The asymmetry of the unstirred water layer in permeability experiments.

abstract：PURPOSE:The objective of this investigation is to develop a rational design of Osteotropic Drug Delivery System (ODDS), which we have proposed as a novel method for drug delivery to the skeleton via bisphosphonic prodrug, based on the relationship between physicochemical and pharmacokinetic properties of bisphosphonate...

journal_title：Pharmaceutical research

authors： Hirabayashi H,Sawamoto T,Fujisaki J,Tokunaga Y,Kimura S,Hata T

更新日期：2001-05-01 00:00:00

abstract：PURPOSE:Supramolecular Biovectors (SMBV) consist of cross-linked cationic nanoparticles surrounded by a lipid membrane. The purpose was to study the structure of the lipid membrane and to characterise its interaction with the nanoparticles in order to differentiate SMBV from other polymer/lipid associations. METHODS:T...

journal_title：Pharmaceutical research

authors： De Miguel I,Imbertie L,Rieumajou V,Major M,Kravtzoff R,Betbeder D

更新日期：2000-07-01 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：PURPOSE:A mechanism-based PK-PD model was developed to predict the time course of dopamine D(2) receptor occupancy (D(2)RO) in rat striatum following administration of olanzapine, an atypical antipsychotic drug. METHODS:A population approach was utilized to quantify both the pharmacokinetics and pharmacodynamics of ol...

journal_title：Pharmaceutical research

authors： Johnson M,Kozielska M,Pilla Reddy V,Vermeulen A,Li C,Grimwood S,de Greef R,Groothuis GM,Danhof M,Proost JH

更新日期：2011-10-01 00:00:00

abstract：PURPOSE:Tissue partitioning is an important component of drug distribution and half-life. Protein binding and lipid partitioning together determine drug distribution. METHODS:Two structure-based models to predict partitioning into microsomal membranes are presented. An orientation-based model was developed using a mem...

journal_title：Pharmaceutical research

authors： Nagar S,Korzekwa K

更新日期：2017-03-01 00:00:00

abstract：PURPOSE:Knowledge about the uptake mechanism and subsequent intracellular routing of non-viral gene delivery systems is important for the development of more efficient carriers. In this study we compared two established cationic polymers pDMAEMA and PEI with regard to their transfection efficiency and mechanism of cell...

journal_title：Pharmaceutical research

authors： van der Aa MA,Huth US,Häfele SY,Schubert R,Oosting RS,Mastrobattista E,Hennink WE,Peschka-Süss R,Koning GA,Crommelin DJ

更新日期：2007-08-01 00:00:00

abstract：PURPOSE:Pluronics are known as inhibitors of multidrug resistance thus making tumor cells sensitive to therapeutic doses of drugs. The purpose of our study consists in revealing molecular targets of the hydrophobic poly(propylene oxide) block of pluronics in living cells and the dependence of the polymers chemosensitiz...

journal_title：Pharmaceutical research

authors： Zhirnov A,Nam E,Badun G,Romanyuk A,Ezhov A,Melik-Nubarov N,Grozdova I

更新日期：2018-09-06 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

authors： Gietz U,Alder R,Langguth P,Arvinte T,Merkle HP

更新日期：1998-09-01 00:00:00

abstract：PURPOSE:Recombinant human serum albumin (rHSA), secreted by a Pichia pastoris expression system, was purified by a fast and efficient method, the essential feature of which is strong but reversible binding of the protein to Blue Sepharose. The structural characteristics, stability, and ligand-binding properties of the ...

journal_title：Pharmaceutical research

authors： Watanabe H,Yamasaki K,Kragh-Hansen U,Tanase S,Harada K,Suenaga A,Otagiri M

更新日期：2001-12-01 00:00:00

abstract：PURPOSE:The purpose of the present study was to use the human colorectal carcinoma cell line. Caco-2, as a human intestinal epithelial model for studying the effects of cyclodextrins as absorption enhancers. METHODS:Cyclodextrins of varying sizes and physicochemical characters were investigated. The effects of the cyc...

journal_title：Pharmaceutical research

authors： Hovgaard L,Brøndsted H

更新日期：1995-09-01 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

authors： Townsend MW,Byron PR,DeLuca PP

更新日期：1990-10-01 00:00:00

abstract：PURPOSE:One of the major hurdles facing nanomedicines is the antibody production against nanoparticles that subsequently results in their opsonization and clearance by macrophages. The objective of this research was to examine and identify the sequence of a low-immunogenic peptide based on recombinant elastin-like poly...

journal_title：Pharmaceutical research

authors： Nouri FS,Wang X,Chen X,Hatefi A

更新日期：2015-09-01 00:00:00

abstract：PURPOSE:4-Phenylbutyrate (4-PBA) is expected to be a potential therapeutic for several neurodegenerative diseases. These activities require 4-PBA transport into the brain across the blood-brain barrier (BBB). The objective of the present study was to characterize the brain transport mechanism of 4-PBA through the BBB. ...

journal_title：Pharmaceutical research

authors： Lee NY,Kang YS

更新日期：2016-07-01 00:00:00

abstract：PURPOSE:There is evidence that cholesterol affects the ATPase and transport functions of P-glycoprotein (P-gp). To study the influence of cholesterol on P-gp in a well defined lipid environment, we reconstituted P-gp in egg phosphatidylcholine (PhC) and PhC/cholesterol proteoliposomes with negligible residual amounts o...

journal_title：Pharmaceutical research

authors： Bucher K,Belli S,Wunderli-Allenspach H,Krämer SD

更新日期：2007-11-01 00:00:00

abstract：PURPOSE:The specific interactions between three lectin-latex conjugates and different structures of rat intestinal mucosa have been studied ex vivo. METHODS:These systems were prepared by covalent coupling of different ligands, i.e., tomato lectin (TL), asparagus pea lectin (AL), mycoplasma gallisepticum lectin (ML), ...

journal_title：Pharmaceutical research

authors： Irache JM,Durrer C,Duchêne D,Ponchel G

更新日期：1996-11-01 00:00:00

abstract：:New generation vaccines, particularly those based on recombinant proteins and DNA, are likely to be less reactogenic than traditional vaccines but are also less immunogenic. Therefore, there is an urgent need for the development of new and improved vaccine adjuvants. Adjuvants can be broadly separated into two classes...

journal_title：Pharmaceutical research

authors： Singh M,O'Hagan DT

更新日期：2002-06-01 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

authors： Kagatani S,Inaba N,Fukui M,Sonobe T

更新日期：1998-01-01 00:00:00

abstract：:Pharmacokinetic-pharmacodynamic modeling algorithms, in general, rely on hysteresis minimization techniques that assume time-invariant pharmacodynamics (constant biophase concentration-effect relationships). When time-variant pharmacodynamics are observed, a specific model for tolerance or sensitization is required. H...

journal_title：Pharmaceutical research

authors： Gastonguay MR,Schwartz SL

更新日期：1994-12-01 00:00:00

abstract：PURPOSE:To investigate the influence of primary crystallization conditions on the mechanical properties and secondary processing behaviour of fluticasone propionate (FP) for carrier based dry powder inhaler (DPI) formulations. METHODS:Young's modulus of FP crystals produced using different anti-solvents was determined...

journal_title：Pharmaceutical research

authors： Kubavat HA,Shur J,Ruecroft G,Hipkiss D,Price R

更新日期：2012-04-01 00:00:00

abstract：PURPOSE:The purpose of this study was to use a replicate designed trial to assess the overall, intra- and inter-subject variabilities in pharmacokinetic parameters of CGP 33101 after oral administration of tablets relative to that of powder suspended in water, and to determine the relative proportion of the intra-subje...

journal_title：Pharmaceutical research

authors： Cheung WK,Kianifard F,Wong A,Mathieu J,Cook T,John V,Redalieu E,Chan K

更新日期：1995-12-01 00:00:00

abstract：PURPOSE:Propofol is a widely used anesthetic agent with highly desirable fast "on" and "off" effects. It is currently formulated as lipid emulsions, which are known to support microbial growth. In this study, a novel, lipid-free nanodispersion formulation of propofol was characterized. METHODS:The formulation was eval...

journal_title：Pharmaceutical research

authors： Chen H,Zhang Z,Almarsson O,Marier JF,Berkovitz D,Gardner CR

更新日期：2005-03-01 00:00:00

abstract：PURPOSE:In principle, maximum transepidermal fluxes of solutes should be similar for different vehicles, except when the solute or vehicle modifies the skin. Here we estimated maximum flux, stratum corneum solubility, diffusivity and permeability coefficient for a range of similarly sized phenolic compounds with varyin...

journal_title：Pharmaceutical research

authors： Zhang Q,Li P,Liu D,Roberts MS

更新日期：2013-01-01 00:00:00

abstract：:Seven healthy, male volunteers were entered into a randomized, open crossover study of the gastrointestinal transit of two enteric-coated 500-mg naproxen tablets. Two radiolabeled tablets were given to each volunteer on two occasions separated by 7 days, once in the fasted state and once after breakfast. Radiolabeling...

journal_title：Pharmaceutical research

authors： Wilding IR,Hardy JG,Sparrow RA,Davis SS,Daly PB,English JR

更新日期：1992-11-01 00:00:00

abstract：PURPOSE:The objective of this study was to develop and characterize long-circulating, biodegradable, and biocompatible nanoparticulate formulation as an intracellular delivery vehicle. METHODS:Poly(ethylene glycol) (PEG)-modified gelatin was synthesized by reacting Type-B gelatin with PEG-epoxide. The nanoparticles, p...

journal_title：Pharmaceutical research

authors： Kaul G,Amiji M

更新日期：2002-07-01 00:00:00

abstract：PURPOSE:To compare the physical stability of amorphous molecular level solid dispersions of nifedipine and felodipine, in the presence of poly(vinylpyrrolidone) (PVP) and small amounts of moisture. METHODS:Thin amorphous films of nifedipine and felodipine and amorphous molecular level solid dispersions with PVP were s...

journal_title：Pharmaceutical research

authors： Marsac PJ,Konno H,Rumondor AC,Taylor LS

更新日期：2008-03-01 00:00:00

abstract：PURPOSE:PHBHHx (poly(3-hydroxybutyrate-co-3-hydroxyhexanoate)) is an excellent biomaterial for tissue repair. Here, we aim to develop a PHBHHx-based three-dimensional (3D) scaffold system for sustained delivery of proteins (insulin serves as a model protein). METHODS:The insulin-phospholipid complex (INS-PLC) was prep...

journal_title：Pharmaceutical research

authors： Peng Q,Yang YJ,Zhang T,Wu CY,Yang Q,Sun X,Gong T,Zhang L,Zhang ZR

更新日期：2013-04-01 00:00:00

abstract：PURPOSE:Pancreatic cancer remains the fourth most common cause of cancer-related death in the United States. Therefore, novel strategies for the prevention and/or treatment are urgently needed. Genistein has been found to be responsible for lowering the rate of pancreatic cancer. However, the molecular mechanisms by wh...

journal_title：Pharmaceutical research

authors： Wang Z,Ahmad A,Banerjee S,Azmi A,Kong D,Li Y,Sarkar FH

更新日期：2010-06-01 00:00:00

abstract：:Aucubin, a promising hepatoprotecting iridoid glucoside, was given intravenously (iv), orally (po), intraperitoneally (ip), and hepatoportally (pv) to rats. A linear pharmacokinetic behavior was obtained after iv administation of 400-400 mg/kg of aucubin. The half-life of aucubin in the postdistributive phase (t1/2, b...

journal_title：Pharmaceutical research

authors： Suh NJ,Shim CK,Lee MH,Kim SK,Chang IM

更新日期：1991-08-01 00:00:00

abstract：:The effects of skin storage, skin preparation, skin pretreatment with a penetration enhancer, and skin barrier removal by adhesive tape-stripping on the concurrent cutaneous transport and metabolism of nitroglycerin (GTN) have been studied in vitro using hairless mouse skin. Storing the skin for 10 days at 4 degrees C...

journal_title：Pharmaceutical research

authors： Higo N,Hinz RS,Lau DT,Benet LZ,Guy RH

更新日期：1992-03-01 00:00:00

abstract：PURPOSE:Hydrogen/deuterium (H/D) exchange over a range of temperatures suggests a protein structural/mobility transition in the solid state below the system glass transition temperature (Tg). The purpose of this study was to determine whether solid-state protein stability correlates with the difference between storage ...

journal_title：Pharmaceutical research

authors： Fang R,Obeidat W,Pikal MJ,Bogner RH

更新日期：2020-08-13 00:00:00