Assessment of physical stability of an antibody drug conjugate by higher order structure analysis: impact of thiol- maleimide chemistry.

abstract：PURPOSE:The aim of the study is to investigate the effect of polymer blending on entrapment and release of ganciclovir (GCV) from poly(D,L-lactide-co-glycolide) (PLGA) microspheres using a set of empirical equations. METHODS:Two grades of PLGA, PLGA 7525 [D,L-lactide:glycolide(75:25), MW 90,000-126,000 Da] and Resomer...

journal_title：Pharmaceutical research

authors： Duvvuri S,Gaurav Janoria K,Mitra AK

更新日期：2006-01-01 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：: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：: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：: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：:Many drugs and desirable phytochemicals are bitter, and bitter tastes are aversive. Food and pharmaceutical manufacturers share a common need for bitterness-masking strategies that allow them to deliver useful quantities of the active compounds in an acceptable form and in this review we compare and contrast the chall...

journal_title：Pharmaceutical research

authors： Coupland JN,Hayes JE

更新日期：2014-11-01 00:00:00

abstract：PURPOSE:To develop a liposomal system with high drug loading (DL) for intravenous (i.v.) delivery of a poorly water-soluble basic drug, asulacrine (ASL). METHODS:A thin-film hydration and extrusion method was used to fabricate the PEGylated liposomal membranes followed by a freeze and thaw process. A novel active drug...

journal_title：Pharmaceutical research

authors： Zhang W,Wang G,Falconer JR,Baguley BC,Shaw JP,Liu J,Xu H,See E,Sun J,Aa J,Wu Z

更新日期：2015-04-01 00:00:00

abstract：PURPOSE:The purpose of this study was (a) to suggest a novel dermatopharmacokinetic (DPK) approach from which pharmacokinetic parameters relevant to the bioequivalence (BE) assessment of a topical formulation can be deduced while circumventing the need for numerous measurements and assumptions, and (b) to investigate w...

journal_title：Pharmaceutical research

authors： Ozdin D,Kanfer I,Ducharme MP

更新日期：2020-01-02 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:To examine the presence of multiplicity for the biliary excretion of xenobiotic conjugates, we studied the disposition of glycyrrhizin (GR), which has glucuronide within its molecular structure and has the ability to inhibit the biliary excretion of liquiritigenin (LG) glucuronides. METHODS:GR was administered...

journal_title：Pharmaceutical research

authors： Shimamura H,Suzuki H,Tagaya O,Horie T,Sugiyama Y

更新日期：1996-12-01 00:00:00

abstract：PURPOSE:To develop a safe and effective non-viral vector for gene delivery and transfection in macrophages for potential anti-inflammatory therapy. METHODS:Solid nanoparticles-in-emulsion (NiE) multi-compartmental delivery system was designed using plasmid DNA-encapsulated type B gelatin nanoparticles suspended in the...

journal_title：Pharmaceutical research

authors： Attarwala H,Amiji M

更新日期：2012-06-01 00:00:00

abstract：:The in situ rat gut technique was used to study the effects of hypothermia on the intestinal absorption of a 1 mg/ml solution of sodium pentobarbital in 0.01 M phosphate buffer (pH 6.0). Male Sprague-Dawley rats weighing between 300 and 370 g were exposed to an atmosphere of helox (helium:oxygen, 80:20) at 0-4 degrees...

journal_title：Pharmaceutical research

authors： Stavchansky S,Tung IL

更新日期：1987-06-01 00:00:00

abstract：PURPOSE:To monitor the biodistribution of IgG1 aggregates upon subcutaneous (SC) and intravenous (IV) administration in mice and measure their propensity to stimulate an early immune response. METHODS:A human mAb (IgG1) was fluorescently labeled, aggregated by agitation stress and injected in SKH1 mice through SC and ...

journal_title：Pharmaceutical research

authors： Filipe V,Que I,Carpenter JF,Löwik C,Jiskoot W

更新日期：2014-01-01 00:00:00

abstract：PURPOSE:The purpose of this study is to investigate the characteristics of pGlu-L-Dopa-Pro as a prodrug of L-Dopa. METHODS:pGlu-L-Dopa-Pro and L-Dopa-Pro were synthesized using the standard procedures of peptide synthesis. The conversion of pGlu-L-Dopa-Pro to L-Dopa was studied using pyroglutamyl aminopeptidase I and ...

journal_title：Pharmaceutical research

authors： Bai JP

更新日期：1995-07-01 00:00:00

abstract：:Porcine pancreatic elastase, a well-characterized serine protease, has been used as a model to assess the effects of excessive humidity on solid-state stability of the lyophilized protein. Elastase lyophilized without excipients retained full activity immediately after freeze-drying but became denatured upon continued...

journal_title：Pharmaceutical research

authors： Chang BS,Randall CS,Lee YS

更新日期：1993-10-01 00:00:00

abstract：:Micelle-associated epoetin is still a possible explanation for the upsurge of pure red blood cell aplasia associated with subcutaneous use of epoetin alpha in patients with chronic renal failure. ...

journal_title：Pharmaceutical research

authors： Hermeling S,Jiskoot W,Crommelin DJ,Schellekens H

更新日期：2006-03-01 00:00:00

abstract：:Sodium taurodihydrofusidate (STDHF) is one of the most promising absorption enhancers for nasal delivery of peptide drugs. Drugs and additives in nasal formulations should not interfere with the self-cleaning capacity of the nose by the ciliary epithelium. Measured in vitro on human adenoid tissue with a photoelectric...

journal_title：Pharmaceutical research

authors： Hermens WA,Hooymans PM,Verhoef JC,Merkus FW

更新日期：1990-02-01 00:00:00

abstract：:Prinomide tromethamine, a nonsteroidal antiinflammatory drug, was orally administered at doses of 250, 500, and 1000 mg every 12 hr for 28 days to healthy male volunteers. The pharmacokinetic behavior of prinomide and its primary plasma metabolite displayed nonlinear characteristics, while those of free prinomide and ...

journal_title：Pharmaceutical research

authors： Kochak GM,Pai S,Iannucci R,Honc F,Kachmar D,Perrino P,Egger H

更新日期：1993-01-01 00:00:00

abstract：PURPOSE:To investigate the properties of phenylboronic acid-functional poly(amido amine) polymers (BA-PAA) in forming multilayered thin films with poly(vinyl alcohol) (PVA) and chondroitin sulfate (ChS), and to evaluate their compatibility with COS-7 cells. METHODS:Copolymers of phenylboronic acid-functional poly(amid...

journal_title：Pharmaceutical research

authors： Hujaya SD,Engbersen JF,Paulusse JM

更新日期：2015-09-01 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：: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 evaluate the effects of several buffers and excipients on the stability of glucagon during freeze-drying and storage as dried powder formulations. METHODS:The chemical and physical stability of glucagon in freeze-dried solid formulations was evaluated by a variety of techniques including mass spectrometry (...

journal_title：Pharmaceutical research

authors： Fang WJ,Qi W,Kinzell J,Prestrelski S,Carpenter JF

更新日期：2012-12-01 00:00:00

abstract：PURPOSE:The heparin-paclitaxel conjugates using amino acid as linker (HD2), with low anticoagulant activity, the similar anticancer activity as paclitaxel, offer great potential for further investigation. METHODS:Two types of heparin-paclitaxel conjugates (HD) have been developed, in which O-acetylated heparin as carr...

journal_title：Pharmaceutical research

authors： Wang Y,Xin D,Liu K,Xiang J

更新日期：2009-04-01 00:00:00

abstract：PURPOSE:To examine the effect of particle size and morphology on aerosol dispersion using jet-milled and spray-dried mannitol particles in narrow size distributions within the respirable range. METHODS:Particle size and morphology were examined by laser diffraction and scanning electron microscopy, respectively. Aeros...

journal_title：Pharmaceutical research

authors： Louey MD,Van Oort M,Hickey AJ

更新日期：2004-07-01 00:00:00

abstract：PURPOSE:The sensitivity and effectiveness of indirect metrics proposed for the assessment of comparative absorption rates in bioequivalence studies [Cmax, Tmax, partial AUC (AUCp), feathered slope (SLf), intercept metric (I)] were originally tested by assuming first-order absorption. The present study re-evaluates thei...

journal_title：Pharmaceutical research

authors： Ring A,Tothfalusi L,Endrenyi L,Weiss M

更新日期：2000-05-01 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: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：PURPOSE:The aim of this work was to develop a quantitative, flow cytometric method for tracking the endolysosomal escape of a fluorescently labelled saporin toxin. METHODS:Flow cytometric measurements of fluorescent pulse width and height were used to track the endocytic uptake into Daudi cells of a fluorescently labe...

journal_title：Pharmaceutical research

authors： Wensley HJ,Johnston DA,Smith WS,Holmes SE,Flavell SU,Flavell DJ

更新日期：2019-12-23 00:00:00

abstract：PURPOSE:Platinum-based therapies are the first line treatments for most types of cancer including ovarian cancer. However, their use is associated with dose-limiting toxicities and resistance. We report initial translational studies of a theranostic nanoemulsion loaded with a cisplatin derivative, myrisplatin and pro-a...

journal_title：Pharmaceutical research

authors： Ganta S,Singh A,Kulkarni P,Keeler AW,Piroyan A,Sawant RR,Patel NR,Davis B,Ferris C,O'Neal S,Zamboni W,Amiji MM,Coleman TP

更新日期：2015-08-01 00:00:00

abstract：:The fluxes of nitroglycerine (NG) through human abdominal epidermis from different individuals were measured in vitro at 32°C. The mean NG flux for the entire group was 16.9 µg/cm(2) × hr, with a standard deviation of 47.7%. There are no significant differences in the means and the variances of NG fluxes between males...

journal_title：Pharmaceutical research

authors： Langguth P,Spahn H,Mutschler E

更新日期：1986-02-01 00:00:00