2-Acetylpyridine thiosemicarbazones XI: 2-(alpha-Hydroxyacetyl)pyridine thiosemicarbazones as antimalarial and antibacterial agents.

abstract：:The increased incidence of human immunodeficiency virus infection in women has identified an urgent need to develop a female-controlled method to prevent acquisition of human immunodeficiency virus and other sexually transmitted diseases. Women would apply the product intravaginally before intercourse. Development of ...

journal_title：Journal of pharmaceutical sciences

authors： Sassi AB,McCullough KD,Cost MR,Hillier SL,Rohan LC

更新日期：2004-08-01 00:00:00

abstract：:A three-way crossover bioavailability study was performed using nine adult male volunteers with three different commercial prednisone tablets. Plasma samples were assayed for prednisolone, the active metabolite of prednisone, by a radioimmunoassay method. Statistical analysis showed significant differences in the rate...

journal_title：Journal of pharmaceutical sciences

authors： Sullivan TJ,Sakmar E,Albert KS,Blair DC,Wagner JG

更新日期：1975-10-01 00:00:00

abstract：:A new parameter, the kinetic ratio, is suggested for estimating product potency during storage under ambient warehouse temperatures. Actual warehouse temperature data were integrated using Arrhenius kinetics, and the resulting potency errors, due both to the integration method and to temperature averaging, were evalua...

journal_title：Journal of pharmaceutical sciences

authors： Scher M

更新日期：1980-03-01 00:00:00

abstract：:Role of water in chemical (in)stability is revisited, with focus on deamidation in freeze-dried amorphous proteins and peptides. Two distinct patterns for deamidation versus water have been reported, that is, a consistent increase in rate constant with water, and a "hockey stick"-type behavior. For the latter, deamida...

journal_title：Journal of pharmaceutical sciences

authors： Ohtake S,Feng S,Shalaev E

更新日期：2018-01-01 00:00:00

abstract：:A simultaneous GLC determination for methyl salicylate and menthol in a topical analgesic formulation is reported. n-Nonadecane is used as the internal standard. The method is rapid, accurate, precise, and selective in the presence of salicylic acid and ethyl salicylate. ...

journal_title：Journal of pharmaceutical sciences

authors： Sapio JP,Sethachutkul K,Moody JE

更新日期：1979-04-01 00:00:00

abstract：:Dolasetron mesilate (Anzemet) ((2 alpha, 6 alpha, 8 alpha, 9a beta)-octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl-1 H-indole-3-carboxylate monomethane-sulfonate) is a 5-HT3 receptor antagonist, which is in development for the treatment of chemotherapy-induced emesis. The ketone moiety of dolasetron is rapidly reduced...

journal_title：Journal of pharmaceutical sciences

authors： Dow J,Francesco GF,Berg C

更新日期：1996-07-01 00:00:00

abstract：:The aim of the present study was to investigate the mechanism of aqueous degradation of Salinosporamide A (NPI-0052; 1), a potent proteasome inhibitor that is currently in Phase I clinical trials for the treatment of cancer and is characterized by a unique beta-lactone-gamma-lactam bicyclic ring structure. The degrada...

journal_title：Journal of pharmaceutical sciences

authors： Denora N,Potts BC,Stella VJ

更新日期：2007-08-01 00:00:00

abstract：:Recently, our laboratory reported that intravenous immunoglobulin (IVIG) treatment increased antiplatelet antibody (7E3) clearance in a rat model of immune thrombocytopenic purpura (ITP). However, due to the multifaceted nature of IVIG therapy, the contribution of this increase in antiplatelet antibody clearance to th...

journal_title：Journal of pharmaceutical sciences

authors： Hansen RJ,Balthasar JP

更新日期：2003-06-01 00:00:00

abstract：:The bioavailability of three different brands and three different dosage forms of doxycycline was studied in normal subjects. Single doses, equivalent to 200 mg of doxycycline, were administered to six subjects in a crossover design as the innovator's intravenous solution given orally (Treatment A), the innovator's ca...

journal_title：Journal of pharmaceutical sciences

authors： Antal EJ,Jaffe JM,Poust RI,Colaizzi JL

更新日期：1975-12-01 00:00:00

abstract：:The pharmacologically active compound (33% reduction in rabbit intraocular pressure recovery rate assay) 1-ethyl-6-fluoro-1,2,3,4-tetrahydroquinoline (MC4), which showed ocular hypotensive action and had optimum physicochemical properties, was characterized for its ocular absorption and distribution properties to bett...

journal_title：Journal of pharmaceutical sciences

authors： Pamulapati CR,Schoenwald RD

更新日期：2011-12-01 00:00:00

abstract：:A simple enzyme immunoassay for the determination of captopril was developed. A specific antibody for captopril was produced in rabbits that were immunized with a hapten-bovine immunoglobulin G conjugate, which was prepared by using 4-(maleimidomethyl)cyclohexane carboxylic acid as a spacer group. The limit of detecti...

journal_title：Journal of pharmaceutical sciences

authors： Kinoshita H,Nakamaru R,Tanaka S,Tohira Y,Sawada M

更新日期：1986-07-01 00:00:00

abstract：:Flumizole is a potent anti-inflammatory agent in animal models with an inhibitory activity severalfold that of indomethacin in rat foot edema and prostaglandin synthetase tests. The drug was well absorbed from the GI tract when administered in the solution used in pharmacological assays. However, markedly poorer absor...

journal_title：Journal of pharmaceutical sciences

authors： Wiseman EH,McIlhenny HM,Bettis JW

更新日期：1975-09-01 00:00:00

abstract：:An electron-capture GLC method was developed for measuring pindolol in human plasma and urine. The unchanged drug was extracted with benzene from alkalinized plasma or urine using propranolol as the internal standard. Both compounds subsequently were back-extracted into 0.1 M HCl and then into benzene. After evaporati...

journal_title：Journal of pharmaceutical sciences

authors： Guerret M,Lavene D,Kiechel JR

更新日期：1980-10-01 00:00:00

abstract：:The hydrophobic substituent parameter for a system of meta- and para-disubstituted benzenes, XC6H4Y, defined as pi X/PhY = log PXC6H4Y - log PC6H5Y, where P is the octanol-water partition coefficient and X and Y are variable and fixed substituents, respectively, varies from one system to another, according to the vari...

journal_title：Journal of pharmaceutical sciences

authors： Fujita T

更新日期：1983-03-01 00:00:00

abstract：:We previously reported nonaqueous silicone elastomer gels (SEGs) for sustained vaginal administration of the CCR5-targeted entry inhibitor maraviroc (MVC). Here, we describe chemically modified SEGs (h-SEGs) in which the hydrophobic cyclomethicone component was partially replaced with relatively hydrophilic silanol-te...

journal_title：Journal of pharmaceutical sciences

authors： Forbes CJ,McCoy CF,Murphy DJ,Woolfson AD,Moore JP,Evans A,Shattock RJ,Malcolm RK

更新日期：2014-05-01 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：:Comparability studies used to assess a proposed manufacturing change for a biological product include sensitive analytical studies to confirm there are no significant differences in structural or functional attributes that may contribute to clinically meaningful changes in efficacy or safety. When a proposed change is...

journal_title：Journal of pharmaceutical sciences

authors： Grampp G,McElroy PL,Camblin G,Pollock A

更新日期：2018-06-01 00:00:00

abstract：:Unlike most organic compounds, both digoxin and digitoxin melted over a wide temperature range, with the widest range being 88 and 33 degrees for both compounds, respectively. Furthermore, the melting ranges varied markedly among several untriturated powders obtained from commercial sources and after recrystallization...

journal_title：Journal of pharmaceutical sciences

authors： Chiou WL,Kyle LE

更新日期：1979-10-01 00:00:00

abstract：:Postabsorptive factors which can affect systemic drug exposure are assumed to be dependent on the active pharmaceutical ingredient (API), and thus independent of formulation. In contrast, preabsorptive factors, for example, hypochlorhydria, might affect systemic exposure in both an API and a formulation-dependent way....

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Patel N,Dressman JB

更新日期：2017-02-01 00:00:00

abstract：:Three dimensional terahertz pulsed imaging (TPI) was evaluated as a novel tool for the nondestructive characterization of different solid oral dosage forms. The time-domain reflection signal of coherent pulsed light in the far infrared was used to investigate film-coated tablets, sugar-coated tablets, multilayered con...

journal_title：Journal of pharmaceutical sciences

authors： Zeitler JA,Shen Y,Baker C,Taday PF,Pepper M,Rades T

更新日期：2007-02-01 00:00:00

abstract：:The suppression of imipramine hydrochloride (IMP)- induced hemolysis by native cyclodextrins (alpha-, beta-, and gamma-CDs) and beta-CD derivatives is measured as a function of CD concentration and is quantitatively correlated with the surface tension of the solution determined at 37.0 degrees C. The modified beta-CDs...

journal_title：Journal of pharmaceutical sciences

authors： Funasaki N,Okuda T,Neya S

更新日期：2001-08-01 00:00:00

abstract：:Although inaccurate true density affects analysis of powder compaction data, such effects have not been systematically evaluated in the literature. This work is aimed at quantitatively evaluating effects of inaccurate true density on tableting data analysis using the Ryshkewitch equation, sigma = sigma0 e - bepsilon, ...

journal_title：Journal of pharmaceutical sciences

authors： Sun CC

更新日期：2005-09-01 00:00:00

abstract：:The anticonvulsant and CNS-depressant activities of 16 commercially available antiepileptics were subjected to regression analysis. For the maximal electroshock seizure test and pentylenetetrazol seizure threshold test, good correlations were obtained only after diazepam, clonazepam, and carbamazepam were deleted; for...

journal_title：Journal of pharmaceutical sciences

authors： Lien EJ,Liao RC,Shinouda HG

更新日期：1979-04-01 00:00:00

abstract：:The purpose of the study is to understand the effect of altitude on the performance of selected pressurized metered dose inhalers (pMDIs) and dry powder inhalers (DPIs). A testing apparatus that created consistent breath profiles through the Alberta Idealized Throat was designed to test five pMDIs and two DPIs at alti...

journal_title：Journal of pharmaceutical sciences

authors： Titosky JTF,Morin CMD,Suderman JD,Olfert JS,Finlay WH,Vehring R

更新日期：2014-07-01 00:00:00

abstract：:Bioadhesive polymers that bind to the gastric mucin or epithelial cell surface are useful in drug delivery for the purposes of (a) retaining a dosage from in the GI tract and (b) increasing the intimacy and duration of contact of drug with the absorbing membrane. Polycarbophil has previously been shown to have bioadhe...

journal_title：Journal of pharmaceutical sciences

authors： Longer MA,Ch'ng HS,Robinson JR

更新日期：1985-04-01 00:00:00

abstract：:Mixing Fungizone with a fat emulsion used for nutritional purpose (Intralipid or Lipofundin ) was reported to decrease Amphotericin B (AmB) toxicity in clinical use. In an effort to understand the reason for this phenomenon, spectral and morphological analyses were done for the Fungizone and Fungizone /Lipofundin admi...

journal_title：Journal of pharmaceutical sciences

authors： Egito ES,Araújo IB,Damasceno BP,Price JC

更新日期：2002-11-01 00:00:00

abstract：:Vitamin E tocopherol polyethylene glycol succinate (TPGS) is a non-ionic surface active agent, known to enhance the bioavailability of lipophilic compounds via wettability, solubility, and in some cases permeability enhancement. MK-0536 is an anti-retroviral drug with poor wettability and solubility and a high dose. B...

journal_title：Journal of pharmaceutical sciences

authors： Tatavarti A,Kesisoglou F

更新日期：2015-11-01 00:00:00

abstract：:It is now becoming apparent that a common pathway of protein aggregation involves the unimolecular structural rearrangement from the native state to a slightly expanded aggregation-competent species. It is the goal of this study to understand the aggregation and the effects of buffer on the stability of IFN-tau. In th...

journal_title：Journal of pharmaceutical sciences

authors： Katayama DS,Nayar R,Chou DK,Valente JJ,Cooper J,Henry CS,Vander Velde DG,Villarete L,Liu CP,Manning MC

更新日期：2006-06-01 00:00:00

abstract：:NF-kappaB activation is clearly linked to the pathogenesis of multiple inflammatory diseases including arthritis. The prominent role of IkappaB kinase-2 (IKK-2) in regulating NF-kappaB signaling in response to proinflammatory stimuli has made IKK-2 a primary anti-inflammation therapeutic target. PHA-408, a potent and ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,Kishore NN,Thompson DC

更新日期：2010-03-01 00:00:00

abstract：:A semi-automated protein binding assay using equilibrium dialysis (ED) and a novel mixed-matrix methodology has been developed. This method decreases mass spectrometer run time and reduces the likelihood of experimental artifacts. In this cassette-based approach, a single matrix is prepared following dialysis by mixin...

journal_title：Journal of pharmaceutical sciences

authors： Plise EG,Tran D,Salphati L

更新日期：2010-12-01 00:00:00