abstract：:In this study, powder surface imaging was utilized in evaluation of particle size-related segregation behavior of granules during vibration and tableting processes. Altogether, eight granule batches were manufactured using a fluidized bed granulator. The particle size distribution of each batch was measured with sieve...

journal_title：Journal of pharmaceutical sciences

authors： Lakio S,Hatara J,Tervakangas H,Sandler N

更新日期：2012-06-01 00:00:00

abstract：:The application of raster image correlation spectroscopy (RICS) as a tool for the characterisation of protein diffusion was assessed using a model protein, bovine serum albumin (BSA), as a function of formulation and denaturing conditions. RICS results were also validated against dynamic light scattering and fluoresce...

journal_title：Journal of pharmaceutical sciences

authors： Hamrang Z,Pluen A,Zindy E,Clarke D

更新日期：2012-06-01 00:00:00

abstract：:The objective of this study is to understand the underlying mechanisms responsible for the superior stability of indomethacin (INM)-Eudragit® E PO (E PO) system by exploring the miscibility and intermolecular interactions through the combination of thermal, rheological, and spectroscopic analysis. The zero shear-rate ...

journal_title：Journal of pharmaceutical sciences

authors： Liu H,Zhang X,Suwardie H,Wang P,Gogos CG

更新日期：2012-06-01 00:00:00

abstract：:The vaporization, fusion, and sublimation enthalpies of (R,S)- and (R)-flurbiprofen at T = 298.15 K are reported and compared with literature values when available. Correlation gas chromatography experiments were first performed to identify appropriate standards that could be used for materials containing a single flu...

journal_title：Journal of pharmaceutical sciences

authors： Umnahanant P,Hasty D,Chickos J

更新日期：2012-06-01 00:00:00

abstract：:A novel technique is presented to allow measurement of the kinetics of protein inactivation during drying of an acoustically levitated single droplet. Droplets/particles are removed from the acoustic field after various times during drying, and the state of the protein within them is analyzed. The influence of drying ...

journal_title：Journal of pharmaceutical sciences

authors： Lorenzen E,Lee G

更新日期：2012-06-01 00:00:00

abstract：:An alumina (Al(2)O(3))-steroid-ethanol model is used for forced degradation testing of corticosteroids to predict chemical stability and degradation products in pressurized metered-dose inhaler (pMDI) solution formulations. The model involves an ethanolic solution of a test steroid with Al(2)O(3), stressed at elevated...

journal_title：Journal of pharmaceutical sciences

authors： Wu ZZ,Thatcher ML,Lundberg JK,Ogawa MK,Jacoby CB,Battiste JL,Ledoux KA

更新日期：2012-06-01 00:00:00

abstract：:The aim of this study was to utilize high-speed video imaging for understanding the disintegrability of compacts and disintegrant action upon wetting. High-speed video imaging was used to visualize the disintegration of compacts and effect of wetting on free disintegrant particles. Acquired images were processed using...

journal_title：Journal of pharmaceutical sciences

authors： Desai PM,Liew CV,Heng PW

更新日期：2012-06-01 00:00:00

abstract：:(13) C cross-polarization magic-angle spinning nuclear magnetic resonance (CPMAS NMR) spectroscopy was applied to the identification and characterization of carvedilol (1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)-ethylamino]-propan-2-ol) in pharmaceutical preparations. Solid-state spectra (standard linewidth and l...

journal_title：Journal of pharmaceutical sciences

authors： Zielińska-Pisklak M,Pisklak DM,Wawer I

更新日期：2012-05-01 00:00:00

abstract：:Various complex mechanisms and their multifactorial pathways decisively provoke low-grade local and systemic inflammation in β-cells of pancreatic islets and peripheral tissues to induce β-cells' dysfunction and apoptosis, insulin resistance, and ultimately, overt type 2 diabetes mellitus (T2DM). Conventional antidiab...

journal_title：Journal of pharmaceutical sciences

authors： Akash MS,Shen Q,Rehman K,Chen S

更新日期：2012-05-01 00:00:00

abstract：:The dependency of metformin in vivo disposition on the rate and extent of dissolution was studied. The analysis includes the use of fundamental principles of drug input, permeability, and intestinal transit time within the framework of a compartmental absorption transit model to predict key pharmacokinetic (PK) parame...

journal_title：Journal of pharmaceutical sciences

authors： Crison JR,Timmins P,Keung A,Upreti VV,Boulton DW,Scheer BJ

更新日期：2012-05-01 00:00:00

abstract：:The objective of the current study was to evaluate the performance of Raman and near-infrared (NIR) techniques combined with chemometrics in characterizing the critical quality attributes of brompheniramine (BP)-tannate complexes. Seven complexes were prepared and evaluated for chemical interactions, solubilities, dis...

journal_title：Journal of pharmaceutical sciences

authors： Zidan AS,Rahman Z,Khan MA

更新日期：2012-04-01 00:00:00

abstract：:The objective of this article was to monitor phase transformation in thiamine hydrochloride, from a nonstoichiometric hydrate (NSH) to a hemihydrate (HH), in stored tablets, prepared both by direct compression and wet granulation, and to relate the storage-induced phase transformation with changes in tablet microstruc...

journal_title：Journal of pharmaceutical sciences

authors： Chakravarty P,Suryanarayanan R,Govindarajan R

更新日期：2012-04-01 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

authors： Poutiainen S,Honkanen M,Becker J,Nachtweide D,Järvinen K,Ketolainen J

更新日期：2012-04-01 00:00:00

abstract：:Curcumin has been investigated as a potential photosensitizer (PS) in antimicrobial photodynamic therapy (aPDT). The phototoxic effect of curcumin is dependent on proper formulations of the compound because of the lipophilic nature of the molecule and the extremely low water solubility at physiological conditions. In ...

journal_title：Journal of pharmaceutical sciences

authors： Hegge AB,Nielsen TT,Larsen KL,Bruzell E,Tønnesen HH

更新日期：2012-04-01 00:00:00

abstract：:Foam granulation is a relatively newer wet granulation process whereby foamed binder solutions are added to powders in a mixer. It is essential to understand the effect of powder substrate on foam drainage and half-life, which are relevant to nucleation and agglomeration during foam granulation. Hydroxypropyl methylce...

journal_title：Journal of pharmaceutical sciences

authors： Koo OM,Ji J,Li J

更新日期：2012-04-01 00:00:00

abstract：:Historically, recovery had been used to evaluate the data quality of plasma protein binding or tissue binding obtained from equilibrium dialysis assays. Low recovery was often indicative of high nonspecific binding, instability, or low solubility. This study showed that, when equilibrium was fully established in the d...

journal_title：Journal of pharmaceutical sciences

authors： Di L,Umland JP,Trapa PE,Maurer TS

更新日期：2012-03-01 00:00:00

abstract：:To elucidate drug lipophilicity effects on the bioavailability (BA) of drugs from skin after administration by dissolving microneedles, nine compounds with different lipophilicity indexes (log p value) were formulated into two-layered dissolving microneedles and administered percutaneously to rat skin: desmopressin (D...

journal_title：Journal of pharmaceutical sciences

authors： Ito Y,Yoshimura M,Tanaka T,Takada K

更新日期：2012-03-01 00:00:00

abstract：:The objective of this study was to propose novel surface-modified nanostructured lipid carriers with partially deacetylated water-soluble chitosan (NLC-PDSC) as an efficient ocular delivery system to improve its transcorneal penetration and precorneal retention. PDSC with a deacetylation degree of around 50% was synth...

journal_title：Journal of pharmaceutical sciences

authors： Tian B,Luo Q,Song S,Liu D,Pan H,Zhang W,He L,Ma S,Yang X,Pan W

更新日期：2012-03-01 00:00:00

abstract：:The aim of this study was to investigate the bioavailability enhancement of the biopharmaceutics classification system class II compound ezetimibe loaded in ordered mesoporous silica (OMS) in dogs. The OMS was characterized as highly ordered mesoporous material with a narrow pore size distribution. Ezetimibe was loade...

journal_title：Journal of pharmaceutical sciences

authors： Kiekens F,Eelen S,Verheyden L,Daems T,Martens J,Van Den Mooter G

更新日期：2012-03-01 00:00:00

abstract：:Microbicide intravaginal rings (IVRs) are a promising woman-controlled strategy for preventing sexual transmission of human immunodeficiency virus (HIV). An IVR was prepared and developed from polyether urethane (PU) elastomers for the sustained delivery of UC781, a highly potent nonnucleoside reverse transcriptase in...

journal_title：Journal of pharmaceutical sciences

authors： Clark MR,Johnson TJ,McCabe RT,Clark JT,Tuitupou A,Elgendy H,Friend DR,Kiser PF

更新日期：2012-02-01 00:00:00

abstract：:Dissolution testing is routinely conducted in the pharmaceutical industry to provide in vitro drug release information for quality control purposes. The most common dissolution testing system for solid dosage forms is the United States Pharmacopeia (USP) Dissolution Testing Apparatus 2. This apparatus is very sensitiv...

journal_title：Journal of pharmaceutical sciences

authors： Wang Y,Armenante PM

更新日期：2012-02-01 00:00:00

abstract：:Detection and quantification of the amorphous phase of etoricoxib bulk drug substances, a selective cycloogenase-2 inhibitor used for the treatment of osteoarthritis, rheumatoid arthritis, and dental pain, was carried out using modulated differential scanning calorimetry (MDSC), dynamic mechanical analysis (DMA), and ...

journal_title：Journal of pharmaceutical sciences

authors： Clas SD,Lalonde K,Khougaz K,Dalton CR,Bilbeisi R

更新日期：2012-02-01 00:00:00

abstract：:Surface adsorption of two monoclonal antibodies (mAb1 and mAb2), with widely different hydrophobicity and self-association behavior in solution, was examined by quartz crystal microbalance with dissipation monitoring to understand how adsorption and protein self-interactions near the surface are impacted by their intr...

journal_title：Journal of pharmaceutical sciences

authors： Oom A,Poggi M,Wikström J,Sukumar M

更新日期：2012-02-01 00:00:00

abstract：:The aim of this study was to prepare and characterize thiolated chitosan (TC) nanoparticles (NPs) of tizanidine HCl (TZ) and to evaluate its transport across monolayer of RPMI 2650 cells (Human nasal septum carcinoma cell line) followed by assessment of their pharmacokinetic and pharmacodynamic attributes, after intra...

journal_title：Journal of pharmaceutical sciences

authors： Patel D,Naik S,Misra A

更新日期：2012-02-01 00:00:00

abstract：:For development and optimization of protein formulation sensitive analytical tools are required to follow both aggregation and changes in protein structure. The latter can be seen as the beginning of physical instability leading to aggregation. The focus of this work laid on the development of a novel analysis simulta...

journal_title：Journal of pharmaceutical sciences

authors： Printz M,Friess W

更新日期：2012-02-01 00:00:00

abstract：:Biopolymer-based hydrogels such as mucus and the basal lamina play a key role in biology, where they control the exchange of material between different compartments. They also pose a barrier that needs to be overcome for successful drug delivery. Characterizing the permeability properties of such hydrogels is mandator...

journal_title：Journal of pharmaceutical sciences

authors： Vladescu I,Lieleg O,Jang S,Ribbeck K

更新日期：2012-01-01 00:00:00

abstract：:A carboxymethyl derivative of scleroglucan (Scl-CM) with derivatization degree 300 ± 10 was synthesized and characterized by Fourier transform infrared spectroscopy, potentiometer titration, mucus adhesion studies, and rheological measurements. Rheological measurements showed the ability of the polymer to undergo sol-...

journal_title：Journal of pharmaceutical sciences

authors： Corrente F,Paolicelli P,Matricardi P,Tita B,Vitali F,Casadei MA

更新日期：2012-01-01 00:00:00

abstract：:An emerging technology subtype that has been adopted by formulators to address low-solubility issues is the supersaturating drug delivery system; this system is based on the "spring" and "parachute" design elements, which have been applied to lipid-based formulations, S(M)EDDS, solid dispersions, nano-based systems, a...

journal_title：Journal of pharmaceutical sciences

authors： Augustijns P,Brewster ME

更新日期：2012-01-01 00:00:00

abstract：:Determining the aggregation propensity of protein-based biotherapeutics is an important step in the drug development process. Typically, a great deal of data collected over a large period of time is needed to estimate the aggregation propensity of biotherapeutics. Thus, candidates cannot be screened early on for aggre...

journal_title：Journal of pharmaceutical sciences

authors： Lauer TM,Agrawal NJ,Chennamsetty N,Egodage K,Helk B,Trout BL

更新日期：2012-01-01 00:00:00

abstract：:The pharmacologically active compound (33% reduction in rabbit intraocular pressure recovery rate assay) 1-ethyl-6-fluoro-1,2,3,4-tetrahydroquinoline (MC4), which showed ocular hypotensive action and had optimum physicochemical properties, was characterized for its ocular absorption and distribution properties to bett...

journal_title：Journal of pharmaceutical sciences

authors： Pamulapati CR,Schoenwald RD

更新日期：2011-12-01 00:00:00

abstract：:Development of high-throughput release and characterization assays is critical for the effective support of the rapidly growing biologics pipeline for biotherapeutics. Clipping of polypeptide chains is commonly monitored during process optimization, formulation development, and stability studies. A reduced capillary e...

journal_title：Journal of pharmaceutical sciences

authors： Stackhouse N,Miller AK,Gadgil HS

更新日期：2011-12-01 00:00:00

abstract：:The purpose of this study was to elucidate the effect of heat treatment on the miscibility of multiple concentrated solutes that mimic biopharmaceutical formulations in frozen solutions. The first heating thermal analysis of frozen solutions containing either a low-molecular-weight saccharide (e.g., sucrose, trehalose...

journal_title：Journal of pharmaceutical sciences

authors： Izutsu K,Yomota C,Kawanishi T

更新日期：2011-12-01 00:00:00

abstract：:The aim of this study was to characterize the in vitro hepatic uptake kinetics of sodium fluorescein (NaFluo) and identify the transporters involved. NaFluo exhibited saturable uptake kinetics in suspended rat and human hepatocytes as reflected by K(m) values of 22.5 and 14.1 µM, and V(max) values of 98.3 and 5.8 pmol...

journal_title：Journal of pharmaceutical sciences

authors： De Bruyn T,Fattah S,Stieger B,Augustijns P,Annaert P

更新日期：2011-11-01 00:00:00

abstract：:Hyperlipidemia (HL) was previously shown to lower liver uptake of the more potent (-) enantiomer of ketoconazole (KTZ) in rat. The current study examined the possible modifying influence of experimental HL on a KTZ pharmacokinetic interaction with midazolam (MDZ). Normolipidemic and hyperlipidemic rats were administer...

journal_title：Journal of pharmaceutical sciences

authors： Hamdy DA,Brocks DR

更新日期：2011-11-01 00:00:00

abstract：:Circular dichroism (CD) spectroscopy is routinely used in the biopharmaceutical industry to study the effects of manufacturing, formulation, and storage conditions on protein conformation and stability, and these results are often included in regulatory filings. In this context, the purpose of CD spectroscopy is often...

journal_title：Journal of pharmaceutical sciences

authors： Li CH,Nguyen X,Narhi L,Chemmalil L,Towers E,Muzammil S,Gabrielson J,Jiang Y

更新日期：2011-11-01 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

authors： Berezhkovskiy LM

更新日期：2011-11-01 00:00:00

abstract：:Poor water solubility leads to low dissolution rate and consequently, it can limit bioavailability. Solid dispersions, where the drug is dispersed into an inert, hydrophilic polymer matrix can enhance drug dissolution. Solid dispersions were prepared using phenacetin and phenylbutazone as model drugs with polyethylene...

journal_title：Journal of pharmaceutical sciences

authors： Khan S,Batchelor H,Hanson P,Perrie Y,Mohammed AR

更新日期：2011-10-01 00:00:00

abstract：:Amorphous nifedipine (NFD), which has a smooth surface immediately after preparation, was shown to have structures resembling clusters of curling and branching fibers approximately 1 μm wide by atomic force microscopy (AFM) after storage at 25°C. The size of the cluster-like structures increased with storage over time...

journal_title：Journal of pharmaceutical sciences

authors： Miyazaki T,Aso Y,Kawanishi T

更新日期：2011-10-01 00:00:00

abstract：:Resveratrol trimethyl ether (trans-3,5,4'-trimethoxystilbene, RTE) is a naturally occurring and pharmacologically active resveratrol derivative. To evaluate its suitability as a drug candidate, a pharmacokinetic study was carried out in Sprague-Dawley rats with the emphasis to identify the impact of aqueous solubility...

journal_title：Journal of pharmaceutical sciences

authors： Lin HS,Ho PC

更新日期：2011-10-01 00:00:00

abstract：:A method is described for screening compounds that inhibit crystallization in solution to enable more accurate measurement of amorphous drug solubility. Three polymers [polyvinylpyrrolidone, hydroxypropyl methylcellulose, and hydroxypropyl methylcellulose acetate succinate (HPMCAS)] were screened for their ability to ...

journal_title：Journal of pharmaceutical sciences

authors： Murdande SB,Pikal MJ,Shanker RM,Bogner RH

更新日期：2011-10-01 00:00:00