Abstract:
PURPOSE:To provide the physicochemical properties of vitrified trehalose for predicting its recrystallization. METHODS:Thin films of vitrified trehalose solutions were prepared at room temperature and exposed to various humid and temperature atmospheres. The in-situ amount of retained water in the vacuum-dried trehalose thin film during exposure was determined using its FTIR spectrum by quantifying the extremely infinitesimal amount of retained water in the trehalose solution. Recrystallization of the sample was also assessed by the FTIR spectrum of trehalose dihydrate. RESULTS:The effective water absorption coefficient, h meff , exponentially increased to the water activity of the trehalose sample, A w , at 25°C and 40°C at which the increasing rates are comparable. The surface energy of trehalose dihydrate, γ, was found to be lower than the value calculated from the reported equation, neglecting the effects of the activity of the solute and solvent water. CONCLUSIONS:The retained water in trehalose considerably increases its affinity for water vapor, and the change in this affinity with regard to the water activity is nearly independent of temperature. The dihydrate nucleation rate of trehalose-water system is maximal when trehalose weight ratio is ~0.8 at 25°C and is slightly higher (~0.85) at 40°C.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Shirakashi R,Takano Kdoi
10.1007/s11095-018-2420-7subject
Has Abstractpub_date
2018-05-10 00:00:00pages
139issue
7eissn
0724-8741issn
1573-904Xpii
10.1007/s11095-018-2420-7journal_volume
35pub_type
杂志文章abstract:PURPOSE:To identify the key formulation factors controlling the initial drug and polymer dissolution rates from an amorphous solid dispersion (ASD). METHODS:Ketoconazole (KTZ) ASDs using PVP, PVP-VA, HMPC, or HPMC-AS as polymeric matrix were prepared. For each drug-polymer system, two types of formulations with the sa...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-1969-2
更新日期:2016-10-01 00:00:00
abstract::Magnetic nanoparticles are useful as contrast agents for magnetic resonance imaging (MRI). Paramagnetic contrast agents have been used for a long time, but more recently superparamagnetic iron oxide nanoparticles (SPIOs) have been discovered to influence MRI contrast as well. In contrast to paramagnetic contrast agent...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-012-0711-y
更新日期:2012-05-01 00:00:00
abstract:PURPOSE:To point out the importance of heterogeneity in drug distribution processes and develop a noncompartmental approach for the description of the distribution of drug in the body. METHODS:A dichotomous branching network of vessels for the arterial tree connected to a similar venous network was used to describe th...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016031129053
更新日期:1996-05-01 00:00:00
abstract::The relative effectiveness of two beta-cyclodextrin derivatives, i.e., dimethyl-beta-cyclodextrin (DM beta CD) and hydroxypropyl-beta-cyclodextrin (HP beta CD), in enhancing enteral absorption of insulin was evaluated in the lower jejunal/upper ileal segments of the rat by means of an in situ closed loop method. The i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018997101542
更新日期:1994-08-01 00:00:00
abstract::One of the barriers to transdermal delivery of peptides is the metabolic activity of the epidermis. To define this metabolic activity, aminopeptidase activity and Leu-enkephalin metabolism were measured in the epidermis obtained from neonatal mouse skin and in cultured mouse keratinocytes. Aminopeptidase activity was ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015882323677
更新日期:1991-01-01 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::Molecular modeling has been used to study the complexation between alpha, beta, or gamma-cyclodextrin (CD) and a group of amine compounds having the diphenylmethyl functionality. The computer program SYBYL 5.3 and the Tripos force field (version 5.2) were used for all the calculations. Three-dimensional structures of ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015816215751
更新日期:1991-10-01 00:00:00
abstract::A simple viscometric method was used to quantify mucin-polymer bioadhesive bond strength. Viscosities of 15% (w/v) porcine gastric mucin dispersions in 0.1 N HCl (pH 1) or 0.1 N acetate buffer (pH 5.5) were measured with a Brookfield viscometer in the absence (eta m) or presence (eta t) of selected neutral, anionic, a...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015812615635
更新日期:1990-05-01 00:00:00
abstract:PURPOSE:A key step of delivering extracellular agents to its intracellular target is to escape from endosomal/lysosomal compartments, while minimizing the release of digestive enzymes that may compromise cellular functions. In this study, we examined the intracellular distribution of both fluorecent cargoes and enzymes...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1619-0
更新日期:2015-07-01 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:PURPOSE:Following extracellular drug clearance, we analyzed the rate of doxorubicin efflux from the nucleus of three human leukemic cells (K562, Molt4 and CCRF-CEM) and related it to their differential sensitivity to this drug, after a short drug pulse. RESULTS:For many pulse-chase regimes, K562 cell viability was lea...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9369-2
更新日期:2007-11-01 00:00:00
abstract:PURPOSE:The purpose of this work was to investigate the mechanisms of cocrystal formation during cogrinding and storage of solid reactants, and to establish the effects of water by cogrinding with hydrated form of reactants and varying RH conditions during storage. METHODS:The hydrogen bonded 1:1 carbamazepine-sacchar...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9110-6
更新日期:2006-10-01 00:00:00
abstract:PURPOSE:To develop resource-sparing in silico approaches that aim to reduce experimental effort and material required by developability assessments (DA) of monoclonal antibody (mAb) drug candidates. METHODS:A battery of standardized biophysical experiments was performed on high concentration formulations of 16 drug pr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2466-6
更新日期:2018-08-20 00:00:00
abstract:PURPOSE:The described structure pharmacokinetic pharmacodynamic relationships (SPPR) study explored the utilization of tetramethylcyclopropane analogues of valpromide (VPD), or tetramethylcyclopropane carboxamide derivatives of valproic acid (VPA) as new antiepileptics. METHODS:The study was carried out by investigati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016055517724
更新日期:1996-02-01 00:00:00
abstract:PURPOSE:Iontophoresis was employed for enhancing the transdermal delivery of acyclovir through nude mouse skin in vitro, with the aim of understanding the mechanisms responsible for drug transport, in order to properly set the conditions of therapeutical application. METHODS:Experiments were done in horizontal diffusi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016284815501
更新日期:1995-11-01 00:00:00
abstract:PURPOSE:To evaluate the potential for the acidic intestinal unstirred water layer (UWL) to induce drug supersaturation and enhance drug absorption from intestinal mixed micelles, via the promotion of fatty acid absorption. METHODS:Using a single-pass rat jejunal perfusion model, the absorptive-flux of cinnarizine and ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1104-6
更新日期:2013-12-01 00:00:00
abstract:PURPOSE:Cationic host defence peptides constitute a promising class of therapeutic drug leads with a wide range of therapeutic applications, including anticancer therapy, immunomodulation, and antimicrobial activity. Although potent and efficacious, systemic toxicity and low chemical stability have hampered their comme...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1658-6
更新日期:2015-08-01 00:00:00
abstract:PURPOSE:HSP90 (Heat shock protein 90kD) has been validated as a therapeutic target in Castrate Resistant Prostate Cancer. Unfortunately, HSP90 inhibitors suffer from dose-limiting toxicities that hinder their clinical applications. Previously developed polymeric delivery systems for HSP90 inhibitors had either low drug...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2249-5
更新日期:2017-12-01 00:00:00
abstract:PURPOSE:The aim of this study was to investigate the specific changes in body distribution of camptothecin (CA) through incorporation into solid lipid nanoparticles (SLN) by peroral route. METHODS:Camptothecin loaded solid lipid nanoparticles (CA-SLN) coated with poloxamer 188 were produced by high pressure homogeniza...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018888927852
更新日期:1999-05-01 00:00:00
abstract::Animal models are used commonly in various stages of drug discovery and development to aid in the prospective assessment of drug-drug interaction (DDI) potential and the understanding of the underlying mechanism for DDI of a drug candidate. In vivo assessments in an appropriate animal model can be very valuable, when ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-010-0157-z
更新日期:2010-09-01 00:00:00
abstract:PURPOSE:The type and relative importance of saturated and unsaturated phospholipid components of surfactant within the epithelial lining fluid (ELF) of the inner and outer surfaces of the lung is not known. METHODS:Seven healthy dogs were anesthetized and a bronchoalveolar lavage (BAL) was performed, immediately follo...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-7677-y
更新日期:2005-11-01 00:00:00
abstract::The pentahydrate (alpha form) of cefazolin sodium (CEZ) exhibited sharp X-ray diffraction peaks, while the dehydrated alpha form showed weak but distinct diffraction peaks. As expected the amorphous form exhibited a diffuse and halo diffraction pattern. The X-ray procedure to estimate the degree of crystallinity of CE...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015984300692
更新日期:1988-07-01 00:00:00
abstract:PURPOSE:To investigate the effect of atomization conditions on particle size and stability of spray-freeze dried protein. METHODS:Atomization variables were explored for excipient-free (no zinc added) and zinc-complexed bovine serum albumin (BSA). Particle size was measured by laser diffraction light scattering follow...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007570030368
更新日期:2000-11-01 00:00:00
abstract:PURPOSE:To evaluate the reaction of a large series of pharmacologically significant 1,4-dihydropyridine (1,4-DHP) compounds with superoxide (O2.-) in dimethylsulfoxide using differential pulse voltammetry and controlled potential electrolysis. METHODS:Differential pulse voltammetry was used to track the consumption of...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1022291624933
更新日期:2003-02-01 00:00:00
abstract:PURPOSE:To evaluate the effect of re-directing the uptake mechanism of polyplexes containing oligodeoxynucleotide (ODN) decoys to nuclear factor kappa B (NF-kappaB) from absorptive-mediated to receptor-mediated endocytosis. MATERIALS AND METHODS:Complexes of ODNs and a co-polymer of biotin-polyethylenglycol and polyet...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9389-y
更新日期:2008-03-01 00:00:00
abstract:OBJECTIVE:The objective of this work was to determine plasma protein adsorption and macrophage phagocytosis of biodegradable polyanhydride, polylactic acid and polylactic-co-glycolic acid microspheres prepared by both spray-drying and solvent evaporation techniques. METHODS:Microspheres were characterized by scanning ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011935222652
更新日期:1998-02-01 00:00:00
abstract:PURPOSE:To determine whether LHRH-receptor is expressed in Calu-3, a human bronchial epithelial cell line, and to further determine whether this receptor plays a role in the transport of deslorelin, an LHRH agonist. METHODS:Using cultured monolayers of Calu-3 grown at air-interface, the presence and localization of LH...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000029294.70707.74
更新日期:2004-06-01 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: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: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