Microbial and mammalian metabolism studies of the semisynthetic antimalarial, anhydrodihydroartemisinin.

abstract：:Semitelechelic poly[N-(2-hydroxypropyl)methacrylamide]s (ST-PHPMA) containing one amino end-group and differing in molecular weight were synthesized by radical polymerization in the presence of 2-aminoethanethiol (AET) as chain transfer agent. These polymers were covalently attached via amide bonds to the surface of n...

journal_title：Pharmaceutical research

authors： Kamei S,Kopecek J

更新日期：1995-05-01 00:00:00

abstract：PURPOSE:To investigate the influence of nanocarrier molecular size and shape on breast duct retention in normal rats using a non-invasive optical imaging method. METHODS:Fluorescein-labeled PEG nanocarriers of different molecular weights and shapes (linear, two-arm, four-arm, and eight-arm) were intraductally administ...

journal_title：Pharmaceutical research

authors： Singh Y,Gao D,Gu Z,Li S,Rivera KA,Stein S,Love S,Sinko PJ

更新日期：2012-09-01 00:00:00

abstract：:Lidocaine was administered to healthy volunteers at different sites in the rectum. Unchanged drug and monoethylglycinexylidide (MEGX) concentrations were measured in plasma with a newly developed gas chromatographic method. Lidocaine was given rectally by means of an osmotic system (Osmet(®)) which delivered 25 mg/h a...

journal_title：Pharmaceutical research

authors： de Leede LG,de Boer AG,Feijen CD,Breimer DD

更新日期：1984-05-01 00:00:00

abstract：PURPOSE:To study the expression of P-glycoprotein (P-gp), lung resistance-related protein (LRP), and caveolin-1 (cav-1) in the human bronchial epithelial cell line 16HBE14o-. METHODS:The presence of P-gp, LRP, and cav-1 in 16HBE14o- cell layers was evaluated using immunocytochemical staining and visualization with con...

journal_title：Pharmaceutical research

authors： Ehrhardt C,Kneuer C,Laue M,Schaefer UF,Kim KJ,Lehr CM

更新日期：2003-04-01 00:00:00

abstract：PURPOSE:Knowledge about the uptake mechanism and subsequent intracellular routing of non-viral gene delivery systems is important for the development of more efficient carriers. In this study we compared two established cationic polymers pDMAEMA and PEI with regard to their transfection efficiency and mechanism of cell...

journal_title：Pharmaceutical research

authors： van der Aa MA,Huth US,Häfele SY,Schubert R,Oosting RS,Mastrobattista E,Hennink WE,Peschka-Süss R,Koning GA,Crommelin DJ

更新日期：2007-08-01 00:00:00

abstract：PURPOSE:We examined the subcellular distribution of the basic drugs, chlorpromazine (CPZ), imipramine (IMP) and biperiden (BP), in rat liver, and evaluated the contribution of lysosome (Lys) to their intracellular distribution in comparison with that of mitochondria (Mit). METHODS:In an in vivo distribution, the conce...

journal_title：Pharmaceutical research

authors： Ishizaki J,Yokogawa K,Hirano M,Nakashima E,Sai Y,Ohkuma S,Ohshima T,Ichimura F

更新日期：1996-06-01 00:00:00

abstract：PURPOSE:Nonlinear conjugation metabolic rate of valproic acid (VPA) has been speculated previously from plasma elimination and liver concentration of VPA in guinea pigs. The purposes of the present study were to assess our speculation by direct measurement of VPA glucuronidation rate in vitro. METHODS:VPA at various c...

journal_title：Pharmaceutical research

authors： Yu HY,Shen YZ

更新日期：1996-08-01 00:00:00

abstract：PURPOSE:The aim of this study was to identify new surfactants with low skin irritant properties for use in pharmaceutical and cosmetic formulations, employing cell culture as an alternative method to in vivo testing. In addition, we sought to establish whether potential cytotoxic properties were related to the size of ...

journal_title：Pharmaceutical research

authors： Sanchez L,Mitjans M,Infante MR,Vinardell MP

更新日期：2004-09-01 00:00:00

abstract：PURPOSE:Melanoma is an aggressive neoplasm with a propensity for metastases and resistance to therapy. Previously, we showed that (-)-epigallocatechin-3-gallate (EGCG), the major polyphenolic antioxidant present in green tea, resulted in a significant decrease in the viability and growth of melanoma and induction of ap...

journal_title：Pharmaceutical research

authors： Nihal M,Roelke CT,Wood GS

更新日期：2010-06-01 00:00:00

abstract：:One of the barriers to transdermal delivery of peptides is the metabolic activity of the epidermis. To define this metabolic activity, aminopeptidase activity and Leu-enkephalin metabolism were measured in the epidermis obtained from neonatal mouse skin and in cultured mouse keratinocytes. Aminopeptidase activity was ...

journal_title：Pharmaceutical research

authors： Shah PK,Borchardt RT

更新日期：1991-01-01 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：: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：: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:We have already demonstrated that the HMG-CoA reductase inhibitor, pravastatin is actively taken up by isolated rat hepatocytes via a multispecific anion transporter (Yamazaki et al., Am. J. Physiol. 264, G36-44, (1993)). We further attempted the quantitative evaluation of this uptake in different experimental ...

journal_title：Pharmaceutical research

authors： Ishigami M,Tokui T,Komai T,Tsukahara K,Yamazaki M,Sugiyama Y

更新日期：1995-11-01 00:00:00

abstract：PURPOSE:To evaluate and classify the hydrolases of the primate lung. METHODS:Homologous series of aromatic, aliphatic, and choline ester substrates were assayed with the pH-stat method to obtain the Michaelis-Menten kinetic constants, Vmax and K(m), for the enzymes in pulmonary alveolar tissue with esterase activity. ...

journal_title：Pharmaceutical research

authors： Leng HM,Syce JA

更新日期：1997-02-01 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：PURPOSE:The long-term stability and nasal absorption characteristics of a basic nasal formulation of azetirelin, a thyrotropin-releasing hormone analog and its absorption enhancement by incorporation of acylcarnitines in the formulation were investigated. METHODS:The long-term stability of basic nasal azetirelin formu...

journal_title：Pharmaceutical research

authors： Kagatani S,Inaba N,Fukui M,Sonobe T

更新日期：1998-01-01 00:00:00

abstract：:The mechanism of release from sustained-release adinazolam mesylate tablets was assessed by the Higuchi equation and by analysis of drug release profiles through 60% released using the Peppas equation. Computed values of the diffusional exponent, n, ranged from 0.59 to 0.66. Values of n in this range are consistent wi...

journal_title：Pharmaceutical research

authors： Skoug JW,Borin MT,Fleishaker JC,Cooper AM

更新日期：1991-12-01 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:Although flomoxef (FMOX) has attracted substantial attention as an antibiotic against extended-spectrum beta-lactamase-producing Escherichia coli (ESBL-producing E. coli), the pharmacokinetics/pharmacodynamics (PK/PD) characteristics of FMOX against ESBL-producing E. coli is unclear. The aim of this study was t...

journal_title：Pharmaceutical research

authors： Tashiro S,Hayashi M,Takemura W,Igarashi Y,Liu X,Mizukami Y,Kojima N,Enoki Y,Taguchi K,Yokoyama Y,Nakamura T,Matsumoto K

更新日期：2021-01-06 00:00:00

abstract：PURPOSE:To elucidate the key parameters affecting solute transport from semi-interpenetrating networks (sIPNs) comprised of poly(ethylene glycol) diacrylate (PEGdA) and gelatin that are partially crosslinked, water-swellable and biodegradable. Effects of material compositions, solute size, solubility, and loading densi...

journal_title：Pharmaceutical research

authors： Fu Y,Kao WJ

更新日期：2009-09-01 00:00:00

abstract：PURPOSE:This study addresses the effect of freezing and thawing on a therapeutic monoclonal antibody (mAb) solution and the corresponding buffer formulation. Particle formation, crystallization behaviour, morphology changes and cryo-concentration effects were studied after varying the freezing and thawing rates, buffer...

journal_title：Pharmaceutical research

authors： Hauptmann A,Podgoršek K,Kuzman D,Srčič S,Hoelzl G,Loerting T

更新日期：2018-03-19 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:Cell-based permeability screens are widely used to identify drug-P-glycoprotein (PGP) interaction in vitro. However, their reliability in predicting the impact of PGP on human drug pharmacokinetics is poorly defined. The aim was to determine whether a quantitative relationship exists between PGP-mediated altera...

journal_title：Pharmaceutical research

authors： Collett A,Tanianis-Hughes J,Hallifax D,Warhurst G

更新日期：2004-05-01 00:00:00

abstract：PURPOSE:To assess the efficacy of the novel clinical formulation of fenretinide (LAU-7b) for the treatment of allergic asthma. To study the association between LAU-7b treatment in allergic asthma and the modulation of very long chain ceramides (VLCC). METHODS:We used two allergens (OVA and HDM) to induce asthma in mou...

journal_title：Pharmaceutical research

authors： Youssef M,De Sanctis JB,Kanagaratham C,Tao S,Ahmed E,Radzioch D

更新日期：2020-01-08 00:00:00

abstract：PURPOSE:To assess the efficacy of lipid-protein-sugar particles (LPSPs) in providing prolonged duration local anesthesia by percutaneous injection. METHODS:Bupivacaine-containing LPSPs were characterized and optimized in vitro. Male Sprague-Dawley rats were given sciatic nerve blocks with bupivacaine-containing LPSPs....

journal_title：Pharmaceutical research

authors： Kohane DS,Lipp M,Kinney RC,Lotan N,Langer R

更新日期：2000-10-01 00:00:00

abstract：PURPOSE:Previous literature has suggested the absence of an effective barrier between the nasal mucosa and the brain for compounds administered via the nasal route. These experiments were conducted to elucidate the role of the blood-brain barrier efflux transporter P-glycoprotein (P-gp) in attenuating delivery of P-gp ...

journal_title：Pharmaceutical research

authors： Graff CL,Pollack GM

更新日期：2003-08-01 00:00:00

abstract：PURPOSE:Paclitaxel is active and widely used to treat multiple types of solid tumors. The commercially available paclitaxel formulation uses Cremophor/ethanol (C/E) as the solubilizers. Other formulations including nanoparticles have been introduced. This study evaluated the effects of nanoparticle formulation of pacli...

journal_title：Pharmaceutical research

authors： Yeh TK,Lu Z,Wientjes MG,Au JL

更新日期：2005-06-01 00:00:00

abstract：PURPOSE:A double-mutant E224A/E262A full-length botulinum neurotoxin (BoNT) Type A with structural similarity to native BoNT/A but lacking the endopeptidase activity provides an ideal surrogate for testing pharmacokinetics and immunochemical characteristics of BoNT. METHODS:We determined lethality (LD50) of deactivate...

journal_title：Pharmaceutical research

authors： Ravichandran E,Janardhanan P,Patel K,Riding S,Cai S,Singh BR

更新日期：2016-03-01 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