Molecular structure and dynamics of cis(Z)-and trans(E)-flupenthixol and clopenthixol.

abstract：PURPOSE:The purpose of this study was to assess the antifungal activity and renal and hepatic toxicity of amphotericin B (AmpB) following administration of Fungizone (FZ) and a heat-treated form of FZ (HFZ) to rats infected with Aspergillus fumigatus. METHODS:Infected rats were administered FZ and HFZ at a dosing regi...

journal_title：Pharmaceutical research

authors： Sivak O,Bartlett K,Wasan KM

更新日期：2004-09-01 00:00:00

abstract：:A 1H-NMR spectroscopic method for the determination of the optical purity of threo-methylphenidate hydrochloride is presented. Complexation of the free-base form of the substrate with a chiral Eu(III) shift reagent resulted in two distinct enantiomeric ester methyl proton signals of utility for quantitative work. The ...

journal_title：Pharmaceutical research

authors： Hanna GM,Lau-Cam CA

更新日期：1990-07-01 00:00:00

abstract：PURPOSE:To develop an enzymatically-controlled pulsatile drug release system based on an impermeable capsule body, which contains the drug and is closed by an erodible pectin/pectinase-plug. METHODS:The plug was prepared by direct compression of pectin and pectinase in different ratios. In addition to the disintegrati...

journal_title：Pharmaceutical research

authors： Krögel I,Bodmeier R

更新日期：1999-09-01 00:00:00

abstract：PURPOSE:Mannosylation of vaccines is a promising strategy to selectively target vaccine antigens to the mannose receptor expressed on dendritic cells (DCs). The purpose of this study was to investigate the effect of mannan (MN) chemically conjugated to poly(D, L-lactide-co-glycolic acid) (PLGA) nanoparticles (NPs) on a...

journal_title：Pharmaceutical research

authors： Hamdy S,Haddadi A,Shayeganpour A,Samuel J,Lavasanifar A

更新日期：2011-09-01 00:00:00

abstract：:Hyaluronan (HA: hyaluronic acid) is produced in the interstitium and reaches the blood circulation through the lymph. It is rapidly eliminated by means of specific receptors on liver endothelium. The elimination characteristics of intravenously administered HA were studied in 10 conscious sheep at the normal plasma HA...

journal_title：Pharmaceutical research

authors： Lebel L,Fraser JR,Kimpton WS,Gabrielsson J,Gerdin B,Laurent TC

更新日期：1989-08-01 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：:The absorption of insulin across the vaginal mucosa into the systemic circulation was studied in ovariectomized rats given subsequent estrogen treatment. Blood glucose levels were determined as an indirect measure of insulin absorption, and the effect of various enhancers on the hypoglycemic response was investigated....

journal_title：Pharmaceutical research

authors： Richardson JL,Illum L,Thomas NW

更新日期：1992-07-01 00:00:00

abstract：PURPOSE:Indomethacin is well known to be metabolized via O-demethylation and N-deacylation. In this paper we found an enzyme involved in the hydrolysis of amide-linkage of indomethacin and partially characterized it as well as its substrate specificity. METHODS:An indomethacin hydrolyzing enzyme was purified to homoge...

journal_title：Pharmaceutical research

authors： Terashima K,Takai S,Usami Y,Adachi T,Sugiyama T,Katagiri Y,Hirano K

更新日期：1996-09-01 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:Modulation of 5-HT3 receptor in the central nervous system (CNS) is a promising approach for treatment of neuropathic pain. The goal was to evaluate the role of P-glycoprotein (Pgp) in limiting exposure of different parts of the CNS to ondansetron (5-HT3 receptor antagonist) using wild-type and genetic knockout...

journal_title：Pharmaceutical research

authors： Chiang M,Back HM,Lee JB,Oh S,Guo T,Girgis S,Park C,Haroutounian S,Kagan L

更新日期：2020-09-28 00:00:00

abstract：:Intranasal route continues to be one of the main focuses of drug delivery research. Although it is generally perceived that the nasal route could avoid the first-pass metabolism in liver and gastrointestinal tract, the role of metabolic conversions in systemic and brain-targeted deliveries of the parent compounds and ...

journal_title：Pharmaceutical research

authors： Wong YC,Zuo Z

更新日期：2010-07-01 00:00:00

abstract：PURPOSE:To investigate the possible pathways for transport of wheat germ agglutinin conjugated PEG-PLA nanoparticles (WGA-NP) into the brain after nasal administration. METHODS:The nose-to-brain pathways were investigated using WGA-NP containing 6-coumarin (as a fluorescent marker) and (125)I-labeled WGA-NP. Ex vivo i...

journal_title：Pharmaceutical research

authors： Liu Q,Shen Y,Chen J,Gao X,Feng C,Wang L,Zhang Q,Jiang X

更新日期：2012-02-01 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：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：:The glass transition temperature of an amorphous pharmaceutical solid is a critical physical property which can dramatically influence its chemical stability, physical stability, and viscoelastic properties. Water frequently acts as a potent plasticizer for such materials, and since many amorphous solids spontaneously...

journal_title：Pharmaceutical research

authors： Hancock BC,Zografi G

更新日期：1994-04-01 00:00:00

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：:The origin of the microheterogeneity of a highly purified antiinflammatory humanized monoclonal antibody prepared in mammalian cell culture has been investigated. This antibody is an IgG directed toward human CD18 (a subunit of leukocyte integrins). When the IgG preparation is subjected to isoelectric focusing, it is ...

journal_title：Pharmaceutical research

authors： Tsai PK,Bruner MW,Irwin JI,Ip CC,Oliver CN,Nelson RW,Volkin DB,Middaugh CR

更新日期：1993-11-01 00:00:00

abstract：PURPOSE:To identify High Molecular Weight Products (HMWP) formed in human insulin formulation during storage. METHODS:Commercial formulation of human insulin was stored at 37°C for 1 year and HMWP was isolated using preparative size exclusion chromatography (SEC) and reverse phase (RP) chromatography. The primary stru...

journal_title：Pharmaceutical research

authors： Hjorth CF,Hubálek F,Andersson J,Poulsen C,Otzen D,Naver H

更新日期：2015-06-01 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：:Aucubin, a promising hepatoprotecting iridoid glucoside, was given intravenously (iv), orally (po), intraperitoneally (ip), and hepatoportally (pv) to rats. A linear pharmacokinetic behavior was obtained after iv administation of 400-400 mg/kg of aucubin. The half-life of aucubin in the postdistributive phase (t1/2, b...

journal_title：Pharmaceutical research

authors： Suh NJ,Shim CK,Lee MH,Kim SK,Chang IM

更新日期：1991-08-01 00:00:00

abstract：:The pharmacokinetics of cefixime, a new orally active cephalosporin, was studied after an intravenous dose of 50 mg/kg to four beagle dogs. Cefixime was shown to exhibit concentration dependent serum protein binding and saturable tubular reabsorption. The drug was excreted mainly in the urine, the net result of glomer...

journal_title：Pharmaceutical research

authors： Tonelli AP,Bialer M,Look ZM,Carson S,Yacobi A

更新日期：1986-06-01 00:00:00

abstract：PURPOSE:In this work, the alacepril thiolesterase, which catalyzes the hydrolyzing reaction of the thiolester linkage in alacepril and the conversion from alacepril to deacetylalacepril, was purified from rat liver cytosol and characterized. METHODS:A purification procedure for the thiolesterase consisted of ammonium ...

journal_title：Pharmaceutical research

authors： Usui S,Kubota M,Iguchi K,Kiho T,Sugiyama T,Katagiri Y,Hirano K

更新日期：2003-08-01 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：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：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:Supramolecular Biovectors (SMBV) consist of cross-linked cationic nanoparticles surrounded by a lipid membrane. The purpose was to study the structure of the lipid membrane and to characterise its interaction with the nanoparticles in order to differentiate SMBV from other polymer/lipid associations. METHODS:T...

journal_title：Pharmaceutical research

authors： De Miguel I,Imbertie L,Rieumajou V,Major M,Kravtzoff R,Betbeder D

更新日期：2000-07-01 00:00:00

abstract：:The role of phosphatidylserine in the cellular and subcellular lung distribution of quinidine was investigated in rats, since quinidine was found to bind preferentially to phosphatidylserine. The concentration of phosphatidylserine in the cellular and subcellular fractions was determined after separation by two-dimens...

journal_title：Pharmaceutical research

authors： Nishiura A,Murakami T,Higashi Y,Yata N

更新日期：1988-04-01 00:00:00

abstract：PURPOSE:To gain information on the chemical stability pattern and the kinetics of the degradation of recombinant hirudin variant HV1 (rHir), a thrombin-specific inhibitor protein of 65 amino acids, in aqueous solution as a function of pH. METHODS:Stability of rHir was monitored at 50 degrees C in the framework of a cl...

journal_title：Pharmaceutical research

authors： Gietz U,Alder R,Langguth P,Arvinte T,Merkle HP

更新日期：1998-09-01 00:00:00

abstract：:The dermal route is an attractive route for vaccine delivery due to the easy skin accessibility and a dense network of immune cells in the skin. The development of microneedles is crucial to take advantage of the skin immunization and simultaneously to overcome problems related to vaccination by conventional needles (...

journal_title：Pharmaceutical research

authors： Leone M,Mönkäre J,Bouwstra JA,Kersten G

更新日期：2017-11-01 00:00:00

abstract：PURPOSE:Good glycaemic control is essential to minimize the risk for diabetes-induced complications. Also, compliance is likely to be higher if the procedure is simple and painless. This study was designed to validate painless intradermal delivery via a patch-like microneedle array. MATERIALS AND METHODS:Diabetes was ...

journal_title：Pharmaceutical research

authors： Nordquist L,Roxhed N,Griss P,Stemme G

更新日期：2007-07-01 00:00:00