In vivo predictive release methods for medicated chewing gums.

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：:The hypothesis that higher molecular weight (MW) quaternary ammoniums (QAs) form lipophilic ion-pair complexes with bile salts in the liver, and are subsequently excreted into bile via a canalicular transporter, P-gp, was re-examined in the present study for its validity. The biliary excretion of tributylmethyl ammoni...

journal_title：Biopharmaceutics & drug disposition

authors： Choi MK,Song IS,Kim DD,Chung SJ,Shim CK

更新日期：2007-12-01 00:00:00

abstract：:Twenty-four healthy volunteers, aged 21-59 years, received single 30 mg oral doses of the benzodiazepine hypnotic temazepam. Levels of intact temazepam were determined in multiple plasma samples drawn during 48 h after dosage. Intact temazepam, its direct glucuronide conjugate, and the conjugate of its demethylated (o...

journal_title：Biopharmaceutics & drug disposition

authors： Locniskar A,Greenblatt DJ

更新日期：1990-08-01 00:00:00

abstract：PURPOSE:The sonodynamically induced anti-tumor effect of chlorin-e6 (Ce6) was studied in mice bearing hepatoma-22 solid tumors. METHODS:In order to determine the optimum timing of ultrasound exposure after administration of Ce6, the Ce6 concentrations in plasma, skin, muscle and tumor were estimated by measuring the f...

journal_title：Biopharmaceutics & drug disposition

authors： Shi H,Liu Q,Qin X,Wang P,Wang X

更新日期：2011-09-01 00:00:00

abstract：:The pharmacokinetics and pharmacodynamics of torasemide were evaluated after intravenous administration of the same total dose of torasemide at a dose of 1mg/kg to rabbits with different infusion times, 1 min (treatment I), 30 min (treatment II) and 2 h (treatment III). The loss of water and electrolytes in urine indu...

journal_title：Biopharmaceutics & drug disposition

authors： Kim YC,Lee MG,Ko SH,Kim SH

更新日期：2004-07-01 00:00:00

abstract：:Although nifedipine has been characterized in terms of its general vasodilatory effects, this dihydropyridine must still be regarded as investigational with regard to available pharmacokinetic and pharmacodynamic data. Although limited studies are available, it is clear that the pharmacokinetic and pharmacodynamic dat...

journal_title：Biopharmaceutics & drug disposition

authors： Hamann SR,Piascik MT,McAllister RG Jr

更新日期：1986-01-01 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：:A three-way crossover study in 18 healthy male volunteers was conducted to evaluate the bioequivalence of three different 200 mg anhydrous theophylline immediate-release (IR) capsules. The products had not been rated as therapeutically equivalent by the US Food and Drug Administration (FDA) owing to a lack of bioequiv...

journal_title：Biopharmaceutics & drug disposition

authors： Meyer MC,Jarvi EJ,Straughn AB,Pelsor FR,Williams RL,Shah VP

更新日期：1999-12-01 00:00:00

abstract：:The objective of this study was to investigate the absorption behavior of chikusetsusaponin IVa (CHS-IVa) in the rat intestine using single-pass intestinal perfusion (SPIP) and to classify CHS-IVa into the biopharmaceutics classification system (BCS). The equilibrium solubility of CHS-IVa was determined by the shaker ...

journal_title：Biopharmaceutics & drug disposition

authors： Zhang W,Liu H,Liu C

更新日期：2019-09-01 00:00:00

abstract：:In a double-blind, placebo-controlled, single-dose ascending pharmacokinetics and tolerance study, we evaluated the bispyridinium oxime HI-6 dichloride monohydrate (62.5, 125, 250, and 500 mg), administered intramuscularly with atropine sulphate, 2 mg, in 24 healthy male volunteers. The plasma HI-6 peak concentration ...

journal_title：Biopharmaceutics & drug disposition

authors： Clement JG,Bailey DG,Madill HD,Tran LT,Spence JD

更新日期：1995-07-01 00:00:00

abstract：:The plasma levels and tissue penetration of pefloxacin were studied after prophylactic administration to patients undergoing elective biliary surgery. Pefloxacin was administered as a single dose of 800 mg given intravenously as an infusion 1 h before surgery. Over a period of two years, cultures of bile and stone wer...

journal_title：Biopharmaceutics & drug disposition

authors： Gascón AR,Campo E,Olea E,Hernández RM,Calvo B,Errasti J,Pedraz JL

更新日期：2002-10-01 00:00:00

abstract：:Pharmacokinetics of ragaglitazar (a novel phenoxazine derivative of aryl propanoic acid), a potent insulin sensitizing and lipid-lowering compound was studied in Wistar rats. A single dose of 1, 3 or 10 mg/kg of ragaglitazar was given orally to male rats (n=4 per dose level) to evaluate dose proportionality. In anothe...

journal_title：Biopharmaceutics & drug disposition

authors： Jagannath K,Chaluvadi MR,Mullangi R,Mamidi NV,Srinivas NR

更新日期：2004-10-01 00:00:00

abstract：:Mivacurium, a non-depolarizing neuromuscular blocking agent, consists of three isomers; trans-trans (57%), cis-trans (36%) and cis-cis (7%). The purpose of this study was to characterize the pharmacokinetics and pharmacodynamics of mivacurium after various inputs. Four beagle dogs weighing between 7.95 and 9.89 kg wer...

journal_title：Biopharmaceutics & drug disposition

authors： Lugo SI,Liang Z,Eddington ND

更新日期：1998-11-01 00:00:00

abstract：:Regional pharmacokinetics is the study of the drug concentrations in specific regions of the body. It allows greater insight into the mechanisms of drug disposition than the study of systemic blood concentrations. Experimental methods in regional pharmacokinetics and their applications and limitations are reviewed. Po...

journal_title：Biopharmaceutics & drug disposition

authors： Upton RN,Runciman WB,Mather LE

更新日期：1990-12-01 00:00:00

abstract：:The study sought to investigate the effect of genetic variants of OCT1 (OCT1-P283L and -P341L) and OCT2 (OCT2-T199I, -T201M and -A270S), which were identified in a Korean population, on the transport of lamivudine in vitro and to compare the substrate dependent effects of OCT1 and OCT2 variants with 1-methyl-4-phenylp...

journal_title：Biopharmaceutics & drug disposition

authors： Choi MK,Song IS

更新日期：2012-04-01 00:00:00

abstract：:A relative bioavailability study of conventional tablet of propranolol hydrochloride was conducted in a group of 18 healthy volunteers employing the innovator's product as the reference tablet formation. Based on plasma levels of propranolol for the 24 h following administration of 2 x 40 mg oral propranolol hydrochlo...

journal_title：Biopharmaceutics & drug disposition

authors： Roscoe R,Cooper J,Wilson TW,Joshi NN,Midha KK

更新日期：1982-04-01 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：:Infliximab (IFX) is used as a therapeutic agent for ulcerative colitis (UC) and Crohn's disease (CD). Although the dosage regimen has been established through clinical trial experience, it has yet to be assessed with a pharmacokinetic and pharmacodynamic model. The present study analysed sequential changes of clinical...

journal_title：Biopharmaceutics & drug disposition

authors： Kimura K,Yoshida A,Katagiri F,Takayanagi R,Yamada Y

更新日期：2019-07-01 00:00:00

abstract：:Betahistine, a potent histamine H3 receptor antagonist, is being developed for the treatment of attention deficit hyperactivity disorder (ADHD) that manifests with symptoms such as hyperactivity, impulsivity and inattention. This study describes the pharmacokinetics of betahistine in ADHD subjects at doses higher than...

journal_title：Biopharmaceutics & drug disposition

authors： Moorthy G,Sallee F,Gabbita P,Zemlan F,Sallans L,Desai PB

更新日期：2015-10-01 00:00:00

abstract：:Fexofenadine hydrochloride is a non-sedating antihistamine that is used in the treatment of symptoms associated with seasonal allergic rhinitis and chronic idiopathic urticaria. A pooled analysis of pharmacokinetic data from children 6 months to 12 years of age and adults was conducted to identify the dose(s) in child...

journal_title：Biopharmaceutics & drug disposition

authors： Krishna R,Krishnaswami S,Kittner B,Sankoh AJ,Jensen BK

更新日期：2004-12-01 00:00:00

abstract：:The pharmacokinetics and pharmacodynamics of furosemide were compared after an oral administration or a direct administration of Lasix into the duodenum in humans (40 mg). Furosemide was absorbed quickly after a direct administration of Lasix into the duodenum; the peak plasma concentration of furosemide was reached w...

journal_title：Biopharmaceutics & drug disposition

authors： Lee WI,Yoon WH,Shin WG,Song IS,Lee MG

更新日期：1997-12-01 00:00:00

abstract：:EXP631, 4-(3-thienyl)-alpha, alpha,1-trimethyl-4-piperidine-methanol hemi-fumarate salt (I), is a centrally acting non-opioid analgesic compound with monoamine uptake blocking properties. EXP631 has analgesic effects in several animal models. It is intended to be used for the treatment of moderate to moderately severe...

journal_title：Biopharmaceutics & drug disposition

authors： Wong YN,Burcham DL,Huang SM,Quon CY

更新日期：1993-08-01 00:00:00

abstract：:A major component of physiologically based pharmacokinetic (PBPK) models is the prediction of the rate and extent of absorption of orally dosed drugs for which knowledge of effective passive intestinal permeability (Peff ) is essential. Single-pass intestinal perfusion (SPIP) studies are used to establish effective pe...

journal_title：Biopharmaceutics & drug disposition

authors： Pade D,Jamei M,Rostami-Hodjegan A,Turner DB

更新日期：2017-03-01 00:00:00

abstract：:In a multiple dose cross-over experiment in 12 healthy male adults the bioavailability and sustained release characteristics of new once daily BY912 400 mg theophylline capsules (= B, Byk Gulden Research Laboratories, FRG) were studied using Theo-24 capsules (= T, Searle & Co., USA) as reference. Both products were gi...

journal_title：Biopharmaceutics & drug disposition

authors： Jonkman JH,Steinijans VW,Beier W,van der Boon WJ,Crasmeijer G

更新日期：1989-03-01 00:00:00

abstract：:The effects of age on hepatic microsomal enzyme induction were studied in male CD-1 mice. Six week old and 1 year old animals were treated with either phenobarbital (80 mg kg-1) or saline once daily for 3d. Twenty-four hours after the last treatment, animals were sacrificed and livers were harvested. Hepatic microsoma...

journal_title：Biopharmaceutics & drug disposition

authors： Charpentier KP,von Moltke LL,Poku JW,Harmatz JS,Shader RI,Greenblatt DJ

更新日期：1997-03-01 00:00:00

abstract：:Utilization of nitric oxide (NO) synthase (NOS) inhibitors to probe the role of NO in various central nervous system processes requires use of an inhibitor selective for neuronal NOS, and is facilitated by knowledge of the pharmacokinetics of the inhibitor. The present project was undertaken to elucidate the dispositi...

journal_title：Biopharmaceutics & drug disposition

authors： Bush MA,Pollack GM

更新日期：2000-09-01 00:00:00

abstract：:The usefulness of a limited sampling method (LSM) to determine the bioequivalence of highly variable drugs with long half-lives was investigated. The LSM uses multiple linear regression of observed drug plasma concentrations versus area under the curve (AUC) or C(max) (peak plasma concentration) to obtain a best set o...

journal_title：Biopharmaceutics & drug disposition

authors： Jackson AJ

更新日期：2001-07-01 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：: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：: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