Scale of health: indices of safety and efficacy in the evolving environment of large biological datasets.

abstract：PURPOSE:To examine the theoretical/practical utility of the liver-to-blood partition coefficient (Kpuu) for predicting drug-drug interactions (DDIs), and compare the Kpuu-approach to the extended clearance concept AUCR-approach. METHODS:The Kpuu relationship was derived from first principles. Theoretical simulations i...

journal_title：Pharmaceutical research

authors： Sodhi JK,Liu S,Benet LZ

更新日期：2020-03-25 00:00:00

abstract：PURPOSE:Indocyanine green (ICG), an FDA-approved near infrared (NIR) dye, has potential application as a contrast agent for tumor detection. Because ICG binds strongly to plasma proteins and exhibits aqueous, photo, and thermal instability, its current applications are largely limited to monitoring blood flow. To addre...

journal_title：Pharmaceutical research

authors： Kim TH,Chen Y,Mount CW,Gombotz WR,Li X,Pun SH

更新日期：2010-09-01 00:00:00

abstract：PURPOSE:To determine the different conformations of the acyloxyalkoxy-linked cyclic prodrug 1 of the model hexapeptide 2 in solution and to investigate the relationship between these solution conformations and the cellular permeability characteristics of this prodrug. METHODS:Two-dimensional Homonuclear Hartmann-Hahn ...

journal_title：Pharmaceutical research

authors： Gangwar S,Jois SD,Siahaan TJ,Vander Velde DG,Stella VJ,Borchardt RT

更新日期：1996-11-01 00:00:00

abstract：:Assessment of bioavailability/bioequivalence generally relies on the comparison of rate and extent of drug absorption between products. Rate of absorption is commonly expressed by peak concentration (C(max)) and time to peak concentration (T(max)), although these parameters are indirect measures of absorption rate. Re...

journal_title：Pharmaceutical research

authors： Chen ML,Davit B,Lionberger R,Wahba Z,Ahn HY,Yu LX

更新日期：2011-08-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate the effect of cyclodextrins (beta-CD, HP-beta-CD and (SBE)7m-beta-CD), and co-administration of a water-soluble polymer (HPMC) and cyclodextrins, on the oral bioavailability of glibenclamide in dogs. METHODS:Effects of cyclodextrins on the aqueous solubility of glibencl...

journal_title：Pharmaceutical research

authors： Savolainen J,Järvinen K,Taipale H,Jarho P,Loftsson T,Järvinen T

更新日期：1998-11-01 00:00:00

abstract：PURPOSE:Orally absorbable anticancer medications have great advantages for conventional cancer therapies to patients. Here we evaluated the potent anticancer effect of orally absorbable LHD, a chemical conjugate of low-molecular-weight heparin and deoxycholic acid, on tumor graft growth models. METHODS:We characterize...

journal_title：Pharmaceutical research

authors： Lee DY,Lee SW,Kim SK,Lee M,Chang HW,Moon HT,Byun Y,Kim SY

更新日期：2009-12-01 00:00:00

abstract：PURPOSE:To develop a streamlined strategy for pharmaceutical cocrystal preparation without knowledge of the stoichiometric ratio by preparing and characterizing the cocrystals of myricetin (MYR) with four cocrystal coformers (CCF). METHODS:An approach based on the phase solubility diagram (PSD) was used for MYR cocrys...

journal_title：Pharmaceutical research

authors： Hong C,Xie Y,Yao Y,Li G,Yuan X,Shen H

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:Little is known about the affinity and stability of 99mTc-labeled 2-methoxyisobutylisonitrile (99mTc-MIBI) and tetrofosmin (99mTc-TF) for imaging of multiple drug resistance transporters in cancer. We examined the affinity of 99mTc-labeled compounds for these transporters and their stability. METHODS:99mTc-...

journal_title：Pharmaceutical research

authors： Kobayashi M,Tsujiuchi T,Okui Y,Mizutani A,Nishi K,Nakanishi T,Nishii R,Fukuchi K,Tamai I,Kawai K

更新日期：2018-11-29 00:00:00

abstract：:A fluorescence measurement system and methods of data analysis were developed to measure rapid kinetics of transdermal transport in vitro. Three variations on the technique were demonstrated, where the receptor compartment concentration was determined by: 1) fluorescence measurements of aliquots removed at discrete ti...

journal_title：Pharmaceutical research

authors： Pliquett U,Prausnitz MR,Chizmadzhev YA,Weaver JC

更新日期：1995-04-01 00:00:00

abstract：PURPOSE:To improve upon the theory of reasoned action and apply it to pharmaceutical research, we investigated the effects of relevant appraisals attributes, and past behavior of physicians on the use of drug information sources. We also examined the moderating effects of practice characteristics. METHODS:A mail quest...

journal_title：Pharmaceutical research

authors： Gaither CA,Bagozzi RP,Ascione FJ,Kirking DM

更新日期：1997-10-01 00:00:00

abstract：PURPOSE:Several phenomena in tablets indicate that an inhomogeneous pore distribution is formed during the compaction process. Examples are lamination and the capping of corners. In order to gain an understanding of the relation between structure and compact properties, analyzing the structure in a location dependent m...

journal_title：Pharmaceutical research

authors： Wu YS,Frijlink HW,van Vliet LJ,Stokroos I,van der Voort Maarschalk K

更新日期：2005-08-01 00:00:00

abstract：:The effect of different concentrations of polyvinyl alcohol 14000 and 72000 (PVA 14 and 72) on the activity of betamethasone and phenylephrine hydrochloride in the rabbit eye was investigated. The polymer of higher molecular weight exerts a more pronounced effect at relatively lower viscosities. Effects on the intraoc...

journal_title：Pharmaceutical research

authors： Kassem MA,Attia MA,Habib FS,Mohamed AR

更新日期：1986-08-01 00:00:00

abstract：PURPOSE:To assess the blood-brain barrier (BBB) permeability of 12 clinically-used drugs in mdr1a(+/+) and mdr1a(-/-) mice, and investigate the influence of lipophilicity, nonspecific brain tissue binding, and P-gp-mediated efflux on the rate of brain uptake. METHODS:The BBB partition coefficient (PS) was determined u...

journal_title：Pharmaceutical research

authors： Zhao R,Kalvass JC,Pollack GM

更新日期：2009-07-01 00:00:00

abstract：:Significant efforts are made to characterize molecular liabilities and degradation of the drug substance (DS) and drug product (DP) during various product life-cycle stages. The in vivo fate of a therapeutic protein is usually only considered in terms of pharmacokinetics (PKs) and pharmacodynamics (PDs). However, the ...

journal_title：Pharmaceutical research

authors： Schuster J,Koulov A,Mahler HC,Detampel P,Huwyler J,Singh S,Mathaes R

更新日期：2020-01-03 00:00:00

abstract：PURPOSE:The purpose of this study was to develop a new computational fluid dynamics (CFD)-based model of the complex transport and droplet drying kinetics within a laboratory-scale spray dryer, and relate CFD-predicted drying parameters to powder aerosolization metrics from a reference dry powder inhaler (DPI). METHOD...

journal_title：Pharmaceutical research

authors： Longest PW,Farkas D,Hassan A,Hindle M

更新日期：2020-05-21 00:00:00

abstract：PURPOSE:To develop a new intradermal antigen delivery system by coating microneedle arrays with lipid bilayer-coated, antigen-loaded mesoporous silica nanoparticles (LB-MSN-OVA). METHODS:Synthesis of MSNs with 10-nm pores was performed and the nanoparticles were loaded with the model antigen ovalbumin (OVA), and coate...

journal_title：Pharmaceutical research

authors： Tu J,Du G,Reza Nejadnik M,Mönkäre J,van der Maaden K,Bomans PHH,Sommerdijk NAJM,Slütter B,Jiskoot W,Bouwstra JA,Kros A

更新日期：2017-08-01 00:00:00

abstract：PURPOSE:In this study, modulation of the immune response against diphtheria toxoid (DT) by various adjuvants in transcutaneous immunization (TCI) with microneedle array pretreatment was investigated. METHODS:TCI was performed on BALB/c mice with or without microneedle array pretreatment using DT as a model antigen co-...

journal_title：Pharmaceutical research

authors： Ding Z,Van Riet E,Romeijn S,Kersten GF,Jiskoot W,Bouwstra JA

更新日期：2009-07-01 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：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：:The topical antifungal Sch-39304 is a racemic compound comprised of two enantiomers, Sch-42427 and Sch-42426, only one of which (Sch-42427) is pharmacologically active. The pure enantiomers have a lower melting point and, therefore, a higher solubility than the racemic compound. Because of these differences in physico...

journal_title：Pharmaceutical research

authors： Wearley L,Antonacci B,Cacciapuoti A,Assenza S,Chaudry I,Eckhart C,Levine N,Loebenberg D,Norris C,Parmegiani R

更新日期：1993-01-01 00:00:00

abstract：PURPOSE:To characterize the distribution of water among various components in a powder blend using solid-state NMR spectroscopy. METHODS:Water sorption behavior of theophylline anhydrate and excipients was determined by dynamic vapor sorption (DVS) and Karl Fischer Titration (KFT) after storing them in humidity chambe...

journal_title：Pharmaceutical research

authors： Mistry P,Chakravarty P,Lubach JW

更新日期：2016-10-01 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：:Primaquine, an 8-aminoquinoline antimalarial, is shown to undergo unexpectedly rapid aromatic proton exchange with the medium. At a pH less than 4, the exchange of C-5 is so fast as to be unmeasurable by proton nmr methods. At a pH of 6-6.5 the half-time for exchange is 4 to 5 minutes. This unexpectedly high rate of e...

journal_title：Pharmaceutical research

authors： McChesney JD,Sarangan S

更新日期：1984-07-01 00:00:00

abstract：:Recently a new in vivo approach in man, using a regional intestinal perfusion technique, has been developed. The perfusion tube consists of a multichannel tube with two inflatable balloons, which are placed 10 cm apart. The tube is introduced orally and the time required for insertion and positioning of the tube is ap...

journal_title：Pharmaceutical research

authors： Lennernäs H,Ahrenstedt O,Hällgren R,Knutson L,Ryde M,Paalzow LK

更新日期：1992-10-01 00:00:00

abstract：PURPOSE:Nanocrystalline drug-polymer dispersions are of significant interest in pharmaceutical delivery. The purpose of this work is to demonstrate the applicability of methods based on two-dimensional (2D) and multinuclear solid-state NMR (SSNMR) to a novel nanocrystalline pharmaceutical dispersion of ebselen with pol...

journal_title：Pharmaceutical research

authors： Vogt FG,Williams GR

更新日期：2012-07-01 00:00:00

abstract：:High molecular weight drugs in general, and peptides in particular, are usually delivered by parenteral route because they are poorly absorbed or degraded in the gastrointestinal tract. To optimize therapy, it is desirable to search for nonparenteral routes of administration and to deliver the drug in a controlled-rel...

journal_title：Pharmaceutical research

authors： Golomb G,Avramoff A,Hoffman A

更新日期：1993-06-01 00:00:00

abstract：PURPOSE:To explore whether miR-19 is involved in the regulation of multidrug resistance (MDR), one of the main causes of breast cancer mortality, and modulates sensitivity of tumor cells to chemotherapeutic agents. METHODS:We analyzed miRNA expression levels in three MDR cell lines in comparison with their parent cell...

journal_title：Pharmaceutical research

authors： Liang Z,Li Y,Huang K,Wagar N,Shim H

更新日期：2011-12-01 00:00:00

abstract：PURPOSE:The aim of this work was to investigate the influence of the oily nucleus composition on physico-chemical properties and anesthetic activity of poly (lactide-co-glycolide) nanocapsules with benzocaine. METHODS:Nanocapsules containing benzocaine were prepared with three different oily nucleus composition and ch...

journal_title：Pharmaceutical research

authors： de Melo NF,Grillo R,Guilherme VA,de Araujo DR,de Paula E,Rosa AH,Fraceto LF

更新日期：2011-08-01 00:00:00

abstract：PURPOSE:Since glomerular filtration rate (GFR) is responsible for the elimination of a large number of water-soluble drugs, the aim of this study was to develop a semi-physiological function for GFR maturation from neonates to adults. METHODS:In the pharmacokinetic analysis (NONMEM VI) based on data of gentamicin, tob...

journal_title：Pharmaceutical research

authors： De Cock RF,Allegaert K,Brussee JM,Sherwin CM,Mulla H,de Hoog M,van den Anker JN,Danhof M,Knibbe CA

更新日期：2014-10-01 00:00:00

abstract：:Excessive production of reactive oxygen species by alveolar macrophages (AMs) in response to inhaled toxic substances is a major cause of oxidative lung injury. Therapeutic approaches designed to protect the lungs from oxidative injury by administering native antioxidant enzymes such as catalase and superoxide dismuta...

journal_title：Pharmaceutical research

authors： Harrison J,Shi X,Wang L,Ma JK,Rojanasakul Y

更新日期：1994-08-01 00:00:00