Attaching zanamivir to a polymer markedly enhances its activity against drug-resistant strains of influenza a virus.

abstract：:The plasma concentrations and urinary excretions of bisoprolol enantiomers in four Japanese male healthy volunteers after a single oral administration of 20 mg of racemic bisoprolol were evaluated. The AUC(infinity) and elimination half-life of (S)-(-)-bisoprolol were slightly larger than those of (R)-(+)-bisoprolol i...

journal_title：Journal of pharmaceutical sciences

authors： Horikiri Y,Suzuki T,Mizobe M

更新日期：1998-03-01 00:00:00

abstract：:The neuroprotective blood-brain barrier (BBB) keeps many drug candidates below therapeutic levels in the central nervous system. Glutathione PEGylated liposomal doxorubicin (2B3-101) has been developed to safely enhance the delivery of doxorubicin to brain tumors. However, doxorubicin concentration in extracellular br...

journal_title：Journal of pharmaceutical sciences

authors： Birngruber T,Raml R,Gladdines W,Gatschelhofer C,Gander E,Ghosh A,Kroath T,Gaillard PJ,Pieber TR,Sinner F

更新日期：2014-07-01 00:00:00

abstract：:A novel approach using a self-setting hydroxyapatite (HAP) cement as a skeletal drug-delivery system has been proposed to solve the problem of delivering drugs to skeletal tissue at sufficiently high local concentrations for desirable therapeutic effects. HAP cements loaded with antibiotics can be formed in situ and c...

journal_title：Journal of pharmaceutical sciences

authors： Yu D,Wong J,Matsuda Y,Fox JL,Higuchi WI,Otsuka M

更新日期：1992-06-01 00:00:00

abstract：:The synthesis, hydrolysis rate, and bioavailability of 1-(p-acetaminophenoxy)-1-ethoxyethane, an acetaminophen prodrug, are described. The prodrug is less soluble than acetaminophen and stable at neutral pH. However, in an acidic environment, the compound cleaves rapidly, generating acetaminophen. When both the prodru...

journal_title：Journal of pharmaceutical sciences

authors： Hussain A,Kulkarni P,Perrier D

更新日期：1978-04-01 00:00:00

abstract：:An isothermal chromatographic (GC) method employing an SE-30 column and flame-ionization detection has been developed for the simultaneous assay of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations. The method, which uses a silica column chromatographic cleanu...

journal_title：Journal of pharmaceutical sciences

authors： Schieffer GW,Palermo PJ,Pollard-Walker S

更新日期：1984-01-01 00:00:00

abstract：:The entropy of fusion of 84 disubstituted benzenes was essentially constant and independent of the participation of the compounds in intramolecular or intermolecular hydrogen bonding. It was also independent of the shapes, sizes, and dipole moments of the rigid molecules studied. While the entropy of fusion was indepe...

journal_title：Journal of pharmaceutical sciences

authors： Martin E,Yalkowsky SH,Wells JE

更新日期：1979-05-01 00:00:00

abstract：:Two types of drug release mechanisms-matrix controlled (Q - t1/2 relationship) and partition controlled (Q - t relationship)-were reported previously. The dependency of the transition between these two processes on the solution solubility of drug is now analyzed. Mathematical expressions are derived to treat the syste...

journal_title：Journal of pharmaceutical sciences

authors： Chien YW,Lambert HJ,Lin TK

更新日期：1975-10-01 00:00:00

abstract：:A method of depicting dimensional illustrations of molecules in vacuo that are sensitive to small electronic perturbations was attempted. This method would be useful in determining the effects of either perturbing groups from other molecules or changes produced by the addition or modification of an existing atom or ch...

journal_title：Journal of pharmaceutical sciences

authors： Breon TL,Petersen H Jr,Paruta AN

更新日期：1978-01-01 00:00:00

abstract：:The purpose of this study was to evaluate the therapeutic efficacy of a new calcium phosphate (CaP)-based formulation in improving the bone mineral deficiency in ovariectomized (OVX) rats. The ions release experiments for CaP preparations (G2: 0.46% Mg, 5.78% Zn, and 2.5% F; G3:3.1% Mg, 0.03% Zn, and 3.01% F; G4: 1.25...

journal_title：Journal of pharmaceutical sciences

authors： Otsuka M,Oshinbe A,Legeros RZ,Tokudome Y,Ito A,Otsuka K,Higuchi WI

更新日期：2008-01-01 00:00:00

abstract：:A heparin derivative sufficiently lipophilic to be bound to plastics, forming blood-compatible supports, or to be used as an anticoagulant by transdermal or oral routes would be of great pharmaceutical interest. For such applications, the functional groups within heparin's antithrombin III binding site, responsible fo...

journal_title：Journal of pharmaceutical sciences

authors： Liu J,Pervin A,Gallo CM,Desai UR,Van Gorp CL,Linhardt RJ

更新日期：1994-07-01 00:00:00

abstract：:Application of low-frequency ultrasound has been shown to enhance transdermal transport of drugs (low-frequency sonophoresis). In this paper, we show that the efficacy of low-frequency ultrasound in enhancing transdermal transport can be further increased by its combination with sodium lauryl sulfate (SLS), a well-kno...

journal_title：Journal of pharmaceutical sciences

authors： Mitragotri S,Ray D,Farrell J,Tang H,Yu B,Kost J,Blankschtein D,Langer R

更新日期：2000-07-01 00:00:00

abstract：:Peptidomimetic drugs have favorable bioavailability owing to H(+)/peptide transporter 1 (PEPT1) located in the intestine. Sartans are commonly used and likely coadministered with peptidomimetic drugs in the clinic; however, in vivo interactions between sartans and peptidomimetic drugs have not been systemically unders...

journal_title：Journal of pharmaceutical sciences

authors： Huo X,Liu Q,Wang C,Meng Q,Sun H,Peng J,Ma X,Sun P,Liu K

更新日期：2014-02-01 00:00:00

abstract：:The micellar properties of Poloxamer 213 (1), a Pluronic copolymer shown to affect lipid absorption and serum cholesterol level in experimental animals, are investigated by surface tension measurements, photon correlation spectroscopy (PCS), Reichardt's dye solubilization technique, differential scanning calorimetry (...

journal_title：Journal of pharmaceutical sciences

authors： Cheng HY,Holl WW

更新日期：1990-10-01 00:00:00

abstract：:Understanding the effect of surfactant properties is critical when designing vesicular delivery systems. This review evaluates previous studies to explain the influence of surfactant properties on the behavior of lipid vesicular systems, specifically their size, charge, stability, entrapment efficiency, pharmacokineti...

journal_title：Journal of pharmaceutical sciences

authors： Bnyan R,Khan I,Ehtezazi T,Saleem I,Gordon S,O'Neill F,Roberts M

更新日期：2018-05-01 00:00:00

abstract：:Polymethyl [1-14C]methacrylate nanoparticles were administered orally to bile cannulated rats. Ten to fifteen percent of the administered radioactivity was absorbed and found in the bile and urine. Within 48 h, 94-97% of the absorbed radioactivity had been eliminated from the body. After 8 d, the highest residual radi...

journal_title：Journal of pharmaceutical sciences

authors： Nefzger M,Kreuter J,Voges R,Liehl E,Czok R

更新日期：1984-09-01 00:00:00

abstract：:2,2'-Anhydro-1-beta-D-arabinofuranosylcytosine (I) is a more potent and less toxic antineoplastic agent than is cytarabine (1-beta-D-arabinofuranosylcytosine) (II). The anhydronucleoside (I) was found to be readily transformed by hydrogen peroxide into 2,2'-anhydro-5-hydroxy-1-beta-D-arabinofuranosylcytosine (III) by ...

journal_title：Journal of pharmaceutical sciences

authors： Kikugawa K

更新日期：1975-03-01 00:00:00

abstract：:We characterized a glucose-sensitive, controlled-release insulin delivery system. Insulin release rates increased when glucose was perfused in the release media surrounding the matrix. The system was composed of solid, particulate insulin, incorporated into an ethylene-vinyl acetate copolymer (EVAc) matrix. Feedback c...

journal_title：Journal of pharmaceutical sciences

authors： Brown LR,Edelman ER,Fischel-Ghodsian F,Langer R

更新日期：1996-12-01 00:00:00

abstract：:Twenty-two neutral, lipid-soluble 99mTc complexes have been synthesized from diamine dithiol (DADT) ligands which vary in alkyl substitution pattern on nitrogen and carbon. The logarithm of the partition coefficients (log PC), as well as the capacity factor k', of the purified complexes increased linearly with molecul...

journal_title：Journal of pharmaceutical sciences

authors： Lever SZ,Sun SY,Scheffel UA,Kaltovich FA,Baidoo KE,Goldfarb H,Wagner HN Jr

更新日期：1994-06-01 00:00:00

abstract：:3,6-Diformyl- and 3,6-dipropanoylmorphine and 6-formyl- and 6-propanoylmorphine were prepared to obtain longer acting, heroin-like compounds. The 6-acylated compounds were more potent than heroin subcutaneously and were orally effective, and their duration of action was at least two to three times greater than that of...

journal_title：Journal of pharmaceutical sciences

authors： May EL,Jacobson AE

更新日期：1977-02-01 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

abstract：:The expression of carboxylesterase (CES) and the transdermal movement of an ester prodrug were studied in rat skin. Ethyl-fexofenadine (ethyl-FXD) was used as a model lipophilic prodrug that is slowly hydrolyzed to its parent drug, FXD (MW 502). Among the CES1 and CES2 isozymes, Hydrolase A is predominant in rat skin ...

journal_title：Journal of pharmaceutical sciences

authors： Imai T,Ariyoshi S,Ohura K,Sawada T,Nakada Y

更新日期：2016-02-01 00:00:00

abstract：:The physicochemical properties of ricobendazole (RBZ) were characterized using conventional methods. Solubility in some pharmaceutical solvents, pH-solubility, ionization properties, and lipophilicity are described. The solubility of RBZ in water is 62 mug/mL and very poor in common pharmaceutical solvents, for exampl...

journal_title：Journal of pharmaceutical sciences

authors： Wu Z,Razzak M,Tucker IG,Medlicott NJ

更新日期：2005-05-01 00:00:00

abstract：:A high-performance liquid chromatographic method with spectrofluorometric detection has been developed for the analysis of a new substituted benzamide and its metabolite in body fluids. The detection was performed at 270 nm for excitation, and 370 nm for emission. The proposed technique is selective, reliable, and sen...

journal_title：Journal of pharmaceutical sciences

authors： Bressolle F,Bres J,Moulin A

更新日期：1990-06-01 00:00:00

abstract：:The metabolic disposition of 14C-labeled carprofen [(+/-)-6-chloro-alpha-methylcarbazole-2-acetic acid] was investigated in rats, dogs, and humans. Carprofen is eliminated predominantly by biotransformation in these three species. In dogs and rats, the direct conjugation of carprofen to form an ester glucuronide and o...

journal_title：Journal of pharmaceutical sciences

authors： Rubio F,Seawall S,Pocelinko R,DeBarbieri B,Benz W,Berger L,Morgan L,Pao J,Williams TH,Koechlin B

更新日期：1980-11-01 00:00:00

abstract：:A method is described for screening compounds that inhibit crystallization in solution to enable more accurate measurement of amorphous drug solubility. Three polymers [polyvinylpyrrolidone, hydroxypropyl methylcellulose, and hydroxypropyl methylcellulose acetate succinate (HPMCAS)] were screened for their ability to ...

journal_title：Journal of pharmaceutical sciences

authors： Murdande SB,Pikal MJ,Shanker RM,Bogner RH

更新日期：2011-10-01 00:00:00

abstract：:Respirable crystals of cromoglycic acid (CA) were prepared by precipitation of CA with hydrochloric acid from aqueous solutions of cromolyn sodium and subsequent recrystallization from hot water or mixtures of dimethyl sulphoxide and water. The properties of the materials were established by melting point measurements...

journal_title：Journal of pharmaceutical sciences

authors： Chan HK,Gonda I

更新日期：1989-02-01 00:00:00

abstract：:A GLC method is presented for the quantitative determination of menthol, phenol, benzocaine, and pyrilamine maleate. The propellent was exhausted from a pressurized can, and an aliquot of the alcoholic base was weighed. After the addition of the internal standard diluted with chloroform, 1 microliter of the mixture wa...

journal_title：Journal of pharmaceutical sciences

authors： De Fabrizio F

更新日期：1981-10-01 00:00:00

abstract：:Hydrazine levels in formulations of hydralazine, isoniazid, and phenelzine have been measured over a 2-year period under ambient conditions and under temperature and humidity stress. Hydralazine tablets are stable under ambient conditions, but the hydrazine level in an injectable formulation increased from 4.5 to 10 m...

journal_title：Journal of pharmaceutical sciences

authors： Lovering EG,Matsui F,Curran NM,Robertson DL,Sears RW

更新日期：1983-08-01 00:00:00

abstract：:We report a programed drug delivery system that can tailor the release of anesthetic bupivacaine in a spatiotemporally controlled manner. The drug delivery system was developed through the combination of a collagen-based injectable hydrogel and 2 types of poly(lactic-co-glycolic acid) (PLGA) particles. As a rapid-rele...

journal_title：Journal of pharmaceutical sciences

authors： Dinh VV,Suh YS,Yang HK,Lim YT

更新日期：2016-12-01 00:00:00

abstract：:Historically, recovery had been used to evaluate the data quality of plasma protein binding or tissue binding obtained from equilibrium dialysis assays. Low recovery was often indicative of high nonspecific binding, instability, or low solubility. This study showed that, when equilibrium was fully established in the d...

journal_title：Journal of pharmaceutical sciences

authors： Di L,Umland JP,Trapa PE,Maurer TS

更新日期：2012-03-01 00:00:00