Chemical and physical stability of chimeric L6, a mouse-human monoclonal antibody.

abstract：PURPOSE:We reported that suramin produced chemosensitization at nontoxic doses. This benefit was lost at the approximately 10-fold higher, maximally tolerated doses (MTD). The aim of the current study was to identify in patients the chemosensitizing suramin dose that delivers 10-50 microM plasma concentrations over 48 ...

journal_title：Pharmaceutical research

authors： Chen D,Song SH,Wientjes MG,Yeh TK,Zhao L,Villalona-Calero M,Otterson GA,Jensen R,Grever M,Murgo AJ,Au JL

更新日期：2006-06-01 00:00:00

abstract：PURPOSE:In vitro in vivo correlation (IVIVC) is a biopharmaceutical tool recommended for use in formulation development. When validated, IVIVC can be used to set dissolution limits and, based on the dissolution limits, as a surrogate for an in vivo study. The purpose of this paper is to study the various methods used t...

journal_title：Pharmaceutical research

authors： Roudier B,Davit BM,Beyssac E,Cardot JM

更新日期：2014-09-01 00:00:00

abstract：PURPOSE:To examine whether the glass transition temperature (Tg) of freeze-dried formulations containing polymer excipients can be accurately predicted by molecular dynamics simulation using software currently available on the market. Molecular dynamics simulations were carried out for isomaltodecaose, a fragment of de...

journal_title：Pharmaceutical research

authors： Yoshioka S,Aso Y,Kojima S

更新日期：2003-06-01 00:00:00

abstract：:Previous work from this laboratory showed site-dependent variations in the apparent permeability of insulin as measured using the everted rat gut sac technique, with the greatest permeability in the distal jejunum and the lowest in the duodenum (5). To quantify better the rate and extent of insulin absorption from the...

journal_title：Pharmaceutical research

authors： Schilling RJ,Mitra AK

更新日期：1992-08-01 00:00:00

abstract：PURPOSE:Drug transfer into milk is a general concern during lactation. Because data are limited in human subjects, particularly for new drugs, experimental animal models of lactational drug transfer are critical. This study analyzed drug transfer into milk in a mouse model, as well as the contribution of similar and di...

journal_title：Pharmaceutical research

authors： Ito N,Ito K,Koshimichi H,Hisaka A,Honma M,Igarashi T,Suzuki H

更新日期：2013-09-01 00:00:00

abstract：:A novel application of attenuated total reflectance IR spectroscopy (ATR-IR) was used to monitor the outer several microns of the stratum corneum (SC) and, thereby, demonstrate enhanced percutaneous absorption in vivo in man. 4-Cyanophenol (CP) as a model permeant yielded a unique IR signal, distinct from those of the...

journal_title：Pharmaceutical research

authors： Mak VH,Potts RO,Guy RH

更新日期：1990-08-01 00:00:00

abstract：PURPOSE:To study the relative thermodynamic and kinetic stabilities of neotame anhydrate polymorphs A, D, F, and G, and to develop a quantitative method for analyzing polymorphic mixtures of A and G by powder X-ray diffractometry (PXRD). METHODS:Based on the melting points, heats of fusion, and densities of the four p...

journal_title：Pharmaceutical research

authors： Dong Z,Munson EJ,Schroeder SA,Prakash I,Grant DJ

更新日期：2002-09-01 00:00:00

abstract：PURPOSE:Paclitaxel is a first-line drug for the therapy of lung cancer, however, drug resistance is a serious limiting factor, related to overexpression of anti-apoptotic proteins like survivin. To overcome this phenomenon, developing novel ultrasound responsive nanobubbles - nanosized drug delivery system- for the del...

journal_title：Pharmaceutical research

authors： Akbaba H,Erel-Akbaba G,Kotmakçı M,Başpınar Y

更新日期：2020-08-05 00:00:00

abstract：:The delivery of therapeutic nucleic acids to neurons has the potential to treat neurological disease and spinal cord injury. While select viral vectors have shown promise as gene carriers to neurons, their potential as therapeutic agents is limited by their toxicity and immunogenicity, their broad tropism, and the cos...

journal_title：Pharmaceutical research

authors： Bergen JM,Park IK,Horner PJ,Pun SH

更新日期：2008-05-01 00:00:00

abstract：PURPOSE:To develop a non-viral gene delivery system in the form of an oil-in-water (o/w) lipid emulsion. METHOD:Cationic lipid emulsions were formulated with soybean oil, 1,2-dioleoyl-sn-glycero-3-trimethylammonium-propane (DOTAP) as a cationic emulsifier and other co-emulsifiers. The physical characteristics of the l...

journal_title：Pharmaceutical research

authors： Yi SW,Yune TY,Kim TW,Chung H,Choi YW,Kwon IC,Lee EB,Jeong SY

更新日期：2000-03-01 00:00:00

abstract：PURPOSE:Our previous studies showed that the mRNA level of human organic anion transporter (hOAT) 3 in the kidney was correlated with the rate of elimination of an anionic antibiotic cefazolin. However, the correlation coefficient was not so high. In the present study, therefore, we enrolled more patients to examine wh...

journal_title：Pharmaceutical research

authors： Sakurai Y,Motohashi H,Ogasawara K,Terada T,Masuda S,Katsura T,Mori N,Matsuura M,Doi T,Fukatsu A,Inui K

更新日期：2005-12-01 00:00:00

abstract：:A new technique has been developed to calculate rapidly the solid-state room-temperature degradation rate of drugs and drug candidates. The technique utilizes measurements of the initial rate of heat output at several elevated temperatures by isothermal calorimetry and the degradation rate of the compound determined a...

journal_title：Pharmaceutical research

authors： Koenigbauer MJ,Brooks SH,Rullo G,Couch RA

更新日期：1992-07-01 00:00:00

abstract：PURPOSE:The current study aimed to examine the pharmaceutical applications of the focused-ion-beam (FIB) in the inhalation aerosol field, particularly to particle porosity determination (i.e. percentage of particles having a porous interior). MATERIALS AND METHODS:The interior of various spray dried particles (bovine ...

journal_title：Pharmaceutical research

authors： Heng D,Tang P,Cairney JM,Chan HK,Cutler DJ,Salama R,Yun J

更新日期：2007-09-01 00:00:00

abstract：:An open, randomized, six-way crossover study was conducted in 12 healthy males to assess pharmacokinetics and bioinversion of ibuprofen enantiomers. The mean plasma terminal half-life (t1/2) of R(-)ibuprofen was 1.74 hr when intravenously infused as a racemic mixture and was 1.84 hr when intravenously infused alone. T...

journal_title：Pharmaceutical research

authors： Cheng H,Rogers JD,Demetriades JL,Holland SD,Seibold JR,Depuy E

更新日期：1994-06-01 00:00:00

abstract：PURPOSE:This work explores the distribution of water and its effects on molecular mobilities in poly(vinylpyrrolidone) (PVP) glasses using molecular dynamics (MD) simulation technology. METHODS:PVP glasses containing 0.5% and 10% w/w water and a small amount of ammonia and Phe-Asn-Gly were generated. Physical aging pr...

journal_title：Pharmaceutical research

authors： Xiang TX,Anderson BD

更新日期：2005-08-01 00:00:00

abstract：PURPOSE:To compare the ability of alkyl-aryl isothiocyanates (ITCs) to increase the activities of the Phase 2 detoxification enzymes NAD[P]H:quinone acceptor oxidoreductase 1 (NQO1) and glutathione S-transferases (GST) in rat tissues in vivo and in cells in vitro. MATERIALS AND METHODS:Twelve alkyl-aryl ITCs and the f...

journal_title：Pharmaceutical research

authors： Munday R,Zhang Y,Munday CM,Bapardekar MV,Paonessa JD

更新日期：2008-09-01 00:00:00

abstract：:The pentahydrate (alpha form) of cefazolin sodium (CEZ) exhibited sharp X-ray diffraction peaks, while the dehydrated alpha form showed weak but distinct diffraction peaks. As expected the amorphous form exhibited a diffuse and halo diffraction pattern. The X-ray procedure to estimate the degree of crystallinity of CE...

journal_title：Pharmaceutical research

authors： Kamat MS,Osawa T,DeAngelis RJ,Koyama Y,DeLuca PP

更新日期：1988-07-01 00:00:00

abstract：PURPOSE:The aim was to replace the traditional 21-day Caco-2 permeability protocol by a more high-throughput assay. METHODS:Caco-2 cells were seeded at high density in 96-well plates in novel cell culture boxes. After 7 days, drug permeability studies were performed. Samples were analyzed by a new UV detection method....

journal_title：Pharmaceutical research

authors： Alsenz J,Haenel E

更新日期：2003-12-01 00:00:00

abstract：:The effect of buprenorphine on bremazocine-induced diuresis was tested in the rat to determine the nature of buprenorphine's action at the ϰ opioid receptor. Both morphine-tolerant and naive rats were used to account for possible antidiuretic effects of buprenorphine at the µ site. Separate experiments established tha...

journal_title：Pharmaceutical research

authors： Richards ML,Sadée W

更新日期：1985-07-01 00:00:00

abstract：PURPOSE:The possibility of direct delivery of steroids through the skin to the trachea and the effect of iontophoresis on delivery efficacy were evaluated after the application of an ionic steroidal prodrug, prednisolone sodium succinate (PS-Na), to the throat skin. METHODS:Fluorescein sodium salt (FL-Na) and PS-Na we...

journal_title：Pharmaceutical research

authors： Ishii H,Suzuki T,Todo H,Kamimura M,Sugibayashi K

更新日期：2011-04-01 00:00:00

abstract：:Nanotechnology has continuously contributed to the fast development of diagnostic and therapeutic agents. Theranostic nanomedicine has encompassed the ongoing efforts on concurrent molecular imaging of biomarkers, delivery of therapeutic agents, and monitoring of therapy response. Among these formulations, polymer-bas...

journal_title：Pharmaceutical research

authors： Wang Z,Niu G,Chen X

更新日期：2014-06-01 00:00:00

abstract：PURPOSE:Generalizations based upon behavior of small molecules have established that a crystalline solid is generally much more stable toward chemical degradation than is the amorphous solid. This study examines the validity of this generalization for proteins using biosynthetic human insulin as the model protein. MET...

journal_title：Pharmaceutical research

authors： Pikal MJ,Rigsbee DR

更新日期：1997-10-01 00:00:00

abstract：PURPOSE:To study the reaction of artelinic acid with chemical model systems of cytochrome P-450 as a means of obtaining authentic samples of the putative metabolites necessary for identification of the mammalian metabolites of artelinic acid. METHODS:Artelinic acid was reacted with different organic complexes of iron(...

journal_title：Pharmaceutical research

authors： Idowu OR,Lin AJ,Grace JM,Peggins JO

更新日期：1997-10-01 00:00:00

abstract：PURPOSE:Chemically modified heparin-DOCA was prepared and found to have markedly lower anticoagulant activity than heparin. In the present study, we elucidated the antiangiogenic and antitumoral activities of heparin-DOCA derivative. METHODS:To evaluate the antiangiogenic and antitumoral effects of heparin-DOCA, capil...

journal_title：Pharmaceutical research

authors： Park K,Kim YS,Lee GY,Nam JO,Lee SK,Park RW,Kim SY,Kim IS,Byun Y

更新日期：2007-01-01 00:00:00

abstract：PURPOSE:In the present study we investigated the root-cause of an interference signal (100-200 nm) of sugar-containing solutions in dynamic light scattering (DLS) and nanoparticle tracking analysis (NTA) and its consequences for the analysis of particles in biopharmaceutical drug products. METHODS:Different sugars as ...

journal_title：Pharmaceutical research

authors： Weinbuch D,Cheung JK,Ketelaars J,Filipe V,Hawe A,den Engelsman J,Jiskoot W

更新日期：2015-07-01 00:00:00

abstract：PURPOSE:The growing amount of heterogeneous bioactivity data requires effective strategies to assess the promiscuity/selectivity of small-molecules and aid drug discovery. In the current study, we aim to evaluate the potential of assay profiles (APs, i.e., unique combinations of assay-related features describing how ac...

journal_title：Pharmaceutical research

authors： Avram S,Curpan R,Bora A,Neanu C,Halip L

更新日期：2018-10-18 00:00:00

abstract：PURPOSE:The combination of morphine and gabapentin seems promising for the treatment of postoperative and neuropathic pain. Despite the well characterised pharmacodynamic interaction, little is known about possible pharmacokinetic interactions. The aim of this study was to evaluate whether co-administration of the two ...

journal_title：Pharmaceutical research

authors： Papathanasiou T,Juul RV,Gabel-Jensen C,Kreilgaard M,Lund TM

更新日期：2016-11-01 00:00:00

abstract：PURPOSE:To assess the uridine diphosphate (UDP)-glucuronosyltransferase (UGT) isozymes involved in the glucuronidation of niflumic acid in human liver. METHODS:The glucuronidation activity of niflumic acid was determined in liver microsomes and recombinant UGT isozymes by incubation of niflumic acid with UDP-glucuroni...

journal_title：Pharmaceutical research

authors： Mano Y,Usui T,Kamimura H

更新日期：2006-07-01 00:00:00

abstract：PURPOSE:To examine the inhibitory potential of enalapril [and other angiotensin converting enzyme (ACE) inhibitors] on glycylsarcosine (GlySar) transport by the high-affinity renal peptide transporter. METHODS:Studies were performed in rabbit renal brush border membrane vesicles in which the uptake of radiolabeled Gly...

journal_title：Pharmaceutical research

authors： Lin CJ,Akarawut W,Smith DE

更新日期：1999-05-01 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