Factors affecting the stability of nanoemulsions--use of artificial neural networks.

abstract：:Molecular modeling has been used to study the complexation between alpha, beta, or gamma-cyclodextrin (CD) and a group of amine compounds having the diphenylmethyl functionality. The computer program SYBYL 5.3 and the Tripos force field (version 5.2) were used for all the calculations. Three-dimensional structures of ...

journal_title：Pharmaceutical research

authors： Tong WQ,Lach JL,Chin TF,Guillory JK

更新日期：1991-10-01 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:The purpose of this study was to determine the potential effect of probenecid on the pharmacokinetics of zalcitabine in HIV-positive patients. METHODS:Twelve patients received single oral 1.5 mg doses of zalcitabine alone and during probenecid treatment (500 mg at 8 and 2 hours before and 4 hours after zalcita...

journal_title：Pharmaceutical research

authors： Massarella JW,Nazareno LA,Passe S,Min B

更新日期：1996-03-01 00:00:00

abstract：PURPOSE:The passage of molecules across cell membranes is a crucial step in many physiological processes. We therefore seek physical models of this process, in order to predict permeation for new molecules, and to better understand the important interactions which determine the rate of permeation. METHODS:Several sets...

journal_title：Pharmaceutical research

authors： Platts JA,Abraham MH,Hersey A,Butina D

更新日期：2000-08-01 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：PURPOSE:This study was carried out to examine the blood-brain barrier (BBB) transport of human basic fibroblast growth factor (bFGF) and investigate its mechanism. METHODS:The BBB transport of 125I-bFGF was measured by several in vivo methods including intravenous administration, in situ internal carotid artery perfus...

journal_title：Pharmaceutical research

authors： Deguchi Y,Naito T,Yuge T,Furukawa A,Yamada S,Pardridge WM,Kimura R

更新日期：2000-01-01 00:00:00

abstract：PURPOSE:Generalizations based upon behavior of small molecules have established that a crystalline solid is generally much more stable toward chemical degradation than is the amorphous solid. This study examines the validity of this generalization for proteins using biosynthetic human insulin as the model protein. MET...

journal_title：Pharmaceutical research

authors： Pikal MJ,Rigsbee DR

更新日期：1997-10-01 00:00:00

abstract：:The synthesis of an homologous series of new water-soluble derivatives of pilocarpine is described. The new compounds, referred to as soft quaternary salts, are water soluble by virtue of a cationic ammonium head and their lipophilicity can be modulated by manipulating the size and the nature of the substituent in the...

journal_title：Pharmaceutical research

authors： Druzgala P,Winwood D,Drewniak-Deyrup M,Smith S,Bodor N,Kaminski JJ

更新日期：1992-03-01 00:00:00

abstract：PURPOSE:To investigate plasmid DNA interactions with liposomes prepared from dimyristoylglyceroethylphosphocholine (EDMPC) and DOPE using high sensitivity differential scanning calorimetry (HSDSC). MATERIALS AND METHODS:Large unilamellar liposomes of EDMPC with DOPE (mol ratio 0-50%) were prepared. Plasmid DNA was add...

journal_title：Pharmaceutical research

authors： Saunders M,Taylor KM,Craig DQ,Palin K,Robson H

更新日期：2007-10-01 00:00:00

abstract：:Interleukin-1 receptor antagonist (IL-1Ra) is a naturally occurring anti-inflammatory antagonist of interleukin-1 family of pro-inflammatory cytokines. The broad spectrum anti-inflammatory effects of IL-1Ra have been investigated against various auto-immune diseases such as diabetes mellitus, rheumatoid arthritis. Des...

journal_title：Pharmaceutical research

authors： Akash MS,Rehman K,Chen S

更新日期：2013-11-01 00:00:00

abstract：PURPOSE:The work aims at investigating the correlation of water sorption potential with different measures of molecular mobility in an annealed amorphous model compound (trehalose). METHODS:Amorphous trehalose, prepared by freeze-drying, was annealed at 100°C (17°C < T (g)) for up to 120 h. Global mo...

journal_title：Pharmaceutical research

authors： Bhardwaj SP,Suryanarayanan R

更新日期：2013-03-01 00:00:00

abstract：PURPOSE:Long-acting injectables (LAIs) are increasingly recognized as an effective therapeutic approach for treating chronic conditions. Many LAIs are formulated to create a poorly soluble depot from which the active agent is delivered over time. This long residing depot can cause localized chronic-active inflammation ...

journal_title：Pharmaceutical research

authors： Paquette SM,Dawit H,Hickey MB,Merisko-Liversidge E,Almarsson O,Deaver DR

更新日期：2014-08-01 00:00:00

abstract：PURPOSE:Heparin immobilized porous poly(D,L-lactic-co-glycolic acid) (PLGA) microspheres were prepared for sustained release of basic fibroblast growth factor (bFGF) to induce angiogenesis. MATERIALS AND METHODS:Porous PLGA microspheres having primary amine groups on the surface were prepared using an oil-in-water (O/...

journal_title：Pharmaceutical research

authors： Chung HJ,Kim HK,Yoon JJ,Park TG

更新日期：2006-08-01 00:00:00

abstract：PURPOSE:Performance of a transdermal delivery system (TDS) can be affected by exposure to elevated temperature, which can lead to unintended safety issues. This study investigated TDS and skin temperatures and their relationship in vivo, characterized the effective thermal resistance of skin, and identified the in vitr...

journal_title：Pharmaceutical research

authors： Zhang Q,Murawsky M,LaCount T,Hao J,Kasting GB,Newman B,Ghosh P,Raney SG,Li SK

更新日期：2017-07-01 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：PURPOSE:E-selectin is a cell adhesion molecule that is specifically expressed in the inflammatory vascular endothelium in response to cytokines such as IL-1 beta and TNF-alpha, and interacts with specific ligands containing sialyl Lewis X (Neu5Ac alpha 2-3Gal beta 1-4(Fuc alpha 1-3)GlcNAc-, SLex). In order to investiga...

journal_title：Pharmaceutical research

authors： Horie K,Sakagami M,Kuramochi K,Hanasaki K,Hamana H,Ito T

更新日期：1999-02-01 00:00:00

abstract：PURPOSE:Hydroxylation of the antidepressant and smoking deterrent drug bupropion is a clinically important bioactivation and elimination pathway. Bupropion hydroxylation is catalyzed selectively by cytochrome P4502B6 (CYP2B6). CYP2B6-catalyzed bupropion hydroxylation has been used as an in vitro and in vivo phenotypic ...

journal_title：Pharmaceutical research

authors： Coles R,Kharasch ED

更新日期：2008-06-01 00:00:00

abstract：PURPOSE:The gastric mucoadhesive property of tetracycline-sucralfate acidic complex (CO) was evaluated by using a novel method in vitro to compare with the in vivo test. The mucoadhesive mechanism of the acidic complex was also studied. METHODS:The gastric mucosa removed from a rat was placed covering the end of a plu...

journal_title：Pharmaceutical research

authors： Higo S,Ori K,Takeuchi H,Yamamoto H,Hino T,Kawashima Y

更新日期：2004-03-01 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：PURPOSE:Mannosylation of vaccines is a promising strategy to selectively target vaccine antigens to the mannose receptor expressed on dendritic cells (DCs). The purpose of this study was to investigate the effect of mannan (MN) chemically conjugated to poly(D, L-lactide-co-glycolic acid) (PLGA) nanoparticles (NPs) on a...

journal_title：Pharmaceutical research

authors： Hamdy S,Haddadi A,Shayeganpour A,Samuel J,Lavasanifar A

更新日期：2011-09-01 00:00:00

abstract：PURPOSE:The prognosis for glioma patients is poor, and development of new treatments is critical. Previously, we engineered polymer-based vaccines that control GM-CSF, CpG-oligonucleotide, and tumor-lysate presentation to regulate immune cell trafficking and activation, which promoted potent immune responses against pe...

journal_title：Pharmaceutical research

authors： Ali OA,Doherty E,Bell WJ,Fradet T,Hudak J,Laliberte MT,Mooney DJ,Emerich DF

更新日期：2011-05-01 00:00:00

abstract：PURPOSE:Using human lung cancer cells, we evaluated the involvement of plasminogen activator inhibitor-1 (PAI-1) in the anti-invasive action of cannabidiol, a non-psychoactive cannabinoid. METHODS:Invasion was quantified by a modified Boyden chamber assay. PAI-1 protein in cell culture media and PAI-1 mRNA were determ...

journal_title：Pharmaceutical research

authors： Ramer R,Rohde A,Merkord J,Rohde H,Hinz B

更新日期：2010-10-01 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: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:The aim of this study is to investigate the effects of 50% ethyl acetate extracts of grapefruit juice (GFJ) and orange juice (OJ) on the transport activity of P-glycoprotein (P-gp) in the rat small intestine. METHODS:The efflux of P-gp substrates from rat everted sac in the absence or presence of verapamil, GF...

journal_title：Pharmaceutical research

authors： Tian R,Koyabu N,Takanaga H,Matsuo H,Ohtani H,Sawada Y

更新日期：2002-06-01 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:A thermodynamic analysis of the binding to rat cortex adenosine A1 receptor of N6-substituted (full agonists) and N6-substituted-deoxyribose (partial agonists) adenosine derivatives was performed. The intrinsic activity of the compounds was evaluated by measurements of the inhibition of forskolin stimulated 3',...

journal_title：Pharmaceutical research

authors： Dalpiaz A,Scatturin A,Pavan B,Varani K,IJzerman AP,Andrea Borea P

更新日期：1999-07-01 00:00:00

abstract：PURPOSE:Reverse micellar solutions of diclofenac sodium were encapsulated in soft gelatine capsules. On contact with aqueous media they exhibited an application induced transformation (AIT) into a semisolid system of liquid crystals (SSLC) which slows down drug release. The aim of the present paper was to study in vitr...

journal_title：Pharmaceutical research

authors： Schneeweis A,Müller-Goymann CC

更新日期：1997-12-01 00:00:00

abstract：PURPOSE:The aim of the study is to determine whether a biodegradable elastomeric device that uses an osmotic pressure delivery mechanism can release different therapeutic proteins at a nearly constant rate in nanomolar concentrations with high bioactivity, given the same formulation conditions. Vascular endothelial gro...

journal_title：Pharmaceutical research

authors： Gu F,Neufeld R,Amsden B

更新日期：2006-04-01 00:00:00

abstract：:Four lipophilic, low molecular weight drugs solubilized in phosphatidylcholine-bile salt mixed micelles were injected s.c. into the hind legs of sheep and their cumulative recoveries in lymph draining from the site of application were determined. Surprisingly, the cumulative recoveries (percentage of dose) varied betw...

journal_title：Pharmaceutical research

authors： Supersaxo A,Hein WR,Steffen H

更新日期：1991-10-01 00:00:00