Structural interpretation in composite systems using powder X-ray diffraction: applications of error propagation to the pair distribution function.

abstract：PURPOSE:To describe a computational tool to calculate molecular descriptors of potential application in ADME virtual screening of antitumor Pt(II) drug candidates. METHODS:The multistep computational procedure consists in (a) building and optimization (PM3) of the 3D structures of the investigated complexes, (b) param...

journal_title：Pharmaceutical research

authors： Caron G,Ravera M,Ermondi G

更新日期：2011-03-01 00:00:00

abstract：PURPOSE:To study epidermal and polyethylene membrane penetration and retention of the sunscreen benzophenone-3 (BP) from a range of single solvent vehicles and evaluate solvent effects on permeability parameters. METHODS:The solubility of BP was measured in a number of solvents. Penetration of BP across human epidermi...

journal_title：Pharmaceutical research

authors： Jiang R,Benson HA,Cross SE,Roberts MS

更新日期：1998-12-01 00:00:00

abstract：PURPOSE:Multidrug and toxin extrusion proteins (MATEs) are multispecific organic cation transporters mediating the efflux of various cationic drugs into the urine. The present study aimed at identifying endogenous compounds in human plasma and urine specimens as biomarkers to evaluate drug interactions involving MATEs ...

journal_title：Pharmaceutical research

authors： Kato K,Mori H,Kito T,Yokochi M,Ito S,Inoue K,Yonezawa A,Katsura T,Kumagai Y,Yuasa H,Moriyama Y,Inui K,Kusuhara H,Sugiyama Y

更新日期：2014-01-01 00:00:00

abstract：:To achieve time-controlled or site-specific drug delivery in the gastrointestinal tract, a sigmoidal release system (SRS) was developed, which achieved a prolonged lag time, followed by rapid release. The theophylline beads with a thick Eudragit RS film coating showed very low drug release in water, whereas the releas...

journal_title：Pharmaceutical research

authors： Narisawa S,Nagata M,Danyoshi C,Yoshino H,Murata K,Hirakawa Y,Noda K

更新日期：1994-01-01 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:The acne skin is characteristic of a relatively lower pH microenvironment compared to the healthy skin. The aim of this work was to utilize such pH discrepancy as a site-specific trigger for on-demand topical adapalene delivery. METHODS:The anti-acne agent, adapalene, was encapsulated in acid-responsive polyme...

journal_title：Pharmaceutical research

authors： Guo C,Khengar RH,Sun M,Wang Z,Fan A,Zhao Y

更新日期：2014-11-01 00:00:00

abstract：PURPOSE:To prepare acylated exenatide analogues and investigate their biological properties for guiding the development of PLGA formulations of exenatide. METHODS:The acylated exenatide analogues were prepared by reaction with glycolic acid (GA), one constitutional unit of PLGA, and characterized by HPLC-MS/MS and Cir...

journal_title：Pharmaceutical research

authors： Liang R,Li X,Zhang R,Shi Y,Wang A,Chen D,Sun K,Liu W,Li Y

更新日期：2014-08-01 00:00:00

abstract：PURPOSE:Present study assessed the influence of gallate esterification on the anti-cancer activity of procyanidin B2 (B2) in androgen-dependent human prostate carcinoma LNCaP cells employing B2-3,3'-di-O-gallate (B2-G(2)), two mono-gallate esters B2-3-O-gallate (B2-3G) and B2-3'-O-gallate (B2-3'G) and the parent compou...

journal_title：Pharmaceutical research

authors： Chou SC,Kaur M,Thompson JA,Agarwal R,Agarwal C

更新日期：2010-04-01 00:00:00

abstract：:The new generation of nanotechnology-based drug formulations is challenging the accepted ways of cancer treatment. Multi-functional nanomaterial constructs have the capability to be delivered directly to the tumor site and eradicate cancer cells selectively, while sparing healthy cells. Tailoring of the nano-construct...

journal_title：Pharmaceutical research

authors： Farrell D,Ptak K,Panaro NJ,Grodzinski P

更新日期：2011-02-01 00:00:00

abstract：PURPOSE:The objective of this study was to develop and evaluate a pulsatile drug delivery system based on an impermeable capsule body filled with drug and an erodible plug placed in the opening of the capsule body. METHODS:The erodible plugs were either prepared by direct compression followed by placing the tablets in...

journal_title：Pharmaceutical research

authors： Krögel I,Bodmeier R

更新日期：1998-03-01 00:00:00

abstract：:An on-line simultaneous assay for the enantiomers of verapamil (VA) and its three metabolites in plasma was developed with column-switching HPLC. This system consists of an ovomucoid protein chiral stationary phase coupled to an achiral reversed-phase column via a dilution tube and a trapping column. The reversed-phas...

journal_title：Pharmaceutical research

authors： Oda Y,Asakawa N,Kajima T,Yoshida Y,Sato T

更新日期：1991-08-01 00:00:00

abstract：PURPOSE:To compare the permeation characteristics of amide bond-containing HIV-1 protease inhibitors and their pyrrolinone-containing counterparts across Caco-2 cell monolayers, a model of the intestinal mucosa. METHODS:Transepithelial transport and cellular uptake of three pairs of amide bond-containing and pyrrolino...

journal_title：Pharmaceutical research

authors： Sudoh M,Pauletti GM,Yao W,Moser W,Yokoyama A,Pasternak A,Sprengeler PA,Smith AB 3rd,Hirschmann R,Borchardt RT

更新日期：1998-05-01 00:00:00

abstract：PURPOSE:The purpose of this study was to establish a useful methodology, possibly providing information on the stoichiometry of pharmaceutical drug salts obtained from salt screening by using a multiwell plate and a Raman microscope. METHODS:Tamoxifen salt screening was conducted with monobasic and polybasic acids on ...

journal_title：Pharmaceutical research

authors： Kojima T,Onoue S,Murase N,Katoh F,Mano T,Matsuda Y

更新日期：2006-04-01 00:00:00

abstract：PURPOSE:To investigate the influence of nanocarrier molecular size and shape on breast duct retention in normal rats using a non-invasive optical imaging method. METHODS:Fluorescein-labeled PEG nanocarriers of different molecular weights and shapes (linear, two-arm, four-arm, and eight-arm) were intraductally administ...

journal_title：Pharmaceutical research

authors： Singh Y,Gao D,Gu Z,Li S,Rivera KA,Stein S,Love S,Sinko PJ

更新日期：2012-09-01 00:00:00

abstract：:The dose dependency of carbamazepine pharmacokinetics was characterized in rats, a common test animal for antiepileptic drug efficacy. With a randomized Latin square schedule, 5, 10, and 20 mg/kg doses of carbamazepine were injected intravenously into six Sprague-Dawley rats followed by the administration of a 5 or 10...

journal_title：Pharmaceutical research

authors： Remmel RP,Sinz MW,Cloyd JC

更新日期：1990-05-01 00:00:00

abstract：PURPOSE:This work describes the synthesis of block co-polymeric micelles, methoxy-poly(ethylene glycol)-poly(D,L-lactide) (mPEG-PLA) to encapsulate Curcumin (CUR), thereby improving the dispersibility and chemical stability of curcumin, prolonging its cellular uptake and enhancing its bioavailability. METHODS:CUR-mPEG...

journal_title：Pharmaceutical research

authors： Kumari P,Swami MO,Nadipalli SK,Myneni S,Ghosh B,Biswas S

更新日期：2016-04-01 00:00:00

abstract：PURPOSE:Recombinant human platelet glycoprotein Ibalpha-immunoglobulin G1 chimeric proteins (GPIbalpha-Ig) have varying levels of anti-thrombotic activities based on their ability to compete for platelet mediated adhesion to von Willebrand Factor (vWF). Valine substituted GPIbalpha-Ig chimeras, at certain position, inc...

journal_title：Pharmaceutical research

authors： Wang Q,Shorten D,Xu X,Shaw GD,Schaub RG,Shea C,Brooks J,Sako D,Wiswall E,Xu J,Szklut P,Patel VS

更新日期：2006-08-01 00:00:00

abstract：PURPOSE:Type I collagen accumulates during liver fibrosis primarily because α-complex protein-2 (αCP(2)), encoded by the poly(rC) binding protein 2 (PCBP2) gene, binds to the 3' end of the collagen mRNA and increases its half-life. This study aimed to reverse the pro-fibrogenic effect of alcohol on hepatic stellate cel...

journal_title：Pharmaceutical research

authors： Shukla RS,Qin B,Wan YJ,Cheng K

更新日期：2011-12-01 00:00:00

abstract：:The transport characteristics of the renin inhibitor ((3S,4S)-4-[N-morpholinoacetyl-(1-naphthyl)-L-alanyl-N-methyl-(4-t hiazolyl)-L- alanyl]amino-3-hydroxy-5-cyclohexyl-1-(4-pyridyl)-1-pentanone; CH3-18) in rat small intestinal brush-border membrane vesicles (BBMV) were examined by a rapid filtration technique. The up...

journal_title：Pharmaceutical research

authors： Hashimoto N,Fujioka T,Toyoda T,Muranushi N,Hirano K

更新日期：1994-10-01 00:00:00

abstract：PURPOSE:Because interleukin-10 (IL-10) seems a promising new antifibrotic drug, we investigated the pharmacokinetic and biodistribution profile of this potent therapeutic cytokine in rats with extensive liver fibrosis (BDL-3). IL-10 receptor expression was also determined in relation to these aspects. METHODS:To study...

journal_title：Pharmaceutical research

authors： Rachmawati H,Beljaars L,Reker-Smit C,Van Loenen-Weemaes AM,Hagens WI,Meijer DK,Poelstra K

更新日期：2004-11-01 00:00:00

abstract：PURPOSE:A series of studies was conducted to evaluate the preclinical pharmacokinetics of SB-239063 (trans-1-(4-hydroxycyclohexyl)-4-(4-fluorophenyl)-5-[(2-methoxy)pyrimidin-4-yl] imidazole), a potent and selective p38 MAP kinase inhibitor. METHODS:SB-239063 was administered both i.v. and p.o. in the rat, dog, cynomol...

journal_title：Pharmaceutical research

authors： Ward KW,Proksch JW,Azzarano LM,Salyers KL,McSurdy-Freed JE,Molnar TM,Levy MA,Smith BR

更新日期：2001-09-01 00:00:00

abstract：PURPOSE:For the assessment of bioequivalence it is assumed that drug clearance in each subject on each of the study days is the same and any observed differences in AUC and/or Cmax between a brand and generic formulation are due to differences in bioavailability. We hypothesized that this assumption was invalid for hig...

journal_title：Pharmaceutical research

authors： Tsang YC,Pop R,Gordon P,Hems J,Spino M

更新日期：1996-06-01 00:00:00

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：PURPOSE:To study the physical and release properties of different molecular weight (MW) pH- and temperature-responsive statistical terpolymers and beads of N-isopropylacrylamide (NIPAAm), butylmethacrylate (BMA) and acrylic acid (AA). METHODS:Random terpolymers of varying MW were synthesized with NIPAAm/BMA/AA of feed...

journal_title：Pharmaceutical research

authors： Ramkissoon-Ganorkar C,Gutowska A,Liu F,Baudys M,Kim SW

更新日期：1999-06-01 00:00:00

abstract：PURPOSE:1. The assessment of the role of hair follicles and sweat glands in skin resistance and percutaneous iontophoretic flux of 9-desglycinamide, 8-arginine vasopressin (DGAVP) by comparing two skin species: human stratum corneum which contained hair follicles, sweat and sebaceous glands, and shed snake skin which l...

journal_title：Pharmaceutical research

authors： Craane-van Hinsberg WH,Verhoef JC,Bax LJ,Junginger HE,Boddé HE

更新日期：1995-10-01 00:00:00

abstract：PURPOSE:To investigate the effect of surface functionalization of mesoporous silica nanoparticles (MSN) on crystallization, loading, release and activity of mitoxantrone (MTX). METHODS:Thiol-, amine-, and mixed thiol/amine-functionalized MSN were synthesized and characterized by electron microscopy, thermogravimetry, ...

journal_title：Pharmaceutical research

authors： Wani A,Muthuswamy E,Savithra GH,Mao G,Brock S,Oupický D

更新日期：2012-09-01 00:00:00

abstract：PURPOSE:This study demonstrates the nasal administration (NA) of nanoemulsions complexed with the plasmid encoding for IDUA protein (pIDUA) as an attempt to reach the brain aiming at MPS I gene therapy. METHODS:Formulations composed of DOPE, DOTAP, MCT (NE), and DSPE-PEG (NE-PEG) were prepared by high-pressure homogen...

journal_title：Pharmaceutical research

authors： Schuh RS,Bidone J,Poletto E,Pinheiro CV,Pasqualim G,de Carvalho TG,Farinon M,da Silva Diel D,Xavier RM,Baldo G,Matte U,Teixeira HF

更新日期：2018-09-26 00:00:00

abstract：PURPOSE:We have already demonstrated that the HMG-CoA reductase inhibitor, pravastatin is actively taken up by isolated rat hepatocytes via a multispecific anion transporter (Yamazaki et al., Am. J. Physiol. 264, G36-44, (1993)). We further attempted the quantitative evaluation of this uptake in different experimental ...

journal_title：Pharmaceutical research

authors： Ishigami M,Tokui T,Komai T,Tsukahara K,Yamazaki M,Sugiyama Y

更新日期：1995-11-01 00:00:00

abstract：PURPOSE:To develop novel biomineral-binding liposomes (BBL) for the prevention of orthopedic implant associated osteomyelitis. METHODS:A biomineral-binding lipid, alendronate-tri(ethyleneglycol)-cholesterol conjugate (ALN-TEG-Chol), was synthesized through Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition (a versatile...

journal_title：Pharmaceutical research

authors： Liu XM,Zhang Y,Chen F,Khutsishvili I,Fehringer EV,Marky LA,Bayles KW,Wang D

更新日期：2012-11-01 00:00:00

abstract：PURPOSE:Prostaglandin E(1) (PGE(1)) is an effective treatment for peripheral vascular diseases. The encapsulation of PGE(1) in nanoparticles for its sustained-release would improve its therapeutic effect and quality of life (QOL) of patients. METHODS:In order to encapsulate PGE(1) in nanoparticles prepared with a poly...

journal_title：Pharmaceutical research

authors： Takeda M,Maeda T,Ishihara T,Sakamoto H,Yuki K,Takasaki N,Nishimura F,Yamashita T,Tanaka K,Takenaga M,Igarashi R,Higaki M,Yamakawa N,Okamoto Y,Ogawa H,Otsuka M,Mizushima Y,Mizushima T

更新日期：2009-07-01 00:00:00