Synthesis of tetracycline ring A analogs.

abstract：:Two polymorphs of the 1:1 fumarate salt of 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester, developed for the treatment of cognitive symptoms of schizophrenia and Alzheimer disease, have been characterized. The 2 crystal structures have been solved, and their phase relationships have been establish...

journal_title：Journal of pharmaceutical sciences

authors： Robert B,Perrin MA,Barrio M,Tamarit JL,Coquerel G,Ceolin R,Rietveld IB

更新日期：2016-01-01 00:00:00

abstract：:Digoxin binding to normal and kwashiorkor serum was studied and found to be inferior in the latter. Digoxin should be used with care in hypoalbuminemic patients. ...

journal_title：Journal of pharmaceutical sciences

authors： Buchanan N,Van der Walt LA,Strickwold B

更新日期：1976-06-01 00:00:00

abstract：:Virtually all biological variables, including those affected by drugs, are subject to adaptive self regulation. In the description of the pharmacodynamics (PD) of drugs, it may be necessary to consider the endogenous control system (ECS) as an integral part of the PD. A PDECS model based on system analysis principles ...

journal_title：Journal of pharmaceutical sciences

authors： Veng-Pedersen P,Modi NB

更新日期：1993-03-01 00:00:00

abstract：:This work was to investigate the effects of particle size and paddle speed on the particle diffusional layer thickness h(app) in a USP dissolution apparatus II. After the determination of the powder dissolution rates of five size fractions of fenofibrate, including <20, 20-32, 32-45, 63-75, and 90-106 microm, the pres...

journal_title：Journal of pharmaceutical sciences

authors： Sheng JJ,Sirois PJ,Dressman JB,Amidon GL

更新日期：2008-11-01 00:00:00

abstract：:Mechanical shock may cause cavitation in vials containing liquid formulations of therapeutic proteins and generate protein aggregates and other particulates. To test whether common formulation components such as protein molecules, air bubbles, or polysorbate 20 (PS20) micelles might nucleate cavitation, a high-speed v...

journal_title：Journal of pharmaceutical sciences

authors： Wu H,Chisholm CF,Puryear M,Movafaghi S,Smith SD,Pokhilchuk Y,Lengsfeld CS,Randolph TW

更新日期：2020-03-01 00:00:00

abstract：:This study describes the synthesis of a new generation of immunotoxins made by a noncovalent interaction between a monoclonal antibody derivatized with a dichlorotriazinic dye and the ribosomal inhibitor protein gelonin. The scheme of preparation has several advantages with respect to the traditional methods, which us...

journal_title：Journal of pharmaceutical sciences

authors： Dosio F,Brusa P,Delprino L,Grosa G,Ceruti M,Cattel L

更新日期：1994-02-01 00:00:00

abstract：:Various concentrations of salicylic acid in hydrophilic ointment were applied repeatedly at daily or weekly intervals to rats in vivo. Salicylic acid absorption through treated skin was monitored by determining the penetration fluxes of salicylic acid through skin excised at various times. A gradual decrease in the sa...

journal_title：Journal of pharmaceutical sciences

authors： Roberts MS,Harlock E

更新日期：1978-12-01 00:00:00

abstract：:Anthralin and its decomposition products were separated by both column chromatographic and TLC techniques. Two decomposition products were characterized by TLC, melting-point data, and UV and IR spectroscopy. Pure anthralin and its decomposition products also were determined quantitatively. ...

journal_title：Journal of pharmaceutical sciences

authors： Elsabbagh HM,Whitworth CW,Schramm LC

更新日期：1979-03-01 00:00:00

abstract：:The chemical shifts of the methyl groups of 2,4-dimethylbenzo[g]quinoline are defined with respect to concentration, showing that the methyl resonances are reversed from their expected positions in concentrations normally used in NMR spectroscopy. The phenomenon is explained in terms of the probably "fixation" of bond...

journal_title：Journal of pharmaceutical sciences

authors： Born JL,Harsin CE

更新日期：1977-08-01 00:00:00

abstract：:The oral absorption of drugs has been represented by various concepts such as the absorption potential, the maximum absorbable dose, the biopharmaceutics classification system, and in vitro-in vivo correlation. The aim of this article is to provide an overview of the theoretical relationships between these concepts. I...

journal_title：Journal of pharmaceutical sciences

authors： Sugano K,Terada K

更新日期：2015-09-01 00:00:00

abstract：:Solid dispersion (SD) of indomethacin with crospovidone (CrosPVP) shows useful characteristics for preparation of dosage forms. This study aimed to determine the types of drugs that could adopt a stable amorphous form in SD. Twenty compounds with various melting points (70-218 degrees C), molecular weights (135-504) a...

journal_title：Journal of pharmaceutical sciences

authors： Shibata Y,Fujii M,Kokudai M,Noda S,Okada H,Kondoh M,Watanabe Y

更新日期：2007-06-01 00:00:00

abstract：:In this paper the development of a new preparation method of liposomes containing a water soluble marker (fluorescein isothiocyanate-dextran (FITC-dextran) or zinc phthalocyanine tetrasulfonic acid (TSZnPc) using supercritical carbon dioxide (called "the supercritical liposome method") is described. The apparatus used...

journal_title：Journal of pharmaceutical sciences

authors： Frederiksen L,Anton K,van Hoogevest P,Keller HR,Leuenberger H

更新日期：1997-08-01 00:00:00

abstract：:The present study pursued to profile the intestinal solubility of nine HIV protease inhibitors (PIs) in fasted- and fed-state human intestinal fluids (FaHIF, FeHIF) aspirated from four volunteers. In addition, the ability of fasted- and fed-state simulated intestinal fluids (FaSSIF, FeSSIF) to predict the intestinal s...

journal_title：Journal of pharmaceutical sciences

authors： Wuyts B,Brouwers J,Mols R,Tack J,Annaert P,Augustijns P

更新日期：2013-10-01 00:00:00

abstract：:Amorphous dispersions provide an excellent way of increasing dissolution rates of poorly soluble drugs, but there may be concerns about stability. One way of assessing the stability of amorphous is the study of relaxation. In this study the relaxation at the surface of amorphous solid dispersions (SDs) was evaluated u...

journal_title：Journal of pharmaceutical sciences

authors： Hasegawa S,Ke P,Buckton G

更新日期：2009-06-01 00:00:00

abstract：:Resveratrol trimethyl ether (trans-3,5,4'-trimethoxystilbene, RTE) is a naturally occurring and pharmacologically active resveratrol derivative. To evaluate its suitability as a drug candidate, a pharmacokinetic study was carried out in Sprague-Dawley rats with the emphasis to identify the impact of aqueous solubility...

journal_title：Journal of pharmaceutical sciences

authors： Lin HS,Ho PC

更新日期：2011-10-01 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 new extraction-spectrophotometric method for the determination of hydralazine, based on its reaction with 2-hydroxy-1-naphthaldehyde at 25 degrees C, is described. The calibration curve was linear between 0.4 and 6 mg/mL of hydralazine. The molar absorbtivity of the product at 408 nm is 40,900 L.mol-1.cm-1. The meth...

journal_title：Journal of pharmaceutical sciences

authors： Mari-Buigues J,Mañes-Vinuesa J,Garcia-Domenech R,Pous-Miralles G

更新日期：1991-07-01 00:00:00

abstract：:Evidence is provided for the existence of a second discrete chemical form of meropenem at clinically relevant concentrations prepared from the marketed formulation of the drug. Proton and carbon-13 NMR spectra in D2O, coupled with tandem mass spectroscopy (MS/MS) and cross polarization/magic angle spinning (CP-MAS) NM...

journal_title：Journal of pharmaceutical sciences

authors： Almarsson O,Kaufman MJ,Stong JD,Wu Y,Mayr SM,Petrich MA,Williams JM

更新日期：1998-05-01 00:00:00

abstract：:Many pathophysiological circumstances vary during 24 h periods. Many physiologic processes undergo biological rhythms, including the sleep-wake rhythm and metabolism. Disruptive effect in the 24 h variations can manifest as the emergence or exacerbation of pathological conditions. So, chronotherapeutics is gaining inc...

journal_title：Journal of pharmaceutical sciences

authors： Ohdo S,Koyanagi S,Matsunaga N,Hamdan A

更新日期：2011-09-01 00:00:00

abstract：:A confocal Raman microscopic technique was optimized to more efficiently detect amorphous-amorphous phase separation in freeze-dried protein formulations. A Renishaw Raman inVia confocal microscope was used to collect 100-200 μm line maps (2 μm step size) of freeze-dried protein-excipient formulations. At each point a...

journal_title：Journal of pharmaceutical sciences

authors： Forney-Stevens KM,Pelletier MJ,Shalaev EY,Pikal MJ,Bogner RH

更新日期：2014-09-01 00:00:00

abstract：:This in vitro study evaluated the extent of the absorption and metabolism of propranolol in human skin from four sources. Between 10.4 +/- 3.1 and 36.6 +/- 2.6% of the applied dose was absorbed; however, only a small portion (between 4.1 +/- 0.9 and 16.1 +/- 1.3%) of the dose permeated through the skin. Naphthoxyaceti...

journal_title：Journal of pharmaceutical sciences

authors： Ademola JI,Chow CA,Wester RC,Maibach HI

更新日期：1993-08-01 00:00:00

abstract：:The objective of the present study was to investigate the iontophoretic transport behavior across multiple membranes of different barrier properties. Spectra/Por(R) (SP) and Ionac membranes were the synthetic membranes and sclera was the biomembrane in this model study. The barrier properties of SP membranes were dete...

journal_title：Journal of pharmaceutical sciences

authors： Molokhia SA,Zhang Y,Higuchi WI,Li SK

更新日期：2008-01-01 00:00:00

abstract：:The nanosizing of poorly soluble drugs as a formulation strategy can eventually enhance their dissolution rate and bioavailability. Standard comminution techniques such as high-pressure homogenization (HPH) or wet bead milling have limitations in reaching the desired mean particle size. Combinative methods have been d...

journal_title：Journal of pharmaceutical sciences

authors： Salazar J,Müller RH,Möschwitzer JP

更新日期：2013-05-01 00:00:00

abstract：:An F(ab')2 fragment of an IgG has been spray-dried on a bench-top machine to examine the presence of insoluble particulates in the redissolved powder product. Preliminary experiments showed that treatment of the F(ab')2 in aqueous solution in a water bath at 65°C for 1 h produced fragmentation and also insoluble parti...

journal_title：Journal of pharmaceutical sciences

authors： Lassner P,Adler M,Lee G

更新日期：2014-04-01 00:00:00

abstract：:Pancreatic islet transplantation is a promising advanced therapy that has been used to treat patients suffering from diabetes type 1. Traditionally, pancreatic islets are infused via the portal vein, which is subsequently intended to engraft in the liver. Severe immunosuppressive treatments are necessary, however, to ...

journal_title：Journal of pharmaceutical sciences

authors： Scheiner KC,Coulter F,Maas-Bakker RF,Ghersi G,Nguyen TT,Steendam R,Duffy GP,Hennink WE,O'Cearbhaill ED,Kok RJ

更新日期：2020-01-01 00:00:00

abstract：:This paper traces the academic genealogy of Professor Takeru Higuchi, who is considered "The Father of Physical Pharmacy" because of his contributions to the science of drug formulation and delivery and his impact in mentoring a whole generation of post-World War II pharmaceutical scientists. As one who was mentored b...

journal_title：Journal of pharmaceutical sciences

authors： Stella VJ

更新日期：2001-08-01 00:00:00

abstract：:Curcumin has been investigated as a potential photosensitizer (PS) in antimicrobial photodynamic therapy (aPDT). The phototoxic effect of curcumin is dependent on proper formulations of the compound because of the lipophilic nature of the molecule and the extremely low water solubility at physiological conditions. In ...

journal_title：Journal of pharmaceutical sciences

authors： Hegge AB,Nielsen TT,Larsen KL,Bruzell E,Tønnesen HH

更新日期：2012-04-01 00:00:00

abstract：:Absorption rates of monobasic beta-lactam antibiotics were measured as a function of lumen solution pH between 4 and 9 by utilizing the rat intestinal recirculating method in situ. Between pH 6.5 and 9, the absorption rate constants of ionized antibiotics were almost identical; but, at pH 4, the unionized species were...

journal_title：Journal of pharmaceutical sciences

authors： Tsuji A,Miyamoto E,Kubo O,Yamana T

更新日期：1979-07-01 00:00:00

abstract：:In the transition of the pharmaceutical industry from batchwise to continuous drug product manufacturing, the drying process has proven challenging to control and understand. In a semicontinuous fluid bed dryer, part of the ConsiGma™ wet granulation line, the aforementioned production methods converge. Previous resear...

journal_title：Journal of pharmaceutical sciences

authors： Ghijs M,Schäfer E,Kumar A,Cappuyns P,Van Assche I,De Leersnyder F,Vanhoorne V,De Beer T,Nopens I

更新日期：2019-06-01 00:00:00

abstract：:Interest in the 5-, 6-, and 7-trifluoromethyl-substituted 2,3-bis(4-methoxyphenyl)indoles as potent, orally active anti-inflammatory agents required a method for their determination in serum, urine, and feces to permit studies of their absorption, metabolism, and excretion. A simple, rapid, sensitive, and specific pro...

journal_title：Journal of pharmaceutical sciences

authors： Kaiser DG,Liggett WF,Forist AA

更新日期：1976-12-01 00:00:00