Synthesis, stability, and pharmacological evaluation of nipecotic acid prodrugs.

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：:The effects of physical aging and antiplasticization on the water transport properties of glassy cellulose acetate film-coated tablets were investigated. The gradual approach toward thermodynamic equilibrium during physical aging decrease the free volume of the polymers. This decrease in free volume is accompanied by ...

journal_title：Journal of pharmaceutical sciences

authors： Guo JH

更新日期：1994-03-01 00:00:00

abstract：:The purpose of this investigation was to determine the effect of body temperature on the pharmacodynamics (convulsant activity) of pentylenetetrazol (PTZ). Rats received an iv infusion of PTZ until the onset of maximal seizures, at which time samples of cerebrospinal fluid (CSF), brain, and blood (for serum) were obta...

journal_title：Journal of pharmaceutical sciences

authors： Walker JS,Levy G

更新日期：1991-10-01 00:00:00

abstract：:The poor aqueous solubility of carbamazepine was dramatically increased via complexation with various chemically modified beta-cyclodextrins and gamma-cyclodextrins. A preparation of carbamazepine and 2-hydroxypropyl-beta-cyclodextrin was found to be stable to steam sterilization and to storage under a variety of cond...

journal_title：Journal of pharmaceutical sciences

authors： Brewster ME,Anderson WR,Estes KS,Bodor N

更新日期：1991-04-01 00:00:00

abstract：:The aminoxyl (nitroxyl) labeled (2-chloroethyl)nitrosocarbamoyl (CNC) derivatives of amino acids, i.e., N-[[N'-(2-chloroethyl)-N'-nitrosoamino]carbonyl]-A-(1-oxy-2,2,6,6- tetramethylpiperidin-4-yl)amides, A = glycyl (10a), A = L-alanyl (10b), A = L-valyl (10c), A = L-phenylalanyl (10d), were synthesized and evaluated ...

journal_title：Journal of pharmaceutical sciences

authors： Sosnovsky G,Baysal M,Erciyas E

更新日期：1994-07-01 00:00:00

abstract：:Tritium-labeled progesterone was administered to mature female rats in the proestrous stage by three different routes, gastric intubation, subcutaneous injection, and uterine intraluminal instillation, to study the kinetics involved in the uptake and retention of radioactivity by the uterus and various other tissues. ...

journal_title：Journal of pharmaceutical sciences

authors： Fang SM,Lin CS,Lyon V

更新日期：1977-12-01 00:00:00

abstract：:Both developing (Days --1-+12 relative to inoculation) and established (Days +18-+29) stages of Mycobacterium butyricum adjuvant-induced polyarthritis in rats were treated orally with cryogenine (100 mg/kg/day), a prototype anti-inflammatory (phenylbutazone, 100 mg/kg/day), or a prototype immunosuppressive (cyclophosp...

journal_title：Journal of pharmaceutical sciences

authors： Watson WC,Malone MH

更新日期：1977-09-01 00:00:00

abstract：:Reactive high gravity controlled precipitation (HGCP) was carried out to produce salbutamol sulphate (SS) particles suitable for inhalation. Aqueous solutions of free salbutamol base and sulphuric acid were mixed intensely inside a HGCP reactor to form the particles. Spray drying was employed to obtain dry powders. Ph...

journal_title：Journal of pharmaceutical sciences

authors： Hu T,Chiou H,Chan HK,Chen JF,Yun J

更新日期：2008-02-01 00:00:00

abstract：:A novel method for creating water soluble prodrugs of cisplatin analogues bearing chelating diamines is introduced. When 2-(amino-methyl)aniline is reacted with K2PtCl4 between a pH of 6 and 7, the neutral chelated complex [2-(aminomethyl)aniline)dichloroplatinum(II) (1) is isolated. On the other hand, when the comple...

journal_title：Journal of pharmaceutical sciences

authors： Köckerbauer R,Bednarski PJ

更新日期：1995-07-01 00:00:00

abstract：:The pharmaceutical preparation, chromatography, and biological distribution of a series of new chemical analogs of palmitic acid and diethylenetriaminepentaacetic acid, ethylenediaminetetraacetic acid, or diethylenetriamine are described. The biological distribution in rabbits 30 min after intravenous administration o...

journal_title：Journal of pharmaceutical sciences

authors： Karesh SM,Eckelman WC,Reba RC

更新日期：1977-02-01 00:00:00

abstract：:Thirty-four vasodilators were screened in several in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to beta 1-,beta 2-, and alpha-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation. Isoproterenol and perhexiline only exhibi...

journal_title：Journal of pharmaceutical sciences

authors： Greenslade FC,Scott CK,Newquist KL,Krider KM,Chasin M

更新日期：1982-01-01 00:00:00

abstract：:A GLC method for the determination of procainamide in biological fluids is presented. By using a dipropyl analog of procainamide as an internal standard, both compounds can be chromatographed directly, yielding linear calibration curves and a sensitivity that allows quantitative determination of concentrations as low ...

journal_title：Journal of pharmaceutical sciences

authors： Simons KJ,Levy RH

更新日期：1975-12-01 00:00:00

abstract：:Multidrug resistance (MDR) mediated by the overexpression of the drug efflux protein P-glycoprotein is one of the major obstacles to successful cancer chemotherapy. The development of safe and effective MDR-reversing agents is an important approach to addressing this problem clinically. In this study, we evaluated the...

journal_title：Journal of pharmaceutical sciences

authors： Liu R,Zhang Y,Chen Y,Qi J,Ren S,Xushi MY,Yang C,Zhu H,Xiong D

更新日期：2010-07-01 00:00:00

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：:Arginine-glycine-aspartate (RGD) has been shown to be essential for the recognition of integrins overexpressed in tumor cells, especially during tumor invasion, angiogenesis, and metasis. In this study, a novel tetrapeptide, RGD-valine (RGDV), was designed and attached to the N position of 1-β-D-arabinofuranosylcytosi...

journal_title：Journal of pharmaceutical sciences

authors： Wang F,Cui C,Ren Z,Wang L,Liu H,Cui G

更新日期：2012-12-01 00:00:00

abstract：:The objective of this study was to determine reasons behind the low oral (p.o.) bioavailability of glucosamine. By using male Sprague-Dawley rats, the movement of glucosamine through everted gut, the effect of dose and glucose, and inhibition of a glucose transporter (GLUT2) by quercetin were studied. Glucosamine phar...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim A,Gilzad-kohan MH,Aghazadeh-Habashi A,Jamali F

更新日期：2012-07-01 00:00:00

abstract：:Colonic drug delivery is intended for local or systemic therapies. The lack of predictive in vitro or animal model leads to considerable time delays in colonic product development. The objective of this scintigraphic study was to provide "proof of concept" for a novel capsule-type colonic delivery system (Colon-Target...

journal_title：Journal of pharmaceutical sciences

authors： Ishibashi T,Pitcairn GR,Yoshino H,Mizobe M,Wilding IR

更新日期：1998-05-01 00:00:00

abstract：:The disposition of radioactivity following oral administration of 14C-norgestimate was compared to that following administration of the drug in combination with 3H-ethinyl estradiol in humans. Seven normal, healthy female subjects were each administered one capsule orally containing 14C-norgestimate either alone (74.4...

journal_title：Journal of pharmaceutical sciences

authors： Weintraub HS,Abrams LS,Patrick JE,McGuire JL

更新日期：1978-10-01 00:00:00

abstract：:In this paper, we demonstrate that by employing a combination of sedimentation field-flow fractionation (sedFFF) and other characterization techniques, such as photon correlation spectroscopy (PCS) and freeze-fracture electron microscopy (EM), it is possible to show that commercial fat emulsions of similar overall che...

journal_title：Journal of pharmaceutical sciences

authors： Li J,Caldwell KD

更新日期：1994-11-01 00:00:00

abstract：:Gold nanoparticles through nucleation of Au clusters have been extensively studied. However, due to low potency, prolonged tissue retention, and irreversible accumulation, the safety considerations have limited their therapeutic and diagnostic applications. Novel gold nanostructures with retained physical properties a...

journal_title：Journal of pharmaceutical sciences

authors： Gao Y,Mu Q,Zhu L,Li Z,Ho RJY

更新日期：2020-05-01 00:00:00

abstract：:Although displacement from plasma protein binding (dPB) is usually of little clinical significance, it should be taken into account when interpreting changes in total plasma concentrations of drugs subject to metabolically based drug-drug interactions (mDDI). The aim of this study was to develop an approach to predict...

journal_title：Journal of pharmaceutical sciences

authors： Christensen H,Baker M,Tucker GT,Rostami-Hodjegan A

更新日期：2006-12-01 00:00:00

abstract：:Injectable microcapsules containing 75% (w/w) cyclazocine, a narcotic antagonist, were prepared with dl-poly(lactic acid) as the coating material. Capsule fractions falling between 105 and 295 mum released about 90% of their cyclazocine in 8 days of rotating-bottle extraction at 37 degrees in pH 7.4 phosphate buffer. ...

journal_title：Journal of pharmaceutical sciences

authors： Mason N,Thies C,Cicero TJ

更新日期：1976-06-01 00:00:00

abstract：:A high-pressure liquid chromatographic procedure for quantitative dexamethasone and dexamethasone sodium phosphate determinations in all types of commercially available pharmaceutical dosage forms was developed. The method also separates dexamethasone from its phosphate salt and separates dexamethasone or its salt fro...

journal_title：Journal of pharmaceutical sciences

authors： Gupta VD

更新日期：1979-07-01 00:00:00

abstract：:At low protein concentrations (c2), non-native protein aggregation rates are known to be sensitive to changes in conformational stability and "weak" or "colloidal" protein-protein interactions. Protein-protein interactions are also known to be strong functions of c2. In the present work, protein-protein interactions a...

journal_title：Journal of pharmaceutical sciences

authors： Ghosh R,Calero-Rubio C,Saluja A,Roberts CJ

更新日期：2016-03-01 00:00:00

abstract：:A series of unrelated steroids were tested for antimineralocorticoid activity by Kagawa's test in male rats and by modified test in female rats. Adrenalectomized male rats given 12 mcg desoxycorticosterone (DOC) and 2.5 ml normal saline received 1 mg of the test steroid, and their urine was analyzed for sodium and po...

journal_title：Journal of pharmaceutical sciences

authors： Solymoss B,Krajny M,Varga S

更新日期：1970-05-01 00:00:00

abstract：:The objective was to examine the influence of Pluronic block-copolymers on the interaction between the drug efflux transporter, P-glycoprotein and HIV-1 protease inhibitors (PIs). The ATPase assay determined the effect of various Pluronics on PI-stimulated P-gp ATPase activity. Cellular accumulation studies were condu...

journal_title：Journal of pharmaceutical sciences

authors： Shaik N,Pan G,Elmquist WF

更新日期：2008-12-01 00:00:00

abstract：:Upon exposure to shaking stress, an IgG1 mAb formulation in both the liquid and lyophilized state formed subvisible particles. Because freeze-drying was expected to minimize protein physical instability under these conditions, the extent and nature of aggregate formation in the lyophilized preparation were examined us...

journal_title：Journal of pharmaceutical sciences

authors： Telikepalli S,Kumru OS,Kim JH,Joshi SB,O'Berry KB,Blake-Haskins AW,Perkins MD,Middaugh CR,Volkin DB

更新日期：2015-02-01 00:00:00

abstract：:Male fertility has reportedly been regulated by the long-term, continuous administration of testosterone. To deliver the testosterone at a controlled rate for a month or longer, a bandage-type, testosterone-releasing, disk-shaped device was developed. In vitro drug elution studies demonstrated that a constant release ...

journal_title：Journal of pharmaceutical sciences

authors： Chien YW

更新日期：1984-08-01 00:00:00

abstract：:Four solvates of erythromycin have been crystallographically characterized. The solvates of THF and dioxane are very similar but differ in notable ways. The isopropanol solvate exhibits uncommon modes of hydrogen bonding, which have previously been seen only in the erythomycin B hydrate. The methanol solvate is striki...

journal_title：Journal of pharmaceutical sciences

authors： Henry R,Zhang GG

更新日期：2007-05-01 00:00:00

abstract：:Product temperature (Tb) and drying time constitute critical material attributes and process parameters in the lyophilization process and especially during the primary drying stage. In the study, we performed a temperature measurement by the sublimation rate (TMbySR) to monitor the Tb value and determine the end point...

journal_title：Journal of pharmaceutical sciences

authors： Kawasaki H,Shimanouchi T,Sawada H,Hosomi H,Hamabe Y,Kimura Y

更新日期：2019-07-01 00:00:00