Preformulation studies in a drug development program for tablet formulations.

abstract：:The blood-brain barrier (BBB) limits the distribution of systemically administered therapeutics to the central nervous system (CNS). Intranasal delivery is a noninvasive method that targets drugs to the brain and spinal cord along olfactory and trigeminal neural pathways, bypassing the BBB and minimizing systemic expo...

journal_title：Journal of pharmaceutical sciences

authors： Dhuria SV,Hanson LR,Frey WH 2nd

更新日期：2009-07-01 00:00:00

abstract：:Methadyl acetate was metabolized by microsomal preparations of rat liver to yield nor-methadyl acetate and 6-(dimethylamino)-4,4-diphenyl-3-heptanol. The identification and separation of these three compounds was established by TLC, using iodoplatinate spray as a visualizing agent. ...

journal_title：Journal of pharmaceutical sciences

authors： Kochhar MM,Hamrick ME,Bavda LT

更新日期：1976-01-01 00:00:00

abstract：:The structural integrity and conformational stability of various IgG1-Fc proteins produced from the yeast Pichia pastoris with different glycosylation site occupancy (di-, mono-, and nonglycosylated) were determined. In addition, the physical stability profiles of three different forms of nonglycosylated Fc molecules ...

journal_title：Journal of pharmaceutical sciences

authors： Alsenaidy MA,Okbazghi SZ,Kim JH,Joshi SB,Middaugh CR,Tolbert TJ,Volkin DB

更新日期：2014-06-01 00:00:00

abstract：:The purpose of this study was to examine the role of multidrug resistance-associated protein-1 and -2 (Mrp1 and Mrp2) in the efflux transport of organic anions across the blood-cerebrospinal fluid (CSF) barrier. The CSF concentration of estradiol-17beta-glucuronide (E(2)17betaG) and 2,4-dinitrophenyl-S-glutathione (DN...

journal_title：Journal of pharmaceutical sciences

authors： Lee YJ,Kusuhara H,Sugiyama Y

更新日期：2004-01-01 00:00:00

abstract：:Anionic surfactants compromise skin's barrier function by damaging stratum corneum lipids and proteins. The objective of this study was to examine anionic surfactant-induced changes in the skin's polar and transcellular pathways and the resulting impact on surfactant penetration into the skin. Three anionic surfactant...

journal_title：Journal of pharmaceutical sciences

authors： Morris SAV,Ananthapadmanabhan KP,Kasting GB

更新日期：2019-11-01 00:00:00

abstract：:The stereoselective pharmacokinetics of suprofen enantiomers has been studied in humans by means of stable isotope-labeled pseudoracemate-diastereomer methodology. After a single oral dose of a near equimolar mixture of unlabeled-(R)-(-)- and [2H3]-(S)-(+)-suprofen [or unlabeled-(S)- and [2H3]-(R)-suprofen] to three h...

journal_title：Journal of pharmaceutical sciences

authors： Shinohara Y,Magara H,Baba S

更新日期：1991-11-01 00:00:00

abstract：:It was reported that wax matrix (WM) particles composed of low-melting-point microcrystalline wax showed unique release behaviors; the particles released only a small amount of the entrapped drug (non-diffusion-controlled release) at 37°C, whereas it showed comparatively fast drug release in a diffusion-controlled man...

journal_title：Journal of pharmaceutical sciences

authors： Matsumoto K,Kimura SI,Noguchi S,Itai S,Kondo H,Iwao Y

更新日期：2019-06-01 00:00:00

abstract：:A pharmacokinetic model that permits prediction of aqueous humor pilocarpine levels following topical application to rabbit eyes was developed. The model is able to account for changes in both instilled solution volume and drug concentration. The model, although simplified, relies mainly on experimentally verifiable a...

journal_title：Journal of pharmaceutical sciences

authors： Himmelstein KJ,Guvenir I,Patton TF

更新日期：1978-05-01 00:00:00

abstract：:A series of mono-, di-, and trimethylated derivatives of 4-chloro- and 4-methoxybenzanilide was synthesized and evaluated for anticonvulsant activity. This series was prepared in the course of studies designed to examine the relationship between anticonvulsant effects and benzamide structure. The compounds were tested...

journal_title：Journal of pharmaceutical sciences

authors： Clark CR,McMillian CL

更新日期：1990-03-01 00:00:00

abstract：:From a consideration of the basic processes involved in drug elimination, the fraction of drug cleared by the gut and by the liver were described as functions of availability and hepatic clearance. For a drug given orally, a plot of the fraction of drug cleared by the gut or liver against alpha, a proportionality cons...

journal_title：Journal of pharmaceutical sciences

authors： Minchin RF,Ilett KF

更新日期：1982-04-01 00:00:00

abstract：:In a continuing search for new biologically active agents derived from indolizine, 3-(2-aminoethyl)-2-methylindolizine, 3-(2-aminoethyl)-2-methyl-5,6,7,8-tetrahydroindolizine, and some mono- and di-N-substituted derivatives were prepared. Initial pharmacological screening showed that these compounds possess anti-5-hyd...

journal_title：Journal of pharmaceutical sciences

authors： Antonini I,Claudi F,Gulini U,Micossi L,Venturi F

更新日期：1979-03-01 00:00:00

abstract：:The affinity chromatographic technique was used to study the interaction of bovine serum albumin and salicylic acid at 3.3 +/- 1.1 degrees. Beaded agarose gel, on which the albumin was immobilized by covalent linkage, was packed in a column as an affinity adsorbent. Frontal analysis was performed on this column to eva...

journal_title：Journal of pharmaceutical sciences

authors： Nakano NI,Oshio T,Fujimoto Y,Amiya T

更新日期：1978-07-01 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 biphasic degradation of delta9-tetrahydrocannabinol (I), as monitored by flame-ionization GLC, produced delta8-tetrahydrocannabinol (II), cannabidiol (X), 9-hydroxyhexahydrocannabinol (VI), 9,10-dihydro-9-hydroxyisocannabidiol (VI), and and 6,12-dihydro-6-hydroxycannabidiol (VIII) in acidic solutions. Further iden...

journal_title：Journal of pharmaceutical sciences

authors： Garrett ER,Gouyette AJ,Roseboom H

更新日期：1978-01-01 00:00:00

abstract：:The intrinsic dissolution rate and solubility of carbamazepine was measured in aqueous solutions of sodium lauryl sulfate (SLS) prepared with two different grades of purity, 95 and 99%, and 95% SLS in 0.15 M NaCl to determine the effect of surface-active impurities and electrolytes. Four significant observations resul...

journal_title：Journal of pharmaceutical sciences

authors： Crison JR,Weiner ND,Amidon GL

更新日期：1997-03-01 00:00:00

abstract：:A novel method is described for the preparation of sterile and pyrogen-free submicron liposomes of narrow size distribution. The method is based on the formation of a homogeneous dispersion of lipids in water-soluble carrier materials. To obtain the lipid-containing solid dispersion, liposome-forming lipids and water-...

journal_title：Journal of pharmaceutical sciences

authors： Li C,Deng Y

更新日期：2004-06-01 00:00:00

abstract：:Phenylpropanolamine was determined by measuring its fluorescent fluorescamine derivative. The method is rapid, sensitive, and easily automated. Statistics are presented for an effervescent cold product, and recovery data are presented for other commercially available products. ...

journal_title：Journal of pharmaceutical sciences

authors： Shankle LL

更新日期：1978-11-01 00:00:00

abstract：:Owing to proliferation of antibiotic-resistant bacteria, the use of antibiotics for livestock growth promotion is banned in many countries and alternatives to in-feed antibiotics are needed. Cinnamon essential oil exhibits strong in vitro antibacterial activity; however, direct addition of essential oils to animal fee...

journal_title：Journal of pharmaceutical sciences

authors： Ma YH,Wang Q,Gong J,Wu XY

更新日期：2016-03-01 00:00:00

abstract：:Review of the current literature on racial differences in pharmacokinetics of drugs supports the premise that only pharmacokinetic processes which are biologically or biochemically mediated have the potential to exhibit differences between racial or ethnic groups. Thus, the pharmacokinetic factors which can be expecte...

journal_title：Journal of pharmaceutical sciences

authors： Johnson JA

更新日期：1997-12-01 00:00:00

abstract：:A new polymorphic form of Alprazolam (Xanax), 8-chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo-[4,3-alpha][1,4]benzodiazepine, C(17)H(13)ClN(4), has been investigated by means of X-ray powder diffraction (XRPD), single crystal X-ray diffraction, and differential scanning calorimetry (DSC). This polymorphic form (form III...

journal_title：Journal of pharmaceutical sciences

authors： de Armas HN,Peeters OM,Van den Mooter G,Blaton N

更新日期：2007-05-01 00:00:00

abstract：:The permeability coefficient, Kp, of pure unbranched alkanoic acids (C2-C7) applied to isolated porcine skin, reached a maximum in the solubility parameter (delta 2) range of 9.7-10 cal1 /2/cm3/2. When these and other penetrants were delivered from a solvent vehicle, the following linear relationships could be demonst...

journal_title：Journal of pharmaceutical sciences

authors： Liron Z,Cohen S

更新日期：1984-04-01 00:00:00

abstract：:Controlling residual solvent levels is a major concern in pharmaceutical freeze-drying from co-solvent systems. This review provides an overview of the factors influencing this process and estimates their potential to reduce residual solvents in freeze-dried products. Decreased solvent contents are potentially correla...

journal_title：Journal of pharmaceutical sciences

authors： Kunz C,Gieseler H

更新日期：2018-08-01 00:00:00

abstract：:Fluconazole concentrations in biological fluids were determined by high-performance gas chromatography. A simple extraction procedure with chloroform, under basic conditions and after the addition of UK-47,265 as the internal standard and with no evaporation stage, was carried out prior to analysis. A solid injector a...

journal_title：Journal of pharmaceutical sciences

authors： Debruyne D,Ryckelynck JP,Bigot MC,Moulin M

更新日期：1988-06-01 00:00:00

abstract：:Observed venous plasma concentrations of furosemide, propranolol, griseofulvin, and theophylline at 0.33 and 0.66 min after intravenous bolus injections to unanesthetized dogs were compared with those extrapolated using the instantaneous input hypothesis. At 0.33 min, extrapolated/observed plasma level ratios as high ...

journal_title：Journal of pharmaceutical sciences

authors： Chiou WL,Lam G,Chen ML,Lee MG

更新日期：1981-09-01 00:00:00

abstract：:High pressure liquid chromatography using reversed-phase and/or ion-pair techniques was used to optimize resolution of aspirin-containing muscle relaxant mixtures as well as other therapeutic agents commonly found in muscle relaxant-analgesic mixtures. The compounds were chromatographed on an octadecylsilane column us...

journal_title：Journal of pharmaceutical sciences

authors： Stewart JT,Honigberg IL,Coldren JW

更新日期：1979-01-01 00:00:00

abstract：:The objective of the present research was to investigate the stability of an amorphous drug, Delta(9)-tetrahydrocannabinol (THC) in polymer-based transmucosal systems. THC was incorporated in polyethylene oxide and hydroxypropylcellulose matrices by a hot-melt fabrication procedure, utilizing various processing aids. ...

journal_title：Journal of pharmaceutical sciences

authors： Munjal M,Stodghill SP,Elsohly MA,Repka MA

更新日期：2006-08-01 00:00:00

abstract：:The vaporization, fusion, and sublimation enthalpies of (R,S)- and (R)-flurbiprofen at T = 298.15 K are reported and compared with literature values when available. Correlation gas chromatography experiments were first performed to identify appropriate standards that could be used for materials containing a single flu...

journal_title：Journal of pharmaceutical sciences

authors： Umnahanant P,Hasty D,Chickos J

更新日期：2012-06-01 00:00:00

abstract：:A method is reported for studying the effects of several factors at room temperature on the oxygen permeability of soft gelatin capsule shell films. The method involves the use of a permeability cell assembly and the spectrophotometric determïnation of oxygen with an alkaline pyrogallic acid solution. Factors investig...

journal_title：Journal of pharmaceutical sciences

authors： Hom FS,Veresh SA,Ebert WR

更新日期：1975-05-01 00:00:00

abstract：:Bisphosphonates are widely used for the treatment of bone diseases, including hypercalcemia and osteoporosis. However, the bioavailability (BA) of orally administered bisphosphonates is low, at approximately 0.9%-1.8%. In addition, the oral administration of bisphosphonates is associated with mucosal damage, including...

journal_title：Journal of pharmaceutical sciences

authors： Katsumi H,Takashima M,Sano J,Nishiyama K,Kitamura N,Sakane T,Hibi T,Yamamoto A

更新日期：2011-09-01 00:00:00

abstract：:Previous studies from this laboratory suggested that a solution model (Flory-Huggins equation) modified by a free volume model (Vrentas equation) could satisfactorily describe water absorption into an amorphous solid composed of a sugar or a polymer. This paper has extended the studies of single solutes to binary mixt...

journal_title：Journal of pharmaceutical sciences

authors： Zhang J,Zografi G

更新日期：2001-09-01 00:00:00