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 activation into the short-lived gamma ray-emitting radionuclide, erbium-171. In vitro studies indicated that the dissolution profile, acid resistance, and enteric-coated surface of the pellets were minimally affected by the irradiation procedure. Antimicrobial potency was also unaffected, as determined by microbiological assay. Neutron activation thus appears to simplify the radiolabeling of complex pharmaceutical dosage forms for in vivo study by external gamma scintigraphy.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Parr AF,Digenis GA,Sandefer EP,Ghebre-Sellassie I,Iyer U,Nesbitt RU,Scheinthal BMdoi
10.1023/a:1015826229323subject
Has Abstractpub_date
1990-03-01 00:00:00pages
264-9issue
3eissn
0724-8741issn
1573-904Xjournal_volume
7pub_type
杂志文章abstract:PURPOSE:To study the use of poly (lactide-co-glycolide) (PLGA) microparticles in respirable sizes as carriers for recombinant tuberculosis (TB) antigen, TB10.4-Ag85B, with the ultimate goal of pulmonary delivery as vaccine for the prevention of TB. MATERIALS AND METHODS:Recombinant TB antigens were purified from E. co...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-0028-7
更新日期:2010-02-01 00:00:00
abstract::Defined size fractions of polyethyleneglycol powder (MW = 10,000) were mixed with defined size fractions of alpha-lactose monohydrate in order to study the effect of compaction as a function of the weight ratios of the two excipients. For a precise control of the compression cycle, tablets were compressed on a Univers...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015864415693
更新日期:1990-02-01 00:00:00
abstract:PURPOSE:To examine whether the glass transition temperature (Tg) of freeze-dried formulations containing polymer excipients can be accurately predicted by molecular dynamics simulation using software currently available on the market. Molecular dynamics simulations were carried out for isomaltodecaose, a fragment of de...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1023831102203
更新日期:2003-06-01 00:00:00
abstract:PURPOSE:The purpose of the present study was to investigate the transport of organic monocarboxylic acids mediated by the anion exchanger AE2, which has been already reported to be present at several tissue cell membranes, including intestinal brush border membrane in rabbit. METHODS:Membrane transport of organic mono...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011920213991
更新日期:1998-03-01 00:00:00
abstract:PURPOSE:Using monolayers of human pancreatic adenocarcinoma cells (Panc-1) that express multidrug resistance-associated protein (MRP), the present work investigates the effects of Pluronic block copolymers on the functional activity of MRP. METHODS:The studies examined the accumulation and efflux of the MRP selective ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018873702411
更新日期:1999-03-01 00:00:00
abstract:PURPOSE:This prospective study aimed to evaluate the effects of genetic polymorphisms in sulindac-related metabolizing enzyme genes including FMO3 and AOX1 on the population pharmacokinetics of sulindac in 58 pregnant women with preterm labor. METHODS:Plasma samples were collected at 1.5, 4, and 10 h after first oral ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-2765-6
更新日期:2020-01-28 00:00:00
abstract:PURPOSE:We recently developed prostaglandin E(1) (PGE(1))-encapsulated nanoparticles, prepared with a poly(lactide) homopolymer (PLA, Mw = 17,500) and monomethoxy poly(ethyleneglycol)-PLA block copolymer (PEG-PLA) (NP-L20). In this study, we tested whether the accelerated blood clearance (ABC) phenomenon is observed wi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-9943-x
更新日期:2009-10-01 00:00:00
abstract:PURPOSE:Orally absorbable anticancer medications have great advantages for conventional cancer therapies to patients. Here we evaluated the potent anticancer effect of orally absorbable LHD, a chemical conjugate of low-molecular-weight heparin and deoxycholic acid, on tumor graft growth models. METHODS:We characterize...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-9989-9
更新日期:2009-12-01 00:00:00
abstract::The simultaneous diffusion and metabolism of the D- and L-isomers of the aminopeptidase substrate, leucine-p-nitroanilide (LPNA), were examined in vitro in the hamster cheek pouch. L-LPNA was completely hydrolyzed during diffusion across the cheek pouch, whereas D-LPNA crossed the cheek pouch intact. The metabolic bar...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015949614437
更新日期:1989-11-01 00:00:00
abstract:PURPOSE:To develop a dose dependent version of BCS and identify a critical dose after which the amount absorbed is independent from the dose. METHODS:We utilized a mathematical model of drug absorption in order to produce simulations of the fraction of dose absorbed (F) and the amount absorbed as function of the dose ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0815-4
更新日期:2012-11-01 00:00:00
abstract:PURPOSE:To explain thermal stability enhancement of an organic compound, sucralose, with cyclodextrin based metal organic frameworks. METHODS:Micron and nanometer sized basic CD-MOFs were successfully synthesized by a modified vapor diffusion method and further neutralized with glacial acetic acid. Sucralose was loade...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2059-1
更新日期:2017-02-01 00:00:00
abstract:PURPOSE:Manufacturing processes for polypeptide/protein drugs are designed to ensure robust quality, efficacy and safety. Process differences introduced by follow-on manufacturers may result in changes in quality and clinical outcomes. This study investigated the impact of production methods on the stability and impuri...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02817-9
更新日期:2020-06-08 00:00:00
abstract:PURPOSE:The purpose of this human intestinal perfusion study was to investigate the transport and metabolism of R/S-verapamil in the human jejunum (in vivo). METHODS:A regional single-pass perfusion of the jejunum was performed using a Loc-I-Gut perfusion tube in 12 healthy volunteers. Each perfusion lasted for 200 mi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011916329863
更新日期:1998-06-01 00:00:00
abstract::A series of multilamellar liposome dispersions was prepared from lipids of soy phosphatidylcholine or hydrogenated soy phosphatidylcholine containing from 0 to 30 mol% of either cholesterol, stearylamine, or dipalmitoyl phosphatidylglycerol. The liposome dispersions were aerosolized with a Collison nebulizer for 80 mi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015924124180
更新日期:1990-11-01 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::Micelle-associated epoetin is still a possible explanation for the upsurge of pure red blood cell aplasia associated with subcutaneous use of epoetin alpha in patients with chronic renal failure. ...
journal_title:Pharmaceutical research
pub_type: 评论,信件
doi:10.1007/s11095-006-9573-5
更新日期:2006-03-01 00:00:00
abstract:PURPOSE:We investigated optimum formulation characteristics in the nasal absorption of salmon calcitonin (sCT) by incorporation of acylcarnitines. METHODS:Nasal sCT formulations were administered to anesthetized rats. Plasma calcium level was measured and pharmacological bioavailability (P.bioav) was calculated. RESU...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016051600828
更新日期:1996-05-01 00:00:00
abstract::The transepithelial transport of arginine vasopressin (AVP) across cultured rat alveolar epithelial cell monolayers was studied. At 0.1 nM donor [125I]AVP, the radiolabel flux measured in the apical-to-basolateral (AB) direction was about 10 times greater than that in the reverse (BA) direction. HPLC analyses of the b...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018918022865
更新日期:1994-11-01 00:00:00
abstract:PURPOSE:This study was conducted to investigate the cause of incomplete protein release from photopolymerized poly(ethylene glycol) (PEG) hydrogels and verify the protein-protection mechanism provided by iminodiacetic acid (IDA). METHODS:The in vitro release of bovine serum albumin (BSA) from PEG hydrogels prepared un...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-9395-x
更新日期:2006-03-01 00:00:00
abstract:PURPOSE:Under different charging conditions, particles can be either attracted or repulsed by each other, causing powder agglomeration or segregation. Such behavior can be detrimental in many processes aimed at achieving particulate mixture homogeneity. Consequently, the effects of electrostatic charges on mixing kinet...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9934-0
更新日期:2006-05-01 00:00:00
abstract::Various diesters of 9-[(1,3-dihydroxy-2-propoxy)-methyl]guanine (DHPG) were screened in order to identify a derivative with improved oral absorption. The solubilities and dissolution rates decreased with increasing chain length and branching of the ester group. However, the dipropionate ester showed an anomalously fas...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016462801968
更新日期:1987-04-01 00:00:00
abstract::A sensitive radioreceptor assay (RRA) to determine the serum concentrations of fentanyl, pentazocine and morphine was developed on the basis of the drug's competition with a labeled tracer ((3)H-naloxone) for the membrane bound opioid receptor in rat brain homogenates. The binding data were computer-fitted to a standa...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016369229440
更新日期:1984-09-01 00:00:00
abstract:PURPOSE:To develop a liposomal system with high drug loading (DL) for intravenous (i.v.) delivery of a poorly water-soluble basic drug, asulacrine (ASL). METHODS:A thin-film hydration and extrusion method was used to fabricate the PEGylated liposomal membranes followed by a freeze and thaw process. A novel active drug...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1551-8
更新日期:2015-04-01 00:00:00
abstract::This paper describes an investigation of the use of poly(lactic/glycolic acid) polymers for long-term delivery of high molecular weight, water-soluble proteins. Poly(lactic/glycolic acid) (PLGA) microspheres, containing (fluorescein isothiocyanate)-labeled bovine serum albumin and (fluorescein isothiocyanate)-labeled ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015841715384
更新日期:1991-06-01 00:00:00
abstract::We describe a simplified and rapid liquid chromatographic determination of antipyrine clearance (CLAP) calculated from peak height ratios of drug/internal standard. Saliva or plasma was collected 24 hr after the oral administration of 1 g of antipyrine to the subject. A 25-microliter aliquot of the sample is deprotein...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015816825920
更新日期:1991-02-01 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
abstract::Polymeric biomaterials have extensively been used in medicinal applications. However, factors that determine their biocompatibility are still not very clear. This article reviews various effects of the chemical structure and the surface properties of polymeric biomaterials on their biocompatibility, including protein ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/b:pham.0000036909.41843.18
更新日期:2004-08-01 00:00:00
abstract:PURPOSE:The encapsulation of pancreatic β-cells in biocompatible matrix has generated great interest in diabetes treatment. Our work has shown improved microcapsules when incorporating the bile acid ursodeoxycholic acid (UDCA), in terms of morphology and cell viability although cell survival remained low. Thus, the stu...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-1863-y
更新日期:2016-05-01 00:00:00
abstract:OBJECTIVES:We recently demonstrated that fibrin-based tissue engineered blood vessels (TEV) exhibited vascular reactivity, matrix remodeling and sufficient strength for implantation into the veins of an ovine animal model, where they remained patent for 15 weeks. Here we present an approach to improve the mechanical pr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9499-6
更新日期:2008-05-01 00:00:00
abstract:PURPOSE:β-Hydroxy-β-methylbutyrate (HMB), a nutritional supplement, elicits anabolic activity in muscle. Here we investigated the mechanism of HMB uptake in muscle cells. METHODS:Murine muscle cells (C2C12) and human mammary epithelial cells (MCF7) were used for uptake. As HMB is a monocarboxylate, focus was on monoca...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2626-3
更新日期:2019-04-17 00:00:00