Chemical and enzymatic degradation of ganciclovir prodrugs: enhanced stability of the diadamantoate prodrug under acid conditions.

abstract：:A biopharmaceutics drug classification scheme for correlating in vitro drug product dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling rate and extent of drug absorption. This analysis uses a transp...

journal_title：Pharmaceutical research

authors： Amidon GL,Lennernäs H,Shah VP,Crison JR

更新日期：1995-03-01 00:00:00

abstract：PURPOSE:Previously, a respirable powder (RP) formulation of pirfenidone (PFD) was developed for reducing phototoxic risk; however, PFD-RP demonstrated unacceptable in vitro inhalation performance. The present study aimed to develop a new RP system of PFD with favorable inhalation properties by spray-drying method. MET...

journal_title：Pharmaceutical research

authors： Seto Y,Suzuki G,Leung SS,Chan HK,Onoue S

更新日期：2016-06-01 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：PURPOSE:PHBHHx (poly(3-hydroxybutyrate-co-3-hydroxyhexanoate)) is an excellent biomaterial for tissue repair. Here, we aim to develop a PHBHHx-based three-dimensional (3D) scaffold system for sustained delivery of proteins (insulin serves as a model protein). METHODS:The insulin-phospholipid complex (INS-PLC) was prep...

journal_title：Pharmaceutical research

authors： Peng Q,Yang YJ,Zhang T,Wu CY,Yang Q,Sun X,Gong T,Zhang L,Zhang ZR

更新日期：2013-04-01 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：PURPOSE:The objective of this work was to assess, in vitro, the passage of P-glycoprotein dependent drugs across brain capillary endothelial cells, when these drugs are associated with a reversing agent. METHODS:An in vitro model of the blood-brain barrier consisting of a coculture of brain capillary endothelial cells...

journal_title：Pharmaceutical research

authors： Fenart L,Buée-Scherrer V,Descamps L,Duhem C,Poullain MG,Cecchelli R,Dehouck MP

更新日期：1998-07-01 00:00:00

abstract：PURPOSE:To assess the effects of co-delivering osteoinductive DNA and/or small interfering RNA in directing the osteogenic differentiation of human adipose-derived stem cells (hADSCs) using a combinatorial, non-viral gene delivery approach. METHODS:hADSCs were transfected using combinations of the following genes: BMP...

journal_title：Pharmaceutical research

authors： Ramasubramanian A,Shiigi S,Lee GK,Yang F

更新日期：2011-06-01 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：:Nonstereospecific studies have indicated that the pharmacokinetics of propranolol (PR) are altered in inflammatory conditions such as arthritis. However, as the kinetics and dynamics of PR are stereoselective, we examined the effect of adjuvant arthritis (AA) on the disposition of the individual enantiomers. A novel n...

journal_title：Pharmaceutical research

authors： Piquette-Miller M,Jamali F

更新日期：1993-02-01 00:00:00

abstract：PURPOSE:This study was aimed to investigate the effects of a phenolic antioxidant, butylated hydroxyanisole (BHA) and its metabolite, tert-butylhydroquinone (tBHQ) on the induction of HO-1, NQO1 and Nrf2 proteins and their regulatory mechanisms in primary-cultured hepatocytes. METHODS:After exposure of BHA and tBHQ to...

journal_title：Pharmaceutical research

authors： Keum YS,Han YH,Liew C,Kim JH,Xu C,Yuan X,Shakarjian MP,Chong S,Kong AN

更新日期：2006-11-01 00:00:00

abstract：PURPOSE:The goal of this investigation was to demonstrate whether the intrinsic flux of a drug diffusing across a membrane mounted in a flow-through diffusion cell may be accurately and easily determined by accounting for the accumulation in the receiver chamber. METHODS:Mathematical modeling, applied to transdermal d...

journal_title：Pharmaceutical research

authors： Harrison DJ,Knutson K

更新日期：1995-12-01 00:00:00

abstract：:The possible mechanism of hepatic uptake of colchicine (CLC), a microtubule system disrupting agent, was examined using isolated rat hepatocytes. The existence of a carrier-mediated active transport system for CLC was demonstrated. This transport system is saturable, is affected by metabolic inhibitors (dinitrophenol,...

journal_title：Pharmaceutical research

authors： Wierzba K,Sugiyama Y,Okudaira K,Iga T,Hanano M

更新日期：1989-03-01 00:00:00

abstract：PURPOSE:To study the physical and release properties of different molecular weight (MW) pH- and temperature-responsive statistical terpolymers and beads of N-isopropylacrylamide (NIPAAm), butylmethacrylate (BMA) and acrylic acid (AA). METHODS:Random terpolymers of varying MW were synthesized with NIPAAm/BMA/AA of feed...

journal_title：Pharmaceutical research

authors： Ramkissoon-Ganorkar C,Gutowska A,Liu F,Baudys M,Kim SW

更新日期：1999-06-01 00:00:00

abstract：PURPOSE:To measure the charge to mass (Q/M) ratios of the impactor stage masses (ISM) from commercial Flixotide™ 250 μg Evohaler, containing fluticasone propionate (FP), Serevent™ 25 μg Evohaler, containing salmeterol xinafoate (SX), and a combination Seretide™ 250/25 μg (FP/SX) Evohaler metered dose inhalers (MDIs). M...

journal_title：Pharmaceutical research

authors： Rowland M,Cavecchi A,Thielmann F,Kulon J,Shur J,Price R

更新日期：2018-11-26 00:00:00

abstract：:Turbidimetric or light scattering assays can be used to determine the extent of aggregation in protein formulations. Using low molecular weight urokinase (LMW-UK) as a model protein, the effect of polymeric additives on heat-induced aggregation was evaluated. Previous work has shown that under 60 degrees C heat treatm...

journal_title：Pharmaceutical research

authors： Vrkljan M,Foster TM,Powers ME,Henkin J,Porter WR,Staack H,Carpenter JF,Manning MC

更新日期：1994-07-01 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：:Interogan variation in tissue distribution of weakly basic drugs such as quinidine, propranolol, and imipramine was investigated as a function of binding to phosphatidylserine (PhS) in tissues. Tissue distributions of these drugs were determined using 10 different tissues at a steady-state plasma concentration and wer...

journal_title：Pharmaceutical research

authors： Yata N,Toyoda T,Murakami T,Nishiura A,Higashi Y

更新日期：1990-10-01 00:00:00

abstract：:The delivery of therapeutic nucleic acids to neurons has the potential to treat neurological disease and spinal cord injury. While select viral vectors have shown promise as gene carriers to neurons, their potential as therapeutic agents is limited by their toxicity and immunogenicity, their broad tropism, and the cos...

journal_title：Pharmaceutical research

authors： Bergen JM,Park IK,Horner PJ,Pun SH

更新日期：2008-05-01 00:00:00

abstract：:We investigated the effects of increased concentrations of the solutes, salicylic acid, benzoic acid, and o-, m-, and p-methoxy benzoic acids, on the anisotropic properties of a liquid crystal solvent. The lamellar liquid crystal was composed of 37% polyoxyethylene (20) isohexadecyl ether in aqueous buffer of pH 1. Ph...

journal_title：Pharmaceutical research

authors： Ibrahim HG,Sallam ES,Takieddin M,Habboub M

更新日期：1993-05-01 00:00:00

abstract：PURPOSE:To examine the presence of multiplicity for the biliary excretion of xenobiotic conjugates, we studied the disposition of glycyrrhizin (GR), which has glucuronide within its molecular structure and has the ability to inhibit the biliary excretion of liquiritigenin (LG) glucuronides. METHODS:GR was administered...

journal_title：Pharmaceutical research

authors： Shimamura H,Suzuki H,Tagaya O,Horie T,Sugiyama Y

更新日期：1996-12-01 00:00:00

abstract：:Sulfasalazine, 60 mg/kg, was administered orally to groups of rats (n = 4) along with 1, 5, or 10 mg/kg of riboflavin. Plasma and urine were assayed for 5-aminosalicylic acid, acetyl-5-aminosalicylic acid, sulfapyridine, and acetyl-sulfapyridine using an HPLC method. The mean percent of dose recovered as total metabol...

journal_title：Pharmaceutical research

authors： Chungi VS,Dittert LW,Shargel L

更新日期：1989-12-01 00:00:00

abstract：PURPOSE:Since the adoption of highly active antiretroviral therapy, HIV disease progression has slowed across the world; however, patients are often required to take multiple medications daily of poorly bioavailable drugs via the oral route, leading to gastrointestinal irritation. Recently, long acting antiretroviral i...

journal_title：Pharmaceutical research

authors： Collier MA,Gallovic MD,Bachelder EM,Sykes CD,Kashuba A,Ainslie KM

更新日期：2016-08-01 00:00:00

abstract：PURPOSE:In pharmacokinetic (PK)/pharmacodynamic (PD) modelling and simulations (M&S), omitting dropouts can cause inaccuracies in parameter estimation and clinical trial simulations (CTS). This study examines the impact of different imputation methods for missing data on the interpretation of model results, as well as ...

journal_title：Pharmaceutical research

authors： Yuen E,Gueorguieva I,Aarons L

更新日期：2014-10-01 00:00:00

abstract：:The relative effectiveness of two beta-cyclodextrin derivatives, i.e., dimethyl-beta-cyclodextrin (DM beta CD) and hydroxypropyl-beta-cyclodextrin (HP beta CD), in enhancing enteral absorption of insulin was evaluated in the lower jejunal/upper ileal segments of the rat by means of an in situ closed loop method. The i...

journal_title：Pharmaceutical research

authors： Shao Z,Li Y,Chermak T,Mitra AK

更新日期：1994-08-01 00:00:00

abstract：PURPOSE:Cell-based permeability screens are widely used to identify drug-P-glycoprotein (PGP) interaction in vitro. However, their reliability in predicting the impact of PGP on human drug pharmacokinetics is poorly defined. The aim was to determine whether a quantitative relationship exists between PGP-mediated altera...

journal_title：Pharmaceutical research

authors： Collett A,Tanianis-Hughes J,Hallifax D,Warhurst G

更新日期：2004-05-01 00:00:00

abstract：PURPOSE:This study aims to develop liposomal formulations containing synergistic antibiotics of colistin and ciprofloxacin for the treatment of infections caused by multidrug-resistant Pseudomonas aeruginosa. METHODS:Colistin (Col) and ciprofloxacin (Cip) were co-encapsulated in anionic liposomes by ammonium sulfate g...

journal_title：Pharmaceutical research

authors： Wang S,Yu S,Lin Y,Zou P,Chai G,Yu HH,Wickremasinghe H,Shetty N,Ling J,Li J,Zhou QT

更新日期：2018-08-09 00:00:00

abstract：:A sensitive radioreceptor assay (RRA) to determine the serum concentrations of fentanyl, pentazocine and morphine was developed on the basis of the drug's competition with a labeled tracer ((3)H-naloxone) for the membrane bound opioid receptor in rat brain homogenates. The binding data were computer-fitted to a standa...

journal_title：Pharmaceutical research

authors： Grevel J,Thomas J,Richards ML,Sadée W

更新日期：1984-09-01 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:Indomethacin is well known to be metabolized via O-demethylation and N-deacylation. In this paper we found an enzyme involved in the hydrolysis of amide-linkage of indomethacin and partially characterized it as well as its substrate specificity. METHODS:An indomethacin hydrolyzing enzyme was purified to homoge...

journal_title：Pharmaceutical research

authors： Terashima K,Takai S,Usami Y,Adachi T,Sugiyama T,Katagiri Y,Hirano K

更新日期：1996-09-01 00:00:00

abstract：:The effect of the penetration enhancers Azone, oleic acid, 1-dodecanol, dodecyl N,N-dimethylaminoacetate (DDAA), and dodecyl N,N-dimethylaminoisopropionate (DDAIP) on epithelial membrane lipids was examined using human buccal cell membranes as a model for epithelial lipid bilayer. Buccal epithelial cells (BEC) were la...

journal_title：Pharmaceutical research

authors： Turunen TM,Urtti A,Paronen P,Audus KL,Rytting JH

更新日期：1994-02-01 00:00:00