Plasma protein binding of zomepirac sodium.

abstract：:The estimation of aqueous solubilities of organic nonelectrolytes by the General Solubility Equation (GSE) as proposed by Valvani and Yalkowsky (1980) is used in this study. The data and assumptions on which the GSE are based are reevaluated, and the equation is revised. The revised GSE is validated on a set of 580 ph...

journal_title：Journal of pharmaceutical sciences

authors： Jain N,Yalkowsky SH

更新日期：2001-02-01 00:00:00

abstract：:Co-amorphous drug-amino acid systems have gained growing interest as an alternative to common amorphous formulations which contain polymers as stabilizers. Several preparation methods have recently been investigated, including vibrational ball milling on a laboratory scale or spray drying in a larger scale. In this st...

journal_title：Journal of pharmaceutical sciences

authors： Lenz E,Löbmann K,Rades T,Knop K,Kleinebudde P

更新日期：2017-01-01 00:00:00

abstract：:Pharmaceutical cocrystals have garnered significant interest as potential solids to address issues associated with formulation development of drug substances. However, studies concerning the understanding of formulation behavior of cocrystals are still at the nascent stage. We present results of our attempts to evalua...

journal_title：Journal of pharmaceutical sciences

authors： Aitipamula S,Wong ABH,Kanaujia P

更新日期：2018-02-01 00:00:00

abstract：:Health authorities require that suitable stability of the drug substance be shown in relevant materials of construction. ICH Q1A(R2) explicitly states that "stability studies should be conducted on drug substance packaged in a container closure system that is the same as or simulates the packaging proposed for storage...

journal_title：Journal of pharmaceutical sciences

authors： Klair N,Kim MT,Lee A,Xiao NJ,Patel AR

更新日期：2020-10-07 00:00:00

abstract：:Solid samples of 1-hydroxymethyl- and 1,5-dihydroxymethylallopurinol, 1-hydroxymethylglutethimide, and 1-hydroxymethylphenobarbital were prepared, and equilibrium constants for their formation from formaldehyde and allopurinol, glutethimide, or phenobarbital were calculated. The N-hydroxymethyl derivatives had higher ...

journal_title：Journal of pharmaceutical sciences

authors： Bansal PC,Pitman IH,Higuchi T

更新日期：1981-08-01 00:00:00

abstract：:The antifungal drug, 5-fluorocytosine (FC), is marketed as a capsule (250 or 500 mg strength) instead of the preferred tablet dosage form. Through systematic characterization of solid-state properties, including mechanical properties, we identify tabletability and poor physical stability of FC as the problems that lik...

journal_title：Journal of pharmaceutical sciences

authors： Perumalla SR,Sun CC

更新日期：2014-04-01 00:00:00

abstract：:Two novel series of steroidal derivatives containing various thiourea and substituted thiazoline moieties attached to the 2- or 4-position of estrone were synthesized and examined for in vitro effect on bovine pancreatic ribonuclease activity. All compounds studied exhibited a catabolic activity. The steroidal thiazol...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim ES,Omar AM,Habib NS,Aboulwafa OM,El-Sewedy SM,Bourdais J

更新日期：1983-10-01 00:00:00

abstract：:A novel method was established for the preparation of Eudragit S, Eudragit L, and Eudispert high-viscosity (hv) hydrogel and xerogel preparations containing a medicinal component such as pentoxifylline (an agent that improves cerebral microcirculation). A significant correlation was found between the in vitro mean dis...

journal_title：Journal of pharmaceutical sciences

authors： Kim NS,Kawata M,Uchida T,Goto S

更新日期：1992-06-01 00:00:00

abstract：:A revised classification system for oral drugs was developed using the biopharmaceutics classification system (BCS) as a starting point. The revised system is designed to have a greater focus on drug developability. Intestinal solubility, the compensatory nature of solubility and permeability in the small intestine an...

journal_title：Journal of pharmaceutical sciences

authors： Butler JM,Dressman JB

更新日期：2010-12-01 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：:Solvent influences on the crystallization of polymorph and hydrate forms of the nootropic drug piracetam (2-oxo-pyrrolidineacetamide) were investigated from water, methanol, 2-propanol, isobutanol, and nitromethane. Crystal growth profiles of piracetam polymorphs were constructed using time-resolved diffraction snapsh...

journal_title：Journal of pharmaceutical sciences

authors： DeMatos LL,Williams AC,Booth SW,Petts CR,Taylor DJ,Blagden N

更新日期：2007-05-01 00:00:00

abstract：:Amphiphilic cyclodextrins (CDs) are biocompatible derivatives of natural CDs and are able to form nanoparticles or polyplexes spontaneously. In this study, nanoparticles prepared from nonionic (6OCaproβCD) or cationic amphiphilic CD (PC βCDC6) were used comparatively to develop nanoparticles intended for breast cancer...

journal_title：Journal of pharmaceutical sciences

authors： Varan G,Öncül S,Ercan A,Benito JM,Ortiz Mellet C,Bilensoy E

更新日期：2016-10-01 00:00:00

abstract：:Near-infrared spectroscopy was used to monitor the phase conversion for two solvatomorphs of caffeine, an anhydrous form and a nonstoichiometric hydrate, as a function of time, temperature, and relative humidity. The transformation kinetics between these caffeine forms was determined to increase with temperature. The ...

journal_title：Journal of pharmaceutical sciences

authors： Krzyzaniak JF,Williams GR,Ni N

更新日期：2007-05-01 00:00:00

abstract：:The inclusion complexation of homologous derivatives of steroid hormones with cyclodextrins and 2-hydroxypropyl-beta-cyclodextrin (2-HP-beta-CD) was investigated with regard to underlying structure-interaction relationship. The interaction was studied by phase solubility analysis and stabilization effects of complex f...

journal_title：Journal of pharmaceutical sciences

authors： Albers E,Müller BW

更新日期：1992-08-01 00:00:00

abstract：:Blood levels of intact chloroprocaine were determined using a GLC procedure capable of detecting as little as 10 ng of chloroprocaine/ml of blood. It was necessary to detective plasma cholinesterases in collected samples by adding echothiophate iodide to blood sampling tubes. An extraction procedure, followed by a TLC...

journal_title：Journal of pharmaceutical sciences

authors： O'Brien JE,Abbey V,Hinsvark O,Perel J,Finster M

更新日期：1979-01-01 00:00:00

abstract：:The solubility of a series of compounds was determined in a wide polarity spectrum of normal aliphatic alcohols over a limited temperature range. The solutes chosen were the methyl through n-butyl p-hydroxybenzoates, several of these being useful preservatives. Solubility profiles were determined for these compounds, ...

journal_title：Journal of pharmaceutical sciences

authors： Alexander KS,Mauger JW,Petersen H Jr,Paruta AN

更新日期：1977-01-01 00:00:00

abstract：:Sugars and polyols have been used routinely with lyophilized proteins and peptides as bulking agents, cryoprotectants, and lyoprotectants. However, reducing sugars may present a problem as excipients since they are potentially reactive with proteins. In this stability study of recombinant human relaxin (Rix) with vari...

journal_title：Journal of pharmaceutical sciences

authors： Li S,Patapoff TW,Overcashier D,Hsu C,Nguyen TH,Borchardt RT

更新日期：1996-08-01 00:00:00

abstract：:Employing the roots of Iris missouriensis, two known triterpenes, iso-iridogermanal and zeorin, were isolated and identified. As presently reported, they were found to demonstrate cytotoxic activity toward cultured P-388 cells (ED50 = 0.1 and 1.1 microgram/mL, respectively). Additionally, a new triterpene that demonst...

journal_title：Journal of pharmaceutical sciences

authors： Wong SM,Oshima Y,Pezzuto JM,Fong HH,Farnsworth NR

更新日期：1986-03-01 00:00:00

abstract：:The effect of caffeine on the absorption of ergotamine from the rat small intestine was studied. The results of a series of experiments showed that caffeine significantly enhanced absorption of ergotamine from solutions of pH 5.0 when both substances were in solution and when an intact blood supply was either absent (...

journal_title：Journal of pharmaceutical sciences

authors： Anderson JR,Drehsen G,Pitman IH

更新日期：1981-06-01 00:00:00

abstract：:A study was undertaken to develop a method that could be used an an indication of the absorption of steroids. It was demonstrated that 17-hydroxycorticosteroids in urine could be quantitatively determined via absorptivity values obtained through the use of standard hydrocortisone-alcohol solutions or standard solution...

journal_title：Journal of pharmaceutical sciences

authors： Feinstein W,Sciarra JJ

更新日期：1975-06-01 00:00:00

abstract：:Complexation of ferrous cytochrome P450 by metabolic intermediates formed during NADPH-catalyzed metabolism of compounds structurally related to orphenadrine was studied. This so-called metabolic intermediate complexation was determined in rat liver microsomes, obtained from phenobarbital-pretreated rats, at 455 nm us...

journal_title：Journal of pharmaceutical sciences

authors： Bast A,Savenije-Chapel EM,Noordhoek J

更新日期：1984-07-01 00:00:00

abstract：:The crystal structure of the common therapeutic agent, the pentahydrated sodium salt of L-thyroxine hormone (3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]-L-alanine), has been determined and discussed in relation to the drug's stability. The stoichiometry and absolute configuration (-)-C(8)S-[C15H10I4NO4]-.Na+....

journal_title：Journal of pharmaceutical sciences

authors： Katrusiak A,Katrusiak A

更新日期：2004-12-01 00:00:00

abstract：:The disposition kinetics of nicotine and cotinine enantiomers was determined in rabbits. The clearance of (R)-nicotine was similar to that of (S)-nicotine, but clearance of (R)-cotinine was twice that of (S)-cotinine. Fractional conversions of both enantiomers of nicotine to cotinine were approximately 50%. These resu...

journal_title：Journal of pharmaceutical sciences

authors： Jacob P 3rd,Benowitz NL,Copeland JR,Risner ME,Cone EJ

更新日期：1988-05-01 00:00:00

abstract：:The diffusion model for percutaneous absorption is developed for the specific case of delivery to the skin being limited by the application of a finite amount of solute. Two cases are considered; in the first, there is an application of a finite donor (vehicle) volume, and in the second, there are solvent-deposited so...

journal_title：Journal of pharmaceutical sciences

authors： Anissimov YG,Roberts MS

更新日期：2001-04-01 00:00:00

abstract：:Release of drug from a single-layer film containing dispersed drug follows a diffusion-controlled matrix model, where the quantity released per unit area is proportional to the square root of time. The kinetics may be made linear with time (zero order) by laminating a second film without drug to the releasing side of ...

journal_title：Journal of pharmaceutical sciences

authors： Borodkin S,Tucker FE

更新日期：1975-08-01 00:00:00

abstract：:The analysis of corticosteroid prodrugs in pharmacokinetic (PK) studies poses the risk of overestimation of corticosteroid concentrations due to in vitro hydrolysis of prodrugs after sample collection. This study tests the effectiveness of enzyme inhibitors as stabilizers for betamethasone sodium phosphate (BSP) in pr...

journal_title：Journal of pharmaceutical sciences

authors： Samtani MN,Schwab M,Nathanielsz PW,Jusko WJ

更新日期：2004-03-01 00:00:00

abstract：:Pharmaceutical scientists are often asked to assess the impact of modifications to the illumination in the manufacturing and product packaging environment on product quality. To assess the impact of switching light sources, four model compounds were exposed to standard fluorescent light, LED, and "yellow light" and th...

journal_title：Journal of pharmaceutical sciences

authors： Wasylaschuk W,Pierce B,Geng X,Socia A,Kim D,Wuelfing WP,Abend A

更新日期：2020-11-01 00:00:00

abstract：:This work investigated the feasibility of developing benznidazole (BZL) tablets, allowing fast, reproducible, and complete drug dissolution, by compressing BZL-Polyethylene Glycol (PEG) 6000 physical mixtures (PMs) and solid dispersions (SDs). SDs were prepared by the solvent evaporation method at different drug:polym...

journal_title：Journal of pharmaceutical sciences

authors： Leonardi D,Salomon CJ

更新日期：2013-03-01 00:00:00

abstract：:Using liquid scintillation counting and liquid chromatographic techniques, it has been demonstrated that the anthracycline antibiotics, doxorubicin hydrochloride, N-trifluoroacetyladriamycin-14-valerate, and N-trifluoroacetyladriamycin-14-octanoate, can be strongly absorbed to the walls of containers, depending on the...

journal_title：Journal of pharmaceutical sciences

authors： Tomlinson E,Malspeis L

更新日期：1982-10-01 00:00:00

abstract：:The aim of the study was to determine and compare the degree of swelling and the swelling kinetics of poly(ethylene oxide) (PEO) hydrophilic matrix tablets without any additives for matrixes with different molecular weight polydispersities. A wide range of "mixed" polydisperse PEO tablets were obtained by mixing two P...

journal_title：Journal of pharmaceutical sciences

authors： Körner A,Larsson A,Andersson A,Piculell L

更新日期：2010-03-01 00:00:00