Analysis of the compression mechanics of pharmaceutical agglomerates of different porosity and composition using the Adams and Kawakita equations.

abstract：PURPOSE:Proteasome inhibition induces endoplasmic reticulum (ER) stress and compensatory autophagy to relieve ER stress. Disturbance of intracellular calcium homeostasis can lead to ER stress and alter the autophagy process. It has been suggested that inhibition of the proteasome disrupts intracellular calcium homeosta...

journal_title：Pharmaceutical research

authors： Williams JA,Hou Y,Ni HM,Ding WX

更新日期：2013-09-01 00:00:00

abstract：PURPOSE:A mechanism-based PK-PD model was developed to predict the time course of dopamine D(2) receptor occupancy (D(2)RO) in rat striatum following administration of olanzapine, an atypical antipsychotic drug. METHODS:A population approach was utilized to quantify both the pharmacokinetics and pharmacodynamics of ol...

journal_title：Pharmaceutical research

authors： Johnson M,Kozielska M,Pilla Reddy V,Vermeulen A,Li C,Grimwood S,de Greef R,Groothuis GM,Danhof M,Proost JH

更新日期：2011-10-01 00:00:00

abstract：:The intrasubject and intersubject variabilities for CGS 16617, an angiotensin converting enzyme inhibitor, were evaluated in an open-label, repeat single-dose bioavailability trial. Eight healthy male volunteers each received a 20-mg oral dose of CGS 16617 as an aqueous solution on four separate occasions. Components ...

journal_title：Pharmaceutical research

authors： Kochak GM,Smith RA,Choi RL,John V,Tipnis V,Honc F,deSilva JK,Weidler DJ

更新日期：1989-04-01 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:The objective of this study was to determine the influence of the peptide bond with emphasis on the carbonyl group on the interaction with and transport by the intestinal small-peptide carrier. Therefore enalapril, a known substrate for the small-peptide carrier, has been modified to an analogue with a reduced ...

journal_title：Pharmaceutical research

authors： Schoenmakers RG,Stehouwer MC,Tukker JJ

更新日期：1999-01-01 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: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 examine if sparging with CO2(g) could be used to establish stable biorelevant bicarbonate buffers, in aqueous medium, for use in dissolution characterization of low-solubility ionizable drugs. METHODS:Preparation of the bicarbonate-containing dissolution medium was monitored by use...

journal_title：Pharmaceutical research

authors： McNamara DP,Whitney KM,Goss SL

更新日期：2003-10-01 00:00:00

abstract：:Polymeric biomaterials have extensively been used in medicinal applications. However, factors that determine their biocompatibility are still not very clear. This article reviews various effects of the chemical structure and the surface properties of polymeric biomaterials on their biocompatibility, including protein ...

journal_title：Pharmaceutical research

authors： Wang YX,Robertson JL,Spillman WB Jr,Claus RO

更新日期：2004-08-01 00:00:00

abstract：PURPOSE:Some therapeutic peptides exhibit amyloidogenic properties that cause insolubility and cytotoxicity against neuronal cells in vitro. Here, we characterize the conformational change in monomeric therapeutic peptide to its fibrillar aggregate in order to prevent amyloidogenic formation during clinical application...

journal_title：Pharmaceutical research

authors： Onoue S,Ohshima K,Debari K,Koh K,Shioda S,Iwasa S,Kashimoto K,Yajima T

更新日期：2004-07-01 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:The development of a physiologically based absorption model for orally administered drugs in rats is described. METHODS:Unlike other models that use a multicompartmental approach, the GI tract is modeled as a continuous tube with spatially varying properties. The mass transport through the intestinal lumen is ...

journal_title：Pharmaceutical research

authors： Willmann S,Schmitt W,Keldenich J,Dressman JB

更新日期：2003-11-01 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 demonstrate that polyanhydride copolymer chemistry affects the uptake and intracellular compartmentalization of nanospheres by THP-1 human monocytic cells. METHODS:Polyanhydride nanospheres were prepared by an anti-solvent nanoprecipitation technique. Morphology and particle diameter were confirmed via scan...

journal_title：Pharmaceutical research

authors： Ulery BD,Phanse Y,Sinha A,Wannemuehler MJ,Narasimhan B,Bellaire BH

更新日期：2009-03-01 00:00:00

abstract：PURPOSE:Vancomycin (VCM) concentration is often out of therapeutic range (10-20 μg/ml) in patients receiving continuous renal replacement therapy (CRRT). The purposes of this study were to develop a practical VCM population pharmacokinetic (PPK) model and to evaluate the potential of Bayesian prediction-based therapeut...

journal_title：Pharmaceutical research

authors： Oda K,Jono H,Kamohara H,Nishi K,Tanoue N,Saito H

更新日期：2020-05-28 00:00:00

abstract：PURPOSE:To examine the effect of particle size and morphology on aerosol dispersion using jet-milled and spray-dried mannitol particles in narrow size distributions within the respirable range. METHODS:Particle size and morphology were examined by laser diffraction and scanning electron microscopy, respectively. Aeros...

journal_title：Pharmaceutical research

authors： Louey MD,Van Oort M,Hickey AJ

更新日期：2004-07-01 00:00:00

abstract：PURPOSE:For selective inhibition of endothelial cell activation in chronic inflammation, we have developed a dexamethasone-anti-E-selectin immunoconjugate. The present study was performed to evaluate the cellular handling of this immunoconjugate by activated primary endothelial cells and to compare its drug delivery ca...

journal_title：Pharmaceutical research

authors： Kok RJ,Everts M,Asgeirsdóttir SA,Meijer DK,Molema G

更新日期：2002-11-01 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:Levofloxacin, a quinolone antibacterial drug, is a zwitterion at physiological pH. We examined the effect of cationic and anionic drugs on renal excretion of levofloxacin by means of in vivo clearance to characterize the mechanisms of renal excretion of this drug. METHODS:In vivo clearance was studied in male ...

journal_title：Pharmaceutical research

authors： Yano I,Ito T,Takano M,Inui K

更新日期：1997-04-01 00:00:00

abstract：PURPOSE:The purpose of the present study was to explore the involvement of indoxyl sulfate (IS) in nephrotoxicity and central nervous system (CNS) toxicity in cisplatin (CDDP)-treated rats. MATERIALS AND METHODS:Renal function was evaluated by serum creatinine and BUN levels. The IS levels in the serum, brain and kidn...

journal_title：Pharmaceutical research

authors： Iwata K,Watanabe H,Morisaki T,Matsuzaki T,Ohmura T,Hamada A,Saito H

更新日期：2007-04-01 00:00:00

abstract：PURPOSE:VLPs displaying tumor targeting single-chain variable fragments (VLP-rscFvs) which targets tumor-associated glycoprotein-72 (TAG-72) marker protein have a potential for immunotherapy against colon carcinoma tumors. In this study, scFvs anchored on VLPs using glycosylphosphatidylinositol (GPI) were prepared to t...

journal_title：Pharmaceutical research

authors： Deo VK,Yui M,Alam J,Yamazaki M,Kato T,Park EY

更新日期：2014-08-01 00:00:00

abstract：:In this study the intestinal degradation and absorption of a synthetic pentapeptide, metkephamid, were investigated in the rat by determination of its wall permeabilities in the small and large intestine and the extent and mechanism of its intestinal degradation. The peptide was metabolized in the gut wall through con...

journal_title：Pharmaceutical research

authors： Langguth P,Merkle HP,Amidon GL

更新日期：1994-04-01 00:00:00

abstract：PURPOSE:The current study was designed to develop thiolated-graphene quantum dots (SH-GQDs) as a theranostic nanocarrier and evaluate its potential for the optimal scavenging of reactive oxygen species (ROS) in macrophages. METHODS:SH-GQDs were prepared by hydrothermal pyrolysis of carbon source (citric acid) in the p...

journal_title：Pharmaceutical research

authors： Oh B,Lee CH

更新日期：2016-11-01 00:00:00

abstract：PURPOSE:Polyethylenimine (PEI) is a highly effective gene delivery vector, but because it is an off-the shelf material, its properties may not be optimal. To investigate the effects of the protonation properties of the polymer, we generated PEI derivatives by acetylating varying fractions of the primary and secondary a...

journal_title：Pharmaceutical research

authors： Forrest ML,Meister GE,Koerber JT,Pack DW

更新日期：2004-02-01 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: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：PURPOSE:To design, synthesize, and test synthetic glycopeptide-based delivery systems for gene targeting to hepatocytes by systemic administration. METHODS:All peptides were synthesized by the solid phase method developed using Fmoc chemistry on a peptide synthesizer. The binding of galactosylated peptides to HepG2 ce...

journal_title：Pharmaceutical research

authors： Anwer K,Logan M,Tagliaferri F,Wadhwa M,Monera O,Tung CH,Chen W,Leonard P,French M,Proctor B,Wilson E,Singhal A,Rolland A

更新日期：2000-04-01 00:00:00

abstract：PURPOSE:To evaluate organic anion transporter-mediated drug-drug interaction (DDI) potential for individual active components of Danshen (Salvia miltiorrhiza) vs. combinations using in vitro and in silico approaches. METHODS:Inhibition profiles for single Danshen components and combinations were generated in stably-ex...

journal_title：Pharmaceutical research

authors： Wang L,Venitz J,Sweet DH

更新日期：2014-12-01 00:00:00

abstract：:For the last 50 years we have known of a broad-spectrum agent tilorone dihydrochloride (Tilorone). This is a small-molecule orally bioavailable drug that was originally discovered in the USA and is currently used clinically as an antiviral in Russia and the Ukraine. Over the years there have been numerous clinical and...

journal_title：Pharmaceutical research

authors： Ekins S,Lane TR,Madrid PB

更新日期：2020-03-25 00:00:00

abstract：PURPOSE:The gadopentetic acid (Gd-DTPA)-loaded chitosan nanoparticles (Gd-nanoCPs) were prepared for gadolinium neutron-capture therapy (Gd-NCT) and characterized and evaluated as a device for intratumoral (i.t.) injection. METHODS:Gd-nanoCPs were prepared by a novel emulsion-droplet coalescence technique. The effects...

journal_title：Pharmaceutical research

authors： Tokumitsu H,Ichikawa H,Fukumori Y

更新日期：1999-12-01 00:00:00