A comparison of peptidase activities and peptide metabolism in cultured mouse keratinocytes and neonatal mouse epidermis.

abstract：PURPOSE:To assess the effects of selective lipid extraction and tape stripping on transepidermal water loss (TEWL) at three body regions in the pig. METHODS:Lipids were extracted from the abdominal, inguinal. and back regions using three different solvent extraction procedures or cellophane tape stripping (15x) on Yor...

journal_title：Pharmaceutical research

authors： Monteiro-Riviere NA,Inman AO,Mak V,Wertz P,Riviere JE

更新日期：2001-07-01 00:00:00

abstract：:The effects of skin storage, skin preparation, skin pretreatment with a penetration enhancer, and skin barrier removal by adhesive tape-stripping on the concurrent cutaneous transport and metabolism of nitroglycerin (GTN) have been studied in vitro using hairless mouse skin. Storing the skin for 10 days at 4 degrees C...

journal_title：Pharmaceutical research

authors： Higo N,Hinz RS,Lau DT,Benet LZ,Guy RH

更新日期：1992-03-01 00:00:00

abstract：PURPOSE:To create poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs), where a drug-encapsulating NP core is covered with polyethylene glycol (PEG) in a normal condition but exposes a cell-interactive TAT-modified surface in an environment rich in matrix metalloproteinases (MMPs). METHODS:PLGA NPs were modified w...

journal_title：Pharmaceutical research

authors： Gullotti E,Park J,Yeo Y

更新日期：2013-08-01 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：:During protein lyophilization, it is common practice to complete the freezing step as fast as possible in order to avoid protein denaturation, as well as to obtain a final product of uniform quality. We report a contradictory observation made during lyophilization of recombinant tissue-type plasminogen activator (t-PA...

journal_title：Pharmaceutical research

authors： Hsu CC,Nguyen HM,Yeung DA,Brooks DA,Koe GS,Bewley TA,Pearlman R

更新日期：1995-01-01 00:00:00

abstract：:Penetration of various compounds through shed snake skin was measured in vitro to examine the effect of lipophilicity and molecular size of a compound on permeability through this model membrane. The permeabilities were found to be controlled by the lipophilicity and the molecular size of the permeant. The smaller and...

journal_title：Pharmaceutical research

authors： Itoh T,Magavi R,Casady RL,Nishihata T,Rytting JH

更新日期：1990-12-01 00:00:00

abstract：PURPOSE:To show, using a model study, how electronic structure theory can be applied in combination with LC/UV/MS/MS for the prediction and identification of oxidative degradants. METHODS:The benzyloxazole 1, was used to represent an active pharmaceutical ingredient for oxidative forced degradation studies. Bond disso...

journal_title：Pharmaceutical research

authors： Reid DL,Calvitt CJ,Zell MT,Miller KG,Kingsmill CA

更新日期：2004-09-01 00:00:00

abstract：:Leucine enkephalin (YGGFL) undergoes rapid degradation in sheep nasal mucosa to yield GGFL which is further degraded to FL. The activity of the nasal mucosal homogenate against YGGFL and GGFL (t1/2 12 and 7 min) was significantly greater than that observed with a nasal wash fluid (t1/2 40 and 13 min). The effect of cy...

journal_title：Pharmaceutical research

authors： Irwin WJ,Dwivedi AK,Holbrook PA,Dey MJ

更新日期：1994-12-01 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:We describe the AERX aerosol delivery system, a new, bolus inhalation device that is actuated at preprogrammed values of inspiratory flow rate and inhaled volume. We report on its in vitro characterization using a particular set of conditions used in pharmacokinetic and scintigraphic studies. METHODS:Multiple ...

journal_title：Pharmaceutical research

authors： Schuster J,Rubsamen R,Lloyd P,Lloyd J

更新日期：1997-03-01 00:00:00

abstract：:This study utilized different statistical techniques to evaluate the reliability (internal consistency) and the discriminant validity of the most widely used measures of organizational commitment and intention to quit (the employing organization). Data were obtained from a national mail survey of members of the Americ...

journal_title：Pharmaceutical research

authors： Kong SX,Wertheimer AI,Serradell J,McGhan WF

更新日期：1994-01-01 00:00:00

abstract：:This paper describes an investigation of the use of poly(lactic/glycolic acid) polymers for long-term delivery of high molecular weight, water-soluble proteins. Poly(lactic/glycolic acid) (PLGA) microspheres, containing (fluorescein isothiocyanate)-labeled bovine serum albumin and (fluorescein isothiocyanate)-labeled ...

journal_title：Pharmaceutical research

authors： Cohen S,Yoshioka T,Lucarelli M,Hwang LH,Langer R

更新日期：1991-06-01 00:00:00

abstract：PURPOSE:We evaluated the effect of luminal bacterial metabolism on intestinal absorption of azetirelin in rats. In vitro characteristics of bacterial metabolism of azetirelin were also investigated with the goal of overcoming the low stability of the peptidic drug against luminal microorganisms. METHODS:Plasma azetire...

journal_title：Pharmaceutical research

authors： Sasaki I,Tamura T,Shibakawa T,Fujita T,Murakami M,Yamamoto A,Muranishi S

更新日期：1997-08-01 00:00:00

abstract：:Four lipophilic, low molecular weight drugs solubilized in phosphatidylcholine-bile salt mixed micelles were injected s.c. into the hind legs of sheep and their cumulative recoveries in lymph draining from the site of application were determined. Surprisingly, the cumulative recoveries (percentage of dose) varied betw...

journal_title：Pharmaceutical research

authors： Supersaxo A,Hein WR,Steffen H

更新日期：1991-10-01 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：:A simple viscometric method was used to quantify mucin-polymer bioadhesive bond strength. Viscosities of 15% (w/v) porcine gastric mucin dispersions in 0.1 N HCl (pH 1) or 0.1 N acetate buffer (pH 5.5) were measured with a Brookfield viscometer in the absence (eta m) or presence (eta t) of selected neutral, anionic, a...

journal_title：Pharmaceutical research

authors： Hassan EE,Gallo JM

更新日期：1990-05-01 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:Monoamine oxidases (MAOs) are non-CYP enzymes that contribute to systemic elimination of therapeutic agents, and localized on mitochondrial membranes. The aim of the present study was to validate quantitative estimation of metabolic clearance of MAO substrate drugs using human liver microsomes (HLMs). METHODS:...

journal_title：Pharmaceutical research

authors： Masuo Y,Nagamori S,Hasegawa A,Hayashi K,Isozumi N,Nakamichi N,Kanai Y,Kato Y

更新日期：2017-06-01 00:00:00

abstract：PURPOSE:Some patients are unable to generate the peak inspiratory flow rate (PIFR) necessary to de-agglomerate drug particles from dry powder inhalers (DPIs). In this study we tested the hypothesis that the acoustic parameters of an inhalation are related to the PIFR and hence reflect drug delivery. METHODS:A sensitiv...

journal_title：Pharmaceutical research

authors： Seheult JN,O'Connell P,Tee KC,Bholah T,Al Bannai H,Sulaiman I,MacHale E,D'Arcy S,Holmes MS,Bergin D,Reeves E,Reilly RB,Crispino-O'Connell G,Ehrhardt C,Healy AM,Costello RW

更新日期：2014-10-01 00:00:00

abstract：PURPOSE:To study the pulmonary absorption and tolerability of various formulations of the decapeptide cetrorelix acetate in rats by a new aerosol delivery system (ASTA-ADS) for intratracheal application. METHODS:Using the ASTA-ADS, cetrorelix liquid formulations (aqueous solutions for ultrasonic nebulization) were fir...

journal_title：Pharmaceutical research

authors： Lizio R,Klenner T,Sarlikiotis AW,Romeis P,Marx D,Nolte T,Jahn W,Borchard G,Lehr CM

更新日期：2001-06-01 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：:The physicochemical properties and crystal structures of the crystalline salts formed by the interaction of an achiral anion, salicylate, with homochiral and racemic ephedrinium and pseudoephedrinium cations were determined. The interaction of ephedrinium or pseudoephedrinium with salicylate in aqueous solution yielde...

journal_title：Pharmaceutical research

authors： Duddu SP,Grant DJ

更新日期：1994-11-01 00:00:00

abstract：PURPOSE:The objective of this study was to evaluate the in vivo consequences of glycyl-glutamate coadministration on gabapentin oral absorption. METHODS:Rats were administered gabapentin (10 mg/kg plus radiotracer) by gastric gavage, in the absence and presence of dipeptides, and by intravenous administration. Serial ...

journal_title：Pharmaceutical research

authors： Nguyen TV,Fleisher D,Smith DE

更新日期：2007-08-01 00:00:00

abstract：PURPOSE:To evaluate the potential effects of PEGylated pH-sensitive liposomes on the intracellular activity of a new peptide recently characterized as a novel inhibitor of the human thymidylate synthase (hTS) over-expressed in many drug-resistant human cancer cell lines. METHODS:Peptide-loaded pH-sensitive PEGylated (...

journal_title：Pharmaceutical research

authors： Sacchetti F,Marverti G,D'Arca D,Severi L,Maretti E,Iannuccelli V,Pacifico S,Ponterini G,Costi MP,Leo E

更新日期：2018-09-12 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:The aim of this work was to develop PEGylated poly(alkylcyanoacrylate) nanoparticles from a novel methoxypolyethyleneglycol cyanoacrylate-co-hexadecyl cyanoacrylate copolymer. METHODS:PEGylated and non-PEGylated nanoparticles were formed by nanoprecipitation or by emulsion/solvent evaporation. Nanoparticles si...

journal_title：Pharmaceutical research

authors： Peracchia MT,Vauthier C,Desmaële D,Gulik A,Dedieu JC,Demoy M,d'Angelo J,Couvreur P

更新日期：1998-04-01 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:The purpose of this study was to investigate the pH-dependent passive and active transport of weakly basic drugs across the human intestinal epithelium. METHODS:The bidirectional pH-dependent transport of weak bases was studied in Caco-2 cell monolayers in the physiologic pH range of the gastrointestinal tract...

journal_title：Pharmaceutical research

authors： Neuhoff S,Ungell AL,Zamora I,Artursson P

更新日期：2003-08-01 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：PURPOSE:To evaluate the potential of ascorbate as a novel ligand in the preparation of pharmaceutical nanocarriers with enhanced tumor-cell specific binding and cytotoxicity. METHODS:Palmitoyl ascorbate was incorporated into liposomes at varying concentrations. A stable formulation was selected based on size and zeta ...

journal_title：Pharmaceutical research

authors： D'Souza GG,Wang T,Rockwell K,Torchilin VP

更新日期：2008-11-01 00:00:00