Prodrug approaches to enhancement of physicochemical properties of drugs IX: acetaminophen prodrug.

abstract：:The tissue penetration and distribution of antibiotics is of great importance, since most of the infections occur in the tissue. At the infection site, the free, unbound fraction of the antibiotic is responsible for the antiinfective effect. These free extracellular concentrations can be measured by microdialysis. It ...

journal_title：Journal of pharmaceutical sciences

authors： Nolting A,Costa TD,Vistelle R,Rand KH,Derendorf H

更新日期：1996-04-01 00:00:00

abstract：:The aim of this study is to evaluate the effect of peptide cyclization on the blood-brain barrier (BBB) modulatory activity and plasma stability of His-Ala-Val peptides, which are derived from the extracellular 1 domain of human E-cadherin. The activities to modulate the intercellular junctions by linear HAV4 (Ac-SHAV...

journal_title：Journal of pharmaceutical sciences

authors： Alaofi A,On N,Kiptoo P,Williams TD,Miller DW,Siahaan TJ

更新日期：2016-02-01 00:00:00

abstract：:Gelrite, a heteropolysaccharide that forms a gel in the presence of cations, was tested in humans for its efficacy as an ophthalmic vehicle by a nonivasive fluorometric technique. Fluorescein was used as the tracer, and its concentration in the anterior chamber was used as the principal measure of bioavailability. The...

journal_title：Journal of pharmaceutical sciences

authors： Maurice DM,Srinivas SP

更新日期：1992-07-01 00:00:00

abstract：:To evaluate oral mucosal absorption of drugs in dogs, a newly designed in situ perfusion system with a circulating perfusion chamber was developed. The utility of the perfusion system was investigated by using three drugs: salicylic acid (SA), sulfadimethoxine (SM), and diltiazem (DIL). The oral mucosal absorption of ...

journal_title：Journal of pharmaceutical sciences

authors： Yamahara H,Suzuki T,Mizobe M,Noda K,Samejima M

更新日期：1990-11-01 00:00:00

abstract：:A single method for the quantitative determinations of three active ingredients, phenylephrine hydrochloride, phenylpropanolamine hydrochloride, and brompheniramine maleate, and one inactive ingredient (sodium benzoate) in a commercial product for colds is reported. The method is based on paired ion high-pressure liqu...

journal_title：Journal of pharmaceutical sciences

authors： Ghanekar AG,Das Gupta V

更新日期：1978-06-01 00:00:00

abstract：:In this study, powder surface imaging was utilized in evaluation of particle size-related segregation behavior of granules during vibration and tableting processes. Altogether, eight granule batches were manufactured using a fluidized bed granulator. The particle size distribution of each batch was measured with sieve...

journal_title：Journal of pharmaceutical sciences

authors： Lakio S,Hatara J,Tervakangas H,Sandler N

更新日期：2012-06-01 00:00:00

abstract：:The blood-brain barrier permeation has been investigated by using a topological substructural molecular design approach (TOPS-MODE). A linear regression model was developed to predict the in vivo blood-brain partitioning coefficient on a data set of 119 compounds, treated as the logarithm of the blood-brain concentrat...

journal_title：Journal of pharmaceutical sciences

authors： Cabrera MA,Bermejo M,Pérez M,Ramos R

更新日期：2004-07-01 00:00:00

abstract：:A revised classification system for oral drugs was developed using the biopharmaceutics classification system (BCS) as a starting point. The revised system is designed to have a greater focus on drug developability. Intestinal solubility, the compensatory nature of solubility and permeability in the small intestine an...

journal_title：Journal of pharmaceutical sciences

authors： Butler JM,Dressman JB

更新日期：2010-12-01 00:00:00

abstract：:Stable protein nanostructured particles, produced by spray freezing into liquid (SFL) nitrogen, were encapsulated uniformly into microspheres to reduce the burst release over the first 24 h. The denaturation and aggregation of these bovine serum albumin (BSA) high-surface area particles were minimal due to ultra-rapid...

journal_title：Journal of pharmaceutical sciences

authors： Leach WT,Simpson DT,Val TN,Anuta EC,Yu Z,Williams RO 3rd,Johnston KP

更新日期：2005-01-01 00:00:00

abstract：:The association efficiency of oxytetracycline (OTC) to pharmaceutical available, ionic oil-in-water nanoemulsions is studied. Theoretical mathematical developments allowed us to differentiate by diafiltration (DF) between thermodynamically and kinetically controlled binding of the drug to the nanoemulsions, and relate...

journal_title：Journal of pharmaceutical sciences

authors： Orellana SL,Torres-Gallegos C,Araya-Hermosilla R,Oyarzun-Ampuero F,Moreno-Villoslada I

更新日期：2015-03-01 00:00:00

abstract：:The aim of this study was to develop a pharmacokinetic (PK)/pharmacodynamic (PD) model of a bicyclolide, modithromycin, to explain its concentration-dependent bactericidal activity based on the drug-bacterium interaction model that we developed. We have already reported the applicability of model to the time-dependent...

journal_title：Journal of pharmaceutical sciences

authors： Katsube T,Wajima T,Yamano Y,Yano Y

更新日期：2014-04-01 00:00:00

abstract：:The direct photoisomerization of (E)-4-(1-imidazoylmethyl)-cinnamic acid (IMC), a thromboxane synthetase inhibitor, to its (Z)-isomer at pH 2.0 was decelerated by beta-cyclodextrin (beta-CyD) and heptakis(2,6-di-O-methyl)-beta-cyclodextrin (DM-beta-CyD). The photostationary composition [(Z)-isomer:IMC ratio] was shift...

journal_title：Journal of pharmaceutical sciences

authors： Hirayama F,Utsuki T,Uekama K,Yamasaki M,Harata K

更新日期：1992-08-01 00:00:00

abstract：:Phenytoin-loaded alkyd nanoemulsions were prepared spontaneously using the phase inversion method from a mixture of novel biosourced alkyds and Tween 80 surfactant. Exposure of human adult keratinocytes (HaCaT cells) for 48 h to alkyd nanoemulsions producing phenytoin concentrations of 3.125-200 μg/mL resulted in rela...

journal_title：Journal of pharmaceutical sciences

authors： Teo SY,Yew MY,Lee SY,Rathbone MJ,Gan SN,Coombes AGA

更新日期：2017-01-01 00:00:00

abstract：:Sustained release of ferrous sulfate (FeSO4) from gum arabica pellets has been achieved for 7 h. Release is further sustained for 12 to 600 h by coating the pellets with polyvinyl acetate and ethylene vinyl acetate, respectively. An increase in the amount of gum arabica in the pellets decreases the rate of release due...

journal_title：Journal of pharmaceutical sciences

authors： Batra V,Bhowmick A,Behera BK,Ray AR

更新日期：1994-05-01 00:00:00

abstract：:The transdermal delivery of 2 fluorescent probes with similar molecular weight but different lipophilicity, into and through the skin from 2 commercially available transdermal bases, pluronic lecithin organogel, and Lipoderm® has been evaluated. First, in vitro penetration of fluorescein sodium and fluorescein (free a...

journal_title：Journal of pharmaceutical sciences

authors： Zhang Q,Song Y,Page SW,Garg S

更新日期：2018-02-01 00:00:00

abstract：:Dextran sulfate samples from different sources were examined by 1H and 13C NMR spectroscopy to differentiate the samples on the basis of extent and sites of sulfation. The anomeric (H-1) signal proved to be a good indicator ranging from no sulfation (as in dextran) to virtually complete sulfation at positions 2 and 3,...

journal_title：Journal of pharmaceutical sciences

authors： Neville GA,Rochon P,Rej RN,Perlin AS

更新日期：1991-03-01 00:00:00

abstract：:New dihydropyridine in equilibrium pyridinium salt-type redox carrier systems were developed in which the drug is linked via the ring nitrogen atom of nicotinamide. The rate of oxidation of the dihydropyridine forms, and thus the overall and brain-specific distribution of the corresponding 3-carbamoyl-1-carbamoylalkyl...

journal_title：Journal of pharmaceutical sciences

authors： Bodor N,AbdelAlim AM

更新日期：1985-03-01 00:00:00

abstract：:The plasma nitroglycerin levels obtained after intracardial (0.7 mg/kg), oral (7 mg/kg), and topical (7--14 mg/kg) doses of nitroglycerin in rats are reported. Nitroglycerin followed essentially one-compartment kinetics after intracardial administration, showing a mean half-life of about 4 min and a mean apparent volu...

journal_title：Journal of pharmaceutical sciences

authors： Yap PS,Fung HL

更新日期：1978-04-01 00:00:00

abstract：:A Bayesian approach was developed to determine an amikacin dosage regimen to achieve the desired plasma concentrations for each patient. Statistical characteristics of pharmacokinetic parameters were first evaluated in a group of patients (reference population), which when combined with three individual plasma concent...

journal_title：Journal of pharmaceutical sciences

authors： Garraffo R,Iliadis A,Cano JP,Dellamonica P,Lapalus P

更新日期：1989-09-01 00:00:00

abstract：:A hydraulic calcium phosphate cement made of beta-tricalcium phosphate [beta-Ca3(PO4)2], monocalcium phosphate monohydrate [Ca(H2PO4)2-H2O], and water was used as a delivery system for the antibiotic gentamicin sulfate (GS). GS, added as powder or as aqueous solution, was very beneficial to the physicochemical propert...

journal_title：Journal of pharmaceutical sciences

authors： Bohner M,Lemaître J,Van Landuyt P,Zambelli PY,Merkle HP,Gander B

更新日期：1997-05-01 00:00:00

abstract：:The total synthesis of d-pilocarpine specifically labeled as N-14CH3 is reported. dl-Homopilopic acid was prepared as a key intermediate and resolved into the d-enantiomer via the alpha-methylbenzylamine salt. The penultimate intermediate, 2-mercaptopilocarpine, was desulfurized by oxidation with dilute hydrogen perox...

journal_title：Journal of pharmaceutical sciences

authors： DeGraw JI,Engstrom JS,Willis E

更新日期：1975-10-01 00:00:00

abstract：:Complexation of ferrous cytochrome P450 by metabolic intermediates formed during NADPH-catalyzed metabolism of compounds structurally related to orphenadrine was studied. This so-called metabolic intermediate complexation was determined in rat liver microsomes, obtained from phenobarbital-pretreated rats, at 455 nm us...

journal_title：Journal of pharmaceutical sciences

authors： Bast A,Savenije-Chapel EM,Noordhoek J

更新日期：1984-07-01 00:00:00

abstract：:P,P-Bis(1-aziridinyl)-N-1-adamantylphosphinic amide displayed oncolytic activity against intracerebral and intraperitoneal L-1210 leukemia. Administration of the isotope-labeled compound to rats shows 32P distribution to the brain. ...

journal_title：Journal of pharmaceutical sciences

authors： Cates LA,Cramer MB

更新日期：1976-03-01 00:00:00

abstract：:Bile acid (BA) retention within hepatocytes is an underlying mechanism of cholestatic drug-induced liver injury (DILI). We previously developed an assay using sandwich-cultured human hepatocytes (SCHHs) to evaluate drug-induced hepatocyte toxicity accompanying intracellular BA accumulation. However, due to shortcoming...

journal_title：Journal of pharmaceutical sciences

authors： Susukida T,Sekine S,Nozaki M,Tokizono M,Oizumi K,Horie T,Ito K

更新日期：2016-04-01 00:00:00

abstract：:The interaction of L-tryptophan with alpha-cyclodextrin was investigated in a 0.1 M phosphate buffer at pH 7.4 with a LKB 2277 microcalorimeter, using flow mixed mode at 25 degrees C. The thermodynamic parameters for inclusion complex formation obtained are as follows; DeltaG(0) = - 7.03 kJ/mol (K = 17.0), DeltaH(0) =...

journal_title：Journal of pharmaceutical sciences

authors： Nishijo J,Tsuchitani M

更新日期：2001-02-01 00:00:00

abstract：:The plasma protein binding of zomepirac, a new nonnarcotic analgesic, was studied using equilibrium dialysis. Experiments were performed using human plasma and plasma from mice, rats, and rhesus monkeys, all species of pharmacological or toxicological interest. At concentrations approximating those achieved in vivo, t...

journal_title：Journal of pharmaceutical sciences

authors： O'Neill PJ

更新日期：1981-07-01 00:00:00

abstract：:The quassinoids bruceantin, brucein D, brucein E, bruceoside A, and brusatol significantly inhibited P-388 lymphocytic leukemic cell RNA and protein synthesis in tissue culture. However, DNA synthesis inhibition seemed to correlate more directly with the anti-neoplastic activity of these compounds in the in vivo P-338...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Lee KH,Eigebaly SA,Imakura Y,Sumida Y,Wu RY

更新日期：1979-07-01 00:00:00

abstract：:Water evaporation rates were measured from thin samples of a model layered structure of stratum corneum lipids with 32% water. A model with only free fatty acids present gave the lowest evaporation rates, while a model with only oleic acid gave values approximately 50% higher. Using the total lipid spectrum of stratum...

journal_title：Journal of pharmaceutical sciences

authors： Friberg SE,Kayali I

更新日期：1989-08-01 00:00:00

abstract：:After having been used in treating HIV infection for a decade, zidovudine (AZT) continues to be an essential component of antiretroviral regimens. Because antiviral responses and toxicity of AZT seem to be related to cells in specific target tissues, being able to understand and predict the distribution of AZT into di...

journal_title：Journal of pharmaceutical sciences

authors： Chow HH

更新日期：1997-11-01 00:00:00

abstract：:The aim of the study was to determine and compare the degree of swelling and the swelling kinetics of poly(ethylene oxide) (PEO) hydrophilic matrix tablets without any additives for matrixes with different molecular weight polydispersities. A wide range of "mixed" polydisperse PEO tablets were obtained by mixing two P...

journal_title：Journal of pharmaceutical sciences

authors： Körner A,Larsson A,Andersson A,Piculell L

更新日期：2010-03-01 00:00:00