Dissolution techniques for in vitro testing of dry powders for inhalation.

abstract：PURPOSE:This study was conducted to assess the pharmacokinetics and pharmacodynamics of 7-nitroindazole (7-NI), a selective inhibitor of neuronal nitric oxide synthase (NOS). METHODS:Male Sprague-Dawley rats were equipped with peritoneal/ venous cannulae and a microdialysis probe in the hippocampal cortex. Rats receiv...

journal_title：Pharmaceutical research

authors： Bush MA,Pollack GM

更新日期：2001-11-01 00:00:00

abstract：PURPOSE:To evaluate the transcellular mechanism of novel enhancers absorption enhancement of human growth hormone (hGH), by examining the involvement of a P-glycoprotein-like efflux system, changes in membrane fluidity, and membrane damage. METHODS:Caco-2 cell monolayers were grown on Snapwell filter supports and plac...

journal_title：Pharmaceutical research

authors： Wu SJ,Robinson JR

更新日期：1999-08-01 00:00:00

abstract：PURPOSE:Since the absorption of ceftriaxone (CTO) in the intestine is restricted by its natural physiological characteristics, we developed a series of small synthetic compounds derived from bile acids to promote the absorption of CTO in the gastrointestinal tract. METHODS:Several bile acid derivatives were screened b...

journal_title：Pharmaceutical research

authors： Jeon OC,Hwang SR,Al-Hilal TA,Park JW,Moon HT,Lee S,Park JH,Byun Y

更新日期：2013-04-01 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：:Physicochemical effects caused by intestinal fluids on drugs in the gastrointestinal (GI) tract can be a contributing factor in food induced changes in bioavailability. To identify physicochemical properties of gemfibrozil that may be altered by endogenous and dietary lipids, in vitro studies were conducted in model s...

journal_title：Pharmaceutical research

authors： Luner PE,Babu SR,Radebaugh GW

更新日期：1994-12-01 00:00:00

abstract：:Although much effort has been devoted to opioid research since the identification of enkephalins, understanding of the physiological importance and mechanisms of action of endogenous opioids lags behind understanding of opiate alkaloids such as morphine. In recent years, several novel approaches have been refined with...

journal_title：Pharmaceutical research

authors： Rapaka RS,Porreca F

更新日期：1991-01-01 00:00:00

abstract：PURPOSE:Modulation of 5-HT3 receptor in the central nervous system (CNS) is a promising approach for treatment of neuropathic pain. The goal was to evaluate the role of P-glycoprotein (Pgp) in limiting exposure of different parts of the CNS to ondansetron (5-HT3 receptor antagonist) using wild-type and genetic knockout...

journal_title：Pharmaceutical research

authors： Chiang M,Back HM,Lee JB,Oh S,Guo T,Girgis S,Park C,Haroutounian S,Kagan L

更新日期：2020-09-28 00:00:00

abstract：PURPOSE:To develop a new bionic system from an existing drug dissolution/absorption simulating system (DDASS) to simultaneously predict the release and absorption of enteric-coated formulations. METHODS:In accordance with the pH-dependent characteristics of enteric-coated formulations, the modified DDASS was designed ...

journal_title：Pharmaceutical research

authors： Liu W,He X,Li Z,Gao X,Ma Y,Xun M,Liu C

更新日期：2013-02-01 00:00:00

abstract：:The limitations of traditional gas adsorption models for describing water vapor sorption by amorphous pharmaceutical solids are described and an alternative approach based on polymer solution theories is proposed. The approach is tested by comparing a priori predicted isotherms with literature data for the poly(vinylp...

journal_title：Pharmaceutical research

authors： Hancock BC,Zografi G

更新日期：1993-09-01 00:00:00

abstract：PURPOSE:The cause of antibody positive pure red cell aplasia associated with the subcutaneous administration of EPREX to patients with chronic kidney failure has been determined to be due to the leaching of weakly adjuvant compounds from the uncoated rubber stoppers that were formerly used in prefilled syringes. Other ...

journal_title：Pharmaceutical research

authors： Villalobos AP,Gunturi SR,Heavner GA

更新日期：2005-07-01 00:00:00

abstract：:Dihydropyridine ⇄ pyridinium salt-based brain-selective delivery systems were synthesized for the progestins, ethisterone, norethindrone, and norgestrel. After initial lipophilicity and in vitro studies indicated the feasibility of applying these compounds to brain-specific delivery, in vivo distribution studies were ...

journal_title：Pharmaceutical research

authors： Brewster ME,Estes KS,Bodor N

更新日期：1986-10-01 00:00:00

abstract：:Unsymmetrical aryl(heteroaryl)methyl isopropyl ester analogues of nifedipine, in which the 2-nitrophenyl group at C-4 is replaced by a 2- or 3-pyridyl substituent, were synthesized and evaluated as calcium-channel antagonists using guinea pig ileal longitudinal smooth muscle. The point of attachment of the C-4 pyridyl...

journal_title：Pharmaceutical research

authors： Akula MR,Matowe WC,Wolowyk MW,Knaus EE

更新日期：1990-09-01 00:00:00

abstract：PURPOSE:To study the structure and function of the intestinal H+/ peptide transporter PET1, we compared its amino acid sequence with those of related transporters belonging to the oligopeptide transporter family PTR, and with more distant transporter families. METHODS:We have developed a new approach to the sequence a...

journal_title：Pharmaceutical research

authors： Graul RC,Sadée W

更新日期：1997-04-01 00:00:00

abstract：:The binding of diflunisal to hydroxypropyl-beta-cyclodextrin (HP beta CD), bovine serum albumin (BSA), human serum albumin (HSA), normal human plasma, and mixed solutions of HP beta CD/protein was studied at 25 degrees C, pH 7.4, by potentiometry using an electrode selective to diflunisal. The experimental data for di...

journal_title：Pharmaceutical research

authors： Sideris EE,Koupparis MA,Macheras PE

更新日期：1994-01-01 00:00:00

abstract：PURPOSE:Understanding the mechanism of protein-excipient interaction and illuminating the influencing factors on protein stability are key steps in the rational design of protein formulations. The objective of this study was to assess effects of preferential interaction type of excipient and surface aromatic hydrophobi...

journal_title：Pharmaceutical research

authors： Wen L,Zheng X,Wang X,Lan H,Yin Z

更新日期：2017-07-01 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：:5'-Ester derivatives of 5-iodo-2'-deoxyuridine (IDU) with varying degrees of lipophilicity were examined to evaluate the effectiveness of lipophilic ester prodrugs for enhanced and sustained delivery of IDU to the brain parenchyma. Approximately 1.0% (1.0 +/- 0.19; n = 4) of the total radioactivity was found in the br...

journal_title：Pharmaceutical research

authors： Ghosh MK,Mitra AK

更新日期：1992-09-01 00:00:00

abstract：PURPOSE:To investigate the moisture-induced aggregation (i.e., a loss of solubility in water) of DNA in a solid state and to develop rational strategies for its prevention. METHODS:Lyophilized calf thymus DNA was exposed to relative humidity (RH) levels from 11% to 96% at 55 degrees C. Following a 24-h incubation unde...

journal_title：Pharmaceutical research

authors： Sharma VK,Klibanov AM

更新日期：2007-01-01 00:00:00

abstract：PURPOSE:To improve the delivery of liposomes to tumors using P-selectin glycoprotein ligand 1 (PSGL1) mediated binding to selectin molecules, which are upregulated on tumorassociated endothelium. METHODS:PSGL1 was orientated and presented on the surface of liposomes to achieve optimal selectin binding using a novel st...

journal_title：Pharmaceutical research

authors： Carlisle R,Seymour LW,Coussios CC

更新日期：2013-02-01 00:00:00

abstract：PURPOSE:This study was designed to investigate the stability of recombinant FVIII (rFVIII) in solution at different pHs and to probe the cause(s) of rFVIII inactivation under accelerated storage conditions. METHODS:Aqueous stability samples of full-length rFVIII at different pHs were incubated at 40 degrees C for seve...

journal_title：Pharmaceutical research

authors： Wang W,Kelner DN

更新日期：2003-04-01 00:00:00

abstract：PURPOSE:To evaluate micronized powder retention and detachment from inhaler surfaces following reproducible deposition by impaction, coupled with centrifugal particle detachment (CPD). METHODS:Micronized albuterol sulfate (AS) and beclomethasone dipropionate (BDP) were aerosolized as dry powders and deposited by casca...

journal_title：Pharmaceutical research

authors： Clarke MJ,Peart J,Cagnani S,Byron PR

更新日期：2002-03-01 00:00:00

abstract：PURPOSE:Orthorhombic crystals of paracetamol exhibit good technological properties during compression. The purpose of this study was to investigate the compression behavior of this substance and to compare it to that of monoclinic paracetamol. From the crystal structure, it could be hypothesized that sliding planes are...

journal_title：Pharmaceutical research

authors： Joiris E,Di Martino P,Berneron C,Guyot-Hermann AM,Guyot JC

更新日期：1998-07-01 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:The organic cation transporters (OCTs) and multidrug and toxin extrusions (MATEs) together are regarded as an organic cation transport system critical to the disposition and response of many organic cationic drugs. Patient response to the analgesic morphine, a characterized substrate for human OCT1, is highly v...

journal_title：Pharmaceutical research

authors： Zhu P,Ye Z,Guo D,Xiong Z,Huang S,Guo J,Zhang W,Polli JE,Zhou H,Li Q,Shu Y

更新日期：2018-10-25 00:00:00

abstract：PURPOSE:Development of a human mitochondrial gene delivery vector is a critical step in the ability to treat diseases arising from mutations in mitochondrial DNA. Although we have previously cloned the mouse mitochondrial genome in its entirety and developed it as a mitochondrial gene therapy vector, the human mitochon...

journal_title：Pharmaceutical research

authors： Bigger BW,Liao AY,Sergijenko A,Coutelle C

更新日期：2011-11-01 00:00:00

abstract：PURPOSE:The sensitivity and effectiveness of indirect metrics proposed for the assessment of comparative absorption rates in bioequivalence studies [Cmax, Tmax, partial AUC (AUCp), feathered slope (SLf), intercept metric (I)] were originally tested by assuming first-order absorption. The present study re-evaluates thei...

journal_title：Pharmaceutical research

authors： Ring A,Tothfalusi L,Endrenyi L,Weiss M

更新日期：2000-05-01 00:00:00

abstract：PURPOSE:To identify and quantify, in vitro and in vivo (in humans), the charge-carrying species during transdermal iontophoresis of lidocaine hydrochloride as a function of the concentration of drug relative to that of sodium chloride in the anodal solution. METHODS:In vitro experiments in standard diffusion cells qua...

journal_title：Pharmaceutical research

authors： Marro D,Kalia YN,Delgado-Charro MB,Guy RH

更新日期：2001-12-01 00:00:00

abstract：PURPOSE:The purpose of this research was to evaluate the effect of ultrasound on mass transport across fetal membrane for direct fetal drug delivery and sensing of the amniotic fluid in a noninvasive manner. METHODS:Post-delivery human fetal membranes (chorioamnion) were used for in vitro experiments, in which the eff...

journal_title：Pharmaceutical research

authors： Wolloch L,Azagury A,Goldbart R,Traitel T,Groisman G,Hallak M,Kost J

更新日期：2015-02-01 00:00:00

abstract：PURPOSE:It was the aim of this study to synthesize and characterize a novel chitosan-glutathione (GSH) conjugate providing improved mucoadhesive and permeation-enhancing properties. METHODS:Mediated by carbodiimide and N-hydroxysuccinimide, glutathione was covalently attached to chitosan via the formation of an amide ...

journal_title：Pharmaceutical research

authors： Kafedjiiski K,Föger F,Werle M,Bernkop-Schnürch A

更新日期：2005-09-01 00:00:00

abstract：PURPOSE:An ex vivo intact toe model was developed to assess two different applicator designs for iontophoretic delivery of terbinafine into the nail only or the nail and surrounding skin. METHODS:Iontophoretic permeation studies were carried out on intact cadaver toes using nail-only and nail/skin applicators with a c...

journal_title：Pharmaceutical research

authors： Nair AB,Kim HD,Davis SP,Etheredge R,Barsness M,Friden PM,Murthy SN

更新日期：2009-09-01 00:00:00