A method to predict the percutaneous permeability of various compounds: shed snake skin as a model membrane.

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:The objective of this study was to develop and characterize long-circulating, biodegradable, and biocompatible nanoparticulate formulation as an intracellular delivery vehicle. METHODS:Poly(ethylene glycol) (PEG)-modified gelatin was synthesized by reacting Type-B gelatin with PEG-epoxide. The nanoparticles, p...

journal_title：Pharmaceutical research

authors： Kaul G,Amiji M

更新日期：2002-07-01 00:00:00

abstract：PURPOSE:Characterization of virosomes, in late stage preclinical development as vaccines for Respiratory Syncytial Virus (RSV), with a membrane-incorporated synthetic monophosphoryl lipid A, 3D-PHAD® adjuvant. METHODS:Virosomes were initially formed by contacting a lipid film containing 3D-PHAD® with viral membranes s...

journal_title：Pharmaceutical research

authors： Lederhofer J,van Lent J,Bhoelan F,Karneva Z,de Haan A,Wilschut JC,Stegmann T

更新日期：2018-07-03 00:00:00

abstract：PURPOSE:The purpose of this study was to characterize the amorphous state of ursodeoxycholic acid (UDCA) samples by using isothermal microcalorimetry, X-ray diffraction, infrared (IR) spectroscopy and solid state carbon 13 nuclear magnetic resonance (13C-NMR) spectroscopy, and to demonstrate the application of the ther...

journal_title：Pharmaceutical research

authors： Yonemochi E,Ueno Y,Ohmae T,Oguchi T,Nakajima S,Yamamoto K

更新日期：1997-06-01 00:00:00

abstract：PURPOSE:Labrasol and Gelucire 44/14 are defined admixtures of acylglycerols and PEG esters which are substrates for digestive lipases. METHODS:We investigated their in vitro gastrointestinal lipolysis to understand which compounds are, after digestion, responsible for keeping poorly water-soluble drugs in solution. Th...

journal_title：Pharmaceutical research

authors： Fernandez S,Chevrier S,Ritter N,Mahler B,Demarne F,Carrière F,Jannin V

更新日期：2009-08-01 00:00:00

abstract：PURPOSE:To investigate the effect of γ-irradiation of poly(lactic-co-glycolic acid) (PLGA)/Al(OH)₃/0 or 5 wt% diethyl phthalate (DEP) microspheres for active self-healing encapsulation of vaccine antigens. METHODS:Microspheres were irradiated with ⁶⁰Co at 2.5 and 1.8 MRad and 0.37 and 0.20 MRad/h. Encapsulation of tet...

journal_title：Pharmaceutical research

authors： Desai KG,Kadous S,Schwendeman SP

更新日期：2013-07-01 00:00:00

abstract：PURPOSE:To develop novel biomineral-binding liposomes (BBL) for the prevention of orthopedic implant associated osteomyelitis. METHODS:A biomineral-binding lipid, alendronate-tri(ethyleneglycol)-cholesterol conjugate (ALN-TEG-Chol), was synthesized through Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition (a versatile...

journal_title：Pharmaceutical research

authors： Liu XM,Zhang Y,Chen F,Khutsishvili I,Fehringer EV,Marky LA,Bayles KW,Wang D

更新日期：2012-11-01 00:00:00

abstract：PURPOSE:To measure aggregate and particle formation in tumor necrosis factor-alpha (TNF-α) inhibitors etanercept, adalimumab and certolizumab pegol product samples after exposure to freezing temperature conditions similar to storage conditions previously observed in patients' homes. METHODS:TNF-α inhibitors in their o...

journal_title：Pharmaceutical research

authors： Vlieland ND,Nejadnik MR,Gardarsdottir H,Romeijn S,Sediq AS,Bouvy ML,Egberts ACG,van den Bemt BJF,Jiskoot W

更新日期：2018-02-05 00:00:00

abstract：PURPOSE:The purpose of this study is to show how disaccharides differ in their ability to protect lyophilized β-galactosidase from enzymatic activity loss and secondary structure changes during storage. METHODS:β-galactosidase was lyophilized with trehalose, sucrose, cellobiose or melibiose at 2:1, 20:1 and 40:1 excip...

journal_title：Pharmaceutical research

authors： Heljo VP,Jouppila K,Hatanpää T,Juppo AM

更新日期：2011-03-01 00:00:00

abstract：:The pharmacokinetics of methylergometrine were investigated in the rat, with emphasis on the role of biliary excretion and enterohepatic recirculation in the overall disposition of the drug. A linked-rat model, where the bile from a rat receiving a constant rate of iv infusion of methylergometrine was allowed to flow ...

journal_title：Pharmaceutical research

authors： Bredberg U,Paalzow L

更新日期：1990-01-01 00:00:00

abstract：PURPOSE:This work explores the distribution of water and its effects on molecular mobilities in poly(vinylpyrrolidone) (PVP) glasses using molecular dynamics (MD) simulation technology. METHODS:PVP glasses containing 0.5% and 10% w/w water and a small amount of ammonia and Phe-Asn-Gly were generated. Physical aging pr...

journal_title：Pharmaceutical research

authors： Xiang TX,Anderson BD

更新日期：2005-08-01 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：:The topical antifungal Sch-39304 is a racemic compound comprised of two enantiomers, Sch-42427 and Sch-42426, only one of which (Sch-42427) is pharmacologically active. The pure enantiomers have a lower melting point and, therefore, a higher solubility than the racemic compound. Because of these differences in physico...

journal_title：Pharmaceutical research

authors： Wearley L,Antonacci B,Cacciapuoti A,Assenza S,Chaudry I,Eckhart C,Levine N,Loebenberg D,Norris C,Parmegiani R

更新日期：1993-01-01 00:00:00

abstract：PURPOSE:Penetration enhancers (PEs) enhancing efficacy depends on two processes: PEs release from patches and action on skin. Compared with their action on skin, PEs release process was poorly understood. Therefore, the purpose of this study was to make a mechanistic understanding of PEs release from acrylic pressure-s...

journal_title：Pharmaceutical research

authors： Zeng L,Song W,He W,Zhang J,Wang Y,Bian J,Mao Z,Quan D,Liu J

更新日期：2020-08-13 00:00:00

abstract：:An empirical mass-transfer model for enteric-coating dissolution that uses in vivo dissolution data to characterize the pH-dependent solubility properties of the polymer film and a mass-transfer coefficient determined from in vivo dissolution or disintegration studies is developed. Once the in vivo mass-transfer coeff...

journal_title：Pharmaceutical research

authors： Ebel JP,Jay M,Beihn RM

更新日期：1993-02-01 00:00:00

abstract：PURPOSE:To explore whether miR-19 is involved in the regulation of multidrug resistance (MDR), one of the main causes of breast cancer mortality, and modulates sensitivity of tumor cells to chemotherapeutic agents. METHODS:We analyzed miRNA expression levels in three MDR cell lines in comparison with their parent cell...

journal_title：Pharmaceutical research

authors： Liang Z,Li Y,Huang K,Wagar N,Shim H

更新日期：2011-12-01 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：:The crystal growth kinetics of theophylline monohydrate from aqueous buffered supersaturated solutions were investigated at 10, 20, 30, and 40 degrees C. Crystallization experiments were carried out isothermally at pH 6. During growth the crystal count and size distributions were monitored in situ. The growth rate was...

journal_title：Pharmaceutical research

authors： Rodríguez-Hornedo N,Wu HJ

更新日期：1991-05-01 00:00:00

abstract：PURPOSE:TXA9, a novel cardiac glycoside, has a potent anti-proliferative effect against A549 human lung cancer cells, however, possesses a poor water-solubility and a rapid metabolic rate in vivo which limited the further development of TXA9. To overcome the shortcomings of TXA9, four polymer prodrugs of TXA9 were desi...

journal_title：Pharmaceutical research

authors： Li Y,Ye C,Cai C,Zhao M,Han N,Liu Z,Zhai J,Yin J

更新日期：2020-03-12 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：PURPOSE:The objective of the present work was to prepare safe and effective Ciclosporin A Lipid nanocapsule (CsA-LNC) eye-drops for the treatment of DED. METHODS:The phase-inversion method was used to prepared different sizes CsA-LNC. CsA biodistribution in ocular after topical administration in rabbits was analyzed b...

journal_title：Pharmaceutical research

authors： Zhang A,Sun R,Ran M,Deng Y,Ge Y,Zhu Y,Tao X,Shang L,Gou J,He H,Yin T,Wang Y,Zhang Y,Tang X

更新日期：2020-07-14 00:00:00

abstract：PURPOSE:To design, synthesize, and test synthetic glycopeptide-based delivery systems for gene targeting to hepatocytes by systemic administration. METHODS:All peptides were synthesized by the solid phase method developed using Fmoc chemistry on a peptide synthesizer. The binding of galactosylated peptides to HepG2 ce...

journal_title：Pharmaceutical research

authors： Anwer K,Logan M,Tagliaferri F,Wadhwa M,Monera O,Tung CH,Chen W,Leonard P,French M,Proctor B,Wilson E,Singhal A,Rolland A

更新日期：2000-04-01 00:00:00

abstract：PURPOSE:We investigated optimum formulation characteristics in the nasal absorption of salmon calcitonin (sCT) by incorporation of acylcarnitines. METHODS:Nasal sCT formulations were administered to anesthetized rats. Plasma calcium level was measured and pharmacological bioavailability (P.bioav) was calculated. RESU...

journal_title：Pharmaceutical research

authors： Kagatani S,Shinoda T,Fukui M,Ohmura T,Hasumi S,Sonobe T

更新日期：1996-05-01 00:00:00

abstract：:The electrochemical properties of human cadaver skin were studied in a diffusion cell with impedance spectroscopy as a function of time in the absence and presence of penetration enhancers dodecyl N,N-dimethylamino acetate and Azone. An improved electrochemical model of skin is presented, and combining the novel model...

journal_title：Pharmaceutical research

authors： Kontturi K,Murtomäki L,Hirvonen J,Paronen P,Urtti A

更新日期：1993-03-01 00:00:00

abstract：PURPOSE:HSP90 (Heat shock protein 90kD) has been validated as a therapeutic target in Castrate Resistant Prostate Cancer. Unfortunately, HSP90 inhibitors suffer from dose-limiting toxicities that hinder their clinical applications. Previously developed polymeric delivery systems for HSP90 inhibitors had either low drug...

journal_title：Pharmaceutical research

authors： Suárez Del Pino JA,Kolhatkar R

更新日期：2017-12-01 00:00:00

abstract：:Alpha- and beta-cyclodextrins and their hydroxypropyl derivatives were converted by the reaction with chlorosulfonic acid in pyridine to the corresponding sulfates. Cyclodextrin sulfates were shown by fast-atom bombardment mass spectrometry (negative ion mode, triethanolamine matrix) to be mixtures with nearly symmetr...

journal_title：Pharmaceutical research

authors： Pitha J,Mallis LM,Lamb DJ,Irie T,Uekama K

更新日期：1991-09-01 00:00:00

abstract：:Lecithin-stabilized triglyceride emulsions are subject to hydrolysis by pancreatic lipase. The time profiles of these reactions are characterized by a lag-phase and a zero-order phase. Lag phases are more pronounced with long-chain triglycerides. Ca2+ is effective in reducing the lag-phase and activating lipase. Kinet...

journal_title：Pharmaceutical research

authors： Alvarez FJ,Stella VJ

更新日期：1989-06-01 00:00:00

abstract：PURPOSE:To study Cereport (RMP-7, bradykinin B2 agonist) effects on human brain microvascular endothelial cell (HBMEC) monolayer permeability. METHODS:HBMEC grown on transwell membranes were exposed to Cereport. The monolayer permeability was determined with [14C]-inulin (MW. 5,200) and [3H]-dextran (MW. 70,000). RES...

journal_title：Pharmaceutical research

authors： Mackic JB,Stins M,Jovanovic S,Kim KS,Bartus RT,Zlokovic BV

更新日期：1999-09-01 00:00:00

abstract：:HPLC analyses of GM-CSF in solution mixtures containing both GM-CSF and HSA showed losses of GM-CSF which could not be accounted for using conventional electrophoretic and/or RP-HPLC techniques. Further investigation of these mixtures by immunoblotting and by immunoaffinity chromatography demonstrated the presence of ...

journal_title：Pharmaceutical research

authors： Kumarasamy R,Bausch J,Kopcha D,Patel S,McGonigle E

更新日期：1994-03-01 00:00:00

abstract：PURPOSE:Melanoma is an aggressive neoplasm with a propensity for metastases and resistance to therapy. Previously, we showed that (-)-epigallocatechin-3-gallate (EGCG), the major polyphenolic antioxidant present in green tea, resulted in a significant decrease in the viability and growth of melanoma and induction of ap...

journal_title：Pharmaceutical research

authors： Nihal M,Roelke CT,Wood GS

更新日期：2010-06-01 00:00:00