Relationship among physicochemical properties, skin permeability, and topical activity of the racemic compound and pure enantiomers of a new antifungal.

abstract：:Silk is a remarkable biopolymer with a long history of medical use. Silk fabrications have a robust track record for load-bearing applications, including surgical threads and meshes, which are clinically approved for use in humans. The progression of top-down and bottom-up engineering approaches using silk as the basi...

journal_title：Pharmaceutical research

authors： Tran SH,Wilson CG,Seib FP

更新日期：2018-11-05 00:00:00

abstract：:Various carboxylic acid esters of the N-hydroxymethyl derivative of N-benzyloxycarbonylglycine benzylamide, used as a peptide-like model, were prepared and their decomposition kinetics studied in aqueous solution and in human plasma solutions. These N-acyloxymethylamide derivatives were found to undergo a facile decom...

journal_title：Pharmaceutical research

authors： Bundgaard H,Rasmussen GJ

更新日期：1991-10-01 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: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：:The three-dimensional structures and molecular electrostatic potentials of the cis(Z) and trans(E)-isomers of flupenthixol and clopenthixol were examined by computer graphics and molecular mechanical and quantum mechanical calculations, and their internal molecular motions were studied by molecular dynamics simulation...

journal_title：Pharmaceutical research

authors： Sylte I,Dahl SG

更新日期：1991-04-01 00:00:00

abstract：PURPOSE:The purpose of this study was to investigate the pH-dependent passive and active transport of weakly basic drugs across the human intestinal epithelium. METHODS:The bidirectional pH-dependent transport of weak bases was studied in Caco-2 cell monolayers in the physiologic pH range of the gastrointestinal tract...

journal_title：Pharmaceutical research

authors： Neuhoff S,Ungell AL,Zamora I,Artursson P

更新日期：2003-08-01 00:00:00

abstract：PURPOSE:Herein we report the discovery of a group of derivatized alpha-amino acids that increase the oral bioavailability of sodium cromolyn. METHODS:We prepared three N-acylated alpha-amino acids and used these compounds to demonstrate the oral delivery of cromolyn in an in vivo rat model. In vitro experiments, inclu...

journal_title：Pharmaceutical research

authors： Leone-Bay A,Leipold H,Sarubbi D,Variano B,Rivera T,Baughman RA

更新日期：1996-02-01 00:00:00

abstract：PURPOSE:Generation of valuable information about the biphasic geometrical configuration of porcine stratum corneum from Very Small Angle Neutron Scattering (VSANS) data and investigation of its effect on the corresponding effective diffusivity. METHODS:Spectra of porcine stratum corneum are mathematically transformed ...

journal_title：Pharmaceutical research

authors： Charalambopoulou GC,Karamertzanis P,Kikkinides ES,Stubos AK,Kanellopoulos NK,Papaioannou AT

更新日期：2000-09-01 00:00:00

abstract：PURPOSE:Near-infrared reflectance spectroscopy (NIRS) was used to evaluate and quantify the effect of compression force on the NIR spectra of tablets. METHODS:Flat, white tablets with no orientation (scoring, etc.) were manufactured on a Stokes Rotary Tablet Press. NIRS was used to predict tablet hardness on the follo...

journal_title：Pharmaceutical research

authors： Morisseau KM,Rhodes CT

更新日期：1997-01-01 00:00:00

abstract：PURPOSE:To elucidate the catalytic mechanism of the esterase-like activity of serum albumin (SA), the reactivity of SA from six species was investigated using p-nitrophenyl esters as model substrates. METHODS:The effect of pH and the energetic and thermodynamic profiles of SA were determined for all species for p-nitr...

journal_title：Pharmaceutical research

authors： Sakurai Y,Ma SF,Watanabe H,Yamaotsu N,Hirono S,Kurono Y,Kragh-Hansen U,Otagiri M

更新日期：2004-02-01 00:00:00

abstract：:A new technique has been developed to calculate rapidly the solid-state room-temperature degradation rate of drugs and drug candidates. The technique utilizes measurements of the initial rate of heat output at several elevated temperatures by isothermal calorimetry and the degradation rate of the compound determined a...

journal_title：Pharmaceutical research

authors： Koenigbauer MJ,Brooks SH,Rullo G,Couch RA

更新日期：1992-07-01 00:00:00

abstract：PURPOSE:To show, using a model study, how electronic structure theory can be applied in combination with LC/UV/MS/MS for the prediction and identification of oxidative degradants. METHODS:The benzyloxazole 1, was used to represent an active pharmaceutical ingredient for oxidative forced degradation studies. Bond disso...

journal_title：Pharmaceutical research

authors： Reid DL,Calvitt CJ,Zell MT,Miller KG,Kingsmill CA

更新日期：2004-09-01 00:00:00

abstract：:A sensitive activity assay for high volume evaluation of human renin inhibitory peptides (RIPs) in rat sera (range 2-80 ng/ml) was developed based on the low affinity of RIPs to rat renin and their high affinity to human renin. The utility of this activity assay was tested by measuring concentrations of a human RIP, U...

journal_title：Pharmaceutical research

authors： Ruwart MJ,Sharma SK,Harris DW,Lakings DB,Rush BD,Wilkinson KF,Cornette JC,Evans DB,Friis JM,Cook KJ

更新日期：1990-04-01 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 develop a new intradermal antigen delivery system by coating microneedle arrays with lipid bilayer-coated, antigen-loaded mesoporous silica nanoparticles (LB-MSN-OVA). METHODS:Synthesis of MSNs with 10-nm pores was performed and the nanoparticles were loaded with the model antigen ovalbumin (OVA), and coate...

journal_title：Pharmaceutical research

authors： Tu J,Du G,Reza Nejadnik M,Mönkäre J,van der Maaden K,Bomans PHH,Sommerdijk NAJM,Slütter B,Jiskoot W,Bouwstra JA,Kros A

更新日期：2017-08-01 00:00:00

abstract：PURPOSE:To investigate influence of inflammation on metabolism and pharmacokinetics (PK) of midazolam (MDZ) and construct a semi-physiologically based pharmacokinetic (PBPK) model to predict PK in mice with inflammatory disease. METHODS:Glucose-6-phosphate isomerase (GPI)-mediated inflammation was used as a preclinica...

journal_title：Pharmaceutical research

authors： Varkhede N,Patel N,Chang W,Ruterbories K,Forrest ML

更新日期：2018-06-21 00:00:00

abstract：PURPOSE:Previous studies by other investigators have shown an enhancement of mitomycin C (MMC) activity at acidic extracellular pH (pHe) in monolayer cultures of human cells. The goal of the present study was to determine if the efficacy of intravesical MMC therapy in patients treated for superficial bladder cancer can...

journal_title：Pharmaceutical research

authors： Yen WC,Schmittgen T,Au JL

更新日期：1996-12-01 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: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: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 aim of the study is to investigate the effect of polymer blending on entrapment and release of ganciclovir (GCV) from poly(D,L-lactide-co-glycolide) (PLGA) microspheres using a set of empirical equations. METHODS:Two grades of PLGA, PLGA 7525 [D,L-lactide:glycolide(75:25), MW 90,000-126,000 Da] and Resomer...

journal_title：Pharmaceutical research

authors： Duvvuri S,Gaurav Janoria K,Mitra AK

更新日期：2006-01-01 00:00:00

abstract：PURPOSE:Delivery of therapeutics to neurons is paramount to treat neurological conditions, including many lysosomal storage disorders. However, key aspects of drug-carrier behavior in neurons are relatively unknown: the occurrence of non-canonical endocytic pathways (present in other cells); whether carriers that trave...

journal_title：Pharmaceutical research

authors： Hsu J,Hoenicka J,Muro S

更新日期：2015-04-01 00:00:00

abstract：:Many drugs and desirable phytochemicals are bitter, and bitter tastes are aversive. Food and pharmaceutical manufacturers share a common need for bitterness-masking strategies that allow them to deliver useful quantities of the active compounds in an acceptable form and in this review we compare and contrast the chall...

journal_title：Pharmaceutical research

authors： Coupland JN,Hayes JE

更新日期：2014-11-01 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：:A 1H-NMR spectroscopic method for the determination of the optical purity of threo-methylphenidate hydrochloride is presented. Complexation of the free-base form of the substrate with a chiral Eu(III) shift reagent resulted in two distinct enantiomeric ester methyl proton signals of utility for quantitative work. The ...

journal_title：Pharmaceutical research

authors： Hanna GM,Lau-Cam CA

更新日期：1990-07-01 00:00:00

abstract：:The effect of freezing on formation of soluble and insoluble aggregates of human growth hormone (hGH) was studied. The amount of soluble aggregates was affected very little by freezing regardless of the cooling rate. In contrast, the formation of insoluble aggregates (particulates), as determined by light scattering i...

journal_title：Pharmaceutical research

authors： Eckhardt BM,Oeswein JQ,Bewley TA

更新日期：1991-11-01 00:00:00

abstract：:Nanotechnology has continuously contributed to the fast development of diagnostic and therapeutic agents. Theranostic nanomedicine has encompassed the ongoing efforts on concurrent molecular imaging of biomarkers, delivery of therapeutic agents, and monitoring of therapy response. Among these formulations, polymer-bas...

journal_title：Pharmaceutical research

authors： Wang Z,Niu G,Chen X

更新日期：2014-06-01 00:00:00

abstract：:Nucleic acids are increasingly being considered for therapeutic uses, either to interfere with the function of specific nucleic acids or to bind specific proteins. Three types of nucleic acid drugs are discussed in this review: aptamers, compounds which bind specific proteins; triplex forming (antigene) compounds; whi...

journal_title：Pharmaceutical research

authors： Stull RA,Szoka FC Jr

更新日期：1995-04-01 00:00:00

abstract：PURPOSE:To investigate the influence of primary crystallization conditions on the mechanical properties and secondary processing behaviour of fluticasone propionate (FP) for carrier based dry powder inhaler (DPI) formulations. METHODS:Young's modulus of FP crystals produced using different anti-solvents was determined...

journal_title：Pharmaceutical research

authors： Kubavat HA,Shur J,Ruecroft G,Hipkiss D,Price R

更新日期：2012-04-01 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