Correlation between chemical reactivity and the Hammett acidity function in amorphous solids using inversion of sucrose as a model reaction.

abstract：:Simultaneously Manufactured Nano-In-Micro (SIMANIM) particles for the pulmonary delivery of antibodies have been prepared by the spray-drying of a double-emulsion containing human IgG (as a model antibody), lactose, poly(lactide-co-glycolide) (PLGA) and dipalmitoylphosphatidylcholine (DPPC). The one-step drying proces...

journal_title：Journal of pharmaceutical sciences

authors： Kaye RS,Purewal TS,Alpar HO

更新日期：2009-11-01 00:00:00

abstract：:In vivo studies were conducted in rats to determine the role of hyperglycemia and hypoinsulinemia in the previously reported reduction in the hepatic accumulation and increase in the serum concentrations of 70-kDa fluorescein-dextran (FD-70) in diabetic (D) rats. The serum, urine, and hepatic concentrations of FD-70 w...

journal_title：Journal of pharmaceutical sciences

authors： Mehvar R,Reynolds J

更新日期：1994-07-01 00:00:00

abstract：:The in vitro antifungal activity of a novel series of cis- and trans-5-([aryl or aryloxy (or thio)]methyl)-3-(1H-imidazol-1-ylmethyl)-3- (2-thienyl)-2-methylisoxazolidines (13-24) was evaluated and compared with ketoconazole. The title series of compounds was prepared via a 1,3-dipolar cycloaddition reaction of 1-(2-t...

journal_title：Journal of pharmaceutical sciences

authors： Mullen GB,Mitchell JT,Allen SD,St Georgiev V

更新日期：1988-12-01 00:00:00

abstract：:As part of a study to examine cocaine disposition and interaction with ethanol, it was necessary to characterize various properties of cocaine in the blood of the experimental animal. All studies were conducted using blood from healthy adult male Sprague-Dawley rats. Cocaine was incubated in whole blood at 37 degrees ...

journal_title：Journal of pharmaceutical sciences

authors： Sukbuntherng J,Martin DK,Pak Y,Mayersohn M

更新日期：1996-06-01 00:00:00

abstract：:The physical state of a dosage form, crystalline versus amorphous, is critical in determining its solid-state physical and chemical properties. This minireview describes the physics associated with the preparation and storage of amorphous solids including a review of the common theories of the glass transition and rel...

journal_title：Journal of pharmaceutical sciences

authors： Hilden LR,Morris KR

更新日期：2004-01-01 00:00:00

abstract：:The use of second generation cationic liposomes to deliver cytotoxic drugs to solid tumors is a rational and promising therapeutic approach, given the natural affinity of cationic carrier molecules for the tumor microvasculature. Cationic liposomal therapeutics are effective in the treatment of cancers that are resist...

journal_title：Journal of pharmaceutical sciences

authors： Campbell RB,Ying B,Kuesters GM,Hemphill R

更新日期：2009-02-01 00:00:00

abstract：:Here, we report the structural characterization of several amorphous drugs made using the method of quenching molten droplets suspended in an acoustic levitator. (13) C NMR, X-ray, and neutron diffraction results are discussed for glassy cinnarizine, carbamazepine, miconazole nitrate, probucol, and clotrimazole. The (...

journal_title：Journal of pharmaceutical sciences

authors： Benmore CJ,Weber JK,Tailor AN,Cherry BR,Yarger JL,Mou Q,Weber W,Neuefeind J,Byrn SR

更新日期：2013-04-01 00:00:00

abstract：:Time and resource constraints necessitate increasingly early decision making to accelerate or stop preclinical drug discovery programs. Early discovery drug candidates may be potent inhibitors of new targets, but all too often exhibit poor pharmaceutical and pharmacokinetic properties that limit the in vivo exposure. ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,South SA,Foster KA,Daniels JS,Wene SP,Albin LA,Thompson DC

更新日期：2010-07-01 00:00:00

abstract：:First-order rate constants (k) were determined for the hydrolysis of ceftazidime in the pH range of 0.5 to 8.5 at 45, 55, and 65 degrees C by a stability-indicating HPLC assay. In the absence of buffer effects, the pH-rate expression was k = kH1f1(aH+) + kH2f2(aH+) + kH3f3(aH+) + kSf3 + kOHf3(aOH-), where KH and KOH a...

journal_title：Journal of pharmaceutical sciences

authors： Zhou M,Notari RE

更新日期：1995-05-01 00:00:00

abstract：:An extension of the Bischoff-Dedrick pharmacokinetic model is presented. This model is derived from basic considerations of drug distrubition with physiological and anatomical meaning. The Bischoff-Dedrick model can simultaneously predict drug distribution with time in blood, organs, and tissues of pharmacological int...

journal_title：Journal of pharmaceutical sciences

authors： Chen CN,Andrade JD

更新日期：1976-05-01 00:00:00

abstract：:In this paper we describe the synthesis and characterization of magnetic microcapsules, intended for use in vivo, and which contain polyethyleneimine nucleophilic targets capable of trapping electrophilic carcinogens. The microcapsules, 15-50 microns in diameter, consist of a semipermeable cross-linked nylon membrane ...

journal_title：Journal of pharmaceutical sciences

authors： Povey AC,Bartsch H,Nixon JR,O'Neill IK

更新日期：1986-09-01 00:00:00

abstract：:An in vitro technique was developed to characterize the intermittent flume patterns associated with the short bursts of metered-dose aerosols. Two orthogonal video images are utilized to describe the complex shape and direction of the flume pattern. This technique facilitates the evaluation of components manufactured ...

journal_title：Journal of pharmaceutical sciences

authors： Miszuk S,Gupta BM,Chen FC,Clawans C,Knapp JZ

更新日期：1980-06-01 00:00:00

abstract：:In this study, we investigated the potential roles of nanoparticles (<100 nm) and submicron (100-1000 nm) particles in the formation of microparticles (>1000 nm) in protein formulations under some pharmaceutically relevant stress conditions. Exposure of intravenous immunoglobulin solutions to the interface-associated ...

journal_title：Journal of pharmaceutical sciences

authors： Pardeshi NN,Zhou C,Randolph TW,Carpenter JF

更新日期：2018-07-01 00:00:00

abstract：:Controlling residual solvent levels is a major concern in pharmaceutical freeze-drying from co-solvent systems. This review provides an overview of the factors influencing this process and estimates their potential to reduce residual solvents in freeze-dried products. Decreased solvent contents are potentially correla...

journal_title：Journal of pharmaceutical sciences

authors： Kunz C,Gieseler H

更新日期：2018-08-01 00:00:00

abstract：:Carvedilol is a new beta-blocking agent with vasodilating activities, which is a racemic mixture of R(+)- and S(-)-enantiomers. Since the two enantiomers differ in pharmacological properties, it is necessary to individually measure their plasma concentrations in order to evaluate the pharmacological effects of racemic...

journal_title：Journal of pharmaceutical sciences

authors： Fujimaki M,Murakoshi Y,Hakusui H

更新日期：1990-07-01 00:00:00

abstract：:The purpose of the present study was to examine whether the intestinal absorption of low-permeability drugs could be improved by utilization of the intestinal influx transporter PEPT1. We investigated whether peptide derivatives of poorly absorbable nonamino acid-like drugs might be substrates of PEPT1, using rebamipi...

journal_title：Journal of pharmaceutical sciences

authors： Kikuchi A,Tomoyasu T,Tanaka M,Kanamitsu K,Sasabe H,Maeda T,Odomi M,Tamai I

更新日期：2009-05-01 00:00:00

abstract：:The purpose of this study was to elucidate the effect of heat treatment on the miscibility of multiple concentrated solutes that mimic biopharmaceutical formulations in frozen solutions. The first heating thermal analysis of frozen solutions containing either a low-molecular-weight saccharide (e.g., sucrose, trehalose...

journal_title：Journal of pharmaceutical sciences

authors： Izutsu K,Yomota C,Kawanishi T

更新日期：2011-12-01 00:00:00

abstract：:Spherical medicated microglobules were prepared by complex coacervation of Type A gelatin with pectin, having nominal diameters of 5, 10, and 25 micron and containing 37.3, 44.9, and 45.2% (w/w) sulfamerazine, respectively. They were recovered as water-insoluble powders and were spontaneously revertible to highly disp...

journal_title：Journal of pharmaceutical sciences

authors： McMullen JN,Newton DW,Becker CH

更新日期：1984-12-01 00:00:00

abstract：:Acute experiments were performed on overnight fasted chloralose-urethan anesthetized dogs, cats, rabbits, and rats. Under these conditions, somatostatin practically abolished gastric contractions and decreased GI tonus in all species examined. The canine duodenum, jejunum, and ileum exhibited only a contractile respon...

journal_title：Journal of pharmaceutical sciences

authors： Tansy MF,Martin JS,Landin WE,Kendall FM

更新日期：1979-09-01 00:00:00

abstract：:Recent studies have clearly demonstrated that Fourier transform IR spectroscopy can be a powerful tool for the study of protein stabilization during freeze-drying and for optimizing approaches to prevent lyophilization-induced protein aggregation. The purpose of the current review is to provide an overview of these to...

journal_title：Journal of pharmaceutical sciences

authors： Dong A,Prestrelski SJ,Allison SD,Carpenter JF

更新日期：1995-04-01 00:00:00

abstract：:Plasma binding of chlordiazepoxide, diazepam, loraxepam, and oxazepam was determined by equilibrium dialysis in 20 male, healthy volunteers, 25-86 years old. A wide range of binding was observed, with the free fraction varying twofold for lorazepam, fourfold for chlordiazepoxide and diazepam, and over 20-fold for oxa...

journal_title：Journal of pharmaceutical sciences

authors： Johnson RF,Schenker S,Roberts RK,Desmond PV,Wilkinson GR

更新日期：1979-10-01 00:00:00

abstract：:The purpose of this study was to examine the effects of extracts and flavone derivatives from the rhizome of Kaempferia parviflora on P-glycoprotein (P-gp)-mediated transport in LLC-GA5-COL150, a transfectant cell line of a porcine kidney epithelial cell line LLC-PK1 with human MDR1 cDNA. Ethanol extract obtained from...

journal_title：Journal of pharmaceutical sciences

authors： Patanasethanont D,Nagai J,Yumoto R,Murakami T,Sutthanut K,Sripanidkulchai BO,Yenjai C,Takano M

更新日期：2007-01-01 00:00:00

abstract：:Cyclosporin A (CyA) interacts with lipid membranes. Binding reaction and membrane location of CyA and analogs were examined with 2H-NMR, high-sensitivity isothermal titration calorimetry (ITC), and CD spectroscopy. Effects of CyA and charged analogs on the phosphocholine head group and on the membrane interior were in...

journal_title：Journal of pharmaceutical sciences

authors： Schote U,Ganz P,Fahr A,Seelig J

更新日期：2002-03-01 00:00:00

abstract：:The full parameterization for the stratum corneum biphasic microtransport model presented previously in this Journal [95:620-648 (2006)] is developed through a combination of fundamental transport theory and calibration with existing data. Of the five microscopic transport properties, four (D(cor), K(cor/w), D(lip), K...

journal_title：Journal of pharmaceutical sciences

authors： Wang TF,Kasting GB,Nitsche JM

更新日期：2007-11-01 00:00:00

abstract：:The extent of formation of solasodiene from solasodine upon treatment with hydrochloric acid under various conditions was determined. The diene formed was assayed by using the characteristic extinction at 236 nm. Diene formation was effected by the acid concentration and the boiling point of the solvent used. Optimal ...

journal_title：Journal of pharmaceutical sciences

authors： Segal R,Breuer A,Milo-Goldzweig I

更新日期：1978-08-01 00:00:00

abstract：:In this study the relationships between previously reported connectivity indices described by Kier and Hall and steric contributions to the rate constants for several series of reactions are examined. Rate data were examined for four different series of reactions, which were chosen to represent a range of different re...

journal_title：Journal of pharmaceutical sciences

authors： Schug JC,Viers JW,Seeman JI

更新日期：1984-10-01 00:00:00

abstract：:Plasma and various organ concentrations of canrenone, canrenoate, and total 3H-activity were measured following single doses of 20 mg of 3H-canrenoate/kg iv to rabbits. Organs studied included heart, lungs, brain, kidneys, liver, adrenal glands, and spleen. Canrenoate was shown to be in rapid equilibrium with canrenon...

journal_title：Journal of pharmaceutical sciences

authors： Finn AM,Brown R,Sadée W

更新日期：1977-02-01 00:00:00

abstract：:Mathematical models were determined relating preservative concentration and D values (decimal reduction times at 25 degrees C; pH 6.9-7.1) against Escherichia coli in aqueous medium. Preservatives investigated were 2-bromo-2-nitro-1,3-propanediol (Bronopol), N-(hydroxymethyl)-N-(1,3-dihydroxymethyl-2, 5-dioxo-4-imidaz...

journal_title：Journal of pharmaceutical sciences

authors： Hurwitz SJ,McCarthy TJ

更新日期：1985-08-01 00:00:00

abstract：:Capillary gas chromatography using an open tubular fused silica column and NP-FID was applied to the simultaneous analysis of the antihistamine, carbinoxamine, and the antitussive, hydrocodone, in human serum. Carbinoxamine and hydrocodone were extracted into methylene chloride-2-propanol (9:1) under alkaline conditio...

journal_title：Journal of pharmaceutical sciences

authors： Hoffman DJ,Leveque MJ,Thomson T

更新日期：1983-11-01 00:00:00

abstract：:The effect of dietary polyphenols on the intestinal glucuronidation and absorption of a model phenolic drug, alpha-naphthol (alpha-NA), was studied in isolated rat small intestine. (-)-Epicatechin significantly inhibited the glucuronidation of alpha-NA. Chrysin, (-)-epigallocatechin galleate (EGCG), and quercetin decr...

journal_title：Journal of pharmaceutical sciences

authors： Mizuma T,Awazu S

更新日期：2004-09-01 00:00:00