Decomposition of alpha-hydroxyaryl ketones and characterization of some unusual products.

abstract：:Therapeutic use of anti-inflammatory steroids is limited due to their potential suppressive effects on pituitary-adrenal function and the immune system. Based on the antedrug concept, a new class of potent locally active compounds with reduced risk of side effects has been synthesized from prednisolone by introducing ...

journal_title：Journal of pharmaceutical sciences

authors： Heiman AS,Taraporewala IB,McLean HM,Hong D,Lee HJ

更新日期：1990-07-01 00:00:00

abstract：:Under pandemic-caused emergency, evaluation of the potential of existing antiviral drugs for the treatment of COVID-19 is relevant. Triazavirin, an antiviral drug developed in Russia for per-oral administration, is involved in clinical trials against SARS-CoV-2 coronavirus. This virus has affinity to epithelial cells ...

journal_title：Journal of pharmaceutical sciences

authors： Valiulin SV,Onischuk AA,Dubtsov SN,Baklanov AM,An'kov SV,Plokhotnichenko ME,Tolstikova TG,Dultseva GG,Rusinov VL,Charushin VN,Fomin VM

更新日期：2020-11-26 00:00:00

abstract：:Microbicide intravaginal rings (IVRs) are a promising woman-controlled strategy for preventing sexual transmission of human immunodeficiency virus (HIV). An IVR was prepared and developed from polyether urethane (PU) elastomers for the sustained delivery of UC781, a highly potent nonnucleoside reverse transcriptase in...

journal_title：Journal of pharmaceutical sciences

authors： Clark MR,Johnson TJ,McCabe RT,Clark JT,Tuitupou A,Elgendy H,Friend DR,Kiser PF

更新日期：2012-02-01 00:00:00

abstract：:Literature data pertaining to the decision to allow a waiver of in vivo bioequivalence testing for the approval of immediate-release (IR) solid oral dosage forms containing efavirenz as the only active pharmaceutical ingredient (API) are reviewed. Because of lack of conclusive data about efavirenz's permeability and i...

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Nair A,Abrahamsson B,Groot DW,Kopp S,Langguth P,Polli JE,Shah VP,Dressman JB

更新日期：2013-02-01 00:00:00

abstract：:The objective of this study is to understand the underlying mechanisms responsible for the superior stability of indomethacin (INM)-Eudragit® E PO (E PO) system by exploring the miscibility and intermolecular interactions through the combination of thermal, rheological, and spectroscopic analysis. The zero shear-rate ...

journal_title：Journal of pharmaceutical sciences

authors： Liu H,Zhang X,Suwardie H,Wang P,Gogos CG

更新日期：2012-06-01 00:00:00

abstract：:Partial molal volumes (Vi infinity) of physostigmine, ranging from 232.9 to 239.8 cm3.mol-1, and its mole fraction solubilities (Xi), ranging from 0.051 to 0.009, were determined at 25 degrees C in solutions of isopropanol (IPA), isopropyl myristate (IPM), and their mixtures. An inverse relation was found between Vi i...

journal_title：Journal of pharmaceutical sciences

authors： Pardo A,Shiri Y,Cohen S

更新日期：1991-06-01 00:00:00

abstract：:Correlations between the bioavailability parameters for erythromycin stearate tablets from five manufacturers and in vitro tests of these tablets were examined using forward (stepwise), multiple linear regression analysis. Bioavailability parameters were determined in clinical studies employing a balanced, incomplete ...

journal_title：Journal of pharmaceutical sciences

authors： Stavchansky S,Doluisio JT,Martin A,Martin C,Cabana B,Dighe S,Loper A

更新日期：1980-11-01 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：: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：:The effect of dimethyl sulfoxide, dimethyl formamide, and dimethyl acetamide on the basal stratum corneum of excised nude mouse skin was investigated. All of these dipolar aprotic solvents caused a swelling of the basal stratum corneum cells and a disruption of the normal keratin pattern. This behavior suggests that d...

journal_title：Journal of pharmaceutical sciences

authors： Sharata HH,Burnette RR

更新日期：1988-01-01 00:00:00

abstract：:It is shown, using oxalic acid dihydrate as a model, that nonisothermal recrystallization of powders gives rise to particle size distributions which approach log-normality in many cases. The number of particles formed is, primarily, a function of the nucleation rate constants and the particle size distribution, i.e., ...

journal_title：Journal of pharmaceutical sciences

authors： Carstensen JT,Rodriguez-Hornedo N

更新日期：1985-12-01 00:00:00

abstract：:The skin penetration of 10 nonsteroidal antiinflammatory drugs (NSAIDs) was investigated after application in the lipophilic vehicle light mineral oil. The skin permeabilities and maximum fluxes, which were calculated from the concentration decreases of the applied solutions in the steady state phases, were correlated...

journal_title：Journal of pharmaceutical sciences

authors： Wenkers BP,Lippold BC

更新日期：1999-12-01 00:00:00

abstract：:Ensuring the health of street-involved children is a growing public health challenge. These children are vulnerable, neglected, and rarely a priority for basic service providers and governments. Sizable populations of street-involved children are present in major urban areas worldwide and current trends in urbanizatio...

journal_title：Journal of pharmaceutical sciences

authors： Osei-Twum JA,Wasan KM

更新日期：2012-10-01 00:00:00

abstract：:In recent years, controlled release coatings, comprised of drug-polymer composites, have been integrated with medical devices, improving device functionality and performance. However, relationships between material properties, manufacturing environment, composite (micro)structure, and subsequent release kinetics are n...

journal_title：Journal of pharmaceutical sciences

authors： Saylor DM,Kim CS,Patwardhan DV,Warren JA

更新日期：2009-01-01 00:00:00

abstract：:Anhydrotetracycline (AHTC), one of the major toxic decomposition products of the antibiotic tetracycline, contains several potential binding sites to metal ions. The acidity constants of the ligand were calculated in aqueous medium (I = 0.1 M) at 25 and 37 degrees C. We found pKa1 = 3.23 +/- 0.08, pKa2 = 5.94 +/- 0.09...

journal_title：Journal of pharmaceutical sciences

authors： de Siqueira JM,Carvalho S,Paniago EB,Tosi L,Beraldo H

更新日期：1994-03-01 00:00:00

abstract：:p-Bromospiperone was prepared from the reaction of spiperone with bromine. It was tested for dopamine receptor binding affinity in vitro and its ability to stimulate prolactin secretion in vivo. The results indicate no significant change of biological activities due to the bromination of spiperone. ...

journal_title：Journal of pharmaceutical sciences

authors： Huang CC,Friedman AM,So R,Simonovic M,Meltzer HY

更新日期：1980-08-01 00:00:00

abstract：:In recent years, biotechnologically derived peptide and protein-based drugs have developed into mainstream therapeutic agents. Peptide and protein drugs now constitute a substantial portion of the compounds under preclinical and clinical development in the global pharmaceutical industry. Pharmacokinetic and exposure/r...

journal_title：Journal of pharmaceutical sciences

authors： Tang L,Persky AM,Hochhaus G,Meibohm B

更新日期：2004-09-01 00:00:00

abstract：:Corneal permeability data taken from the literature were analyzed for possible quantitative relationships with physicochemical properties. Although a parabolic relationship was obtained with good correlation between lipophilicity, as expressed by the 1-octanol-water partition coefficients, log Poctanol (or the distrib...

journal_title：Journal of pharmaceutical sciences

authors： Yoshida F,Topliss JG

更新日期：1996-08-01 00:00:00

abstract：:Stirred media milling is the main technology for producing colloidal nanocrystalline suspensions. A number of studies have been reported on the effect of different operating parameters for lab, pilot, and industrial scales. However, typical milling tool box that can be used to support candidate from selection up to ph...

journal_title：Journal of pharmaceutical sciences

authors： Nakach M,Authelin JR,Agut C

更新日期：2017-07-01 00:00:00

abstract：:One manifestation of cystic fibrosis (CF) is the presence of a viscid mucus secretion in the lungs. The clearance of this mucus is significantly slower than in "normals" due to uncoordinated beating of the cilia and the increased viscosity of the mucus. In these studies, the permeabilities of p-aminosalicylic acid, is...

journal_title：Journal of pharmaceutical sciences

authors： Bhat PG,Flanagan DR,Donovan MD

更新日期：1996-06-01 00:00:00

abstract：:This work investigates the impact of quality attributes (impurity content, plasmid charge, and compactness) of plasmid DNA isolated with different purification methodologies on the characteristics of lipoplexes prepared thereof (size, zeta potential, stability) and on their ability to transfect mammalian cells. A 3.7 ...

journal_title：Journal of pharmaceutical sciences

authors： De La Vega J,Braak BT,Azzoni AR,Monteiro GA,Prazeres DM

更新日期：2013-11-01 00:00:00

abstract：:A gas chromatographic-mass spectrometric method was developed for the stereoselective quantification of threo-methylphenidate (MPD) and its metabolite, ritalinic acid (RA), in plasma or urine. The plasma concentrations of (+)-MPD after oral administration of two 10-mg conventional tablets containing racemic MPD.HCl or...

journal_title：Journal of pharmaceutical sciences

authors： Aoyama T,Kotaki H,Honda Y,Nakagawa F

更新日期：1990-06-01 00:00:00

abstract：:The crystallization tendency of 2 crystalline polymorphs of indomethacin (Iα, Iγ) in the undercooled melt has been investigated using molecular dynamics simulations. The main thermodynamical and dynamical physical parameters involved in the nucleation and growth processes have been determined. A careful attention has ...

journal_title：Journal of pharmaceutical sciences

authors： Gerges J,Affouard F

更新日期：2020-02-01 00:00:00

abstract：:A novel technique is presented to allow measurement of the kinetics of protein inactivation during drying of an acoustically levitated single droplet. Droplets/particles are removed from the acoustic field after various times during drying, and the state of the protein within them is analyzed. The influence of drying ...

journal_title：Journal of pharmaceutical sciences

authors： Lorenzen E,Lee G

更新日期：2012-06-01 00:00:00

abstract：:The rapid hydrolysis of epoprostenol to 6-keto-prostaglandin F1 alpha is hydronium ion-catalyzed even at pH 10 or higher. In the presence of 1.0% hexadecyltrimethylammonium chloride, the rate was reduced significantly (1580-fold at pH 2 and 283-fold at a physiological pH). This decrease in the hydrolysis rate is attri...

journal_title：Journal of pharmaceutical sciences

authors： Cho MJ

更新日期：1982-04-01 00:00:00

abstract：:A rapid approach for estimating the pK(a) value of small organic molecules was developed using vacuum-assisted multiplexed capillary electrophoresis (VAMCE) with ultraviolet detection. The VAMCE method employed a 96-capillary array, arranged in a standard 8 x 12 microtiter plate configuration, with each row of capilla...

journal_title：Journal of pharmaceutical sciences

authors： Zhou C,Jin Y,Kenseth JR,Stella M,Wehmeyer KR,Heineman WR

更新日期：2005-03-01 00:00:00

abstract：:Quantification analysis with near-infrared (NIR) spectroscopy typically requires utilizing chemometric techniques, such as partial least squares (PLS) method, to achieve the desired selectivity. This article points out a major limitation of these statistical-based calibration methods. The limitation is that the techni...

journal_title：Journal of pharmaceutical sciences

authors： Xiang D,Berry J,Buntz S,Gargiulo P,Cheney J,Joshi Y,Wabuyele B,Wu H,Hamed M,Hussain AS,Khan MA

更新日期：2009-03-01 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 reaction kinetics of blue tetrazolium with selected arylhydrazines were investigated under pseudo-first-order conditions. The reaction rate constants were obtained at various temperatures, and the enthalpy (8.4-11.2 kcal/mole) and entropy (-38--45 eu) of activations were calculated. A Hammett plot yielded a straig...

journal_title：Journal of pharmaceutical sciences

authors： Biehl ER,Wooten R,Kenner CT,Graham RE

更新日期：1978-07-01 00:00:00

abstract：:The solubilization of five model hydrophobic drugs by a series of micelle-forming, water-soluble methoxy poly(ethylene glycol)-block-polycaprolactone diblock copolymers (MePEG-b-PCL) with varying methoxy poly(ethylene glycol) (MePEG) and polycaprolactone (PCL) block lengths was investigated. Variation of the feed weig...

journal_title：Journal of pharmaceutical sciences

authors： Letchford K,Liggins R,Burt H

更新日期：2008-03-01 00:00:00