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 carried out for 12 h in phosphate buffer at 37 ± 0.5°C and 50 rpm. Accelerated dissolution studies were performed for 48 min in distilled water at 90 ± 1°C and 250 rpm. The results obtained from accelerated and sustained dissolution studies were correlated using both linear and linear kinetic correlation methods by a computer program. While r (2) and maximum error between calculated and observed drug release rates were found to be 0.9129 and 15.9%, respectively, in linear correlation method, these values were observed as 0.9938 and 3.6%, respectively, in linear kinetic correlation method. In vivo plasma concentration data were obtained from six New Zealand rabbits after administration of a single dose of Teokap(®) SR 200 mg pellet. Then, the results of in vivo study were evaluated with in vitro accelerated and sustained dissolution results by applying them to in vitro-in vivo linear correlations. As a result of these correlations, it was shown that the in vitro correlation plots were very similar to the plot which was obtained by the in vivo study (f (2) = 73.81-77.11). This study suggested a way to prevent the loss of time for routine dissolution studies of sustained release preparations for quality control procedures using in vitro accelerated dissolution tests. The storage and quarantine periods of the product in process and process controls in the manufactories could be shortened by this method. Calculation of the in vivo performance of sustained release dosage forms using the results of the accelerated dissolution studies may be counted as another advantage of the method.
journal_name
Eur J Drug Metab Pharmacokinetjournal_title
European journal of drug metabolism and pharmacokineticsauthors
Ertan G,Karasulu E,Ozgüney I,Karasulu Y,Apaydın S,Kantarcı G,Yurdasiper A,Ege MAdoi
10.1007/s13318-011-0049-6subject
Has Abstractpub_date
2011-12-01 00:00:00pages
243-8issue
4eissn
0378-7966issn
2107-0180journal_volume
36pub_type
杂志文章abstract::Hydroxylated metabolites of diazepam can be conjugated and are therefore generally thought not to affect the metabolism of diazepam. Liver microsomes, obtained from phenobarbital-pretreated rats, showed an inhibition of diazepam (10(-5) M) metabolism by desmethyldiazepam as well as by N-methyloxazepam or oxazepam (5 X...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03189692
更新日期:1985-01-01 00:00:00
abstract::A new high performance liquid chromatographic procedure has been developed for the simultaneous quantification of piribedil (PD) and its three main basic metabolites in rat plasma and urine, without and after hydrolysis. The procedure relies on isolation of the compounds from plasma and urine constituents using the Se...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190147
更新日期:1992-07-01 00:00:00
abstract::Intermittent inhalation exposure of adult male rats to dichloromethane, trichloroethylene, 1,1,1-trichloroethane, perchloroethylene or to a combination of trichloroethylene and 1,1,1-trichloroethane for 5 days, for 6 h daily, induced significantly different accumulations of solvent molecules in the body. Adipose tissu...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章,评审
doi:10.1007/BF03189473
更新日期:1981-01-01 00:00:00
abstract::The cardioselective beta-adrenergic blocking drug Visacor (ICI 141,292) was dosed to six beagle dogs in a randomized cross-over manner. Five formulations were examined i.e. a 15 mg/kg intravenous solution, a 50 mg/kg oral solution, and 50, 100 and 200 mg/kg oral powder formulations. Whole blood and urine samples were ...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03189616
更新日期:1984-04-01 00:00:00
abstract::The biotransformation of 1-(3-butoxy-2-carbamoyloxypropyl)-5-ethyl-5-phenyl-(1H,3H,5H)-pyrimidine-2,4,6-trione (febarbamate) has been investigated in man. Human volunteers received a single oral dose of 15 mg/kg febarbamate. Twenty two metabolites found in urine were separated and purified by means of an extraction wi...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03188760
更新日期:1983-07-01 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
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/s13318-018-0522-6
更新日期:2019-06-01 00:00:00
abstract::This study describes an approach permitting the determination of compartmental concentration and drug kinetics in the case of chronobiological variations of elimination rate. ...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190035
更新日期:1999-10-01 00:00:00
abstract::It is known that substituted hydrazide hydrazone derivatives have several biological and pharmacological activities; there is limited literature on the metabolism of hydrazide hydrazones in rats. In our previous study, 4-fluorobenzoic acid [(5-nitro-2-furanyl)methylene]hydrazide (S) was found active against Staphyloco...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190075
更新日期:2000-04-01 00:00:00
abstract::A short review on some pharmacokinetic parameters (mean residence time, sojourn time, transit time) is given in relation to compartmental models and some examples and application are discussed. In particular the use of the sojourn time is suggested because this parameter can give useful informations when comparing the...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:
更新日期:1991-01-01 00:00:00
abstract::The pharmacokinetics of nefazodone (NEF) and two of its pharmacologically active metabolites viz hydroxynefazodone (HO-NEF) and m-chlorophenylpiperazine (mCPP) were determined following single oral administration of 100, 200 and 400 mg NEF to 6 beagle dogs in a three-way crossover study. Blood samples were collected f...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190163
更新日期:1992-10-01 00:00:00
abstract::The metabolic fate of the anti-Parkinsonian drug budipine was studied in rats after oral administration. The presence of an aromatic hydroxylation product, metabolite M1, and its O-sulphate conjugate was confirmed. Three new minor metabolites, budipine N-oxide, metabolite M1 N-oxide and a secondary metabolite derived ...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03189947
更新日期:1991-04-01 00:00:00
abstract::We studied the pharmacokinetics of moguisteine, a racemic non-narcotic peripheral antitussive drug, in 12 healthy male subjects after a single oral administration of 200 mg. The unchanged drug was absent in plasma and urine of all subjects. Moguisteine was immediately and completely hydrolyzed to its main active metab...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190242
更新日期:1995-10-01 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
pub_type: 杂志文章
doi:10.1007/s13318-020-00632-6
更新日期:2020-10-01 00:00:00
abstract::Glutathione S-transferases (GSTs) play an important role in the biotransformation of endogenous compounds and xenobiotics as well as in the metabolic inactivation of pharmacologically active substances, including anticancer drugs. Using cisplatin as the prototype drug, we investigated if any correlation exists between...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/s13318-014-0176-y
更新日期:2015-03-01 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
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/s13318-015-0313-2
更新日期:2016-12-01 00:00:00
abstract::Hepatic clearance of 3H-gitoxin was studied in the rabbit using an isolated perfused liver technique with an emulsion of a perfluorocarbon. The liposoluble material in the perfusion medium was extracted with dichloromethane, and gitoxin was assayed in the extract by high performance liquid chromatography. Pharmacokine...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03189704
更新日期:1985-04-01 00:00:00
abstract::UDP-glucuronosyltransferase 1A9 (UGT1A9) contributes to the glucuronidation of numerous drugs. Cynomolgus monkeys are regarded as experimental animals similar to humans in studies on safety evaluation and biotransformation for drug development. In this study, the similarities and differences in the enzymatic propertie...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/s13318-014-0177-x
更新日期:2014-09-01 00:00:00
abstract::Danirixin (GSK1325756) is a small, high-affinity, selective and reversible CXCR2 antagonist in development for treatment of chronic obstructive pulmonary disease. The objective of the study was to evaluate the relative bioavailability, including the inter-subject variability, of a conventional immediate-release (IR) f...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章,随机对照试验
doi:10.1007/s13318-014-0179-8
更新日期:2014-09-01 00:00:00
abstract::Fucithalmic is a newly developed 1% microcrystalline suspension of the antistaphylococcal antibiotic fusidic acid. Penetration into the eye was investigated in twenty patients about to undergo cataract extraction. A single dose produced median antibiotic levels in the aqueous humour of 0.3 mcg/ml, maintained for at le...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03189761
更新日期:1985-10-01 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
pub_type: 杂志文章
doi:10.1007/BF03189640
更新日期:1984-07-01 00:00:00
abstract::Fluvastatin (FV), a new cholesterol-lowering agent, has been studied for its effects on hepatic microsomal drug-metabolizing enzymes in male rats. FV was orally administered in dosages of 1, 5, and 30 mg/kg/day for 7 consecutive days. 3-Hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase activities were markedly decrease...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03189669
更新日期:1995-07-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Maximum plasma concentration of biopharmaceuticals sometimes occurs long after completion of intravenous infusion. The objective of this research was to study the hypothetical adsorption of biopharmaceuticals to endothelium and infusion material, which may theoretically explain this phenomenon...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/s13318-017-0430-1
更新日期:2018-02-01 00:00:00
abstract::The aim of the present study was to investigate the relative bioavailability and bioequivalence of a new tablet formulation of metformin hydrochloride with reference to a standard product in healthy Chinese adult male volunteers. Two randomized, comparative, two-way crossover studies were therefore conducted. In study...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章,随机对照试验
doi:10.1007/BF03190986
更新日期:2007-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Previous studies reported that tapentadol-sulfate represented one of the major metabolites of tapentadol excreted in urine. The current study aimed to identify the human cytosolic sulfotransferases (SULTs) that is(are) capable of sulfating tapentadol and to examine whether human cells and huma...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/s13318-016-0392-8
更新日期:2017-10-01 00:00:00
abstract::The detection and the isolation in phenobarbital-induced rat liver microsomal incubation systems of a new metabolite of benzo(a)pyrene are described. The structure of this metabolite and the way in which it is formed are described. ...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03189442
更新日期:1980-01-01 00:00:00
abstract::The inhibitory effects of 17 flavones and flavonols on ethoxy- and pentoxy-resorufin dealkylases of rat liver were investigated. Several findings concerning the relationship between structure and activity can be pointed out. The presence or lack of hydroxyl groups on the flavane nucleus has no influence on the efficie...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190104
更新日期:1989-07-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Drug-drug interactions (DDIs) can occur when one drug alters the metabolism of another drug. Drug metabolism mediated by cytochrome P450 enzymes (CYPs) is responsible for the majority of metabolism of known drugs and inhibition of CYP enzymes is a well-known cause of DDIs. In the current study...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/s13318-018-0485-7
更新日期:2018-12-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Even though lithium has been used for the treatment of bipolar disorder for several decades, its toxicities are still being reported. The major limitation in the use of lithium is its narrow therapeutic window. Several methods have been proposed to predict lithium doses essential to attain the...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章,评审
doi:10.1007/s13318-017-0421-2
更新日期:2018-02-01 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
pub_type: 杂志文章
doi:10.1007/BF03190121
更新日期:1990-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Methyl 3,4-dihydroxybenzoate (MDHB) has the potential to prevent neurodegenerative diseases (NDDs). The present work aims to reveal the pharmacokinetics and tissue distribution characteristics of MDHB. METHODS:The pharmacokinetics and tissue distribution of MDHB were analyzed using LC-MS/MS a...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/s13318-018-0512-8
更新日期:2019-04-01 00:00:00