Abstract：
:The secondary structure content of microparticulate insulin powders produced by the supercritical antisolvent (SAS) precipitation technique was investigated via Raman spectroscopy. Precipitate samples were generated at 25 and 35 degrees C processing temperatures. Both precipitate samples gave amide I band spectra that were shifted roughly +10 cm-1 relative to the commercial powder. The corresponding secondary structure estimates had significantly increased beta-sheet contents with concomitant decreases in alpha-helix contents relative to the commercial protein; the sum of beta-turn and random coil content remained essentially unchanged. The magnitude of the perturbation was slightly greater for the 35 degrees C sample. Dissolution of the commercial powder and precipitates in 0.01 M HCl yielded solution structure estimates similar to that of the commercial powder. An analysis of insulin in dimethyl sulfoxide, the suspending solvent in the SAS process, indicated that some, but not all, of the structural change observed for the precipitate samples may be attributed to solvent exposure. These results are suggestive of extensive beta-sheet-mediated intermolecular interactions in precipitate states, consistent with analyses of irreversible protein aggregate/fibril states. Interestingly, unlike irreversible protein aggregates, the insulin powders recover essentially full biological activity on reconstitution.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Yeo SD,Debendetti PG,Patro SY,Przybycien TMdoi
10.1002/jps.2600831203subject
Has Abstractpub_date
1994-12-01 00:00:00pages
1651-6issue
12eissn
0022-3549issn
1520-6017pii
S0022-3549(15)49671-6journal_volume
83pub_type
杂志文章abstract：:The degradation kinetics and mechanism of a potent new cephalosporin, cefotaxime sodium, in aqueous solution were investigated at pH 0-10 at 25 degrees and an ionic strength of 0.5. The degradation rates were determined by high-pressure liquid chromatography and were observed to follow pseudo first-order kinetics with...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600720114
更新日期：1983-01-01 00:00:00
abstract：:Near-infrared spectroscopy was used to monitor the phase conversion for two solvatomorphs of caffeine, an anhydrous form and a nonstoichiometric hydrate, as a function of time, temperature, and relative humidity. The transformation kinetics between these caffeine forms was determined to increase with temperature. The ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20941
更新日期：2007-05-01 00:00:00
abstract：:Within the last decade, Quality by Design (QbD) has been getting increased attention in its implementation in the development of pharmaceutical drug products. Understanding of the impact of formulation composition and process on clinical performance is a centerpiece of QbD. Physiologically based pharmacokinetic modeli...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2016.11.022
更新日期：2017-04-01 00:00:00
abstract：:A semi-automated protein binding assay using equilibrium dialysis (ED) and a novel mixed-matrix methodology has been developed. This method decreases mass spectrometer run time and reduces the likelihood of experimental artifacts. In this cassette-based approach, a single matrix is prepared following dialysis by mixin...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22188
更新日期：2010-12-01 00:00:00
abstract：:The affinity chromatographic technique was used to study the interaction of bovine serum albumin and salicylic acid at 3.3 +/- 1.1 degrees. Beaded agarose gel, on which the albumin was immobilized by covalent linkage, was packed in a column as an affinity adsorbent. Frontal analysis was performed on this column to eva...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670737
更新日期：1978-07-01 00:00:00
abstract：:A comprehensive model is developed to describe the swelling/dissolution behaviors and drug release from hydrophilic matrices. The major thrust of this model is to employ an important physical property of the polymer, the polymer disentanglement concentration, rho p,dis, the polymer concentration below which polymer ch...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600841214
更新日期：1995-12-01 00:00:00
abstract：:The purpose of this investigation was to determine the effect of body temperature on the pharmacodynamics (convulsant activity) of pentylenetetrazol (PTZ). Rats received an iv infusion of PTZ until the onset of maximal seizures, at which time samples of cerebrospinal fluid (CSF), brain, and blood (for serum) were obta...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600801005
更新日期：1991-10-01 00:00:00
abstract：:The kinetics and pathways for degradation of (+/-)-4'-ethyl-2-methyl-3-(1-pyrrolidinyl)propiophenone hydrochloride (HY-770; 1), a newly developed muscle-relaxing agent, and its analogues were studied in aqueous solution at 50 degrees C, ionic strength 0.5 M, and pH 8.0-12.0. Compound 1 and its four analogues followed ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600780115
更新日期：1989-01-01 00:00:00
abstract：:High pressure liquid chromatography using reversed-phase and/or ion-pair techniques was used to optimize resolution of aspirin-containing muscle relaxant mixtures as well as other therapeutic agents commonly found in muscle relaxant-analgesic mixtures. The compounds were chromatographed on an octadecylsilane column us...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680112
更新日期：1979-01-01 00:00:00
abstract：:The effects of aspirin on 14C-pirprofen disposition in the rat were studied. An oral 60-mg/kg dose of aspirin significantly reduced plasma radioactivity during the 1--8-hr interval after an intravenous 5-mg/kg injection of 14C-pirprofen. The aspirin-treated group had only 69% as much area under the radioactivity curve...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680820
更新日期：1979-08-01 00:00:00
abstract：:In recent years, controlled release coatings, comprised of drug-polymer composites, have been integrated with medical devices, improving device functionality and performance. However, relationships between material properties, manufacturing environment, composite (micro)structure, and subsequent release kinetics are n...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21416
更新日期：2009-01-01 00:00:00
abstract：:The transdermal delivery of 2 fluorescent probes with similar molecular weight but different lipophilicity, into and through the skin from 2 commercially available transdermal bases, pluronic lecithin organogel, and Lipoderm® has been evaluated. First, in vitro penetration of fluorescein sodium and fluorescein (free a...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2017.09.008
更新日期：2018-02-01 00:00:00
abstract：:The influence of hepatic uptake and efflux, which includes passive diffusion and transporter-mediated component, on drug distribution volumes [steady-state volume of distribution (V(ss)) and terminal volume of distribution (V(β))], mean residence time (MRT), clearance, and terminal half-life is considered using a simp...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22696
更新日期：2011-11-01 00:00:00
abstract：:Observed venous plasma concentrations of furosemide, propranolol, griseofulvin, and theophylline at 0.33 and 0.66 min after intravenous bolus injections to unanesthetized dogs were compared with those extrapolated using the instantaneous input hypothesis. At 0.33 min, extrapolated/observed plasma level ratios as high ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600700918
更新日期：1981-09-01 00:00:00
abstract：:Racemic and homochiral sodium ibuprofen were characterized by thermal analysis and powder X-ray diffractometry. The melting point phase diagram was constructed and thermodynamic calculation was performed. In contrast to racemic ibuprofen, which is a racemic compound, racemic sodium ibuprofen forms both a racemic congl...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10393
更新日期：2003-07-01 00:00:00
abstract：:The synthesis and antibacterial evaluation of a number of 2-(substituted phenylureido)-4-thiocyanatobenzothiazoles are described. The more active compounds against the test organisms in vitro generally were those substituted with halogens on the phenyl and benzothiazole rings. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670247
更新日期：1978-02-01 00:00:00
abstract：:A simple solution model that has lead to successful predictive equations for the partial molar excess properties of a solute in simple binary solvent mixtures containing only nonspecific interactions is extended to include association between the solute and one of the solvent components. An expression is derived and t...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600720822
更新日期：1983-08-01 00:00:00
abstract：:The in vivo dissolution of many poorly soluble drugs is enhanced by the action of surfactants secreted into the upper gastrointestinal (GI) tract. These substances may act by solubilizing individual drug molecules into two separate liquid phases: the free aqueous phase and a micellar phase in which the drug is incorpo...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js9604974
更新日期：1997-10-01 00:00:00
abstract：:The adsorption of cimetidine on selected pharmaceuticals including kaolin, activated charcoal, talc, and nonsystemic antacids was determined at pH 5.0 and 25 degrees. The Langmuir and Freundlich adsorption isotherms showed that cimetidine adsorption was significant with activated charcoal, kaolin, talc, and magnesium ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690329
更新日期：1980-03-01 00:00:00
abstract：:During the drying process of a wet granulate, water-soluble compounds can migrate to the outer layers of the granule with the evaporating solvent. This migration can affect structural and mechanical characteristics of the granules as the solute accumulates on the granule's outer crust. The objective of this study was ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23051
更新日期：2012-04-01 00:00:00
abstract：:During the manufacturing process of biopharmaceuticals, peristaltic pumps are employed at different stages for transferring and dosing of the final product. Commonly used silicone tubings are known for particle shedding from the inner tubing surface due to friction in the pump head. These nanometer sized silicone rubb...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.12.002
更新日期：2020-12-09 00:00:00
abstract：:The entropy of fusion of 84 disubstituted benzenes was essentially constant and independent of the participation of the compounds in intramolecular or intermolecular hydrogen bonding. It was also independent of the shapes, sizes, and dipole moments of the rigid molecules studied. While the entropy of fusion was indepe...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600680512
更新日期：1979-05-01 00:00:00
abstract：:In pharmacokinetic evaluation of mice, using serial sampling methods rather than a terminal blood sampling method could reduce the number of animals needed and lead to more reliable data by excluding individual differences. In addition, using serial sampling methods can be valuable for evaluation of the drug-drug inte...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24236
更新日期：2015-03-01 00:00:00
abstract：:A program is described that permits iterative least-squares nonlinear regression fitting of polyexponential curves using the Hewlett Packard HP 41 CV programmable calculator. The program enables the analysis of pharmacokinetic drug level profiles with a high degree of precision. Up to 15 data pairs can be used, and in...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600740510
更新日期：1985-05-01 00:00:00
abstract：:In vitro iontophoretic administration of drugs through a microporous polyolefin membrane with hydrophilic urethane polymerfilled pores was done for the ionized drugs dexamethasone sodium phosphate, hydrocortisone sodium phosphate, and prednisolone sodium succinate, and for a nonionizable drug cortisone acetate. Curren...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600780308
更新日期：1989-03-01 00:00:00
abstract：:Pharmaceutical aerosols are used to treat many pulmonary diseases. The use of low-density powders has proven useful to support efficient drug delivery. Measurements must account for the low-density, spherical particle features contributing to aerodynamic behavior. Ideally, the aerodynamic particle size distribution (A...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2017.11.005
更新日期：2018-03-01 00:00:00
abstract：:The reaction kinetics of blue tetrazolium with selected arylhydrazines were investigated under pseudo-first-order conditions. The reaction rate constants were obtained at various temperatures, and the enthalpy (8.4-11.2 kcal/mole) and entropy (-38--45 eu) of activations were calculated. A Hammett plot yielded a straig...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670714
更新日期：1978-07-01 00:00:00
abstract：:A highly sensitive and specific electron-capture GLC assay capable of detecting picogram quantities of metoclopramide, a procaine derivative, in biological fluids was developed. This assay consisted of extracting metoclopramide from an alkalinized aqueous layer into benzene. A portion of the organic phase was derivati...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670813
更新日期：1978-08-01 00:00:00
abstract：:The stability of highly purified supercoiled plasmid DNA formulated in simple phosphate or Tris-buffered saline solutions has been characterized to establish the overall degradation processes that occur during storage in aqueous solution. Plasmid DNA stability was monitored during accelerated stability studies (at 50 ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/(SICI)1520-6017(200001)89:1<76::AID-JPS8>3
更新日期：2000-01-01 00:00:00
abstract：:The combined clearance of endogenous 6β-hydroxycortisol and 6β-hydroxycortisone is suggested biomarker for in vivo cytochrome P450 3A (CYP3A) activity. We aimed to determine whether the combined clearance of these two markers together with information of biopharmaceutics classification system (BCS) of drugs could be u...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24566
更新日期：2015-10-01 00:00:00
