Sialic acid 9-O-acetylesterase catalyzes the hydrolyzing reaction from alacepril to deacetylalacepril.

abstract：:The pulmonary deposition and pharmacokinetics of human growth hormone (hGH), administered by aerosol and instillate, in formulations containing 99mTc-DTPA (for gamma scintigraphic imaging) have been studied in five male New Zealand White rabbits. Gamma scintigraphy indicated that the peripheral:central deposition tend...

journal_title：Pharmaceutical research

authors： Colthorpe P,Farr SJ,Smith IJ,Wyatt D,Taylor G

更新日期：1995-03-01 00:00:00

abstract：:The effect of freezing on formation of soluble and insoluble aggregates of human growth hormone (hGH) was studied. The amount of soluble aggregates was affected very little by freezing regardless of the cooling rate. In contrast, the formation of insoluble aggregates (particulates), as determined by light scattering i...

journal_title：Pharmaceutical research

authors： Eckhardt BM,Oeswein JQ,Bewley TA

更新日期：1991-11-01 00:00:00

abstract：:The transport of thyrotropin releasing hormone (TRH) in rabbit buccal mucosa in vitro has been investigated with respect to (a) rate and type of metabolism of TRH on mucosal and serosal sides of buccal mucosa, (b) mechanism of TRH transport including charge effect on its permeability, and (c) pathway and rate-limiting...

journal_title：Pharmaceutical research

authors： Dowty ME,Knuth KE,Irons BK,Robinson JR

更新日期：1992-09-01 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：:Some geminal bisphosphonates are used clinically for a number of important bone/calcium related diseases; however, side effects and lack of selectivity impede their wide use. This work reports the synthesis and evaluation of bisacylphosphonates (e.g., adipoyl- and suberoylbisphosphonate). These compounds were found to...

journal_title：Pharmaceutical research

authors： Golomb G,Schlossman A,Saadeh H,Levi M,Van Gelder JM,Breuer E

更新日期：1992-01-01 00:00:00

abstract：PURPOSE:Ultrasound can be used to release a therapeutic payload encapsulated within a perfluorocarbon (PFC) emulsion via acoustic droplet vaporization (ADV), a process whereby the PFC phase is vaporized and the agent is released. ADV-generated microbubbles have been previously used to selectively occlude blood vessels ...

journal_title：Pharmaceutical research

authors： Fabiilli ML,Lee JA,Kripfgans OD,Carson PL,Fowlkes JB

更新日期：2010-12-01 00:00:00

abstract：:Nucleic acids are increasingly being considered for therapeutic uses, either to interfere with the function of specific nucleic acids or to bind specific proteins. Three types of nucleic acid drugs are discussed in this review: aptamers, compounds which bind specific proteins; triplex forming (antigene) compounds; whi...

journal_title：Pharmaceutical research

authors： Stull RA,Szoka FC Jr

更新日期：1995-04-01 00:00:00

abstract：PURPOSE:Following extracellular drug clearance, we analyzed the rate of doxorubicin efflux from the nucleus of three human leukemic cells (K562, Molt4 and CCRF-CEM) and related it to their differential sensitivity to this drug, after a short drug pulse. RESULTS:For many pulse-chase regimes, K562 cell viability was lea...

journal_title：Pharmaceutical research

authors： Chen VY,Posada MM,Zhao L,Rosania GR

更新日期：2007-11-01 00:00:00

abstract：:Short-lived gamma emitting radioisotopes can be incorporated into polylactide/glycolide polymeric microspheres with various specific activities for possible use in understanding the in-vivo deposition, distribution and clearance of microparticulate drug carrier systems. The incorporated radiolabel is stable with negli...

journal_title：Pharmaceutical research

authors： Thanoo BC,Doll WJ,Mehta RC,Digenis GA,DeLuca PP

更新日期：1995-12-01 00:00:00

abstract：OBJECTIVE:Amorphous pharmaceuticals, a viable approach to enhancing bioavailability, must be stable against crystallization. An amorphous drug can be stabilized by dispersing it in a polymer matrix. To implement this approach, it is desirable to know the drug's solubility in the chosen polymer, which defines the maxima...

journal_title：Pharmaceutical research

authors： Tao J,Sun Y,Zhang GG,Yu L

更新日期：2009-04-01 00:00:00

abstract：PURPOSE:To investigate cellular uptake pathways of novel anionic siRNA-lipoplexes as a function of formulation composition. METHODS:Anionic formulations with anionic lipid/Ca(2+)/siRNA ratio of 1.3/2.5/1 (AF1) and 1.3/0.3/1 (AF2) were utilized. Uptake mechanisms were investigated using uptake inhibition and co-localiz...

journal_title：Pharmaceutical research

authors： Kapoor M,Burgess DJ

更新日期：2013-04-01 00:00:00

abstract：PURPOSE:To study Cereport (RMP-7, bradykinin B2 agonist) effects on human brain microvascular endothelial cell (HBMEC) monolayer permeability. METHODS:HBMEC grown on transwell membranes were exposed to Cereport. The monolayer permeability was determined with [14C]-inulin (MW. 5,200) and [3H]-dextran (MW. 70,000). RES...

journal_title：Pharmaceutical research

authors： Mackic JB,Stins M,Jovanovic S,Kim KS,Bartus RT,Zlokovic BV

更新日期：1999-09-01 00:00:00

abstract：:Despite substantial research carried out over the last decades, it remains difficult to understand the wide range of pharmacological effects of dopaminergic agents. The dopaminergic system is involved in several neurological disorders, such as Parkinson's disease and schizophrenia. This complex system features multipl...

journal_title：Pharmaceutical research

authors： van den Brink WJ,Palic S,Köhler I,de Lange ECM

更新日期：2018-02-15 00:00:00

abstract：PURPOSE:Nine common excipients were examined to determine their ability to cause disproportionation of the HCl salt of a a weakly basic compound. The goal was to determine which excipients were problematic and correlate the results to known properties such as surface pH, slurry pH, or molecular structure. Such a correl...

journal_title：Pharmaceutical research

authors： John CT,Xu W,Lupton LK,Harmon PA

更新日期：2013-06-01 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 evaluate the influence of the main biopharmaceutical factors on the viability of a new probiotic yeast strain, using dynamic in vitro systems simulating human gastric/small intestinal (TIM) and large intestinal (ARCOL) environments. METHODS:The viability of Saccharomyces cerevisiae CNCM I-3856 throughout th...

journal_title：Pharmaceutical research

authors： Blanquet-Diot S,Denis S,Chalancon S,Chaira F,Cardot JM,Alric M

更新日期：2012-06-01 00:00:00

abstract：PURPOSE:To quantitatively compare in vitro dissolution data in biorelevant and compendial media, to investigate whether in vitro differences are reflected in the simulated plasma profile and to specify under which circumstances prediction of the plasma profile of orally administered lipophilic drugs can be achieved. M...

journal_title：Pharmaceutical research

authors： Nicolaides E,Symillides M,Dressman JB,Reppas C

更新日期：2001-03-01 00:00:00

abstract：PURPOSE:Gastrointestinal deposition of nanoparticles was examined after oral administration to mice suffering from an experimental gastric ulcer model. Local drug delivery could reduce side effects and would be a distinct improvement compared to existing therapeutic approaches, e.g. in the local therapy of Helicobacter...

journal_title：Pharmaceutical research

authors： Hassani S,Pellequer Y,Lamprecht A

更新日期：2009-05-01 00:00:00

abstract：PURPOSE:The purpose of this work was to determine whether a new modeling methodology using fuzzy logic c an predict skin permeability coefficients that are given compound descriptors that have been proven to affect percutaneous penetration. METHOD:Three fuzzy inference models were developed using subtractive clusterin...

journal_title：Pharmaceutical research

authors： Pannier AK,Brand RM,Jones DD

更新日期：2003-02-01 00:00:00

abstract：PURPOSE:A pattern fitting procedure using X-ray powder diffraction patterns was applied to study the crystallization kinetics of amorphous griseofulvin. From the optimized parameters obtained by pattern fitting, a change in the quantity and quality of griseofulvin crystals with crystallization was also investigated. M...

journal_title：Pharmaceutical research

authors： Yamamura S,Takahira R,Momose Y

更新日期：2007-05-01 00:00:00

abstract：:The molecular environment of sucrose and mineral oil within sucrose and mineral oil solid state emulsions was investigated by NMR techniques. The 13C and 1H chemical shifts of sucrose and mineral oil to those observed in solid state emulsions (comprised of sucrose and mineral oil) were equivalent, indicating that the ...

journal_title：Pharmaceutical research

authors： Shively ML,Dec SF

更新日期：1994-09-01 00:00:00

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：:Physiologically-based pharmacokinetic (PBPK) models explicitly incorporate tissue-specific blood flows, partition coefficients, and metabolic processes. Since PBPK models are derived using physiologic parameters and interactions of the compound with tissue components, these models are considered to be "bottom up" as o...

journal_title：Pharmaceutical research

authors： Korzekwa K,Nagar S

更新日期：2017-03-01 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:A major challenge facing nanoparticle-based delivery of chemotherapy agents is the natural and unavoidable accumulation of these particles in healthy tissue resulting in local toxicity and dose-limiting side effects. To address this issue, we have designed and characterized a new prodrug nanoparticle with contr...

journal_title：Pharmaceutical research

authors： Schutt C,Ibsen S,Zahavy E,Aryal S,Kuo S,Esener S,Berns M,Esener S

更新日期：2017-10-01 00:00:00

abstract：PURPOSE:To study the PK interaction of L-dopa/benserazide in rats. METHODS:Male rats received a single oral dose of 80 mg/kg L-dopa or 20 mg/kg benserazide or 80/20 mg/kg L-dopa/benserazide. Based on plasma concentrations the kinetics of L-dopa, 3-O-methyldopa (3-OMD), benserazide, and its metabolite Ro 04-5127 were c...

journal_title：Pharmaceutical research

authors： Grange S,Holford NH,Guentert TW

更新日期：2001-08-01 00:00:00

abstract：PURPOSE:To investigate the effect of benzofusion on NO donor properties and related biological activities of the furoxan system. The biological properties considered were the ability to increase the cytosolic levels of cGMP in C6 cells and vasodilation. METHODS:NO donor properties were investigated either in the prese...

journal_title：Pharmaceutical research

authors： Medana C,Di Stilo A,Visentin S,Fruttero R,Gasco A,Ghigo D,Bosia A

更新日期：1999-06-01 00:00:00

abstract：PURPOSE:Recent studies have demonstrated the potential for a triglyceride (TG) mimetic prodrug to promote the delivery of mycophenolic acid (MPA) to the lymphatic system. Here, the metabolic pathways that facilitate the lymphatic transport of the TG prodrug (1,3-dipalmitoyl-2-mycophenoloyl glycerol, 2-MPA-TG) were exam...

journal_title：Pharmaceutical research

authors： Han S,Hu L,Quach T,Simpson JS,Trevaskis NL,Porter CJ

更新日期：2015-05-01 00:00:00

abstract：PURPOSE:Magnetic resonance imaging (MRI) is widely used for diagnostic imaging in preclinical studies and in clinical settings. Considering the intrinsic low sensitivity and poor specificity of standard MRI contrast agents, the enhanced delivery of MRI tracers into tumors is an important challenge to be addressed. This...

journal_title：Pharmaceutical research

authors： Kato Y,Zhu W,Backer MV,Neoh CC,Hapuarachchige S,Sarkar SK,Backer JM,Artemov D

更新日期：2015-11-01 00:00:00

abstract：PURPOSE:The objective of the current study was to investigate whether blood-brain barrier (BBB) permeability studies in vitro could be accelerated by running several compounds together in the same experiment. METHODS:To address this question, we compared the transport of six compounds run separately with the results o...

journal_title：Pharmaceutical research

authors： Berezowski V,Landry C,Lundquist S,Dehouck L,Cecchelli R,Dehouck MP,Fenart L

更新日期：2004-05-01 00:00:00