:00

abstract：:The influence of dose volume on drug absorption following oral administration of a highly and a poorly water soluble drug was examined in male Sprague-Dawley rats. A constant mass of each 14C-labeled compound was given via gavage in dose volumes of 1, 5, 10, and 20 mL kg-1. Blood levels, as well as the quantitative ex...

journal_title：Biopharmaceutics & drug disposition

authors： Nickerson DF,Weaver ML,Tse FL

更新日期：1994-07-01 00:00:00

abstract：:Multidrug resistance (MDR) is common in patients and has been linked to transforming growth factor-β1 (TGF-β1) and overexpression of drug efflux transporters P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), although the molecular mechanisms remain largely unknown. This study aimed to investigate the ...

journal_title：Biopharmaceutics & drug disposition

authors： Kong J,Qiu Y,Li Y,Zhang H,Wang W

更新日期：2019-02-01 00:00:00

abstract：AIM:The aim of this study was to build and verify a preliminary physiologically based pharmacokinetic (PBPK) model of Chinese pregnant women. The model was used to predict maternal pharmacokinetics (PK) of 6 predominantly renally cleared drugs. METHOD:Based on SimCYP Caucasian pregnancy population dataset, the prelimi...

journal_title：Biopharmaceutics & drug disposition

authors： Song L,Yu Z,Xu Y,Li X,Liu X,Liu D,Zhou T

更新日期：2020-06-01 00:00:00

abstract：:Circadian variations in disposition have been observed for a variety of agents, including anticonvulsants. Valproic acid (VPA), an anticonvulsant used to control generalized and partial seizures, has exhibited diurnal oscillations in steady-state concentrations during long-term administration to humans and non-human p...

journal_title：Biopharmaceutics & drug disposition

authors： Arens TL,Pollack GM

更新日期：2001-09-01 00:00:00

abstract：:The objective of this study was to assess the effect of dietary fibers on the transport of losartan, an angiotensin II type 1 receptor blocker, in small intestinal cells. Using Caco-2 cells in vitro, losartan uptake and transport were evaluated in the presence of various fibers (cellulose, chitosan, sodium alginate an...

journal_title：Biopharmaceutics & drug disposition

authors： Iwazaki A,Takahashi N,Miyake R,Hiroshima Y,Abe M,Yasui A,Imai K

更新日期：2016-05-01 00:00:00

abstract：:The first day test dose versus steady-state relationship for predicting drug doses was evaluated for the situation where metabolites are produced. An organ clearance model incorporated into a digital computer program simulated drug and metabolite disposition. When the terminal elimination rate for metabolite was simil...

journal_title：Biopharmaceutics & drug disposition

authors： Devane CL,Jusko WJ

更新日期：1983-01-01 00:00:00

abstract：:Macelignan is a natural phenolic compound that possesses many types of health benefits such as antiinflammation. This study aimed to characterize the metabolism of macelignan via the glucuronidation pathway and to identify the main UGT enzymes involved in macelignan glucuronidation. The rates of glucuronidation were d...

journal_title：Biopharmaceutics & drug disposition

authors： Liu H,Wu Z,Ma Z,Wu B

更新日期：2014-12-01 00:00:00

abstract：:Drugs that are largely restricted to the gastro-intestinal tract (GIT) for their therapeutic efficacy and that are not substantially absorbed into the body are usually inadequately studied in terms of systemic bioavailability. The possibility of systemic effects requires that bioavailabilities be studied to ensure aga...

journal_title：Biopharmaceutics & drug disposition

authors： Fasanmade AA,Akanni AO,Olaniyi AA,Fasanmade AA,Tayo F

更新日期：1994-08-01 00:00:00

abstract：:The objective of this study was to assess the effect of food on the pharmacokinetics of nefazodone (NEF). A group of 24 healthy adult male volunteers received a single 200 mg dose of NEF under fasting conditions as well as 5 min after a high-fat breakfast. There was a 1 week washout between treatments. Serial blood sa...

journal_title：Biopharmaceutics & drug disposition

authors： Dockens RC,Greene DS,Barbhaiya RH

更新日期：1996-03-01 00:00:00

abstract：:After in vitro incubation of cecal content from CVL or gnotobiotic rats with rhein anthraquinone (1 mg g-1) for 18 h at 37 degrees, the anthraquinone was converted to rhein anthrone for 23.5 (SD +/- 3.4) per cent and 19.4 (+/- 4.7) per cent, respectively. Liquid cultures of some strictly anaerobic fecal bacteria of ma...

journal_title：Biopharmaceutics & drug disposition

authors： de Witte P,Van Hoestenberghe A,Eyssen H

更新日期：1992-05-01 00:00:00

abstract：:The pharmacokinetics of methylprednisolone and methylprednisolone phosphate were investigated after intravenous administration of methylprednisolone phosphate to six healthy subjects at seven different doses between 16 and 1000 mg. Plasma, urine, and saliva were analyzed for methylprednisolone and methylprednisolone p...

journal_title：Biopharmaceutics & drug disposition

authors： Möllmann H,Rohdewald P,Barth J,Verho M,Derendorf H

更新日期：1989-09-01 00:00:00

abstract：:The present study aimed to investigate the effect of atorvastatin on the intravenous and oral pharmacokinetics of verapamil in rats. The pharmacokinetic parameters of verapamil were measured after an oral (9 mg/kg) or intravenous (3 mg/kg) administration of verapamil to rats in the presence and absence of atorvastatin...

journal_title：Biopharmaceutics & drug disposition

authors： Choi DH,Chang KS,Hong SP,Choi JS,Han HK

更新日期：2008-01-01 00:00:00

abstract：:The biotransformation of thionorphine (N-cyclopropylmethyl-7alpha-[(s)-1-hydroxy-1-methyl-3-(2thiophene)-propyl]-6,14-endo-ethano tetrahydrooripavine), a new analgesic, was in-vestigated in rats. The results of metabolite analysis by liquid chromatography/electrospray ionization tandem mass spectrometry with positive ...

journal_title：Biopharmaceutics & drug disposition

authors： Wei SX,Zhang ZQ,Wang XY,Guo JF

更新日期：2004-04-01 00:00:00

abstract：:Vitamin K antagonists (VKAs) remain the oral anticoagulant of choice in venous thromboembolic disease. These drugs are characterized by a large inter-individual variability requiring frequent dose tailoring. Genetic polymorphisms for cytochrome CYP2C9 and VKORC1 explain some of the variability, especially in warfarin ...

journal_title：Biopharmaceutics & drug disposition

authors： Espana B,Couturier S,Prouillac C

更新日期：2017-01-01 00:00:00

abstract：PURPOSE:The chromone derivative MBL-II-141, specifically designed to inhibit ABCG2, was previously demonstrated to combine strong inhibition potency, low toxicity and good efficiency in reversing resistance to irinotecan in a xenografted mouse model. Here, the pharmacokinetic interactions in mice between irinotecan, it...

journal_title：Biopharmaceutics & drug disposition

authors： Hénin E,Honorat M,Guitton J,Di Pietro A,Payen L,Tod M

更新日期：2017-07-01 00:00:00

abstract：:The effect of water deprivation on the physiologic, biochemical, and disposition parameters of erythromycin was investigated in rabbits. The packed cell volume, plasma glucose, and total lipid concentration increased significantly in dehydration. The pharmacokinetic parameters of erythromycin after intravenous adminis...

journal_title：Biopharmaceutics & drug disposition

authors： Ahmad M,Niazi SK,Ahmad T,Muzaffar NA,Nawaz M

更新日期：1992-03-01 00:00:00

abstract：:Raltegravir is a human immunodeficiency virus (HIV)-1 integrase strand transfer inhibitor currently marketed at a dose of 400 mg twice-daily (b.i.d.). Raltegravir 1200 mg once-daily (q.d.) (investigational q.d. formulation of 2 × 600 mg tablets; q.d. RAL) was found to be generally well tolerated and non-inferior to th...

journal_title：Biopharmaceutics & drug disposition

authors： Krishna R,East L,Larson P,Valiathan C,Deschamps K,Luk JA,Bethel-Brown C,Manthos H,Brejda J,Gartner M

更新日期：2016-12-01 00:00:00

abstract：:In this comparative bioavailability study in 12 healthy volunteers the blood level profiles of both propranolol and bendrofluazide were studied following the multiple oral administration of the drugs as a fixed combination (Inderetic) and as a free combination at doses of 80 mg propranolol twice daily and 2.5 mg bendr...

journal_title：Biopharmaceutics & drug disposition

authors： McAinsh J,Holmes BF,Baber NS,Young J

更新日期：1981-04-01 00:00:00

abstract：:Sildenafil is the first oral therapeutic agent for the management of male erectile dysfunction. Its oral bioavailability is only 40% due to extensive presystemic elimination, mainly by CYP3A4. This study examined the effect of coadministration of ciprofloxacin or clarithromycin, which inhibit CYP3A4, on the bioavailab...

journal_title：Biopharmaceutics & drug disposition

authors： Hedaya MA,El-Afify DR,El-Maghraby GM

更新日期：2006-03-01 00:00:00

abstract：:This study was conducted to determine the relative bioavailability of Dilacor XR capsules compared to Cardizem CD capsules at both low (180 mg d-1) and high (540 mg d-1) dose levels. Trough and serial plasma samples were obtained and pharmacokinetic parameters were calculated from the steady state concentration-time p...

journal_title：Biopharmaceutics & drug disposition

authors： Lippert CL,Arumugham T,Bhargava VO,Eller M,Weir SJ

更新日期：1996-01-01 00:00:00

abstract：:The pharmacokinetics and the dose proportionality of a new anticonvulsant compound, HEPP (D,L-3-hydroxy-3-ethyl-3-phenylpropionamide) was studied in healthy male volunteers as part of the pharmacological evaluation for new drugs. Study was performed administering doses of 250, 375, 500 and 625 mg of HEPP to six male v...

journal_title：Biopharmaceutics & drug disposition

authors： González-Esquivel DF,Rubio-Donnadieu F,Carvajal-Sandoval G,Jung HC

更新日期：1998-12-01 00:00:00

abstract：:The pharmacokinetics of mexiletine and its metabolite hydroxy-methyl-mexiletine have been investigated following single-dose and during multiple-dose administration of a sustained-release form of mexiletine to six post-myocardial infarct patients. Comparison of single-dose and washout pharmacokinetics, after short-ter...

journal_title：Biopharmaceutics & drug disposition

authors： Bruno R,Santoni Y,Iliadis A,Djiane P,Serradimigni A,Cano JP

更新日期：1992-10-01 00:00:00

abstract：:The study examined the effect of doxorubicin (DOX) on the hepatic expression of CYP2C and its activity for metabolizing tolbutamide (TB), a specific CYP2C substrate, in rats and whether the pharmacokinetics of tolbutamide were altered by doxorubicin exposure. The expression level of hepatic CYP2C11 was depressed 1 day...

journal_title：Biopharmaceutics & drug disposition

authors： Fukuno S,Nagai K,Yamamoto K,Tanimura T,Nabe T,Konishi H

更新日期：2019-07-01 00:00:00

abstract：:In the search for orally available drugs, the prediction of human pharmacokinetics (PK) is essential for successfully selecting compounds that will be clinically useful. This report describes the selection of TAK-272 (SCO-272), a novel orally active renin inhibitor, as a clinical candidate via the detailed investigati...

journal_title：Biopharmaceutics & drug disposition

authors： Ebihara T,Nishihara M,Takahashi J,Jinno F,Tagawa Y

更新日期：2018-03-01 00:00:00

abstract：:The inhibition of rat hepatic mitochondrial aldehyde dehydrogenase (ALDH) isozymes was studied in apparent steady-state conditions after repeated intra-peritoneal cyanamide administration. The low-Km mitochondrial ALDH isozyme was more susceptible to cyanamide-induced inhibition (DI50 = 0.104 mg kg-1) than the high-Km...

journal_title：Biopharmaceutics & drug disposition

authors： Pruñonosa Piera J,Obach R,Sagristá ML,Bozal J

更新日期：1993-07-01 00:00:00

abstract：:The inhibition potencies of aripiprazole and its active metabolite, dehydroaripiprazole, on the activities of human multidrug resistance protein 1 (MDR1/ABCB1; P-glycoprotein), breast cancer resistance protein (BCRP/ABCG2) and multidrug resistance-associated protein 4 (MRP4/ABCC4), that are drug efflux transporters ex...

journal_title：Biopharmaceutics & drug disposition

authors： Nagasaka Y,Oda K,Iwatsubo T,Kawamura A,Usui T

更新日期：2012-09-01 00:00:00

abstract：:This review offers a detailed discussion of the interaction between pharmaceutical compounds and vehicles using the affinity capillary electrophoresis and the microemulsion electrokinetic chromatography. Partition coefficients of drugs were calculated between a micelle and an aqueous phases from the measurement of the...

journal_title：Biopharmaceutics & drug disposition

authors： Reinhard N,Mrestani Y

更新日期：2001-10-01 00:00:00