Disparity of in vitro and in vivo oleic acid-enhanced beta-estradiol percutaneous absorption across human skin.

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:The purpose was to develop a population pharmacokinetic model for montelukast after intravenous administration. Clinical trial simulations were conducted using the model developed to identify the lowest intravenous dose in 6- to 14-year-old children that would give montelukast systemic exposures that were compa...

journal_title：Pharmaceutical research

authors： Ramakrishnan R,Migoya E,Knorr B

更新日期：2005-04-01 00:00:00

abstract：:Knowledge Management (KM) is a key enabler for achieving quality in a lifecycle approach for production of biopharmaceuticals. Due to the important role that it plays towards successful implementation of Quality by Design (QbD), an analysis of KM solutions is needed. This work provides a comprehensive review of the in...

journal_title：Pharmaceutical research

authors： Rathore AS,Garcia-Aponte OF,Golabgir A,Vallejo-Diaz BM,Herwig C

更新日期：2017-02-01 00:00:00

abstract：PURPOSE:Lapatinib, a small molecule EGFR/HER2 inhibitor, partially inhibits the outgrowth of HER2+ brain metastases in preclinical models and in a subset of CNS lesions in clinical trials of HER2+ breast cancer. We investigated the ability of lapatinib to reach therapeutic concentrations in the CNS following (14)C-lapa...

journal_title：Pharmaceutical research

authors： Taskar KS,Rudraraju V,Mittapalli RK,Samala R,Thorsheim HR,Lockman J,Gril B,Hua E,Palmieri D,Polli JW,Castellino S,Rubin SD,Lockman PR,Steeg PS,Smith QR

更新日期：2012-03-01 00:00:00

abstract：:A reverse-phase HPLC method for the analysis of tryptic digests of recombinant porcine growth hormone (pGH) has been developed and validated. Digestion was performed at 4 degrees C for a 20-hr period with TPCK-treated trypsin at a 1:20 (w/w) trypsin:pGH ratio. Gradient elution HPLC, using an Aquapore RP300 C8 column, ...

journal_title：Pharmaceutical research

authors： Charman SA,McCrossin LE,Charman WN

更新日期：1993-10-01 00:00:00

abstract：PURPOSE:The prognosis for glioma patients is poor, and development of new treatments is critical. Previously, we engineered polymer-based vaccines that control GM-CSF, CpG-oligonucleotide, and tumor-lysate presentation to regulate immune cell trafficking and activation, which promoted potent immune responses against pe...

journal_title：Pharmaceutical research

authors： Ali OA,Doherty E,Bell WJ,Fradet T,Hudak J,Laliberte MT,Mooney DJ,Emerich DF

更新日期：2011-05-01 00:00:00

abstract：PURPOSE:We present a smart intradermal interface suitable for skin-attached drug delivery devices. Our solution enables injections or infusions that are less invasive compared to subcutaneous injections and are leakage-free at the location of penetration. METHODS:The intradermal interface is based on a 31-gauge cannul...

journal_title：Pharmaceutical research

authors： Vosseler M,Jugl M,Zengerle R

更新日期：2011-03-01 00:00:00

abstract：:Esmolol hydrochloride degrades in aqueous solutions by the hydrolysis of a labile aliphatic carboxyester group. The products are methanol and ASL-8123. The resulting aliphatic carboxylic acid moiety (ASL-8123) has a pK of 4.80, which is within 1 pH unit of the pH of the formulation. ASL-8123 therefore acts as a "secon...

journal_title：Pharmaceutical research

authors： Rosenberg LS,Hostetler CK,Wagenknecht DM,Aunet DA

更新日期：1988-08-01 00:00:00

abstract：PURPOSE:In this study, we developed and evaluated a novel method to produce insulin-loaded hydrophilic microspheres allowing high encapsulation efficiency and the preservation of peptide stability during particle processing. The preparation method used the diffusion of water by an excess of solvent starting from a wate...

journal_title：Pharmaceutical research

authors： Trotta M,Chirio D,Cavalli R,Peira E

更新日期：2004-08-01 00:00:00

abstract：PURPOSE:To investigate the destruction of clinically-relevant bacteria within biofilms via the sustained release of the antibiotic tetracycline from zein-based electrospun polymeric fibrous matrices and to demonstrate the compatibility of such wound dressing matrices with human skin cells. METHODS:Zein/PCL triple laye...

journal_title：Pharmaceutical research

authors： Alhusein N,Blagbrough IS,Beeton ML,Bolhuis A,De Bank PA

更新日期：2016-01-01 00:00:00

abstract：PURPOSE:Changes in drug absorption and first-pass metabolism have been reported throughout the pediatric age range. Our aim is to characterize both intestinal and hepatic CYP3A-mediated metabolism of midazolam in children in order to predict first-pass and systemic metabolism of CYP3A substrates. METHODS:Pharmacokinet...

journal_title：Pharmaceutical research

authors： Brussee JM,Yu H,Krekels EHJ,Palić S,Brill MJE,Barrett JS,Rostami-Hodjegan A,de Wildt SN,Knibbe CAJ

更新日期：2018-07-30 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：PURPOSE:The purpose of this study was to determine the potential effect of probenecid on the pharmacokinetics of zalcitabine in HIV-positive patients. METHODS:Twelve patients received single oral 1.5 mg doses of zalcitabine alone and during probenecid treatment (500 mg at 8 and 2 hours before and 4 hours after zalcita...

journal_title：Pharmaceutical research

authors： Massarella JW,Nazareno LA,Passe S,Min B

更新日期：1996-03-01 00:00:00

abstract：:A series of multilamellar liposome dispersions was prepared from lipids of soy phosphatidylcholine or hydrogenated soy phosphatidylcholine containing from 0 to 30 mol% of either cholesterol, stearylamine, or dipalmitoyl phosphatidylglycerol. The liposome dispersions were aerosolized with a Collison nebulizer for 80 mi...

journal_title：Pharmaceutical research

authors： Niven RW,Schreier H

更新日期：1990-11-01 00:00:00

abstract：:The transepithelial transport of arginine vasopressin (AVP) across cultured rat alveolar epithelial cell monolayers was studied. At 0.1 nM donor [125I]AVP, the radiolabel flux measured in the apical-to-basolateral (AB) direction was about 10 times greater than that in the reverse (BA) direction. HPLC analyses of the b...

journal_title：Pharmaceutical research

authors： Yamahara H,Morimoto K,Lee VH,Kim KJ

更新日期：1994-11-01 00:00:00

abstract：PURPOSE:Bioadhesion is an important property of biological membranes, that can be utilized in pharmaceutical and biomedical applications. In this study, we have fabricated mucoadhesive drug releasing films with bio-based, non-toxic and biodegradable polymers that do not require chemical modifications. METHODS:Nanofibr...

journal_title：Pharmaceutical research

authors： Laurén P,Paukkonen H,Lipiäinen T,Dong Y,Oksanen T,Räikkönen H,Ehlers H,Laaksonen P,Yliperttula M,Laaksonen T

更新日期：2018-05-22 00:00:00

abstract：PURPOSE:Critical steps in the subcellular processing of poly(ethylene imine)/nucleic acid complexes, especially endosomal/lysosomal escape, were visualized by using living cell confocal laser scanning microscopy (CSLM) to obtain an insight into their mechanism. METHODS:Living cell confocal microscopy was used to exami...

journal_title：Pharmaceutical research

authors： Merdan T,Kunath K,Fischer D,Kopecek J,Kissel T

更新日期：2002-02-01 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：: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 purpose of this study was to investigate the delivery of itraconazole (ITZ) particles to a murine lung model by nebulization. METHODS:Three ITZ formulations were prepared and characterized in the dry state using contact angle, dissolution, X-ray powder diffraction, scanning electron microscopy, and Brunaue...

journal_title：Pharmaceutical research

authors： McConville JT,Overhoff KA,Sinswat P,Vaughn JM,Frei BL,Burgess DS,Talbert RL,Peters JI,Johnston KP,Williams RO 3rd

更新日期：2006-05-01 00:00:00

abstract：PURPOSE:To evaluate the use of an in vitro intestinal permeability model to predict rat and human absorption as well as to evaluate the use of an internal standard to control for intra- and inter-rat variability. METHODS:In vivo peroral absorption and in vitro steady-state intestinal permeability coefficients were det...

journal_title：Pharmaceutical research

authors： Dowty ME,Dietsch CR

更新日期：1997-12-01 00:00:00

abstract：:Biotherapeutics, including recombinant or plasma-derived human proteins and antibody-based molecules, have emerged as an important class of pharmaceuticals. Aggregation and immunogenicity are among the major bottlenecks during discovery and development of biotherapeutics. Computational tools that can predict aggregati...

journal_title：Pharmaceutical research

authors： Kumar S,Singh SK,Wang X,Rup B,Gill D

更新日期：2011-05-01 00:00:00

abstract：PURPOSE:HSP90 (Heat shock protein 90kD) has been validated as a therapeutic target in Castrate Resistant Prostate Cancer. Unfortunately, HSP90 inhibitors suffer from dose-limiting toxicities that hinder their clinical applications. Previously developed polymeric delivery systems for HSP90 inhibitors had either low drug...

journal_title：Pharmaceutical research

authors： Suárez Del Pino JA,Kolhatkar R

更新日期：2017-12-01 00:00:00

abstract：:Monte Carlo simulation technique used to evaluate the effect of the arrangement of concentrations on the efficiency of estimation of population pharmacokinetic parameters in the preclinical setting is described. Although the simulations were restricted to the one compartment model with intravenous bolus input, they pr...

journal_title：Pharmaceutical research

authors： Ette EI,Howie CA,Kelman AW,Whiting B

更新日期：1995-05-01 00:00:00

abstract：PURPOSE:To evaluate the potential of several bis-ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA, adefovir) to enhance the oral absorption of PMEA. METHODS:Caco-2 monolayers were used to estimate intestinal transport and metabolism of the bis(pivaloyloxymethyl)-ester [bis(POM)-] and a s...

journal_title：Pharmaceutical research

authors： Annaert P,Gosselin G,Pompon A,Benzaria S,Valette G,Imbach JL,Naesens L,Hatse S,de Clercq E,Van den Mooter G,Kinget R,Augustijns P

更新日期：1998-02-01 00:00:00

abstract：:A novel method of dipeptide synthesis is described that can be carried out in aqueous solution and does not require complicated protecting and deprotecting procedures. An analgesic neuropeptide named kyotorphin, H-Tyr-Arg-OH, was synthesized from unprotected tyrosine and arginine in a new enzymatic reaction catalyzed ...

journal_title：Pharmaceutical research

authors： Kitabatake S,Tsurutani R,Nakajima H,Tomita K,Yoshihara Y,Ueda H,Takagi H,Imahori K

更新日期：1987-04-01 00:00:00

abstract：PURPOSE:The aim of this study is to investigate the effects of 50% ethyl acetate extracts of grapefruit juice (GFJ) and orange juice (OJ) on the transport activity of P-glycoprotein (P-gp) in the rat small intestine. METHODS:The efflux of P-gp substrates from rat everted sac in the absence or presence of verapamil, GF...

journal_title：Pharmaceutical research

authors： Tian R,Koyabu N,Takanaga H,Matsuo H,Ohtani H,Sawada Y

更新日期：2002-06-01 00:00:00

abstract：:The conditions under which the absorption enhancer palmitoyl L-carnitine chloride (PCC) improved the bioavailability of the poorly absorbed antibiotic cefoxitin throughout the rat intestine has been studied. Cefoxitin alone was appreciably absorbed only in the duodenum (31% vs less than 7% elsewhere). PCC solutions (3...

journal_title：Pharmaceutical research

authors： Sutton SC,LeCluyse EL,Cammack L,Fix JA

更新日期：1992-02-01 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:To determine the different conformations of the acyloxyalkoxy-linked cyclic prodrug 1 of the model hexapeptide 2 in solution and to investigate the relationship between these solution conformations and the cellular permeability characteristics of this prodrug. METHODS:Two-dimensional Homonuclear Hartmann-Hahn ...

journal_title：Pharmaceutical research

authors： Gangwar S,Jois SD,Siahaan TJ,Vander Velde DG,Stella VJ,Borchardt RT

更新日期：1996-11-01 00:00:00