Abstract:
:Alpha- and beta-cyclodextrins and their hydroxypropyl derivatives were converted by the reaction with chlorosulfonic acid in pyridine to the corresponding sulfates. Cyclodextrin sulfates were shown by fast-atom bombardment mass spectrometry (negative ion mode, triethanolamine matrix) to be mixtures with nearly symmetrical distributions of degree of substitution by sulfate groups and by powder X-ray diffraction to be amorphous. Thus, in these aspects, cyclodextrin sulfates are similar to the potent drug solubilizers hydroxypropylcyclodextrins.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Pitha J,Mallis LM,Lamb DJ,Irie T,Uekama Kdoi
10.1023/a:1015854402122subject
Has Abstractpub_date
1991-09-01 00:00:00pages
1151-4issue
9eissn
0724-8741issn
1573-904Xjournal_volume
8pub_type
杂志文章abstract:PURPOSE:To demonstrate that polyanhydride copolymer chemistry affects the uptake and intracellular compartmentalization of nanospheres by THP-1 human monocytic cells. METHODS:Polyanhydride nanospheres were prepared by an anti-solvent nanoprecipitation technique. Morphology and particle diameter were confirmed via scan...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9760-7
更新日期:2009-03-01 00:00:00
abstract:PURPOSE:This study was conducted to demonstrate the use of differential scanning calorimetry (DSC) in detecting and measuring beta-relaxation processes in amorphous pharmaceutical systems. METHODS:DSC was employed to study amorphous samples of poly(vinylpyrrolidone) (PVP), indomethacin (IM), and ursodeoxycholic acid (...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-9044-4
更新日期:2006-02-01 00:00:00
abstract:PURPOSE:Calculation of the ideal solubility of a crystalline solute in a liquid solvent requires knowledge of the difference in the molar heat capacity at constant pressure of the solid and the supercooled liquid forms of the solute, delta Cp. Since this parameter is not usually known, two assumptions have been used to...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012148910975
更新日期:1997-05-01 00:00:00
abstract:PURPOSE:This work describes the synthesis of block co-polymeric micelles, methoxy-poly(ethylene glycol)-poly(D,L-lactide) (mPEG-PLA) to encapsulate Curcumin (CUR), thereby improving the dispersibility and chemical stability of curcumin, prolonging its cellular uptake and enhancing its bioavailability. METHODS:CUR-mPEG...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1830-z
更新日期:2016-04-01 00:00:00
abstract:PURPOSE:The purpose of this study is to show how disaccharides differ in their ability to protect lyophilized β-galactosidase from enzymatic activity loss and secondary structure changes during storage. METHODS:β-galactosidase was lyophilized with trehalose, sucrose, cellobiose or melibiose at 2:1, 20:1 and 40:1 excip...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0300-x
更新日期:2011-03-01 00:00:00
abstract::Celiac disease (CD) is an immune-mediated enteropathy triggered by the ingestion of gluten-containing grains that affects ~1% of the white ethnic population. In the last decades, a rise in prevalence of CD has been observed that cannot be fully explained by improved diagnostics. Genetic predisposition greatly influenc...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0951-x
更新日期:2013-03-01 00:00:00
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::Solution calorimetry has been employed to evaluate the stability constants and enthalpy changes associated with complex formation between alpha-, beta, or gamma-cyclodextrin (CD) and a group of amine compounds having the diphenylmethyl functionality. Data from thermal titrations of the compounds were analyzed using no...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015880218535
更新日期:1991-07-01 00:00:00
abstract:PURPOSE:Carboxylesterases are important in the detoxification of drugs, pesticides and other xenobiotics. This study was to evaluate a series of substrates and inhibitors for characterizing these enzymes. METHODS:A series of novel aliphatic esters and thioesters were used in spectral assays to monitor human, murine an...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016071311190
更新日期:1996-10-01 00:00:00
abstract:PURPOSE:Locoregional recurrence is the most common complication after adenocarcinoma resection in the colon, despite adjuvant chemotherapy. Therapy efficacy could be improved if designed to target malignant cells by incorporating specific recognition factors in the drugs or the drug vehicles. The aim of this study was ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9330-4
更新日期:2008-02-01 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:PURPOSE:The aim was to replace the traditional 21-day Caco-2 permeability protocol by a more high-throughput assay. METHODS:Caco-2 cells were seeded at high density in 96-well plates in novel cell culture boxes. After 7 days, drug permeability studies were performed. Samples were analyzed by a new UV detection method....
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000008043.71001.43
更新日期:2003-12-01 00:00:00
abstract:PURPOSE:To measure the charge to mass (Q/M) ratios of the impactor stage masses (ISM) from commercial Flixotide™ 250 μg Evohaler, containing fluticasone propionate (FP), Serevent™ 25 μg Evohaler, containing salmeterol xinafoate (SX), and a combination Seretide™ 250/25 μg (FP/SX) Evohaler metered dose inhalers (MDIs). M...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2544-9
更新日期:2018-11-26 00:00:00
abstract:PURPOSE:Desmopressin acetate (DDAVP) is used parenterally and intranasally in the control of several diseases. Oral administration of DDAVP, while most desirable, is not practical presently due to low bioavailability. The objective of the present study was to explore the feasibility for employing oil-in-water MucoAdhes...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016023111248
更新日期:1996-07-01 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: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:PURPOSE:The low aqueous solubility of many drugs impedes detailed investigation as the detection limit of standard testing routines is limited. This is further complicated within application relevant thin films typical used in patches or stripes for buccal or topical routes. METHODS:In this work a model system is deve...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1368-5
更新日期:2014-10-01 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 current study aimed to examine the pharmaceutical applications of the focused-ion-beam (FIB) in the inhalation aerosol field, particularly to particle porosity determination (i.e. percentage of particles having a porous interior). MATERIALS AND METHODS:The interior of various spray dried particles (bovine ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9276-6
更新日期:2007-09-01 00:00:00
abstract:PURPOSE:The purpose of this study was to assess the antifungal activity and renal and hepatic toxicity of amphotericin B (AmpB) following administration of Fungizone (FZ) and a heat-treated form of FZ (HFZ) to rats infected with Aspergillus fumigatus. METHODS:Infected rats were administered FZ and HFZ at a dosing regi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000041449.46054.b4
更新日期:2004-09-01 00:00:00
abstract:PURPOSE:The purpose of this study was to obtain an in vitro/in vivo correlation for the sustained release of a protein from poly(ethylene glycol) terephthalate (PEGT)/poly(butylene terephthalate) (PBT) microspheres. METHODS:Radiolabeled lysozyme was encapsulated in PEGT/PBT microspheres via a water-in-oil-in-water emu...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/B:PHAM.0000019303.12086.d1
更新日期:2004-03-01 00:00:00
abstract::The stability of a freeze-dried model protein, ribonuclease A (RNase), was investigated under accelerated storage conditions at 45 degrees C for time periods up to 60 days. Because RNase is a fairly stable molecule around pH 7, lyophilization was performed in phosphate buffers at pH 4.0 or 10.0 to accelerate degradati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015959604616
更新日期:1990-10-01 00:00:00
abstract:PURPOSE:We compared cationic, polyamine-coated microparticles (MPs) and anionic, protein-coated MPs with respect to their phagocytosis and phagosomal fate in dendritic cells (DCs) and macrophages (Mphi). METHODS:Polystyrene MPs were surface modified by covalent coupling with fluorescein isothiocyanate-labeled polyamin...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1022271020390
更新日期:2003-02-01 00:00:00
abstract:PURPOSE:The long-term stability and nasal absorption characteristics of a basic nasal formulation of azetirelin, a thyrotropin-releasing hormone analog and its absorption enhancement by incorporation of acylcarnitines in the formulation were investigated. METHODS:The long-term stability of basic nasal azetirelin formu...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011952804479
更新日期:1998-01-01 00:00:00
abstract:PURPOSE:A series of studies was conducted to evaluate the preclinical pharmacokinetics of SB-239063 (trans-1-(4-hydroxycyclohexyl)-4-(4-fluorophenyl)-5-[(2-methoxy)pyrimidin-4-yl] imidazole), a potent and selective p38 MAP kinase inhibitor. METHODS:SB-239063 was administered both i.v. and p.o. in the rat, dog, cynomol...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1013002414678
更新日期:2001-09-01 00:00:00
abstract:PURPOSE:The aim of this work is to design new chitosan conjugates able to self-organize in aqueous solution in the form of micrometer-size platelets. When mixed with amphotericin B deoxycholate (AmB-DOC), micro-platelets act as a drug booster allowing further improvement in AmB-DOC anti-Candida albicans activity. METH...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2117-3
更新日期:2017-05-01 00:00:00
abstract:PURPOSE:To compare the adjuvanticity of polymeric particles (new-generation adjuvant) and alum (the traditional and FDA-approved adjuvant) for H5N1 influenza split vaccine, and to investigate respective action mode. METHODS:Vaccine formulations were prepared by incubating lyophilized poly(lactic acid) (PLA) microparti...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1224-z
更新日期:2014-04-01 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:PURPOSE:Polyesters with hydrophilic domains, i.e., poly(D,L-lactic-co-glycolic-co-hydroxymethyl glycolic acid) (PLGHMGA) and a multiblock copolymer of poly(ε-caprolactone)-PEG-poly(ε-caprolactone) and poly(L-lactide) ((PC-PEG-PC)-(PL)) are expected to cause less acylation of encapsulated peptides than fully hydrophobic...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1685-3
更新日期:2015-09-01 00:00:00
abstract:PURPOSE:To gain information on the chemical stability pattern and the kinetics of the degradation of recombinant hirudin variant HV1 (rHir), a thrombin-specific inhibitor protein of 65 amino acids, in aqueous solution as a function of pH. METHODS:Stability of rHir was monitored at 50 degrees C in the framework of a cl...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011918108849
更新日期:1998-09-01 00:00:00