Abstract:
PURPOSE:The purpose of this study was to characterize the amorphous state of ursodeoxycholic acid (UDCA) samples by using isothermal microcalorimetry, X-ray diffraction, infrared (IR) spectroscopy and solid state carbon 13 nuclear magnetic resonance (13C-NMR) spectroscopy, and to demonstrate the application of the thermal methods (microcalorimetry and differential scanning calorimetry (DSC) for studying the amorphous state and clarifying the dissolution mechanism of UDCA. METHODS:Amorphous UDCA was prepared by grinding and rapid cooling of the melts. The heat of solution of UDCA was measured by an isothermal heat-conduction twin microcalorimeter at 25.0 degrees C. Some physicochemical properties of amorphous UDCA were also studied. RESULTS:The intensities of X-ray diffraction peaks of crystalline UDCA decreased with an increase in grinding time. The heat levels of solution of crystalline UDCA and UDCA ground for 1 min were endothermic, and became exothermic with an increase in grinding time. A good correlation was obtained between the heat of solution and the heat of crystallization determined from the peak area in DSC. Although no significant difference was observed in X-ray diffraction patterns of amorphous UDCA prepared by the two methods, significant differences were recognized in DSC, IR and 13C-NMR, and the heat of solution indicated different values among the two samples. The stability of amorphous UDCA samples stored under 74.5% relative humidity at 40 degrees C was found to depend upon the preparation methods. CONCLUSIONS:Different states of amorphous UDCA were obtained depending on the preparation method. The application of thermal methods to evaluate the amorphous state was demonstrated. The mechanism of dissolution of UDCA was discussed from the results of the heat of solution examination.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Yonemochi E,Ueno Y,Ohmae T,Oguchi T,Nakajima S,Yamamoto Kdoi
10.1023/a:1012114825513subject
Has Abstractpub_date
1997-06-01 00:00:00pages
798-803issue
6eissn
0724-8741issn
1573-904Xjournal_volume
14pub_type
杂志文章abstract:PURPOSE:Relatively large (>5 microm) and porous (mass density <0.4 g/cm3) particles present advantages for the delivery of drugs to the lungs, e.g., excellent aerosolization properties. The aim of this study was, first, to formulate such particles with excipients that are either FDA-approved for inhalation or endogenou...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018910200420
更新日期:1999-11-01 00:00:00
abstract:PURPOSE:This study seeks to develop fiber membranes for local sustained delivery of 25-hydroxyvitamin D3 to induce the expression and secretion of LL-37 at or near the surgical site, which provides a novel therapeutic approach to minimize the risk of infections. METHODS:25-hydroxyvitamin D3 loaded poly(L-lactide) (PLA...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1667-5
更新日期:2015-09-01 00:00:00
abstract:PURPOSE:To assess the role of intestinal CYP2D6 in oral first-pass drug clearance by comparing the enzyme content and catalytic activity of a prototype CYP2D6 substrate, metoprolol, between microsomes prepared from human intestinal mucosa and from human livers. METHODS:Microsomes were prepared from a panel of 31 human...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018989211864
更新日期:1999-08-01 00:00:00
abstract:PURPOSE:The purpose of this study was to clarify the localization and function of the ATP-binding cassette transporter G2 (ABCG2; BCRP/MXR/ABCP) in retinal capillary endothelial cells, which form the inner blood-retinal barrier, as an efflux transport system. METHODS:The expression was determined by reverse transcript...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-0067-2
更新日期:2006-06-01 00:00:00
abstract:PURPOSE:Characterization of virosomes, in late stage preclinical development as vaccines for Respiratory Syncytial Virus (RSV), with a membrane-incorporated synthetic monophosphoryl lipid A, 3D-PHAD® adjuvant. METHODS:Virosomes were initially formed by contacting a lipid film containing 3D-PHAD® with viral membranes s...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2453-y
更新日期:2018-07-03 00:00:00
abstract::The intrasubject and intersubject variabilities for CGS 16617, an angiotensin converting enzyme inhibitor, were evaluated in an open-label, repeat single-dose bioavailability trial. Eight healthy male volunteers each received a 20-mg oral dose of CGS 16617 as an aqueous solution on four separate occasions. Components ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015954609527
更新日期:1989-04-01 00:00:00
abstract:PURPOSE:To co-crystallise mannitol and lactose with a view to obtaining crystals with more favourable morphological features than either lactose or mannitol alone, suitable for use as carriers in formulations for dry powder inhalers (DPIs) using simultaneous engineering of lactose-mannitol mixtures. METHODS:Mannitol a...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0743-3
更新日期:2012-08-01 00:00:00
abstract::Growing tumors develop additional new blood vessels to meet the demand for adequate nutrients and oxygen, a process called angiogenesis. Cancer is a highly complex disease promoted by excess angiogenesis; interfering with this process poses for an attractive approach for controlling tumor growth. This hypothesis led t...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-008-9634-z
更新日期:2008-12-01 00:00:00
abstract::Human serum albumin (HSA) was encapsulated in a 50:50 copolymer of DL-lactide/glycolide in the form of microspheres. These microspheres were used as a model formulation to study the feasibility of controlling the release of large proteins over a 20- to 30-day period. We show that HSA can be successfully incorporated i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015948829632
更新日期:1990-11-01 00:00:00
abstract:PURPOSE:Covalent binding between N-acetyl-L-cysteine (NAC) and albumin was evaluated kinetically by conducting in vitro experiments. METHOD:After 14C-NAC was incubated with human or rat serum, the solution was analyzed by anion-exchange HPLC. The albumin-bound 14C-NAC was quantified by measuring the radioactivity in t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1020749211745
更新日期:2002-11-01 00:00:00
abstract::Prinomide tromethamine, a nonsteroidal antiinflammatory drug, was orally administered at doses of 250, 500, and 1000 mg every 12 hr for 28 days to healthy male volunteers. The pharmacokinetic behavior of prinomide and its primary plasma metabolite displayed nonlinear characteristics, while those of free prinomide and ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018916811904
更新日期:1993-01-01 00:00:00
abstract::The relationship between pKa and skin irritation in man is studied for a homologous series of benzoic acid derivatives, which permeate through human skin at comparable rates (15-88 micrograms/cm2/hr). Skin irritation and pKa are correlated for pKa less than or equal to 4. Laser Doppler velocimetric assessment of skin ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015931105660
更新日期:1988-10-01 00:00:00
abstract:PURPOSE:To evaluate 26 marketed oncology drugs for time-dependent inhibition (TDI) of cytochrome P450 (CYP) enzymes. Evaluate TDI-positive drugs for potential to generate reactive intermediates. Assess clinical drug-drug interaction (DDI) risk using static mechanistic models. METHODS:Human liver microsomes and CYP-spe...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0724-6
更新日期:2012-07-01 00:00:00
abstract::Published permeability coefficient (Kp) data for the transport of a large group of compounds through mammalian epidermis were analyzed by a simple model based upon permeant size [molecular volume (MV) or molecular weight (MW)] and octanol/water partition coefficient (Koct). The analysis presented is a facile means to ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015810312465
更新日期:1992-05-01 00:00:00
abstract:PURPOSE:To examine the changes in expression levels of CYP3A4 and efflux transporters in CYP3A4-transfected Caco-2 (colon carcinoma) cells in the presence of the inducers sodium butyrate (NaB) and 12-O-tetradecanoylphorbol-13-acetate (TPA). To characterize the transport of [3H]-digoxin and the metabolism of midazolam i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1010914624111
更新日期:2001-08-01 00:00:00
abstract::Cyclosporine (CsA) is commercially available for oral administration as a solution in olive oil with alcohol and an emulsifier. To improve its variable absorption and low patient acceptability, several oral formulations were prepared and tested in vitro and in vivo in dogs. A tablet formulation prepared by direct comp...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015815614959
更新日期:1991-04-01 00:00:00
abstract:PURPOSE:The aim was to design and thoroughly characterize monodisperse Fe3O4@SiO2-Ag nanoparticles with strong antibacterial properties, which makes them a candidate for targeting bacterial infections. METHODS:The monodisperse Fe3O4 nanoparticles were prepared by oleic acid-stabilized thermal decomposition of Fe(III) ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2680-x
更新日期:2019-08-14 00:00:00
abstract::An oral formulation of controlled-release isosorbide-5-nitrate pellets has been used to investigate the location of pellets in the gastrointestinal (GI) tract and, in parallel, to measure the drug absorption from these locations. Using the method of gamma scintigraphy the transit times and spreading of pellets in the ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016423404636
更新日期:1987-12-01 00:00:00
abstract::The glass transition temperature of an amorphous pharmaceutical solid is a critical physical property which can dramatically influence its chemical stability, physical stability, and viscoelastic properties. Water frequently acts as a potent plasticizer for such materials, and since many amorphous solids spontaneously...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018941810744
更新日期:1994-04-01 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:PURPOSE:N-terminal site-specific mono-PEGylation of recombinant human epidermal growth factor (EGF) was accomplished using polyethyleneglycol (PEG) derivatives (Mw = 2000 and 5000) through a reactive terminal aldehyde group. METHODS:The site-specific PEG conjugation was conducted ata slightly acidic pH condition (pH 5...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1023402123119
更新日期:2003-05-01 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 effect of different concentrations of polyvinyl alcohol 14000 and 72000 (PVA 14 and 72) on the activity of betamethasone and phenylephrine hydrochloride in the rabbit eye was investigated. The polymer of higher molecular weight exerts a more pronounced effect at relatively lower viscosities. Effects on the intraoc...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016398915965
更新日期:1986-08-01 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:PURPOSE:PHBHHx (poly(3-hydroxybutyrate-co-3-hydroxyhexanoate)) is an excellent biomaterial for tissue repair. Here, we aim to develop a PHBHHx-based three-dimensional (3D) scaffold system for sustained delivery of proteins (insulin serves as a model protein). METHODS:The insulin-phospholipid complex (INS-PLC) was prep...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0944-9
更新日期:2013-04-01 00:00:00
abstract::A method is described for the assay of phenobarbital N-glucosylation using UDP-D-[6-3H]glucose. The radioactive phenobarbital N-glucoside conjugates [(5R)-PBG, (5S)-PBG] formed during the incubations were resolved from each other and from uncharacterized radioactive products by semipreparative HPLC. The product ratio ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015889707922
更新日期:1992-05-01 00:00:00
abstract:BACKGROUND:Little is known about the affinity and stability of 99mTc-labeled 2-methoxyisobutylisonitrile (99mTc-MIBI) and tetrofosmin (99mTc-TF) for imaging of multiple drug resistance transporters in cancer. We examined the affinity of 99mTc-labeled compounds for these transporters and their stability. METHODS:99mTc-...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2548-5
更新日期:2018-11-29 00:00:00
abstract::Chemoembolization using microspheres of 100- to 200-microns is a useful way to treat primary and secondary hepatic tumors. In a search for a better embolic material, we described in detail the preparation and characterization of a poly(benzyl l-glutamate) (PBLG) microspheres containing cisplatin (CDDP). We determined ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018979703726
更新日期:1994-12-01 00:00:00
abstract::The area function method for assessing zero-order (ko) drug absorption rates was compared to four other methods under conditions where variation occurs in the plasma concentration data and in the elimination rate constant (kel or k10) for one- or two-compartment models. For deviant kel values of a one-compartment mode...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015843811150
更新日期:1990-01-01 00:00:00
abstract:PURPOSE:Three types of acyl tetragastrin (TG), acetyl-TG (C2-TG), butyryl-TG (C4-TG) and caproyl-TG (C6-TG) were synthesized and their in vitro intestinal permeability characteristics were examined using Caco-2 monolayers. METHODS:The disappearance of acyl-TGs from the apical side of Caco-2 monolayers was estimated by...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011997404306
更新日期:1998-09-01 00:00:00