On the Nature of Physiologically-Based Pharmacokinetic Models -A Priori or A Posteriori? Mechanistic or Empirical?

abstract：PURPOSE:To show that atomic force microscopy (AFM) can be used to directly study the electrostatic charging and dissipation of single pharmaceutical particles. MATERIALS AND METHODS:Particles of lactose attached to AFM cantilevers were charged on a glass surface at a relative humidity (RH) of 0.1%. By recording force-...

journal_title：Pharmaceutical research

authors： Bunker MJ,Davies MC,James MB,Roberts CJ

更新日期：2007-06-01 00:00:00

abstract：:Gallopamil is a calcium-channel antagonist with reported activity in experimental animals three to five times higher than that of verapamil. An automated high-performance liquid chromatographic (HPLC) method with fluorescence detection is described for the simultaneous determination of gallopamil and its metabolite no...

journal_title：Pharmaceutical research

authors： McLean AM,Babcock-Atkinson E,Rein K,Ruggirello DA,Gonzalez MA,Noonan PK

更新日期：1987-08-01 00:00:00

abstract：PURPOSE:We examined the ability of a protein transduction domain (PTD), YARA, to penetrate in the skin and carry a conjugated peptide, P20. The results with YARA were compared to those of a well-known PTD (TAT) and a control, nontransducing peptide (YKAc). The combined action of PTDs and lipid penetration enhancers was...

journal_title：Pharmaceutical research

authors： Lopes LB,Brophy CM,Furnish E,Flynn CR,Sparks O,Komalavilas P,Joshi L,Panitch A,Bentley MV

更新日期：2005-05-01 00:00:00

abstract：:A method of immobilizing urokinase on albumin microspheres has been developed. Laser scattering, which was used to follow particle size from the initial emulsification stage to the final aqueous resuspension of the microsphere stage, showed that particle coalescence and crosslinking were critical parameters in manufac...

journal_title：Pharmaceutical research

authors： Bhargava K,Ando HY

更新日期：1992-06-01 00:00:00

abstract：PURPOSE:Some therapeutic peptides exhibit amyloidogenic properties that cause insolubility and cytotoxicity against neuronal cells in vitro. Here, we characterize the conformational change in monomeric therapeutic peptide to its fibrillar aggregate in order to prevent amyloidogenic formation during clinical application...

journal_title：Pharmaceutical research

authors： Onoue S,Ohshima K,Debari K,Koh K,Shioda S,Iwasa S,Kashimoto K,Yajima T

更新日期：2004-07-01 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:To measure the diffusion of nanometer polymersomes through tissue engineered human oral mucosa. METHODS:In vitro models of full thickness tissue engineered oral mucosa (TEOM) were used to assess the penetration properties of two chemically different polymersomes comprising two of block copolymers, PMPC-PDPA an...

journal_title：Pharmaceutical research

authors： Hearnden V,Lomas H,Macneil S,Thornhill M,Murdoch C,Lewis A,Madsen J,Blanazs A,Armes S,Battaglia G

更新日期：2009-07-01 00:00:00

abstract：:The stability of an antibiotic formulation (clindamycin phosphate in dextrose), which is stable at room temperature, was assessed by nonisothermal kinetic analysis at elevated temperatures. A preliminary study, conducted to establish apparent rate order, verified the appropriateness of a first-order kinetic model. The...

journal_title：Pharmaceutical research

authors： Kipp JE,Hlavaty JJ

更新日期：1991-05-01 00:00:00

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

authors： Ulery BD,Phanse Y,Sinha A,Wannemuehler MJ,Narasimhan B,Bellaire BH

更新日期：2009-03-01 00:00:00

abstract：PURPOSE:To determine by pharmacokinetic (PK) means the role of erythropoietin-receptor (EPO-R) upregulation in fetuses on the elimination of erythropoietin (EPO). MATERIALS AND METHODS:Six fetal sheep were catheterized at a gestational age of 125-127 days and phlebotomized daily for 6 days. Paired tracer PK studies us...

journal_title：Pharmaceutical research

authors： Freise KJ,Widness JA,Segar JL,Schmidt RL,Veng-Pedersen P

更新日期：2007-09-01 00:00:00

abstract：:We report the chemical and enzymatic hydrolysis of two hydrophobic prodrugs of ganciclovir (3 = dipropionate ester; 4 = diadamantoate ester). Both prodrugs undergo hydrolysis showing a pH dependence of kobs = kH+aH+ + ko + kHO-aHO- and a pH of maximum stability near pH 5. Only 4 exhibited a shelf life (t90) greater th...

journal_title：Pharmaceutical research

authors： Powell MF,Magill A,Chu N,Hama K,Mau CI,Foster L,Bergstrom R

更新日期：1991-11-01 00:00:00

abstract：:A new method of analysis for the antihypertensive drug, hydralazine, is introduced. The assay involves the addition of p-nitrobenzaldehyde to blood samples containing hydralazine, to form a stable Schiff's base, hydralazine p-nitrobenzaldehyde hydrazone. The derivative is extracted from the blood into hexane and the s...

journal_title：Pharmaceutical research

authors： Semple HA,Tam YK,Tin S,Coutts RT

更新日期：1988-06-01 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

authors： Shatan AB,Venclíková K,Zasońska BA,Patsula V,Pop-Georgievski O,Petrovský E,Horák D

更新日期：2019-08-14 00:00:00

abstract：:The pulmonary deposition and pharmacokinetics of human growth hormone (hGH), administered by aerosol and instillate, in formulations containing 99mTc-DTPA (for gamma scintigraphic imaging) have been studied in five male New Zealand White rabbits. Gamma scintigraphy indicated that the peripheral:central deposition tend...

journal_title：Pharmaceutical research

authors： Colthorpe P,Farr SJ,Smith IJ,Wyatt D,Taylor G

更新日期：1995-03-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate the specific changes in body distribution of camptothecin (CA) through incorporation into solid lipid nanoparticles (SLN) by peroral route. METHODS:Camptothecin loaded solid lipid nanoparticles (CA-SLN) coated with poloxamer 188 were produced by high pressure homogeniza...

journal_title：Pharmaceutical research

authors： Yang S,Zhu J,Lu Y,Liang B,Yang C

更新日期：1999-05-01 00:00:00

abstract：:The use of nanoparticulate pharmaceutical carriers to enhance the in vivo efficiency of many drugs well established itself over the past decade both in pharmaceutical research and clinical setting. The current level of engineering pharmaceutical nanocarriers in some cases allows for drug delivery systems (DDS) to demo...

journal_title：Pharmaceutical research

authors： Torchilin VP

更新日期：2007-12-01 00:00:00

abstract：PURPOSE:Melanoma is an aggressive neoplasm with a propensity for metastases and resistance to therapy. Previously, we showed that (-)-epigallocatechin-3-gallate (EGCG), the major polyphenolic antioxidant present in green tea, resulted in a significant decrease in the viability and growth of melanoma and induction of ap...

journal_title：Pharmaceutical research

authors： Nihal M,Roelke CT,Wood GS

更新日期：2010-06-01 00:00:00

abstract：PURPOSE:Using monolayers of human pancreatic adenocarcinoma cells (Panc-1) that express multidrug resistance-associated protein (MRP), the present work investigates the effects of Pluronic block copolymers on the functional activity of MRP. METHODS:The studies examined the accumulation and efflux of the MRP selective ...

journal_title：Pharmaceutical research

authors： Miller DW,Batrakova EV,Kabanov AV

更新日期：1999-03-01 00:00:00

abstract：PURPOSE:To evaluate the potential effects of PEGylated pH-sensitive liposomes on the intracellular activity of a new peptide recently characterized as a novel inhibitor of the human thymidylate synthase (hTS) over-expressed in many drug-resistant human cancer cell lines. METHODS:Peptide-loaded pH-sensitive PEGylated (...

journal_title：Pharmaceutical research

authors： Sacchetti F,Marverti G,D'Arca D,Severi L,Maretti E,Iannuccelli V,Pacifico S,Ponterini G,Costi MP,Leo E

更新日期：2018-09-12 00:00:00

abstract：PURPOSE:Chitosan-based polymeric micelles (CBPMs) are considered as promising carriers for delivery of anticancer drugs, imaging agents and genes. To optimize the physicochemical, pharmaceutical and biological properties of CBPMs, the molecular mechanisms behind the self-assembly behavior of chitosan (CHI) amphiphilic ...

journal_title：Pharmaceutical research

authors： Mahmoudzadeh M,Fassihi A,Dorkoosh F,Heshmatnejad R,Mahnam K,Sabzyan H,Sadeghi A

更新日期：2015-12-01 00:00:00

abstract：:Molecular dynamics simulations and the generation of ad hoc chemical libraries are playing an increasingly important and recognized role in structure-based virtual screening. These approaches are important for treating target flexibility and improving the drug discovery pipeline. In this article I will comment on thes...

journal_title：Pharmaceutical research

authors： Rastelli G

更新日期：2013-05-01 00:00:00

abstract：:The technique of Affinity capillary electrophoresis (ACE) is a useful tool to characterize complexation and partition equilibria. A wide range of applications in pharmaceutics has been presented: the determination of pKA values, of association constants between drugs and cyclodextrins or amphiphilic compounds as well ...

journal_title：Pharmaceutical research

authors： Neubert RH,Schwarz MA,Mrestani Y,Plätzer M,Raith K

更新日期：1999-11-01 00:00:00

abstract：PURPOSE:To develop an efficient tumor vasculature-targeted polymeric micelle delivery system for combretastatin A4 (CA4), a novel antivascular agent. METHODS:CA4-loaded micelles were prepared from poly (ethylene glycol)-b-poly (d, l-lactide) copolymers. RGD peptides that target integrins alphavbeta3 and alphavbeta5, m...

journal_title：Pharmaceutical research

authors： Wang Y,Yang T,Wang X,Wang J,Zhang X,Zhang Q

更新日期：2010-09-01 00:00:00

abstract：OBJECTIVES:We recently demonstrated that fibrin-based tissue engineered blood vessels (TEV) exhibited vascular reactivity, matrix remodeling and sufficient strength for implantation into the veins of an ovine animal model, where they remained patent for 15 weeks. Here we present an approach to improve the mechanical pr...

journal_title：Pharmaceutical research

authors： Yao L,Liu J,Andreadis ST

更新日期：2008-05-01 00:00:00

abstract：:In order to study the influence of hydrogen bonding in the amide backbone of a peptide on permeability across a cell membrane, a series of tetrapeptide analogues was prepared from D-phenylalanine. The amide nitrogens in the parent oligomer were sequentially methylated to give a series containing from one to four methy...

journal_title：Pharmaceutical research

authors： Conradi RA,Hilgers AR,Ho NF,Burton PS

更新日期：1992-03-01 00:00:00

abstract：PURPOSE:The aim of this study was to test the ability of paclitaxel-loaded poly(butylcyanoacrylate) (PBCA) nanoparticles to overcome multidrug resistance (MDR) in human ovarian resistant cells (A2780/T) and investigate its possible mechanism. METHODS:We prepared paclitaxel-loaded PBCA nanoparticles by interfacial poly...

journal_title：Pharmaceutical research

authors： Ren F,Chen R,Wang Y,Sun Y,Jiang Y,Li G

更新日期：2011-04-01 00:00:00

abstract：:We studied the effects of two verapamil analogs, anipamil and ronipamil, in traumatic shock. Noble-Collip drum trauma produced a shock state characterized by an eight-fold increase in plasma cathepsin D activity, a 13-fold increase in the rate of plasma myocardial depressant factor (MDF) accumulation, and a survival t...

journal_title：Pharmaceutical research

authors： Hock CE,Daitch JS,Lefer AM

更新日期：1985-05-01 00:00:00

abstract：PURPOSE:Since the absorption of ceftriaxone (CTO) in the intestine is restricted by its natural physiological characteristics, we developed a series of small synthetic compounds derived from bile acids to promote the absorption of CTO in the gastrointestinal tract. METHODS:Several bile acid derivatives were screened b...

journal_title：Pharmaceutical research

authors： Jeon OC,Hwang SR,Al-Hilal TA,Park JW,Moon HT,Lee S,Park JH,Byun Y

更新日期：2013-04-01 00:00:00

abstract：:Penetration of various compounds through shed snake skin was measured in vitro to examine the effect of lipophilicity and molecular size of a compound on permeability through this model membrane. The permeabilities were found to be controlled by the lipophilicity and the molecular size of the permeant. The smaller and...

journal_title：Pharmaceutical research

authors： Itoh T,Magavi R,Casady RL,Nishihata T,Rytting JH

更新日期：1990-12-01 00:00:00

abstract：PURPOSE:We have shown that the three human prostate xenograft tumors, i.e. the androgen-dependent CWR22 tumor, and the androgen-resistant CWR22R and CWR91 tumors, are comparable to patient tumors in their expression of prostate specific antigen, multidrug resistance p-glycoprotein, p53 and Bcl-2 and in their sensitivit...

journal_title：Pharmaceutical research

authors： Gan Y,Au JL,Lu J,Wientjes MG

更新日期：1998-11-01 00:00:00