Increasing the proportional content of surfactant (Cremophor EL) relative to lipid in self-emulsifying lipid-based formulations of danazol reduces oral bioavailability in beagle dogs.

abstract：PURPOSE:The effects of liposomes on nitric oxide (NO) production from mouse peritoneal macrophages following intraperitoneal injection of liposomes were investigated. METHODS:Mouse peritoneal macrophages were collected following intraperitoneal injection of liposomes and cultured with and without lipopolysaccharide (L...

journal_title：Pharmaceutical research

authors： Aramaki Y,Arima H,Hara T,Tsuchiya S

更新日期：1996-09-01 00:00:00

abstract：PURPOSE:To develop an enzymatically-controlled pulsatile drug release system based on an impermeable capsule body, which contains the drug and is closed by an erodible pectin/pectinase-plug. METHODS:The plug was prepared by direct compression of pectin and pectinase in different ratios. In addition to the disintegrati...

journal_title：Pharmaceutical research

authors： Krögel I,Bodmeier R

更新日期：1999-09-01 00:00:00

abstract：PURPOSE:To co-crystallise mannitol and lactose with a view to obtaining crystals with more favourable morphological features than either lactose or mannitol alone, suitable for use as carriers in formulations for dry powder inhalers (DPIs) using simultaneous engineering of lactose-mannitol mixtures. METHODS:Mannitol a...

journal_title：Pharmaceutical research

authors： Kaialy W,Larhrib H,Martin GP,Nokhodchi A

更新日期：2012-08-01 00:00:00

abstract：PURPOSE:To evaluate the potential of ascorbate as a novel ligand in the preparation of pharmaceutical nanocarriers with enhanced tumor-cell specific binding and cytotoxicity. METHODS:Palmitoyl ascorbate was incorporated into liposomes at varying concentrations. A stable formulation was selected based on size and zeta ...

journal_title：Pharmaceutical research

authors： D'Souza GG,Wang T,Rockwell K,Torchilin VP

更新日期：2008-11-01 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:Under different charging conditions, particles can be either attracted or repulsed by each other, causing powder agglomeration or segregation. Such behavior can be detrimental in many processes aimed at achieving particulate mixture homogeneity. Consequently, the effects of electrostatic charges on mixing kinet...

journal_title：Pharmaceutical research

authors： Desrosiers Lachiver E,Abatzoglou N,Cartilier L,Simard JS

更新日期：2006-05-01 00:00:00

abstract：OBJECTIVE:Amorphous pharmaceuticals, a viable approach to enhancing bioavailability, must be stable against crystallization. An amorphous drug can be stabilized by dispersing it in a polymer matrix. To implement this approach, it is desirable to know the drug's solubility in the chosen polymer, which defines the maxima...

journal_title：Pharmaceutical research

authors： Tao J,Sun Y,Zhang GG,Yu L

更新日期：2009-04-01 00:00:00

abstract：:Coprecipitates of fluorescein and magnesium hydroxide demonstrate delayed absorption relative to fluorescein solutions when administered to the airways of the isolated perfused rat lung (IPRL). Perfusate concentration vs time profiles showed that dissolution and not epithelial permeability was the rate-controlling fac...

journal_title：Pharmaceutical research

authors： Niven RW,Byron PR

更新日期：1988-09-01 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：:The internalization of a neuromodulatory adrenocorticotropic hormone (ACTH) analogue, [125I]ebiratide (H-Met(O2)-Glu[125I]His-Phe-D-Lys-Phe-NH(CH2)2NH2), was examined in cultured monolayers of bovine brain capillary endothelial cells (BCEC). HPLC analysis of the incubation solution showed that [125I]ebiratide was not ...

journal_title：Pharmaceutical research

authors： Terasaki T,Takakuwa S,Saheki A,Moritani S,Shimura T,Tabata S,Tsuji A

更新日期：1992-04-01 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:This study was conducted to investigate in vivo the impact of interferon-alpha (IFN)-alpha on P-glycoprotein (P-gp) activity in rats by studying how its administration modifies the bioavailability of digoxin, a fairly pure P-gp substrate. METHODS:Human recombinant IFN-alpha was given to rats (n = 5-7 per group...

journal_title：Pharmaceutical research

authors： Ben Reguiga M,Bonhomme-Faivre L,Orbach-Arbouys S,Farinotti R

更新日期：2005-11-01 00:00:00

abstract：PURPOSE:To develop novel bioactive-chylomicrons to solve oral delivery obstacles of Berberine chloride and target the lymphatic system. METHODS:Berberine-loaded bioactive-chylomicrons were prepared and underwent full in vitro characterization. Intestinal permeability was appraised via both non-everted gut sac model an...

journal_title：Pharmaceutical research

authors： Elsheikh MA,Elnaggar YSR,Otify DY,Abdallah OY

更新日期：2018-01-05 00:00:00

abstract：PURPOSE:Excipients are added to lyophilized protein drug formulations to protect the protein during processing and storage, but the mechanisms are poorly understood. Here, hydrogen/deuterium (H/D) exchange with mass spectrometry was used to assess protein conformation and excipient interactions in lyophilized solids. ...

journal_title：Pharmaceutical research

authors： Li Y,Williams TD,Topp EM

更新日期：2008-02-01 00:00:00

abstract：PURPOSE:It was the purpose of this study to develop a new oral drug delivery system for low molecular weight heparin (LMWH) providing an improved bioavailability and a prolonged therapeutic effect. METHODS:The permeation enhancing polycarbophil-cysteine conjugate (PCP-Cys) used in this study displayed 111.4 +/- 6.4 mi...

journal_title：Pharmaceutical research

authors： Kast CE,Guggi D,Langoth N,Bernkop-Schnürch A

更新日期：2003-06-01 00:00:00

abstract：PURPOSE:Exenatide, a potent insulinotropic agent, can be used for the treatment of non-insulin-dependent diabetes mellitus. However, the need for frequent injections seriously limits its therapeutic utility. The aim of present report was to develop an orally available exenatide formulation using goblet cell-targeting n...

journal_title：Pharmaceutical research

authors： Li X,Wang C,Liang R,Sun F,Shi Y,Wang A,Liu W,Sun K,Li Y

更新日期：2015-03-01 00:00:00

abstract：PURPOSE:A novel photo-activated targeted chemotherapy was developed by photochemical internalization (PCI) of glutathione-sensitive polymeric micelles incorporating camptothecin (CPT) prepared from thiolated CPT (CPT-DP) and thiolated poly(ethylene glycol)-b-poly(glutamic acid) (PEG-b-P(Glu-DP)) METHODS: PEG-b-P(Glu-DP...

journal_title：Pharmaceutical research

authors： Cabral H,Nakanishi M,Kumagai M,Jang WD,Nishiyama N,Kataoka K

更新日期：2009-01-01 00:00:00

abstract：PURPOSE:β-Hydroxy-β-methylbutyrate (HMB), a nutritional supplement, elicits anabolic activity in muscle. Here we investigated the mechanism of HMB uptake in muscle cells. METHODS:Murine muscle cells (C2C12) and human mammary epithelial cells (MCF7) were used for uptake. As HMB is a monocarboxylate, focus was on monoca...

journal_title：Pharmaceutical research

authors： Ogura J,Sato T,Higuchi K,Bhutia YD,Babu E,Masuda M,Miyauchi S,Rueda R,Pereira SL,Ganapathy V

更新日期：2019-04-17 00:00:00

abstract：PURPOSE:To evaluate the impact of intestinal first-pass metabolism (Fg) by cytochrome P4503A (CYP3A) and uridine 5'-diphosphate-glucuronosyltransferases (UGT) on in vivo oral absorption of their substrate drugs. METHODS:CYP3A and UGT substrates were orally administered to portal-vein cannulated (PV) rats to evaluate t...

journal_title：Pharmaceutical research

authors： Matsuda Y,Konno Y,Hashimoto T,Nagai M,Taguchi T,Satsukawa M,Yamashita S

更新日期：2015-02-01 00:00:00

abstract：PURPOSE:Drug particle physical properties are critical for the efficiency of a drug delivered to the lung. The purpose of this study was to produce ultrafine sumatriptan succinate particles for inhalation. METHODS:Sumatriptan succinate particles were produced via reactive precipitation without any surfactants. Several...

journal_title：Pharmaceutical research

authors： Yang ZY,Le Y,Hu TT,Shen Z,Chen JF,Yun J

更新日期：2008-09-01 00:00:00

abstract：PURPOSE:To investigate the effect of polyelectrolytes on the formation and physicochemical properties of chitosan nanoparticles (CS-NPs) used for the delivery of an anticancer drug, doxorubicin (DOX). METHOD:Three DOX-loaded CS-NPs were formulated with tripolyphosphate (CS-TP/DOX NPs), dextran sulfate (CS-DS/DOX NPs),...

journal_title：Pharmaceutical research

authors： Ramasamy T,Tran TH,Cho HJ,Kim JH,Kim YI,Jeon JY,Choi HG,Yong CS,Kim JO

更新日期：2014-05-01 00:00:00

abstract：PURPOSE:To design and synthesize fatty acid-RGD peptide amphiphiles with ADA linker for their potential delivery of hydrophobic drugs like paclitaxel targeted to α(v)β(3) integrin overexpressing tumors. METHODS:Four amphiphiles - C16 or C18 fatty acid-RGD peptide and ADA linker were designed and synthesized. CMC, size...

journal_title：Pharmaceutical research

authors： Javali NM,Raj A,Saraf P,Li X,Jasti B

更新日期：2012-12-01 00:00:00

abstract：PURPOSE:Previously, we have shown that complexes of plasmid DNA with the biodegradable polymer poly(2-dimethylamino ethylamino)phosphazene (p(DMAEA)-ppz) mediated tumor selective gene expression after intravenous administration in mice. In this study, we investigated the effect of p(DMAEA)-ppz molecular weight on both ...

journal_title：Pharmaceutical research

authors： de Wolf HK,de Raad M,Snel C,van Steenbergen MJ,Fens MH,Storm G,Hennink WE

更新日期：2007-08-01 00:00:00

abstract：PURPOSE:The purpose of this study was to investigate the effects of formulation factors including varying wax concentration, drug loading and drug particle size, on drug release characteristics from both pure oil and gel formulations prepared with a combination of derivatized vegetable oil (Labrafil 1944 CS) and glycer...

journal_title：Pharmaceutical research

authors： Gao ZH,Shukla AJ,Johnson JR,Crowley WR

更新日期：1995-06-01 00:00:00

abstract：PURPOSE:Radial basis function artificial neural networks and theoretical descriptors were used to develop a quantitative structure-pharmacokinetic relationship for structurally diverse drug compounds. METHODS:Human bioavailability values were taken from the literature and descriptors were generated from the drug struc...

journal_title：Pharmaceutical research

authors： Turner JV,Maddalena DJ,Agatonovic-Kustrin S

更新日期：2004-01-01 00:00:00

abstract：PURPOSE:To advance fundamental biological and translational research with the bacterium Neisseria gonorrhoeae through the prediction of novel small molecule growth inhibitors via naïve Bayesian modeling methodology. METHODS:Inspection and curation of data from the publicly available ChEMBL web site for small molecule ...

journal_title：Pharmaceutical research

authors： Pereira JC,Daher SS,Zorn KM,Sherwood M,Russo R,Perryman AL,Wang X,Freundlich MJ,Ekins S,Freundlich JS

更新日期：2020-07-13 00:00:00

abstract：:The area function method for assessing zero-order (ko) drug absorption rates was compared to four other methods under conditions where variation occurs in the plasma concentration data and in the elimination rate constant (kel or k10) for one- or two-compartment models. For deviant kel values of a one-compartment mode...

journal_title：Pharmaceutical research

authors： Cheng HY,Jusko WJ

更新日期：1990-01-01 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:We have evaluated a new process, involving solution-enhanced dispersion by supercritical fluids (SEDS), for the production of polymeric microparticles. METHODS:The biodegradable polymers, Poly (DL-lactide-co-glycolide): copolymer composition 50:50 (DL-PLG), Poly (L-lactide) (L-PLA), Poly (DL-lactide) (DL-PLA) ...

journal_title：Pharmaceutical research

authors： Ghaderi R,Artursson P,Carlfors J

更新日期：1999-05-01 00:00:00

abstract：PURPOSE:To explore the application of scanning ion occlusion sensing (SIOS) as a novel technology for characterization of nanoparticles. METHODS:Liposomes were employed as model nanoparticles. The size distribution of the liposomes was measured by both SIOS and dynamic light scattering (DLS). Particle number concentra...

journal_title：Pharmaceutical research

authors： Yang L,Broom MF,Tucker IG

更新日期：2012-09-01 00:00:00