Buprenorphine is an Antagonist at the ϰ Opioid Receptor.

abstract：PURPOSE:The possibility of preparing nanoparticles in the supercooled thermotropic liquid crystalline state from cholesterol esters with saturated acyl chains as well as the incorporation of model drugs into the dispersions was investigated using cholesteryl myristate (CM) as a model cholesterol ester. METHODS:Nanopar...

journal_title：Pharmaceutical research

authors： Kuntsche J,Westesen K,Drechsler M,Koch MH,Bunjes H

更新日期：2004-10-01 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:To assess the uridine diphosphate (UDP)-glucuronosyltransferase (UGT) isozymes involved in the glucuronidation of niflumic acid in human liver. METHODS:The glucuronidation activity of niflumic acid was determined in liver microsomes and recombinant UGT isozymes by incubation of niflumic acid with UDP-glucuroni...

journal_title：Pharmaceutical research

authors： Mano Y,Usui T,Kamimura H

更新日期：2006-07-01 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:To assess the blood-brain barrier (BBB) permeability of 12 clinically-used drugs in mdr1a(+/+) and mdr1a(-/-) mice, and investigate the influence of lipophilicity, nonspecific brain tissue binding, and P-gp-mediated efflux on the rate of brain uptake. METHODS:The BBB partition coefficient (PS) was determined u...

journal_title：Pharmaceutical research

authors： Zhao R,Kalvass JC,Pollack GM

更新日期：2009-07-01 00:00:00

abstract：PURPOSE:To characterize temporal exposure and elimination of 5 gold/dendrimer composite nanodevices (CNDs) (5 nm positive, negative, and neutral, 11 nm negative, 22 nm positive) in mice using a physiologically based mathematical model. METHODS:400 ug of CNDs is injected intravenously to mice bearing melanoma cell line...

journal_title：Pharmaceutical research

authors： Mager DE,Mody V,Xu C,Forrest A,Lesniak WG,Nigavekar SS,Kariapper MT,Minc L,Khan MK,Balogh LP

更新日期：2012-09-01 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：:Over the last few decades, intraperitoneal (IP) local drug delivery, providing high drug concentrations with prolonged retention in the peritoneal cavity, has opened a new horizon for the management of life-threatening peritoneal disorders, such as peritoneal carcinomatosis (PC). However, clinical translation of this ...

journal_title：Pharmaceutical research

authors： Alavi S,Haeri A,Mahlooji I,Dadashzadeh S

更新日期：2020-06-03 00:00:00

abstract：PURPOSE:Interleukin-10 (IL-10) is an anti-inflammatory molecule that has achieved interest as a therapeutic for neuropathic pain. In this work, the potential of plasmid DNA-encoding IL-10 (pDNA-IL-10) slowly released from biodegradable microparticles to provide long-term pain relief in an animal model of neuropathic pa...

journal_title：Pharmaceutical research

authors： Soderquist RG,Sloane EM,Loram LC,Harrison JA,Dengler EC,Johnson SM,Amer LD,Young CS,Lewis MT,Poole S,Frank MG,Watkins LR,Milligan ED,Mahoney MJ

更新日期：2010-05-01 00:00:00

abstract：PURPOSE:This paper attempts to correlate the hydrophobic contribution constants (faa) of 21 amino acids in small peptides with commonly used physiochemical parameters. These faa constants can then be used to predict hydrophobicity change in peptides when any one of the amino acid residue is substituted with another. M...

journal_title：Pharmaceutical research

authors： Palekar D,Shiue M,Lien EJ

更新日期：1996-08-01 00:00:00

abstract：:The binding of 1-anilino-8-naphthalenesulfonate (ANS) to bovine serum albumin (BSA), human serum albumin (HSA), and human plasma has been studied by potentiometric titration utilizing a laboratory constructed ion selective electrode (ISE) of ANS. Three classes of ANS binding sites were found on BSA, HSA, and plasma at...

journal_title：Pharmaceutical research

authors： Valsami GN,Macheras PE,Koupparis MA

更新日期：1991-07-01 00:00:00

abstract：PURPOSE:Studies were conducted to evaluate whether the use of an in vitro model of the blood-brain barrier (BBB) resulted in more accurate predictions of the in vivo transport of compounds compared to the use of a human intestinal cell line (Caco-2). METHODS:The in vitro BBB model employs bovine brain capillary endoth...

journal_title：Pharmaceutical research

authors： Lundquist S,Renftel M,Brillault J,Fenart L,Cecchelli R,Dehouck MP

更新日期：2002-07-01 00:00:00

abstract：PURPOSE:To characterize factor(s) contained in apical medium of primary cultured rat alveolar epithelial type II cell-like monolayers (RAECM-II) that enhance insulin absorption across alveolar epithelial cells. MATERIALS AND METHODS:Primary rat alveolar epithelial cell monolayers cultured on Transwells in the presence...

journal_title：Pharmaceutical research

authors： Bahhady R,Kim KJ,Borok Z,Crandall ED,Shen WC

更新日期：2007-09-01 00:00:00

abstract：PURPOSE:Platinum-based therapies are the first line treatments for most types of cancer including ovarian cancer. However, their use is associated with dose-limiting toxicities and resistance. We report initial translational studies of a theranostic nanoemulsion loaded with a cisplatin derivative, myrisplatin and pro-a...

journal_title：Pharmaceutical research

authors： Ganta S,Singh A,Kulkarni P,Keeler AW,Piroyan A,Sawant RR,Patel NR,Davis B,Ferris C,O'Neal S,Zamboni W,Amiji MM,Coleman TP

更新日期：2015-08-01 00:00:00

abstract：PURPOSE:Covalent binding between N-acetyl-L-cysteine (NAC) and albumin was evaluated kinetically by conducting in vitro experiments. METHOD:After 14C-NAC was incubated with human or rat serum, the solution was analyzed by anion-exchange HPLC. The albumin-bound 14C-NAC was quantified by measuring the radioactivity in t...

journal_title：Pharmaceutical research

authors： Harada D,Naito S,Otagiri M

更新日期：2002-11-01 00:00:00

abstract：PURPOSE:The lack of water-solubility hampers the use of many potent pharmaceuticals. Polymeric micelles are self-assembled nanocarriers with versatile properties that can be engineered to solubilize, target, and release hydrophobic drugs in a controlled-release fashion. Unfortunately, their large-scale use is limited b...

journal_title：Pharmaceutical research

authors： Fournier E,Dufresne MH,Smith DC,Ranger M,Leroux JC

更新日期：2004-06-01 00:00:00

abstract：PURPOSE:Targeted delivery of aerosols could not only improve efficacy of inhaled drugs but also reduce side effects resulting from their accumulation in healthy tissue. Here we investigated the impact of magnetized aerosols on model drug accumulation and transgene expression in magnetically targeted lung regions of una...

journal_title：Pharmaceutical research

authors： Hasenpusch G,Geiger J,Wagner K,Mykhaylyk O,Wiekhorst F,Trahms L,Heidsieck A,Gleich B,Bergemann C,Aneja MK,Rudolph C

更新日期：2012-05-01 00:00:00

abstract：PURPOSE:To evaluate 26 marketed oncology drugs for time-dependent inhibition (TDI) of cytochrome P450 (CYP) enzymes. Evaluate TDI-positive drugs for potential to generate reactive intermediates. Assess clinical drug-drug interaction (DDI) risk using static mechanistic models. METHODS:Human liver microsomes and CYP-spe...

journal_title：Pharmaceutical research

authors： Kenny JR,Mukadam S,Zhang C,Tay S,Collins C,Galetin A,Khojasteh SC

更新日期：2012-07-01 00:00:00

abstract：PURPOSE:Understanding the critical factors governing the crystallization tendency of organic compounds is vital when assessing the feasibility of an amorphous formulation to improve oral bioavailability. The objective of this study was to investigate potential links between viscosity and crystallization tendency for or...

journal_title：Pharmaceutical research

authors： Baird JA,Santiago-Quinonez D,Rinaldi C,Taylor LS

更新日期：2012-01-01 00:00:00

abstract：PURPOSE:Chitosan and its derivatives possess several unique properties relevant in the field of pharmaceutics and medicinal chemistry. This study aimed to evaluate the pharmaceutical performance of an innovative chitosan derivative, methyl acrylate chitosan bearing p-nitrobenzaldehyde (MA*CS*pNBA) Schiff base. METHODS...

journal_title：Pharmaceutical research

authors： Ali SS,Kenawy ER,Sonbol FI,Sun J,Al-Etewy M,Ali A,Huizi L,El-Zawawy NA

更新日期：2018-11-07 00:00:00

abstract：:During the past two decades the nanomedicine field has experienced significant progress. To date, over sixty nanoparticle (NP) formulations have been approved in the US and EU while many others are in clinical or preclinical development, indicating a concerted effort to translate promising bench research to commercial...

journal_title：Pharmaceutical research

authors： Clogston JD,Hackley VA,Prina-Mello A,Puri S,Sonzini S,Soo PL

更新日期：2019-12-11 00:00:00

abstract：PURPOSE:The present study evaluates immobilized artificial membrane (IAM) chromatography for predicting drug permeability across the blood-brain barrier (BBB) and outlines the potential and limitations of IAMs as a predictive tool by comparison with conventional methods based on octanol/water partitioning and octadecyl...

journal_title：Pharmaceutical research

authors： Reichel A,Begley DJ

更新日期：1998-08-01 00:00:00

abstract：:The partitioning of a series of nine nitroimidazole drugs in liposomes (log Km) of various compositions has been determined and compared to their partitioning in the n-octanol/saline system (log K) at 30 degrees C. The log Km ranged from 1.5 to 0.5 and was three- to fourfold greater than the log K; further, the linear...

journal_title：Pharmaceutical research

authors： Betageri GV,Rogers JA

更新日期：1989-05-01 00:00:00

abstract：:Celiac disease (CD) is an immune-mediated enteropathy triggered by the ingestion of gluten-containing grains that affects ~1% of the white ethnic population. In the last decades, a rise in prevalence of CD has been observed that cannot be fully explained by improved diagnostics. Genetic predisposition greatly influenc...

journal_title：Pharmaceutical research

authors： Matoori S,Fuhrmann G,Leroux JC

更新日期：2013-03-01 00:00:00

abstract：PURPOSE:To develop a liposomal system with high drug loading (DL) for intravenous (i.v.) delivery of a poorly water-soluble basic drug, asulacrine (ASL). METHODS:A thin-film hydration and extrusion method was used to fabricate the PEGylated liposomal membranes followed by a freeze and thaw process. A novel active drug...

journal_title：Pharmaceutical research

authors： Zhang W,Wang G,Falconer JR,Baguley BC,Shaw JP,Liu J,Xu H,See E,Sun J,Aa J,Wu Z

更新日期：2015-04-01 00:00:00

abstract：PURPOSE:Multidrug and toxin extrusion proteins (MATEs) are multispecific organic cation transporters mediating the efflux of various cationic drugs into the urine. The present study aimed at identifying endogenous compounds in human plasma and urine specimens as biomarkers to evaluate drug interactions involving MATEs ...

journal_title：Pharmaceutical research

authors： Kato K,Mori H,Kito T,Yokochi M,Ito S,Inoue K,Yonezawa A,Katsura T,Kumagai Y,Yuasa H,Moriyama Y,Inui K,Kusuhara H,Sugiyama Y

更新日期：2014-01-01 00:00:00

abstract：PURPOSE:To determine whether a Protected Graft Copolymer (PGC) containing fatty acid can be used as a stabilizing excipient for GLP-1 and whether PGC/GLP-1 given once a week can be an effective treatment for diabetes. METHODS:To create a PGC excipient, polylysine was grafted with methoxypolyethyleneglycol and fatty ac...

journal_title：Pharmaceutical research

authors： Castillo GM,Reichstetter S,Bolotin EM

更新日期：2012-01-01 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：:Inhibition of efflux pumps is an emerging approach in cancer therapy and drug delivery. Since it has been discovered that polymeric pharmaceutical excipients such as Tweens or Pluronics can inhibit efflux pumps, various other polymers have been investigated regarding their potential efflux pump inhibitory activity. Am...

journal_title：Pharmaceutical research

authors： Werle M

更新日期：2008-03-01 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