Abstract：
:A new enteric-coated formulation of sodium ursodeoxycholate was prepared and administered to man. The barrier film disintegrates and releases the drug only at pH > or = 5.5. The sodium salt of glycoursodeoxycholate was also prepared and encapsulated like ursodeoxycholate. Serum levels of ursodeoxycholate and glycoursodeoxycholate were measured by specific enzyme immunoassay after oral administration of their sodium salts in an enteric-coated formulation at equimolar doses of 475 and 540 mg. The same subjects also received in separate experiments ursodeoxycholic acid, sodium ursodeoxycholate, and glycoursodeoxycholic acid in gelatin capsules. The mean area under the curve (mumol/L.hr) following administration of enteric-coated sodium ursodeoxycholate (45 +/- 8) was significantly higher than that of either ursodeoxycholic acid (26 +/- 5; P < 0.01) or sodium ursodeoxycholate (25 +/- 6; P < 0.001) administered in a conventional gelatin capsule. No differences were found when glycoursodeoxycholic acid was administered as an enteric-coated sodium salt or in acid form in gelatin capsules. Ursodeoxycholic was administered at a dose of 10 mumol/min/kg over 1 hr to bile fistula rats both intraduodenally (i.d.) and intravenously (i.v.). The experiment included administration of the sodium salt in solution and the acid as a suspension. A similar experiment was performed with glycoursodeoxycholic acid. The ratio of the amount recovered from bile in the i.d. to that in the i.v. experiment is almost 1 for the sodium salt of ursodeoxycholate in solution, while it drops to 0.55 for ursodeoxycholic acid. No differences were found between i.v. and i.d. administration when glycoursodeoxycholic acid was administered in acid form and as a soluble sodium salt.(ABSTRACT TRUNCATED AT 250 WORDS)
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Roda A,Roda E,Marchi E,Simoni P,Cerrè C,Pistillo A,Polimeni Cdoi
10.1023/a:1018907825281subject
Has Abstractpub_date
1994-05-01 00:00:00pages
642-7issue
5eissn
0724-8741issn
1573-904Xjournal_volume
11pub_type
杂志文章abstract：PURPOSE:To develop a new intradermal antigen delivery system by coating microneedle arrays with lipid bilayer-coated, antigen-loaded mesoporous silica nanoparticles (LB-MSN-OVA). METHODS:Synthesis of MSNs with 10-nm pores was performed and the nanoparticles were loaded with the model antigen ovalbumin (OVA), and coate...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2177-4
更新日期：2017-08-01 00:00:00
abstract：:The role of phosphatidylserine in the cellular and subcellular lung distribution of quinidine was investigated in rats, since quinidine was found to bind preferentially to phosphatidylserine. The concentration of phosphatidylserine in the cellular and subcellular fractions was determined after separation by two-dimens...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015985511653
更新日期：1988-04-01 00:00:00
abstract：PURPOSE:To characterize factor(s) contained in apical medium of primary cultured rat alveolar epithelial type II cell-like monolayers (RAECM-II) that enhance insulin absorption across alveolar epithelial cells. MATERIALS AND METHODS:Primary rat alveolar epithelial cell monolayers cultured on Transwells in the presence...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9301-9
更新日期：2007-09-01 00:00:00
abstract：:Lecithin-stabilized triglyceride emulsions are subject to hydrolysis by pancreatic lipase. The time profiles of these reactions are characterized by a lag-phase and a zero-order phase. Lag phases are more pronounced with long-chain triglycerides. Ca2+ is effective in reducing the lag-phase and activating lipase. Kinet...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015956104500
更新日期：1989-06-01 00:00:00
abstract：:Intraocular enzymes convert the ketoxime analogues of some beta-adrenergic blockers via a sequential bioactivation process involving hydrolysis to the corresponding ketones followed by reduction to the aryloxyaminoalcohols, which then exert known and predictable physiological and pharmacological effects only at the si...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015863521513
更新日期：1990-07-01 00:00:00
abstract：PURPOSE:Gastroduodenal and intestinal permeability were compared after single doses of sustained release and regular release flurbiprofen in the rat to assess possible site-specific formulation-dependent toxicity. METHODS:Pharmacokinetics was assessed and gastrointestinal permeability was evaluated using sucrose and 5...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012134503107
更新日期：1997-11-01 00:00:00
abstract：:During the past two decades the nanomedicine field has experienced significant progress. To date, over sixty nanoparticle (NP) formulations have been approved in the US and EU while many others are in clinical or preclinical development, indicating a concerted effort to translate promising bench research to commercial...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-019-2736-y
更新日期：2019-12-11 00:00:00
abstract：PURPOSE:To determine the different conformations of the acyloxyalkoxy-linked cyclic prodrug 1 of the model hexapeptide 2 in solution and to investigate the relationship between these solution conformations and the cellular permeability characteristics of this prodrug. METHODS:Two-dimensional Homonuclear Hartmann-Hahn ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016484522113
更新日期：1996-11-01 00:00:00
abstract：PURPOSE:4-Phenylbutyrate (4-PBA) is expected to be a potential therapeutic for several neurodegenerative diseases. These activities require 4-PBA transport into the brain across the blood-brain barrier (BBB). The objective of the present study was to characterize the brain transport mechanism of 4-PBA through the BBB. ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1912-6
更新日期：2016-07-01 00:00:00
abstract：PURPOSE:To evaluate the potential of ascorbate as a novel ligand in the preparation of pharmaceutical nanocarriers with enhanced tumor-cell specific binding and cytotoxicity. METHODS:Palmitoyl ascorbate was incorporated into liposomes at varying concentrations. A stable formulation was selected based on size and zeta ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9674-4
更新日期：2008-11-01 00:00:00
abstract：PURPOSE:Some therapeutic peptides exhibit amyloidogenic properties that cause insolubility and cytotoxicity against neuronal cells in vitro. Here, we characterize the conformational change in monomeric therapeutic peptide to its fibrillar aggregate in order to prevent amyloidogenic formation during clinical application...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000033016.36825.2c
更新日期：2004-07-01 00:00:00
abstract：PURPOSE:The in vitro inhibitory effect of Docetaxel (DTX) and Everolimus (EVR) alone and together in poly(ethylene glycol)-block-poly(D,L-lactic acid) (PEG-b-PLA) nanocarriers on angiogenic processes and acute toxicity in mice was evaluated. METHODS:PEG-b-PLA DTX and/or EVR nanocarriers were characterized for size, dr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1188-z
更新日期：2014-03-01 00:00:00
abstract：:One thousand milligrams of aspirin, as its lysine salt was administered intravenously, orally, and intramuscularly to nine male and nine female young healthy adult volunteers. After intravenous injection mean (+/- SD) values of clearance, steady-state volume of distribution, and terminal half-life were 12.2 +/- 2.2 ml...
journal_title：Pharmaceutical research
pub_type： 临床试验,杂志文章
doi：10.1023/a:1015978104017
更新日期：1989-08-01 00:00:00
abstract：PURPOSE:To develop an isolated perfused rat liver (IPRL) model with low baseline levels of tumor necrosis factor (TNF)-alpha in the outlet perfusate to study the effects of immunostimulants and immunosuppressants on the release of TNF-alpha from this organ. METHODS:Isolated rat livers were perfused with a buffer conta...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1013603331899
更新日期：2002-01-01 00:00:00
abstract：:An on-line simultaneous assay for the enantiomers of verapamil (VA) and its three metabolites in plasma was developed with column-switching HPLC. This system consists of an ovomucoid protein chiral stationary phase coupled to an achiral reversed-phase column via a dilution tube and a trapping column. The reversed-phas...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015848806240
更新日期：1991-08-01 00:00:00
abstract：PURPOSE:The study was performed for clarifying the mechanism of interaction between indoxyl sulfate (IS), a typical uremic toxin bound to site II, and site I-ligands when bound to human serum albumin (HSA). The effect of the N to B transition on the interactions was also examined. METHODS:Quantitative investigation of...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011014629551
更新日期：2001-04-01 00:00:00
abstract：:Intranasal route continues to be one of the main focuses of drug delivery research. Although it is generally perceived that the nasal route could avoid the first-pass metabolism in liver and gastrointestinal tract, the role of metabolic conversions in systemic and brain-targeted deliveries of the parent compounds and ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0127-5
更新日期：2010-07-01 00:00:00
abstract：:Although much effort has been devoted to opioid research since the identification of enkephalins, understanding of the physiological importance and mechanisms of action of endogenous opioids lags behind understanding of opiate alkaloids such as morphine. In recent years, several novel approaches have been refined with...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1023/a:1015809702296
更新日期：1991-01-01 00:00:00
abstract：PURPOSE:Drug transfer into milk is a general concern during lactation. Because data are limited in human subjects, particularly for new drugs, experimental animal models of lactational drug transfer are critical. This study analyzed drug transfer into milk in a mouse model, as well as the contribution of similar and di...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1085-5
更新日期：2013-09-01 00:00:00
abstract：PURPOSE:To characterize the distribution of water among various components in a powder blend using solid-state NMR spectroscopy. METHODS:Water sorption behavior of theophylline anhydrate and excipients was determined by dynamic vapor sorption (DVS) and Karl Fischer Titration (KFT) after storing them in humidity chambe...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1972-7
更新日期：2016-10-01 00:00:00
abstract：PURPOSE:An in vitro dynamic pharmacokinetic (PK) cell culture system was developed to more precisely simulate physiologic nanoparticle/drug exposure. METHODS:A dynamic PK cell culture system was developed to more closely reflect physiologic nanoparticle/drug concentrations that are changing with time. Macrophages were...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2576-9
更新日期：2019-02-01 00:00:00
abstract：:The release of lithium carbonate incorporated into polymethylmethacrylate, polyvinyl chloride, hydrogenated vegetable oil, and carbomer matrix tablets was studied in vitro. The formulation containing 10% carbomer showed a sustained-release profile comparable to that of a standard, commercially available, sustained-rel...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015863204732
更新日期：1990-04-01 00:00:00
abstract：PURPOSE:To assess the effects of selective lipid extraction and tape stripping on transepidermal water loss (TEWL) at three body regions in the pig. METHODS:Lipids were extracted from the abdominal, inguinal. and back regions using three different solvent extraction procedures or cellophane tape stripping (15x) on Yor...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1010944529387
更新日期：2001-07-01 00:00:00
abstract：PURPOSE:1. The assessment of the role of hair follicles and sweat glands in skin resistance and percutaneous iontophoretic flux of 9-desglycinamide, 8-arginine vasopressin (DGAVP) by comparing two skin species: human stratum corneum which contained hair follicles, sweat and sebaceous glands, and shed snake skin which l...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016243706415
更新日期：1995-10-01 00:00:00
abstract：PURPOSE:To evaluate the transcellular mechanism of novel enhancers absorption enhancement of human growth hormone (hGH), by examining the involvement of a P-glycoprotein-like efflux system, changes in membrane fluidity, and membrane damage. METHODS:Caco-2 cell monolayers were grown on Snapwell filter supports and plac...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1014809916407
更新日期：1999-08-01 00:00:00
abstract：PURPOSE:To evaluate the potential of several bis-ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA, adefovir) to enhance the oral absorption of PMEA. METHODS:Caco-2 monolayers were used to estimate intestinal transport and metabolism of the bis(pivaloyloxymethyl)-ester [bis(POM)-] and a s...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011914618109
更新日期：1998-02-01 00:00:00
abstract：PURPOSE:The intratumoral heterogeneity observed in breast cancer (BC), in particular with regard to cell surface receptor expression, can hinder the success of many targeted cancer therapies. The development of novel therapeutic agents that target more than one receptor can overcome this inherent property of tumors and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2684-6
更新日期：2020-01-21 00:00:00
abstract：:Molecular dynamics simulations and the generation of ad hoc chemical libraries are playing an increasingly important and recognized role in structure-based virtual screening. These approaches are important for treating target flexibility and improving the drug discovery pipeline. In this article I will comment on thes...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1012-9
更新日期：2013-05-01 00:00:00
abstract：:To achieve time-controlled or site-specific drug delivery in the gastrointestinal tract, a sigmoidal release system (SRS) was developed, which achieved a prolonged lag time, followed by rapid release. The theophylline beads with a thick Eudragit RS film coating showed very low drug release in water, whereas the releas...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018910114436
更新日期：1994-01-01 00:00:00
abstract：:Interleukin-1 receptor antagonist (IL-1Ra) is a naturally occurring anti-inflammatory antagonist of interleukin-1 family of pro-inflammatory cytokines. The broad spectrum anti-inflammatory effects of IL-1Ra have been investigated against various auto-immune diseases such as diabetes mellitus, rheumatoid arthritis. Des...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-013-1118-0
更新日期：2013-11-01 00:00:00
