In vitro and in vivo evaluation of a sulfenamide prodrug of basic metformin.

abstract：:Adequate protein solubility is an important prerequisite for development, manufacture, and administration of biotherapeutic drug candidates, especially for high-concentration protein formulations. A previously established method for determining the relative apparent solubility (thermodynamic activity) of proteins usin...

journal_title：Journal of pharmaceutical sciences

authors： Toprani VM,Joshi SB,Kueltzo LA,Schwartz RM,Middaugh CR,Volkin DB

更新日期：2016-08-01 00:00:00

abstract：:Certain disulfide analogues of cystamine were prepared and evaluated for the ability to inhibit gamma-glutamylcysteine synthetase (GCS), the rate-limiting enzyme in glutathione synthesis. The compound SAPH-3 disulfide (2a) was found to be the most effective inactivator of GCS reported to date. Studies of structural an...

journal_title：Journal of pharmaceutical sciences

authors： Schor NF,Cheng B,Siuda JF

更新日期：1991-04-01 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：:The delamination of glass contact surfaces because of hydrolytic instability has been well documented. However, the lack of glass surface integrity can also lead to other undesirable outcomes prior to visible glass delamination. This work shows how the early stages of delamination, namely, glass corrosion, can influen...

journal_title：Journal of pharmaceutical sciences

authors： Watkins MA,Iacocca RG,Shelbourn TL,Dong X,Stobba-Wiley C

更新日期：2014-08-01 00:00:00

abstract：:Previously available GLC methods for ethambutol may only be used to measure quantities of drugs much greater than those found in biological fluids such as plasma and dialysate. A previously published GLC method for plasma samples is extended to measure ethambutol in dialysate. A second GLC method, involving derivatiza...

journal_title：Journal of pharmaceutical sciences

authors： Lee CS,Benet LZ

更新日期：1978-04-01 00:00:00

abstract：:Preliminary studies indicate that it may be possible to differentiate the effects of a nephrotoxic substance from those of diuretic agents by the measurement of both urine and plasma osmolarity. The nephrotoxic substance, mercuric chloride, decreases urinary osmolality and increases plasma or serum osmolality. The diu...

journal_title：Journal of pharmaceutical sciences

authors： Vogin EE

更新日期：1977-04-01 00:00:00

abstract：:The application of drug ion-selective electrodes as sensors for the direct determination of the released drug in a continuous-flow analyzer for automated dissolution studies is described. Flow-through electrodes, selective to chlorpromazine, amitriptyline, propantheline, cimetidine, and ranitidine, have been construct...

journal_title：Journal of pharmaceutical sciences

authors： Mitsana-Papazoglou A,Christopoulos TK,Diamandis EP,Koupparis MA

更新日期：1987-09-01 00:00:00

abstract：:The aim of this study was to evaluate a new experimental protocol utilizing isolated frog intestinal sacs for the assessment of intestinal drug permeability in humans. Segments of approximately 5.0 cm in length were used for these experiments. The intestinal sacs were filled with a solution of the appropriate drug in ...

journal_title：Journal of pharmaceutical sciences

authors： Trapani G,Franco M,Trapani A,Lopedota A,Latrofa A,Gallucci E,Micelli S,Liso G

更新日期：2004-12-01 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：:Adsorption isotherms for the diazepam-activated carbon system in simulated intestinal fluid (SIF), without pancreatin, and in SIF with different percentages of ethanol were determined as were the solubilities of diazepam in SIF and in SIF with different percentages of ethanol. The surface area of the activated carbon ...

journal_title：Journal of pharmaceutical sciences

authors： Wurster DE,Alkhamis KA,Matheson LE

更新日期：2003-10-01 00:00:00

abstract：:Several factors affecting the dissolution rate of cholesterol in monooctanoin were investigated. This solvent is used clinically for dissolution of residual cholesterol gallstones in the bile duct after cholecystectomy. The effect of added water on dissolution rate, measured using the static- or rotating-disk methods,...

journal_title：Journal of pharmaceutical sciences

authors： Bogardus JB

更新日期：1984-07-01 00:00:00

abstract：:In spite of the recent advances in technology to optimize the absorption, distribution, metabolism and elimination (ADME) properties of new and promising medicinal products to reduce clinical failures, the investigation of drug disposition in the pediatric and elderly populations continues to be under evaluated. With ...

journal_title：Journal of pharmaceutical sciences

authors： Chien JY,Ho RJ

更新日期：2011-01-01 00:00:00

abstract：:The phase behavior of two series of phosphatidylcholines (PC) possessing carbamyloxy-linked fatty acids has been studied by differential scanning calorimetry. These non-natural phosphatidylcholines are of interest because they possess the capability of forming interlipid hydrogen bonds via the carbamyloxy function and...

journal_title：Journal of pharmaceutical sciences

authors： Curatolo W,Bali A,Gupta CM

更新日期：1985-12-01 00:00:00

abstract：:The aims of this study were to evaluate the pharmacokinetics of doripenem (Finibax®, Doribax®, S-4661), a parenteral carbapenem antibiotic, in pediatric patients based on concentrations of doripenem in plasma after administration of 20 mg/kg 2 or 3 times daily and to evaluate the dosing regimens by using Monte-Carlo p...

journal_title：Journal of pharmaceutical sciences

authors： Matsuo Y,Ishibashi T,Matsumoto S,Katsube T,Wajima T

更新日期：2019-09-01 00:00:00

abstract：:When heated at temperatures in excess of 100 degrees, the stability of neomycin in aqueous ophthalmic formulations was improved by the addition of edetate disodium (0.01%). As the exposure temperature was reduced, the degree of stability enhancement diminished until the effect was reversed, and addition of edetate dis...

journal_title：Journal of pharmaceutical sciences

authors： Hodges NA,Walton PG

更新日期：1981-08-01 00:00:00

abstract：:A sensitive high-performance liquid chromatographic (HPLC) assay for N-acetylcysteine in human plasma and urine has been developed. The method employs a prechromatographic stage to produce the dinitrophenyl derivative of N-acetylcysteine, which is chromatographed on a 5-microns C18 bonded reverse-phase column using an...

journal_title：Journal of pharmaceutical sciences

authors： Lewis PA,Woodward AJ,Maddock J

更新日期：1984-07-01 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：:Health interventions developed for wealthy nations are difficult to introduce in developing countries due to a lack of sufficient technological, financial, political, or infrastructural resources. Increasingly, however, product developers are creating new technologies that meet the needs of low-resource settings. Expe...

journal_title：Journal of pharmaceutical sciences

authors： Harner-Jay C,Sherris J

更新日期：2008-12-01 00:00:00

abstract：:A direct high-performance liquid chromatographic (HPLC) method was applied to monitor 2,5-diaziridinyl-3,6-bis(carboethoxyamino)-1,4-benzoquinone (I) and its degradation products in pharmaceutical vehicles at 25 +/- 0.1 degrees. At the optimal pH for stability of I, an increase in buffer concentration [phosphate and t...

journal_title：Journal of pharmaceutical sciences

authors： Poochikian GK,Kelley JA

更新日期：1981-02-01 00:00:00

abstract：:Local variations in compaction behaviour were investigated, for specimens of different shapes and thickness, comparing predictions from finite element (FE) modelling and results from a recently developed method using small-angle X-ray scattering (SAXS). Good agreement was generally obtained between these methods, in t...

journal_title：Journal of pharmaceutical sciences

authors： Laity PR,Han L,Elliott J,Cameron RE

更新日期：2010-10-01 00:00:00

abstract：:(13) C cross-polarization magic-angle spinning nuclear magnetic resonance (CPMAS NMR) spectroscopy was applied to the identification and characterization of carvedilol (1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)-ethylamino]-propan-2-ol) in pharmaceutical preparations. Solid-state spectra (standard linewidth and l...

journal_title：Journal of pharmaceutical sciences

authors： Zielińska-Pisklak M,Pisklak DM,Wawer I

更新日期：2012-05-01 00:00:00

abstract：:The diterpene esters, genkwadaphnin and yuanhuacine, have been shown to possess significant antileukemic activity in the P-388 screen. The major metabolic effects of the diterpene esters were on DNA and protein synthesis. The effects on DNA synthesis in vitro were evoked at a lower concentration than that required for...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Kasai R,Wu RY,Tagahara K,Lee KH

更新日期：1982-11-01 00:00:00

abstract：:The aim of this study was to investigate the role of porosity on the compression behavior and tablet tensile strength for granules produced by a dry granulation procedure. Microcrystalline cellulose was used as a typical pharmaceutical excipient and a comparison was made with the effect of granule porosity on the comp...

journal_title：Journal of pharmaceutical sciences

authors： Nordström J,Alderborn G

更新日期：2015-06-01 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：:A difference spectrophotometric analytical method was developed for the selective determination of p-hydroxybenzoic acid in the presence of its alkyl esters without prior separation. Based on the spectral shift to a shorter wavelength accompanyint carboxyl dissociation, the procedure measures as little as 2% of this a...

journal_title：Journal of pharmaceutical sciences

authors： Fink DW,Fink HC,Tolan JW,Blodinger J

更新日期：1978-06-01 00:00:00

abstract：:The aim of this study to administer hydrocortisone (HC) percutaneously in the form of polymeric nanoparticles (NPs) to alleviate its transcutaneous absorption, and to derive additional wound-healing benefits of chitosan. HC-loaded NPs had varied particle sizes, zeta potentials, and entrapment efficiencies, when drug-t...

journal_title：Journal of pharmaceutical sciences

authors： Hussain Z,Katas H,Amin MC,Kumulosasi E,Sahudin S

更新日期：2013-03-01 00:00:00

abstract：:Studies directed at the synthesis of tetracycline ring A analogs are described. 4-Carbethoxycyclohexane-1,3-dione was converted to the ethyl urethan dispiro[1,3-dioxolane-2,2'-cyclohexane-4',2"(1,3)-dioxolane]-1'-carbamic acid ethyl ester via the dispiro[1,3-dioxolane-2,2'-cyclohexane-4'-2"(1,3)-dioxolane]-1'-carboxyl...

journal_title：Journal of pharmaceutical sciences

authors： Moskalyk RE,Mak AL,Chatten LG,Locock RA

更新日期：1981-05-01 00:00:00

abstract：:Approximately 30% of active pharmaceutical ingredients (APIs) experience agglomeration, granulation, and breakage during agitated drying. Currently, there is no small-scale bench tool to help assess and observe granulation behavior of APIs in the laboratory and subsequently lead to the development of a robust drying m...

journal_title：Journal of pharmaceutical sciences

authors： Zhang S,Lamberto DJ

更新日期：2014-01-01 00:00:00

abstract：:Synthetic peptides corresponding to the variable tandem repeat domain of the cancer-associated antigen MUC1 mucin are candidates for cancer vaccines. In our investigation mice were immunized via subcutaneous injection with poly(d,l-lactic-co-glycolic acid) (PLGA) microspheres containing a MUC1 mucin peptide. It was hy...

journal_title：Journal of pharmaceutical sciences

authors： Newman KD,Sosnowski DL,Kwon GS,Samuel J

更新日期：1998-11-01 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