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 barrier appeared to be localized in the epithelium of the cheek pouch. Addition of an aminopeptidase inhibitor, bestatin, to both diffusion cell reservoirs resulted in decreased hydrolysis of L-LPNA. The experimental results were analyzed with a mathematical model which was developed to describe the simultaneous diffusion and metabolism processes. Using this model it was estimated that the rate of diffusion of L-LPNA across the cheek pouch was less than the capacity of the tissue to hydrolyze L-LPNA.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Garren KW,Topp EM,Repta AJdoi
10.1023/a:1015949614437subject
Has Abstractpub_date
1989-11-01 00:00:00pages
966-70issue
11eissn
0724-8741issn
1573-904Xjournal_volume
6pub_type
杂志文章abstract::A novel method of dipeptide synthesis is described that can be carried out in aqueous solution and does not require complicated protecting and deprotecting procedures. An analgesic neuropeptide named kyotorphin, H-Tyr-Arg-OH, was synthesized from unprotected tyrosine and arginine in a new enzymatic reaction catalyzed ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016479305603
更新日期:1987-04-01 00:00:00
abstract::Seven healthy, male volunteers were entered into a randomized, open crossover study of the gastrointestinal transit of two enteric-coated 500-mg naproxen tablets. Two radiolabeled tablets were given to each volunteer on two occasions separated by 7 days, once in the fasted state and once after breakfast. Radiolabeling...
journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1023/a:1015858829187
更新日期:1992-11-01 00:00:00
abstract:PURPOSE:For passive dry powder inhalers (DPIs) entrainment and emission of the aerosolized drug dose depends strongly on device geometry and the patient's inhalation manoeuvre. We propose a computational method for optimizing the entrainment part of a DPI. The approach assumes that the pulmonary delivery location of ae...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-1992-3
更新日期:2016-11-01 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:PURPOSE:The objective of this work is to understand the sequence specificity of HAV peptides and to improve their selectivity in regulating E-cadherin-E-cadherin interactions in the intercellular junctions. METHODS:Peptide 1 was modified using an alanine scanning method to give peptides 2-6. The ability of these pepti...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011094025008
更新日期:2001-04-01 00:00:00
abstract::The dose dependency of carbamazepine pharmacokinetics was characterized in rats, a common test animal for antiepileptic drug efficacy. With a randomized Latin square schedule, 5, 10, and 20 mg/kg doses of carbamazepine were injected intravenously into six Sprague-Dawley rats followed by the administration of a 5 or 10...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015872901523
更新日期:1990-05-01 00:00:00
abstract::The dermal route is an attractive route for vaccine delivery due to the easy skin accessibility and a dense network of immune cells in the skin. The development of microneedles is crucial to take advantage of the skin immunization and simultaneously to overcome problems related to vaccination by conventional needles (...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-017-2223-2
更新日期:2017-11-01 00:00:00
abstract::Transport studies using intestinal brush-border membrane vesicles isolated from rats and rabbits have failed to demonstrate proton- or Na(+)-dependent carrier-mediated transport of thyrotropin-releasing hormone (TRH), despite a pharmacologically relevant oral bioavailability. To examine the hypothesis that reported le...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018947430018
更新日期:1993-05-01 00:00:00
abstract:PURPOSE:Modulating sialylation of therapeutic glycoproteins may be used to influence their clearance and systemic exposure. We studied the effect of low and high sialylated IL4-10 fusion protein (IL4-10 FP) on in vitro and in vivo bioactivity and evaluated the effect of differential sialylation on pharmacokinetic param...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2744-y
更新日期:2019-12-26 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::Sulfasalazine, 60 mg/kg, was administered orally to groups of rats (n = 4) along with 1, 5, or 10 mg/kg of riboflavin. Plasma and urine were assayed for 5-aminosalicylic acid, acetyl-5-aminosalicylic acid, sulfapyridine, and acetyl-sulfapyridine using an HPLC method. The mean percent of dose recovered as total metabol...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015938706685
更新日期:1989-12-01 00:00:00
abstract:PURPOSE:An integrated ionic mobility-pore model for epidermal iontophoresis is developed from theoretical considerations using both the free volume and pore restriction forms of the model for a range of solute radii (rj) approaching the pore radii (rp) as well as approximation of the pore restriction form for rj/rp < 0...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011907201096
更新日期:1998-10-01 00:00:00
abstract:PURPOSE:Cationic liposomes are expected to be useful as nonviral vectors for gene delivery. Cationic liposomes showed cytotoxicity, and we proposed that the cytotoxicity is through apoptosis. In this study, we examined the effects of liposomal properties, such as liposomal charge, size, membrane fluidity, and PEG coati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1024441702398
更新日期:2003-07-01 00:00:00
abstract:UNLABELLED:PURPOSE; The aim of this study was to investigate asparagine (Asn) deamidation and aspartate (Asp) isomerization and to measure the content of isoaspartate (isoAsp) in recombinant human interleukin-11 (rhIL-11). METHODS:The rhIL-11 control and heat stressed samples were characterized with trypsin and endopr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1019814713428
更新日期:2002-08-01 00:00:00
abstract::Azo polymers based upon 2-hydroxyethyl methacrylate, methyl methacrylate, and methacrylic acid, and containing N,N'-bis [(methacryloyloxyethyl)oxy(carbonylamino)]azobenzene as azo aromatic agent were evaluated in vivo as coating for colon-specific drug delivery. The gastrointestinal absorption of theophylline from cap...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016283027139
更新日期:1995-02-01 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: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::Gallopamil is a calcium-channel antagonist with reported activity in experimental animals three to five times higher than that of verapamil. An automated high-performance liquid chromatographic (HPLC) method with fluorescence detection is described for the simultaneous determination of gallopamil and its metabolite no...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016401405119
更新日期:1987-08-01 00:00:00
abstract:PURPOSE:The gadopentetic acid (Gd-DTPA)-loaded chitosan nanoparticles (Gd-nanoCPs) were prepared for gadolinium neutron-capture therapy (Gd-NCT) and characterized and evaluated as a device for intratumoral (i.t.) injection. METHODS:Gd-nanoCPs were prepared by a novel emulsion-droplet coalescence technique. The effects...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018995124527
更新日期:1999-12-01 00:00:00
abstract:PURPOSE:To elucidate the key parameters affecting solute transport from semi-interpenetrating networks (sIPNs) comprised of poly(ethylene glycol) diacrylate (PEGdA) and gelatin that are partially crosslinked, water-swellable and biodegradable. Effects of material compositions, solute size, solubility, and loading densi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-9923-1
更新日期:2009-09-01 00:00:00
abstract:PURPOSE:Nasal delivery is a favorable route for vaccination against most respiratory infections, as antigen deposited in the nasal turbinate and Waldeyer's ring areas induce mucosal and systemic immune responses. However, little is known about the nasal distribution of the vaccines, specifically for infants. METHODS:A...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02976-9
更新日期:2021-01-15 00:00:00
abstract::The effects of tertiary amine-containing basic drugs on the enzymes located in the mitochondria and the effect of monoamine oxidase inhibitors (MAOIs) on drug accumulation in lung mitochondria have been studied. Various basic drugs inhibited MAO activity but not other mitochondrial marker enzymes. The potency of MAO i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015964623098
更新日期:1989-10-01 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:PURPOSE:To address the problem of precipitation of a poorly soluble drug during dissolution of highly soluble cocrystals by preparing granules intimately mixed with a water-soluble polymer. METHODS:Effectiveness of polymers as precipitation inhibitors during the dissolution of carbamazepine-nicotinamide (CBZ-NCT) cocr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2622-7
更新日期:2019-04-23 00:00:00
abstract::The limitations of traditional gas adsorption models for describing water vapor sorption by amorphous pharmaceutical solids are described and an alternative approach based on polymer solution theories is proposed. The approach is tested by comparing a priori predicted isotherms with literature data for the poly(vinylp...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018901325842
更新日期:1993-09-01 00:00:00
abstract::Using brine shrimp lethality to direct fractionation, extracts of the bark of Annona bullata Rich. (Annonaceae) have yielded 16 alpha-hydroxy-(-)-kauranoic acid as a bioactive plant constituent. This previously known diterpene showed significant (ED50 8.25 x 10(-2) micrograms/ml) and selective cytotoxicity against A-5...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015819422479
更新日期:1990-04-01 00:00:00
abstract:PURPOSE:Evidence suggests that uremic toxins such as hippurate (HA), indoleacetate (IA), indoxyl sulfate (IS), and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF) promote the progression of renal failure by damaging tubular cells via rat organic anion transporter 1 (rOat1) and rOat3 on the basolateral membrane of ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-2486-x
更新日期:2005-04-01 00:00:00
abstract:PURPOSE:Hydrogen/deuterium (H/D) exchange over a range of temperatures suggests a protein structural/mobility transition in the solid state below the system glass transition temperature (Tg). The purpose of this study was to determine whether solid-state protein stability correlates with the difference between storage ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02897-7
更新日期:2020-08-13 00:00:00
abstract:PURPOSE:Interferon beta is commonly used as therapeutic in the first line of therapy for multiple sclerosis. However, depending on the product, it induces an antibody response in up to 60% of patients. This study evaluated the impact of therapy related factors like dose, route of administration and administration frequ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-0992-9
更新日期:2013-06-01 00:00:00
abstract:PURPOSE:We aimed to assess the fate of β-arteether lipid-based drug delivery systems (AE-LBDDS) in terms of resistance to lipolysis and permeation across intestinal cells. METHODS:AE-LBDDS contained Tween 80 or Cremophor EL as surfactants, ethanol, Maisine 35-1 and vegetable oil. The solubilization behavior of AE was ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1094-4
更新日期:2013-10-01 00:00:00