Meropenem exists in equilibrium with a carbon dioxide adduct in bicarbonate solution.

abstract：:The crystal structure of zolpidem hemitartrate hemihydrate (I, Form E) has been solved from high-resolution laboratory powder diffraction data. It crystallizes in the orthorhombic P2(1)2(1)2(1) space group with a = 22.4664(6) A, b = 26.0420(7) A, and c = 7.4391(1) A. Protonation of zolpidem molecules could not be unam...

journal_title：Journal of pharmaceutical sciences

authors： Halasz I,Dinnebier RE

更新日期：2010-02-01 00:00:00

abstract：:Tissue damage caused by subcutaneous and intramuscular administration of three phenytoin prodrugs to rats was assessed. Since two of the prodrugs caused significant irritation, only 3-(hydroxymethyl)-5,5-diphenylhydantoin disodium phosphate ester might be useful as a nonirritant phenytoin prodrug suitable for parenter...

journal_title：Journal of pharmaceutical sciences

authors： Varia SA,Stella VJ

更新日期：1984-08-01 00:00:00

abstract：:The S6-(N-alkyl-N-alkoxycarbonyl)aminomethyl-6-MP (6-CARB-6-MP) prodrugs 5-20 were synthesized from the reaction of 6-MP with N-alkyl-N-alkyoxycarbonylaminomethyl chlorides (4) in dimethyl sulfoxide in overall yields of 5-62%, depending on the N-alkyl and the alkoxy groups involved. The derivatives were fully characte...

journal_title：Journal of pharmaceutical sciences

authors： Siver KG,Sloan KB

更新日期：1990-01-01 00:00:00

abstract：:The dissolution kinetics of theophylline monohydrate and anhydrous theophylline were investigated with a rotating-disk apparatus in buffer solutions at 298 K under sink conditions. The observed dissolution rate of theophylline monohydrate under various conditions agreed well with predictions based on the Extended Simu...

journal_title：Journal of pharmaceutical sciences

authors： de Smidt JH,Fokkens JG,Grijseels H,Crommelin DJ

更新日期：1986-05-01 00:00:00

abstract：:Delayed absorption of nifedipine when administered as a 20 mg immediate release soft gelatin capsule to fasted volunteers has been reported. Physiologically based pharmacokinetic (PBPK) modeling and in vitro dissolution data were used to explore our hypothesis that at high doses of nifedipine it precipitates in the st...

journal_title：Journal of pharmaceutical sciences

authors： Thelen K,Jantratid E,Dressman JB,Lippert J,Willmann S

更新日期：2010-06-01 00:00:00

abstract：:The aim of this study is to explore hot melt extrusion (HME) as a solvent-free drug loading technique for preparation of stable amorphous solid dispersions using mesoporous silica (PSi). Ibuprofen and carvedilol were used as poorly soluble active pharmaceutical ingredients (APIs). Due to the high friction of an API:PS...

journal_title：Journal of pharmaceutical sciences

authors： Genina N,Hadi B,Löbmann K

更新日期：2018-01-01 00:00:00

abstract：:The peptide hormone calcitonin (CT) is a potent drug for the therapy of different bone diseases. Salmon CT (sCT) is reported to be more active than human CT (hCT). Human CT, but not sCT, has a strong tendency to aggregate and fibrillate in aqueous solutions. Recent investigations of the fibrillation mechanisms contrib...

journal_title：Journal of pharmaceutical sciences

authors： Cudd A,Arvinte T,Das RE,Chinni C,MacIntyre I

更新日期：1995-06-01 00:00:00

abstract：:Numerous case reports have documented that phenylpropanolamine (PPA) stimulates the central nervous system with symptoms ranging from anxiety and hallucinations to grand mal seizures produced by overdoses. Most of these reports have occurred following concomitant use of caffeine which in high doses is known to cause s...

journal_title：Journal of pharmaceutical sciences

authors： Walker JS

更新日期：1989-12-01 00:00:00

abstract：:AZD1175 and AZD2207 are 2 highly lipophilic compounds with a significant risk of not achieving therapeutic plasma concentrations due to solubility-limited absorption. The compounds have the same molecular weight and minimal structural differences. The aim of the present work was to investigate whether salts could be a...

journal_title：Journal of pharmaceutical sciences

authors： Tannergren C,Karlsson E,Sigfridsson K,Lindfors L,Ku A,Polentarutti B,Carlert S

更新日期：2016-11-01 00:00:00

abstract：:The transport rate constant of a drug partitioned in a two-phase system from an aqueous to an organic phase (k1obs) and vice versa (k2obs) is a function of the partition coefficient P and of a solvent system-dependent parameter beta. Drug transport is shown to be independent of molecular structure for a number of arbi...

journal_title：Journal of pharmaceutical sciences

authors： van de Waterbeemd H,van Bakel P,Jansen A

更新日期：1981-09-01 00:00:00

abstract：:The crystal and molecular structures of 6-methylmercaptopurine trihydrate and of azathioprine dihydrate were determined by the use of three-dimensional, X-ray, diffractometer data and were refined by least squares. Both molecules crystallize in the N(9)-H tautomer form, in contrast to the N(7)-H tautomer form found in...

journal_title：Journal of pharmaceutical sciences

authors： Cook WJ,Bugg CE

更新日期：1975-02-01 00:00:00

abstract：:In vitro iontophoretic administration of drugs through a microporous polyolefin membrane with hydrophilic urethane polymerfilled pores was done for the ionized drugs dexamethasone sodium phosphate, hydrocortisone sodium phosphate, and prednisolone sodium succinate, and for a nonionizable drug cortisone acetate. Curren...

journal_title：Journal of pharmaceutical sciences

authors： Tu YH,Allen LV Jr

更新日期：1989-03-01 00:00:00

abstract：:In the present work, authors produced tablets of anhydrous sodium naproxen by wet granulation using a high-shear mixer-granulator. Drug hydrated to the tetrahydrated form, as observed by X-ray powder diffractometry. After wet granulation, authors then performed two different drying procedures, obtaining granules of di...

journal_title：Journal of pharmaceutical sciences

authors： Di Martino P,Malaj L,Censi R,Martelli S

更新日期：2008-12-01 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：:Nosocomial diarrhea and pseudomembranous colitis causing toxins A and B from Clostridium difficile were studied at pH 5-8 and over the temperature range of 10-85 degrees C. The proteins were crosslinked with formaldehyde to inactivate them to toxoid forms and permit their use as vaccines. Structural changes and aggreg...

journal_title：Journal of pharmaceutical sciences

authors： Salnikova MS,Joshi SB,Rytting JH,Warny M,Middaugh CR

更新日期：2008-09-01 00:00:00

abstract：:Both bovine enamel and hydroxyapatite pellets were remineralized in a fluoride-containing remineralization solution after prior demineralization for various lengths of time. In both the enamel and pellet systems, the degree of remineralization attainable was directly related to the extent of prior demineralization, al...

journal_title：Journal of pharmaceutical sciences

authors： Yonese M,Fox JL,Nambu N,Hefferren JJ,Higuchi WI

更新日期：1981-08-01 00:00:00

abstract：:A series of gem-cichlorocyclopropyl and cyclopropyl analogs of stilbene congeners was synthesized and examined for estrogenic and antiestrogenic activity using the uterotropic assay in the immature mouse. The relative receptor affinity in vitro was determined by measuring [3H]estradiol displacement from the rat uterin...

journal_title：Journal of pharmaceutical sciences

authors： Stobaugh JF,Magarian RA,Pento JT

更新日期：1982-10-01 00:00:00

abstract：:Disintegration performance was measured by analysing both water ingress and tablet swelling of pure microcrystalline cellulose (MCC) and in mixture with croscarmellose sodium using terahertz pulsed imaging (TPI). Tablets made from pure MCC with porosities of 10% and 15% showed similar swelling and transport kinetics: ...

journal_title：Journal of pharmaceutical sciences

authors： Yassin S,Goodwin DJ,Anderson A,Sibik J,Ian Wilson D,Gladden LF,Axel Zeitler J

更新日期：2015-10-01 00:00:00

abstract：:A procedure for the determination of mianserin, desmethylmianserin, and 8-hydroxymianserin in plasma at therapeutic concentrations by liquid chromatography with electrochemical detection is described. Following a multiple-step extraction from alkaline plasma into methyl-tert-butyl ether, the reconstituted extract was ...

journal_title：Journal of pharmaceutical sciences

authors： Suckow RF,Cooper TB,Quitkin FM,Stewart JW

更新日期：1982-08-01 00:00:00

abstract：:A rapid solubility-screening assay was developed with a focus on Biopharmaceutic Classification Scheme (BCS) class II drug solubility in animal and simulated human gastrointestinal (GI) fluids. The assay enables biologically promising drug leads to be evaluated for solubility limitations earlier in the drug developmen...

journal_title：Journal of pharmaceutical sciences

authors： Guo J,Elzinga PA,Hageman MJ,Herron JN

更新日期：2008-04-01 00:00:00

abstract：:The intrinsic factor-mediated binding of cyanocobalamin to cholestyramine was studied in vitro under varying conditions of pH, added electrolyte, and bile salt. The intrinsic factor-cyanocobalamin complex was adsorbed strongly by the resin at pH 3 in the presence of neutral salt and low concentrations of glycocholic a...

journal_title：Journal of pharmaceutical sciences

authors： Andersen KJ,Schjønsby H

更新日期：1978-11-01 00:00:00

abstract：:The molecular connectivity indexes of various aliphatic alcohols, ketones, ethers, and esters were used to describe structural features influencing chromatographic retention indexes. Good correlations were obtained within chemical classes for a particular stationary phase. ...

journal_title：Journal of pharmaceutical sciences

authors： Kier LB,Hall LH

更新日期：1979-01-01 00:00:00

abstract：:The trichloroacetyl carbamates of 38 corticosteroids and chemically related compounds were prepared, and their NMR spectra in deuterochloroform were obtained. The effects of the introduction of a number of functional groups on the chemical shift of the carbamate proton signals were determined. ...

journal_title：Journal of pharmaceutical sciences

authors： Lanouette M,Legault D,Lodge BA

更新日期：1976-08-01 00:00:00

abstract：:To relate the reported positive effect of food on the oral bioavailability of abiraterone to the intraluminal behavior of abiraterone acetate, an in vivo experiment was performed, in which duodenal fluids and plasma samples were collected from healthy volunteers after the administration of abiraterone acetate in faste...

journal_title：Journal of pharmaceutical sciences

authors： Geboers S,Stappaerts J,Mols R,Snoeys J,Tack J,Annaert P,Augustijns P

更新日期：2016-09-01 00:00:00

abstract：:Scale up of pan coating process is of high importance to the pharmaceutical and food industry. The number of process variables and their interdependence in a pan coating process can make it a rather complex scale-up problem. This review discusses breaking down the coating process variables into three main categories: ...

journal_title：Journal of pharmaceutical sciences

authors： Agrawal AM,Pandey P

更新日期：2015-11-01 00:00:00

abstract：:The association efficiency of oxytetracycline (OTC) to pharmaceutical available, ionic oil-in-water nanoemulsions is studied. Theoretical mathematical developments allowed us to differentiate by diafiltration (DF) between thermodynamically and kinetically controlled binding of the drug to the nanoemulsions, and relate...

journal_title：Journal of pharmaceutical sciences

authors： Orellana SL,Torres-Gallegos C,Araya-Hermosilla R,Oyarzun-Ampuero F,Moreno-Villoslada I

更新日期：2015-03-01 00:00:00

abstract：:The estimates of infinity values obtained using Prony's method are shown to be subject to significant error arising from small errors in the assigned sample times. The error of the estimate may be reduced by increasing the time interval between samples. ...

journal_title：Journal of pharmaceutical sciences

authors： Newburger J,Stavchansky S,Pearlman RS

更新日期：1980-10-01 00:00:00

abstract：:Injectable microcapsules containing 75% (w/w) cyclazocine, a narcotic antagonist, were prepared with dl-poly(lactic acid) as the coating material. Capsule fractions falling between 105 and 295 mum released about 90% of their cyclazocine in 8 days of rotating-bottle extraction at 37 degrees in pH 7.4 phosphate buffer. ...

journal_title：Journal of pharmaceutical sciences

authors： Mason N,Thies C,Cicero TJ

更新日期：1976-06-01 00:00:00

abstract：:To explore the possibility of cyclodextrin click clusters (CCCs) as a new cyclodextrin-based excipient, we prepared three different CCCs; heptakis{6-(4-hydroxymethyl-1H-[1,2,3]triazol-1-yl)-6-deoxy}-β-cyclodextrin (HT-β-CD), heptakis{6-(4-hydroxymethyl-1H-[1,2,3]triazol-1-yl)-6-deoxy}{2,3-di-O-methyl}-β-cyclodextrin (...

journal_title：Journal of pharmaceutical sciences

authors： Le HT,Jeon HM,Lim CW,Kim TW

更新日期：2014-10-01 00:00:00

abstract：:Accurate prediction of target occupancy facilitates central nervous system drug development. In this review, we discuss the predictability of serotonin transporter (SERT) occupancy in human brain estimated from in vitro Ki values for human SERT and plasma concentrations of unbound drug (Cu,plasma), as well as the impa...

journal_title：Journal of pharmaceutical sciences

authors： Yahata M,Chiba K,Watanabe T,Sugiyama Y

更新日期：2017-09-01 00:00:00