Abstract：
:Coprecipitates of fluorescein and magnesium hydroxide demonstrate delayed absorption relative to fluorescein solutions when administered to the airways of the isolated perfused rat lung (IPRL). Perfusate concentration vs time profiles showed that dissolution and not epithelial permeability was the rate-controlling factor in the airway-to-perfusate transfer process. A simple data deconvolution method was developed to determine the fluorescein release from the microparticulate coprecipitates in the airways. The deconvolution technique is generally applicable and provides values for undissolved solute remaining in the airways as a function of time provided that (a) significant binding and/or metabolism does not occur, (b) absorption from solution is apparent first order, and (c) all solid or dissolved material reaching perfused regions is absorbed within the lifetime of the preparation. Increased release rates of fluorescein occurred from precipitates containing greater starting concentrations of the dye. Dissolution profiles were similar to those that occur for log-normally distributed powders. The analysis of two unusual time profiles implied that the regional distribution of solid and dissolved material, between perfused areas and nonperfused areas, could be nonhomogeneous despite the use of a standardized dosing technique. The studies describe a method of using the IPRL with the potential to screen aerosol formulations for extended dissolution in the respiratory tract.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Niven RW,Byron PRdoi
10.1023/a:1015942013413subject
Has Abstractpub_date
1988-09-01 00:00:00pages
574-9issue
9eissn
0724-8741issn
1573-904Xjournal_volume
5pub_type
杂志文章abstract：:The in situ rat gut technique was used to study the effects of hypothermia on the intestinal absorption of a 1 mg/ml solution of sodium pentobarbital in 0.01 M phosphate buffer (pH 6.0). Male Sprague-Dawley rats weighing between 300 and 370 g were exposed to an atmosphere of helox (helium:oxygen, 80:20) at 0-4 degrees...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016416413780
更新日期：1987-06-01 00:00:00
abstract：PURPOSE:Design of intravaginal rings (IVRs) for delivery of antiretrovirals is often guided by in vitro release under sink conditions, based on the assumption that in vivo release will follow a similar release profile. METHODS:We conducted a dose-ranging study in the female reproductive tract of pigtail macaques using...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2224-1
更新日期：2017-10-01 00:00:00
abstract：PURPOSE:To characterize the pharmacokinetics of simvastatin (SV) and simvastatin acid (SVA), a lactone-acid pair known to undergo reversible metabolism, and to better understand mechanisms underlying pharmacokinetic interactions observed between SV and gemfibrozil. METHODS:Pharmacokinetic studies were conducted after ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-6037-2
更新日期：2005-07-01 00:00:00
abstract：:The transport characteristics of the renin inhibitor ((3S,4S)-4-[N-morpholinoacetyl-(1-naphthyl)-L-alanyl-N-methyl-(4-t hiazolyl)-L- alanyl]amino-3-hydroxy-5-cyclohexyl-1-(4-pyridyl)-1-pentanone; CH3-18) in rat small intestinal brush-border membrane vesicles (BBMV) were examined by a rapid filtration technique. The up...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018900124257
更新日期：1994-10-01 00:00:00
abstract：PURPOSE:To develop novel bioactive-chylomicrons to solve oral delivery obstacles of Berberine chloride and target the lymphatic system. METHODS:Berberine-loaded bioactive-chylomicrons were prepared and underwent full in vitro characterization. Intestinal permeability was appraised via both non-everted gut sac model an...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2307-z
更新日期：2018-01-05 00:00:00
abstract：PURPOSE:To investigate the potential of a novel lipid carrier, comprising beads of alpha-cyclodextrin and soybean oil, for topical drug delivery. Adapalene was chosen as a model drug to explore the ability of the beads to encapsulate and release a highly lipophilic compound. MATERIALS AND METHODS:Adapalene-loaded bead...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9395-0
更新日期：2008-02-01 00:00:00
abstract：:Pharmacokinetic-pharmacodynamic modeling algorithms, in general, rely on hysteresis minimization techniques that assume time-invariant pharmacodynamics (constant biophase concentration-effect relationships). When time-variant pharmacodynamics are observed, a specific model for tolerance or sensitization is required. H...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018940122382
更新日期：1994-12-01 00:00:00
abstract：PURPOSE:To determine by pharmacokinetic (PK) means the role of erythropoietin-receptor (EPO-R) upregulation in fetuses on the elimination of erythropoietin (EPO). MATERIALS AND METHODS:Six fetal sheep were catheterized at a gestational age of 125-127 days and phlebotomized daily for 6 days. Paired tracer PK studies us...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9295-3
更新日期：2007-09-01 00:00:00
abstract：PURPOSE:To determine the mechanism(s) by which effervescence induces penetration enhancement of a broad range of compounds ranging in size, structure, and other physiocochemical properties across rat and rabbit small intestinal epithelium. METHODS:Effervescent induced penetration enhancement was investigated in vitro ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011936901638
更新日期：1998-06-01 00:00:00
abstract：PURPOSE:Cynarin, a potential immunosuppressant that blocks the interaction between the CD28 of T-cell receptor and CD80 of antigen presenting cells, was found in Echinacea purpurea by a new pharmaceutical screening method: After Flowing Through Immobilized Receptor (AFTIR; Dong et al., J Med Chem, 49: 1845-1854, 2006)....
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9754-5
更新日期：2009-02-01 00:00:00
abstract：:Microbial metabolism studies of the antimalarial drug arteether (1) have shown that arteether is metabolized by a number of microorganisms. Large-scale fermentation with Aspergillus niger (ATCC 10549) and Nocardia corallina (ATCC 19070) have resulted in the isolation of four microbial metabolites which have been chara...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015845306124
更新日期：1990-02-01 00:00:00
abstract：PURPOSE:The cell surface adhesion molecule CD44 plays important roles in the initiation and development of atherosclerotic plaques. We aim to develop nanoparticles that can selectively target CD44 for the non-invasive detection of atherosclerotic plaques by magnetic resonance imaging. METHODS:Magnetic glyconanoparticl...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1021-8
更新日期：2014-06-01 00:00:00
abstract：:The stability of an antibiotic formulation (clindamycin phosphate in dextrose), which is stable at room temperature, was assessed by nonisothermal kinetic analysis at elevated temperatures. A preliminary study, conducted to establish apparent rate order, verified the appropriateness of a first-order kinetic model. The...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015840320410
更新日期：1991-05-01 00:00:00
abstract：PURPOSE:To assess the uridine diphosphate (UDP)-glucuronosyltransferase (UGT) isozymes involved in the glucuronidation of niflumic acid in human liver. METHODS:The glucuronidation activity of niflumic acid was determined in liver microsomes and recombinant UGT isozymes by incubation of niflumic acid with UDP-glucuroni...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-0250-5
更新日期：2006-07-01 00:00:00
abstract：PURPOSE:This study was aimed to investigate the effects of a phenolic antioxidant, butylated hydroxyanisole (BHA) and its metabolite, tert-butylhydroquinone (tBHQ) on the induction of HO-1, NQO1 and Nrf2 proteins and their regulatory mechanisms in primary-cultured hepatocytes. METHODS:After exposure of BHA and tBHQ to...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9094-2
更新日期：2006-11-01 00:00:00
abstract：PURPOSE:Prostaglandin E(1) (PGE(1)) is an effective treatment for peripheral vascular diseases. The encapsulation of PGE(1) in nanoparticles for its sustained-release would improve its therapeutic effect and quality of life (QOL) of patients. METHODS:In order to encapsulate PGE(1) in nanoparticles prepared with a poly...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9891-5
更新日期：2009-07-01 00:00:00
abstract：:Porcine pancreatic elastase, a well-characterized serine protease, has been used as a model to assess the effects of excessive humidity on solid-state stability of the lyophilized protein. Elastase lyophilized without excipients retained full activity immediately after freeze-drying but became denatured upon continued...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018979410338
更新日期：1993-10-01 00:00:00
abstract：:Esmolol hydrochloride degrades in aqueous solutions by the hydrolysis of a labile aliphatic carboxyester group. The products are methanol and ASL-8123. The resulting aliphatic carboxylic acid moiety (ASL-8123) has a pK of 4.80, which is within 1 pH unit of the pH of the formulation. ASL-8123 therefore acts as a "secon...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015973425708
更新日期：1988-08-01 00:00:00
abstract：:A new transdermal therapeutic system (TTS) for nitroglycerin is presented that controls release of the active substance by means of desorption and diffusion. The drug release, in the dosage range examined under sink conditions, is independent of electrolytes and pH of the aqueous acceptor medium, but it does depend on...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016361921803
更新日期：1985-01-01 00:00:00
abstract：:Nanobiosensors with high sensitivity and specificity have shown great potential in the detection of diseases. The incorporation of therapeutic agents with nanobiosensors allows the simultaneous diagnosis and therapy of diseases. The delivery of nanobiosensors and therapeutic agents using polymers is a common strategy ...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-016-1944-y
更新日期：2016-10-01 00:00:00
abstract：:The present review discusses drugs and counter ions suitable for ion pair transport (IPT). Ion pairing is shown to effectively increase the lipophilicity and transport rate of polar drugs across lipid membranes. The proposed mechanisms of IPT are discussed in detail. A marked change in drug properties upon ion pair fo...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1023/a:1015963128124
更新日期：1989-09-01 00:00:00
abstract：:The role of a bile salt (sodium taurocholate) and lipolysis products (monoglyceride and fatty acid) in the intestinal absorption of a poorly water-soluble drug, diazepam, was investigated. Absorption rates and bioavailabilities were determined with the in situ rat gut technique of Doluisio et al. and analyzing the dia...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016312827680
更新日期：1985-09-01 00:00:00
abstract：:Human monocytes/macrophages (MO/MAC) were isolated from peripheral blood and cultivated on hydrophobic Teflon membranes. This culture system is suitable for HIV infection of MO/MAC in vitro. After transfer into 24-well plates the mature macrophages (infected or uninfected) were used for measurements of phagocytosis. T...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015852732512
更新日期：1992-04-01 00:00:00
abstract：PURPOSE:To investigate the effect of benzofusion on NO donor properties and related biological activities of the furoxan system. The biological properties considered were the ability to increase the cytosolic levels of cGMP in C6 cells and vasodilation. METHODS:NO donor properties were investigated either in the prese...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018974409622
更新日期：1999-06-01 00:00:00
abstract：:To evaluate the effects of a neutron activation radiolabeling technique on an enteric-coated multiparticulate formulation of erythromycin, test quantities were produced under industrial pilot scale conditions. The pellets contained the stable isotope erbium oxide (Er-170), which was later converted by neutron activati...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015826229323
更新日期：1990-03-01 00:00:00
abstract：:The pharmacokinetics of and biologic response modification by recombinant human interferon-beta ser (rIFN-beta ser) were evaluated in 12 healthy male volunteers. Subjects received a single intravenous (iv) injection of 90 x 10(6) IU of rIFN-beta ser followed by a single or eight consecutive daily 90 x 10(6) IU subcuta...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018902120023
更新日期：1993-04-01 00:00:00
abstract：PURPOSE:The structure-function relationship and mechanism of polycations as gene carriers have attracted considerable research interest in recent years. The present study was to investigate the relationship between polycation chain length and transfection efficiency (RCL-TE), and the corresponding mechanism by O-methyl...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1211-4
更新日期：2014-04-01 00:00:00
abstract：PURPOSE:The stability of lipid emulsions (LE) containing various cosurfactants (oleic acid, cholesterol, Tween 80, or HCO-60) was evaluated using the maximum total interaction energy, Vtmax and the energy barrier for coalescence, W. METHODS:The Vtmax and W were calculated from the zeta potential and the rate of increa...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016205203264
更新日期：1995-09-01 00:00:00
abstract：PURPOSE:The purpose of this study was to investigate the effects of formulation factors including varying wax concentration, drug loading and drug particle size, on drug release characteristics from both pure oil and gel formulations prepared with a combination of derivatized vegetable oil (Labrafil 1944 CS) and glycer...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016209020160
更新日期：1995-06-01 00:00:00
abstract：PURPOSE:Proteasome inhibition induces endoplasmic reticulum (ER) stress and compensatory autophagy to relieve ER stress. Disturbance of intracellular calcium homeostasis can lead to ER stress and alter the autophagy process. It has been suggested that inhibition of the proteasome disrupts intracellular calcium homeosta...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1139-8
更新日期：2013-09-01 00:00:00
