Freeze-concentration separates proteins and polymer excipients into different amorphous phases.

abstract：PURPOSE:It is reported that the cerebrospinal fluid (CSF) to plasma unbound concentration ratio of fleroxacin at steady-state is approximately 0.5 in experimental animals. These results can be accounted for by assuming the presence of an active transport system for the efflux of this compound across the choroid plexus....

journal_title：Pharmaceutical research

authors： Ooie T,Suzuki H,Terasaki T,Sugiyama Y

更新日期：1996-04-01 00:00:00

abstract：:Sodium taurodihydrofusidate (STDHF) is one of the most promising absorption enhancers for nasal delivery of peptide drugs. Drugs and additives in nasal formulations should not interfere with the self-cleaning capacity of the nose by the ciliary epithelium. Measured in vitro on human adenoid tissue with a photoelectric...

journal_title：Pharmaceutical research

authors： Hermens WA,Hooymans PM,Verhoef JC,Merkus FW

更新日期：1990-02-01 00:00:00

abstract：PURPOSE:To evaluate the potential of several bis-ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA, adefovir) to enhance the oral absorption of PMEA. METHODS:Caco-2 monolayers were used to estimate intestinal transport and metabolism of the bis(pivaloyloxymethyl)-ester [bis(POM)-] and a s...

journal_title：Pharmaceutical research

authors： Annaert P,Gosselin G,Pompon A,Benzaria S,Valette G,Imbach JL,Naesens L,Hatse S,de Clercq E,Van den Mooter G,Kinget R,Augustijns P

更新日期：1998-02-01 00:00:00

abstract：PURPOSE:To characterize temporal exposure and elimination of 5 gold/dendrimer composite nanodevices (CNDs) (5 nm positive, negative, and neutral, 11 nm negative, 22 nm positive) in mice using a physiologically based mathematical model. METHODS:400 ug of CNDs is injected intravenously to mice bearing melanoma cell line...

journal_title：Pharmaceutical research

authors： Mager DE,Mody V,Xu C,Forrest A,Lesniak WG,Nigavekar SS,Kariapper MT,Minc L,Khan MK,Balogh LP

更新日期：2012-09-01 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

authors： Kenny JR,Mukadam S,Zhang C,Tay S,Collins C,Galetin A,Khojasteh SC

更新日期：2012-07-01 00:00:00

abstract：PURPOSE:The purpose of this work was to study the influence of cell differentiation on the mRNA expression of transporters and channels in Caco-2 cells and to assess Caco-2 cells as a model for carrier-mediated drug transport in the intestines. METHOD:Gene mRNA expression was measured using a custom-designed microarra...

journal_title：Pharmaceutical research

authors： Anderle P,Rakhmanova V,Woodford K,Zerangue N,Sadée W

更新日期：2003-01-01 00:00:00

abstract：PURPOSE:Development of a human mitochondrial gene delivery vector is a critical step in the ability to treat diseases arising from mutations in mitochondrial DNA. Although we have previously cloned the mouse mitochondrial genome in its entirety and developed it as a mitochondrial gene therapy vector, the human mitochon...

journal_title：Pharmaceutical research

authors： Bigger BW,Liao AY,Sergijenko A,Coutelle C

更新日期：2011-11-01 00:00:00

abstract：:For the last 50 years we have known of a broad-spectrum agent tilorone dihydrochloride (Tilorone). This is a small-molecule orally bioavailable drug that was originally discovered in the USA and is currently used clinically as an antiviral in Russia and the Ukraine. Over the years there have been numerous clinical and...

journal_title：Pharmaceutical research

authors： Ekins S,Lane TR,Madrid PB

更新日期：2020-03-25 00:00:00

abstract：:Semitelechelic poly[N-(2-hydroxypropyl)methacrylamide]s (ST-PHPMA) containing one amino end-group and differing in molecular weight were synthesized by radical polymerization in the presence of 2-aminoethanethiol (AET) as chain transfer agent. These polymers were covalently attached via amide bonds to the surface of n...

journal_title：Pharmaceutical research

authors： Kamei S,Kopecek J

更新日期：1995-05-01 00:00:00

abstract：:Under the heading "Methods-Synthesis of the Bioreducible Modified-PAE (mPAE)", on page 3, line 14-17, there is an error. The quantity unit of PAE and 2-iminothiolane hydrochloride needs to be corrected to mg instead of g. ...

journal_title：Pharmaceutical research

authors： Gandhi NS,Godeshala S,Koomoa-Lange DT,Miryala B,Rege K,Chougule MB

更新日期：2018-09-05 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

authors： Shirangi M,Hennink WE,Somsen GW,van Nostrum CF

更新日期：2015-09-01 00:00:00

abstract：PURPOSE:To investigate the moisture-induced aggregation (i.e., a loss of solubility in water) of DNA in a solid state and to develop rational strategies for its prevention. METHODS:Lyophilized calf thymus DNA was exposed to relative humidity (RH) levels from 11% to 96% at 55 degrees C. Following a 24-h incubation unde...

journal_title：Pharmaceutical research

authors： Sharma VK,Klibanov AM

更新日期：2007-01-01 00:00:00

abstract：PURPOSE:The heats of reaction between the enantiomers and racemates of ibuprofen and naproxen and human serum albumin (HSA) are to be measured with and without the addition of octanoic acid. The effects of octanoic acid on the free energies of interaction between the drugs and HSA is to be determined and compared to th...

journal_title：Pharmaceutical research

authors： Cheruvallath VK,Riley CM,Narayanan SR,Lindenbaum S,Perrin JH

更新日期：1996-01-01 00:00:00

abstract：PURPOSE:β-Hydroxy-β-methylbutyrate (HMB), a nutritional supplement, elicits anabolic activity in muscle. Here we investigated the mechanism of HMB uptake in muscle cells. METHODS:Murine muscle cells (C2C12) and human mammary epithelial cells (MCF7) were used for uptake. As HMB is a monocarboxylate, focus was on monoca...

journal_title：Pharmaceutical research

authors： Ogura J,Sato T,Higuchi K,Bhutia YD,Babu E,Masuda M,Miyauchi S,Rueda R,Pereira SL,Ganapathy V

更新日期：2019-04-17 00:00:00

abstract：PURPOSE:The objective of the work was to evaluate the potential of hyaluronan-based nanoparticles as tumor-targeting nano-systems for CD44-overexpressed cancer therapy. METHODS:The synthesized amphiphilic cholesteryl succinoyl hyaluronan (Chol-Suc-HA) conjugates self-assembled into docetaxel(DTX)-loaded nanoparticles ...

journal_title：Pharmaceutical research

authors： Song S,Qi H,Xu J,Guo P,Chen F,Li F,Yang X,Sheng N,Wu Y,Pan W

更新日期：2014-11-01 00:00:00

abstract：PURPOSE:Mannosylation of vaccines is a promising strategy to selectively target vaccine antigens to the mannose receptor expressed on dendritic cells (DCs). The purpose of this study was to investigate the effect of mannan (MN) chemically conjugated to poly(D, L-lactide-co-glycolic acid) (PLGA) nanoparticles (NPs) on a...

journal_title：Pharmaceutical research

authors： Hamdy S,Haddadi A,Shayeganpour A,Samuel J,Lavasanifar A

更新日期：2011-09-01 00:00:00

abstract：PURPOSE:To develop a novel bioadhesive polymer that protects peptide drugs from luminal degradation by aminopeptidase N and to evaluate the system in vitro on porcine mucosa. METHODS:EDTA was covalently bound to chitosan in order to combine the bioadhesive properties of the polymer with the well known capacity of EDTA...

journal_title：Pharmaceutical research

authors： Bernkop-Schnürch A,Paikl C,Valenta C

更新日期：1997-07-01 00:00:00

abstract：:The aim of this investigation was to assess whether immunosuppression induced by total-body irradiation (TBI) affects the pharmacodynamics of centrally acting drugs. Female Sabra rats were exposed to a single dose of gamma irradiation (5.3 Gy). Four days later, when both the cellular and the humoral immune responses w...

journal_title：Pharmaceutical research

authors： Hoffman A,Alfon J,Habib G,Pinto E,Gorodetsky R

更新日期：1994-05-01 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

authors： Soine WH,Safi H,Westkaemper RB

更新日期：1992-05-01 00:00:00

abstract：:Since many chiral pharmaceutical excipients, such as cellulose polymers and cyclodextrins, are used as stationary phases for the separation of enantiomers by high performance liquid chromatography (HPLC), it is hypothesized that one enantiomer of a chiral drug will be released faster than the other from a pharmaceutic...

journal_title：Pharmaceutical research

authors： Duddu SP,Vakilynejad M,Jamali F,Grant DJ

更新日期：1993-11-01 00:00:00

abstract：PURPOSE:Doxorubicin was chemically conjugated to a terminal end group of poly(D,L-lactic-co-glycolic acid) [PLGA] and the doxorubicin-PLGA conjugate was formulated into nanoparticles to sustain the release of doxorubicin. METHODS:A hydroxyl terminal group of PLGA was activated by p-nitrophenyl chloroformate and reacte...

journal_title：Pharmaceutical research

authors： Yoo HS,Oh JE,Lee KH,Park TG

更新日期：1999-07-01 00:00:00

abstract：PURPOSE:The blood-brain barrier (BBB) essentially restricts therapeutic drugs from entering into the brain. This study tests the hypothesis that brain endothelial cell derived exosomes can deliver anticancer drug across the BBB for the treatment of brain cancer in a zebrafish (Danio rerio) model. MATERIALS AND METHODS...

journal_title：Pharmaceutical research

authors： Yang T,Martin P,Fogarty B,Brown A,Schurman K,Phipps R,Yin VP,Lockman P,Bai S

更新日期：2015-06-01 00:00:00

abstract：PURPOSE:To investigate plasmid DNA interactions with liposomes prepared from dimyristoylglyceroethylphosphocholine (EDMPC) and DOPE using high sensitivity differential scanning calorimetry (HSDSC). MATERIALS AND METHODS:Large unilamellar liposomes of EDMPC with DOPE (mol ratio 0-50%) were prepared. Plasmid DNA was add...

journal_title：Pharmaceutical research

authors： Saunders M,Taylor KM,Craig DQ,Palin K,Robson H

更新日期：2007-10-01 00:00:00

abstract：PURPOSE:Low temperature sensitive liposome (LTSL) encapsulated docetaxel were combined with mild hyperthermia (40-42°C) to investigate in vivo biodistribution and efficacy against a castrate resistant prostate cancer. METHOD:Female athymic nude mice with human prostate PC-3 M-luciferase cells grown subcutaneously into...

journal_title：Pharmaceutical research

authors： Ranjan A,Benjamin CJ,Negussie AH,Chokshi S,Chung PH,Volkin D,Yeram N,Linehan WM,Dreher MR,Pinto PA,Wood BJ

更新日期：2016-10-01 00:00:00

abstract：PURPOSE:To elucidate the catalytic mechanism of the esterase-like activity of serum albumin (SA), the reactivity of SA from six species was investigated using p-nitrophenyl esters as model substrates. METHODS:The effect of pH and the energetic and thermodynamic profiles of SA were determined for all species for p-nitr...

journal_title：Pharmaceutical research

authors： Sakurai Y,Ma SF,Watanabe H,Yamaotsu N,Hirono S,Kurono Y,Kragh-Hansen U,Otagiri M

更新日期：2004-02-01 00:00:00

abstract：PURPOSE:Novel itraconazole (ITZ)-based dry powders for inhalation (DPI) were optimized for aerodynamic and dissolution properties and contained excipients that are acceptable for inhalation. METHODS:The DPI were produced by spray drying solutions. The drug content, crystallinity state, and morphological evaluation of ...

journal_title：Pharmaceutical research

authors： Duret C,Wauthoz N,Sebti T,Vanderbist F,Amighi K

更新日期：2012-10-01 00:00:00

abstract：PURPOSE:The aim was to investigate the influence of polymer content and molecular weight on the morphology and heat- and moisture-induced transformations, as indicators of stability, of spray-dried composite particles of amorphous lactose and poly(vinylpyrrolidone) (PVP). METHODS:Amorphous lactose and composite partic...

journal_title：Pharmaceutical research

authors： Berggren J,Alderborn G

更新日期：2003-07-01 00:00:00

abstract：:The absorption of insulin across the vaginal mucosa into the systemic circulation was studied in ovariectomized rats given subsequent estrogen treatment. Blood glucose levels were determined as an indirect measure of insulin absorption, and the effect of various enhancers on the hypoglycemic response was investigated....

journal_title：Pharmaceutical research

authors： Richardson JL,Illum L,Thomas NW

更新日期：1992-07-01 00:00:00

abstract：:This study utilized different statistical techniques to evaluate the reliability (internal consistency) and the discriminant validity of the most widely used measures of organizational commitment and intention to quit (the employing organization). Data were obtained from a national mail survey of members of the Americ...

journal_title：Pharmaceutical research

authors： Kong SX,Wertheimer AI,Serradell J,McGhan WF

更新日期：1994-01-01 00:00:00

abstract：PURPOSE:To develop a dose dependent version of BCS and identify a critical dose after which the amount absorbed is independent from the dose. METHODS:We utilized a mathematical model of drug absorption in order to produce simulations of the fraction of dose absorbed (F) and the amount absorbed as function of the dose ...

journal_title：Pharmaceutical research

authors： Charkoftaki G,Dokoumetzidis A,Valsami G,Macheras P

更新日期：2012-11-01 00:00:00