abstract：:A series of 1-(substituted benzyl)-3,4,5,6-tetrahydro-2(1H)-pyrimidones was synthesized primarily by catalytic hydrogenation of the corresponding 1-(substituted benzyl)-2(1H)-pyrimidone. The pharmacological evaluation of these compounds in mice revealed a unique profile that included evidence of CNS stimulation and de...

journal_title：Journal of pharmaceutical sciences

authors： Ellis KO,Schwan TJ,Wessels FL,Miles NJ

更新日期：1980-10-01 00:00:00

abstract：:Eight analogs of the fentanyl-type analgesics, in which the piperidine ring is restricted into a boat conformation, were evaluated for analgesic activity. All analogs were less active than fentanyl, but interesting conformational and structural relationships were observed. Results of the study are discussed. ...

journal_title：Journal of pharmaceutical sciences

authors： Borne RF,Law SJ,Kapeghian JC,Masten LW

更新日期：1980-09-01 00:00:00

abstract：:Acetylcarnitine, a naturally occurring compound found in high concentration in heart and skeletal muscle of vertebrates, bears structural resemblance to acetylcholine, and studies have shown that it has slight cholinergic properties. Acetylcarnitine was subjected to conformational analysis by extended Hückel theory (E...

journal_title：Journal of pharmaceutical sciences

authors： Reed KW,Murray WJ,Roche EB

更新日期：1980-09-01 00:00:00

abstract：:N-Acetyl-DL-penicillamine (IIIb), a structural analog of N-acetyl-L-cysteine (IIIa), did not protect mice from lethal doses of acetaminophen (I), whereas IIIa offered protection. This lack of efficacy of IIIb probably is due to the decreased nucleophilicity of its sulfhydryl group compared to that of IIIa, the probabl...

journal_title：Journal of pharmaceutical sciences

authors： Zera RT,Nagasawa HT

更新日期：1980-09-01 00:00:00

abstract：:Ascorbic acid (100 mg/ml) and sodium bisulfite (0.5 and 20 mg/ml) prevented more than 10% oxidation of apomorphine hydrochloride in water maintained at room temperature over 1-3 days. Refrigeration at 5 degrees prevented oxidation of apomorphine hydrochloride in aqueous solutions for 1 week. Neither ascorbic acid nor ...

journal_title：Journal of pharmaceutical sciences

authors： Wilcox RE,Humphrey DW,Riffee WH,Smith RV

更新日期：1980-08-01 00:00:00

abstract：:The O-trifluoroacetyl and N,O-trifluoroacetyl derivatives of a series of aporphine and noraporphine alkaloids were prepared, and their GLC and mass spectrometric characteristics were determined. The positional isomers apocodeine and isoapocodeine were resolved chromatographically as their trifluoroacetyl derivatives, ...

journal_title：Journal of pharmaceutical sciences

authors： Green JF,Jham GN,Neumeyer JL,Vouros P

更新日期：1980-08-01 00:00:00

abstract：:p-Bromospiperone was prepared from the reaction of spiperone with bromine. It was tested for dopamine receptor binding affinity in vitro and its ability to stimulate prolactin secretion in vivo. The results indicate no significant change of biological activities due to the bromination of spiperone. ...

journal_title：Journal of pharmaceutical sciences

authors： Huang CC,Friedman AM,So R,Simonovic M,Meltzer HY

更新日期：1980-08-01 00:00:00

abstract：:The solubility of ergotamine tartrate in aqueous solutions of tartaric acid, citric acid, hydrochloric acid, and caffeine and the dissolution rate of ergotamine tartrate in aqueous mixtures containing hydrochloric acid, caffeine, citric acid, or sodium acetate were studied. The Noyes-Whitney model of dissolution is us...

journal_title：Journal of pharmaceutical sciences

authors： Anderson JR,Pitman IH

更新日期：1980-07-01 00:00:00

abstract：:An in vitro technique was developed to characterize the intermittent flume patterns associated with the short bursts of metered-dose aerosols. Two orthogonal video images are utilized to describe the complex shape and direction of the flume pattern. This technique facilitates the evaluation of components manufactured ...

journal_title：Journal of pharmaceutical sciences

authors： Miszuk S,Gupta BM,Chen FC,Clawans C,Knapp JZ

更新日期：1980-06-01 00:00:00

abstract：:Deiodination of diatrizoic acid, an anionic radiopaque, was found to be catalyzed by Cu(II). Through a detailed study of o-iodobenzoic acid, a model compound, the copper-catalyzed SN1 mechanism was established based on observations of common ion, salt, and pH effects. Meta- and para-iodobenzoic acids were unreactive. ...

journal_title：Journal of pharmaceutical sciences

authors： Wang YC

更新日期：1980-06-01 00:00:00

abstract：:The application of direct zero-order UV spectrophotometric and graphical or derivative background correction methods to selected pharmaceutical preparations shows their relative advantages in different situations. The assay of the active components in a changeable matrix is a problem with formulations having a limited...

journal_title：Journal of pharmaceutical sciences

authors： Traveset J,Such V,Gonzalo R,Gelpi E

更新日期：1980-06-01 00:00:00

abstract：:Hydrastine, canadine, and berberine were determined by the acid-dye technique. At pH 5.6, both the tertiary and the quaternary hydrastis alkaloids formed ion-pairs with bromcresol purple. The liberated hydrastine and canadine from the alkaloid-dye complexes were determined spectrophotometrically in the presence of ber...

journal_title：Journal of pharmaceutical sciences

authors： El-Masry S,Korany MA,Abou-Donia AH

更新日期：1980-05-01 00:00:00

abstract：:A procedure is described for the analysis of urushiol content of pharmaceutical preparations containing extracts of poison ivy (Toxicodendron radicans) and poison oak (T. diversilobum) in vegetable oils. The procedure involves extraction of the urushiols from the oily solutions using 90% methanol in water followed by ...

journal_title：Journal of pharmaceutical sciences

authors： Elsohly MA,Turner CE

更新日期：1980-05-01 00:00:00

abstract：:A quantitative high-pressure liquid chromatographic method, using a reversed-phase column coupled to a fluorescence detector, was developed to determine salicylic acid in bulk aspirin and plain and buffered aspirin tablets. The aspirin was dissolved, filtered, and injected into the chromatograph; the fluorescence of t...

journal_title：Journal of pharmaceutical sciences

authors： Kirchhoefer RD,Juhl WE

更新日期：1980-05-01 00:00:00

abstract：:The capacity factors of several penicillins and cephalosporins, as well as those of 7-aminocephalosporanic acid, 6-aminopenicillanic acid, and 7-aminodeacetoxycephalosporanic acid, were determined at pH 2.5-7.5 with different methanol concentrations in the mobile phase. The influence of ionic strength on activity fact...

journal_title：Journal of pharmaceutical sciences

authors： Salto F,Prieto JG,Alemany MT

更新日期：1980-05-01 00:00:00

abstract：:An electron-capture GLC method to measure nofedone in human serum was developed. A homolog of nofedone was added to the serum as an internal standard before the sample was alkalinized with pH 9.5 phosphate buffer and extracted with ethylene dichloride containing 0.5% isopentyl alcohol. This organic phase was extracted...

journal_title：Journal of pharmaceutical sciences

authors： Heusse D,Populaire P,Renard A,Pasquier P,Gregoire J

更新日期：1980-05-01 00:00:00

abstract：:Two previously reported but unidentified phenylburazone degradation products were isolated from a tablet that was stored at 60 degrees for 203 days. The compounds, alpha-(N-phenylcarbamoyl)-N-caproylhydrazobenzene and alpha-hydroxy-alpha-(N-phenylcarbamoyl)-N-caproylhydrazobenzene, were isolated by chromatography, ide...

journal_title：Journal of pharmaceutical sciences

authors： Matsui F,Robertson DL,Poirier MA,Lovering EG

更新日期：1980-04-01 00:00:00

abstract：:Solubilities in isoctane and water were determined for several C1-phenolic esters of prostaglandin F2 alpha and prostaglandin E2 and acetates having the same phenol moiety. Linear free energy relationships for solubility among the series were observed with slopes of approximately 1. These results suggest that the cont...

journal_title：Journal of pharmaceutical sciences

authors： Anderson BD,Conradi RA

更新日期：1980-04-01 00:00:00

abstract：:The release through silicone rubber membranes of benzocaine suspended in carbomer hydrogels containing different concentrations of low molecular weight polysols (ethylene glycol, propylene glycol, glycerol, and sorbitol) was studied to establish general principles and procedures for control of the effects on percutane...

journal_title：Journal of pharmaceutical sciences

authors： Di Colo G,Carelli V,Giannaccini B,Serafini MF,Bottari F

更新日期：1980-04-01 00:00:00

abstract：:The adsorption of cimetidine on selected pharmaceuticals including kaolin, activated charcoal, talc, and nonsystemic antacids was determined at pH 5.0 and 25 degrees. The Langmuir and Freundlich adsorption isotherms showed that cimetidine adsorption was significant with activated charcoal, kaolin, talc, and magnesium ...

journal_title：Journal of pharmaceutical sciences

authors： Ganjian F,Cutie AJ,Jochsberger T

更新日期：1980-03-01 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：:A colorimetric determination of chlorhexidine is described. The method is based on the formation of a yellow complex between the drug and bromcresol green. The absorption peak of this complex, extracted by chloroform, is at 410 nm, and linear response is obtained from 2.5 to 30 micrograms of chlorhexidine/ml. The accu...

journal_title：Journal of pharmaceutical sciences

authors： Andermann G,Buhler MO,Erhart M

更新日期：1980-02-01 00:00:00

abstract：:A rapid, simple, and accurate high-performance liquid chromatographic procedure using an amino-bonded microparticulate column is reported for the determination of chlorpromazine hydrochloride (I) and its two oxidation products, the sulfoxide (II) and the sulfone (III), in commercially available pharmaceutical dosage p...

journal_title：Journal of pharmaceutical sciences

authors： Takahashi DM

更新日期：1980-02-01 00:00:00

abstract：:A rapid, precise, and accurate high-performance liquid chromatographic procedure is presented for the stimultaneous determination of amitriptyline hydrochloride and chlordiazepoxide in two-component tablet formulations. The impurities and decomposition products of both components were separated, making the determinati...

journal_title：Journal of pharmaceutical sciences

authors： Burke D,Sokoloff H

更新日期：1980-02-01 00:00:00

abstract：:Chromatographic gel filtration matrixes used in various separation techniques are subject to microbial contamination. The need for a microbe-free column is critical when preparing materials that require a low or zero microbial count. This report proposes two alternative washing systems: 0.02 N HCl containing 0.81% NaC...

journal_title：Journal of pharmaceutical sciences

authors： Wen LF,Bohannon T,Crabb A,Mamaril F

更新日期：1980-02-01 00:00:00

abstract：:A sensitive and specific method for the determination of chlorambucil and its metabolite in biological fluids is reported. The method is based on selected-ion monitoring detection following simple extraction of the parent compound, its metabolite, and an internal standard (chlorambucil-d8) from plasma and urine sample...

journal_title：Journal of pharmaceutical sciences

authors： Chang SY,Larcom BJ,Alberts DS,Larsen B,Walson PD,Sipes IG

更新日期：1980-01-01 00:00:00

abstract：:The metabolism of tocainide, an experimental antiarrhythmic drug, was studied in humans. Urinary excretion of unchanged drug was 28-55% in 24 hr after oral dosing. Urine hydrolysis with hydrochloric acid or beta-glucuronidase increased tocainide recovery to 55-79%. Saccharo-1,4-lactone inhibited the beta-glucuronidase...

journal_title：Journal of pharmaceutical sciences

authors： Elvin AT,Keenaghan JB,Byrnes EW,Tenthorey PA,McMaster PD,Takman BH,Lalka D,Manion CV,Baer DT,Wolshin EM,Meyer MB,Ronfeld RA

更新日期：1980-01-01 00:00:00

abstract：:A fluorescence method is presented for the determination of nitrofurantoin based on conversion of the drug to a fluorescent substance. The method requires 0.1-0.5 ml of plasma or diluted urine and is 10 times more sensitive than the commonly used colorimetric method. ...

journal_title：Journal of pharmaceutical sciences

authors： Watari N,Funaki T,Kaneniwa N

更新日期：1980-01-01 00:00:00

abstract：:A GLC method was developed for the determination of ethylene oxide and its two reaction products, ethylene chlorohydrin and ethylene glycol, in ophthalmic solutions at the levels recently proposed by the Food and Drug Administration. The method requires no extractions, sample preparations, or elaborate trapping and co...

journal_title：Journal of pharmaceutical sciences

authors： Manius GJ

更新日期：1979-12-01 00:00:00

abstract：:Hydrogen triiodide adducts were prepared from N,N-dimethylacetamide, N-alkylpyrrolidone derivatives, and polyvinylpyrrolidone, and their structures were investigated by IR spectra and X-ray structure analyses and compared with the structure of povidone-iodine USP. The results suggest that the iodine in povidone-iodine...

journal_title：Journal of pharmaceutical sciences

authors： Schenck HU,Simak P,Haedicke E

更新日期：1979-12-01 00:00:00

abstract：:A high-performance liquid chromatographic method for the determination of (Z)- and (E)-doxepin hydrochloride isomers was developed. The analysis employs a column packed with spherical silica microparticles (5-6 mum), and a mobile phase of acetonitrile-chloroform-diethylamine (750:250:0.2) permits baseline resolution a...

journal_title：Journal of pharmaceutical sciences

authors： Whall TJ,Dokladalova J

更新日期：1979-11-01 00:00:00

abstract：:The effect of pretreating callus membranes with dimethyl sulfoxide, dimethylacetamide, dimethylformamide, formamide, dioxane, or methyl orthoformate on sarin permeability was studied at three temperatures to determine the activation energy for transport. In addition, the effect of membrane pretreatment on permeability...

journal_title：Journal of pharmaceutical sciences

authors： Matheson LE,Wurster DE,Ostrenga JA

更新日期：1979-11-01 00:00:00

abstract：:A physical model approach to the topical delivery of a vidarabine ester prodrug was investigated. It involved modeling, theoretical simulations, experimental method development for factoring and quantifying parameters, and, finally, employment of the deduced parameters to determine the steady-state species fluxes and ...

journal_title：Journal of pharmaceutical sciences

authors： Yu CD,Fox JL,Ho NF,Higuchi WI

更新日期：1979-11-01 00:00:00

abstract：:A high-pressure liquid chromatographic procedure for the accurate determination of disopyramide and its chief metabolite in plasma is presented. The method is suitable for monitoring patients receiving disopyramide therapy. A reversed-phase cyanopropylsilane column is utilized with a mobile phase of 50% acetonitrile a...

journal_title：Journal of pharmaceutical sciences

authors： Nygard G,Shelver WH,Khalil SK

更新日期：1979-10-01 00:00:00

abstract：:A procedure was developed for the separation and selective quantitative determination of the (S)(+)- and (R)(-)-enantiomers of the racemic anti-inflammatory drug carprofen as their diastereomeric l-(-)-alpha-methylbenzylamides. These derivatives are obtained in equivalent yields by reacint purified 14C-carprofen from ...

journal_title：Journal of pharmaceutical sciences

authors： Kemmerer JM,Rubio FA,McClain RM,Koechlin BA

更新日期：1979-10-01 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：:Plasma binding of chlordiazepoxide, diazepam, loraxepam, and oxazepam was determined by equilibrium dialysis in 20 male, healthy volunteers, 25-86 years old. A wide range of binding was observed, with the free fraction varying twofold for lorazepam, fourfold for chlordiazepoxide and diazepam, and over 20-fold for oxa...

journal_title：Journal of pharmaceutical sciences

authors： Johnson RF,Schenker S,Roberts RK,Desmond PV,Wilkinson GR

更新日期：1979-10-01 00:00:00

abstract：:In phenobarbital measurement by GLC with the flash-methylation technique, using trimethylanilinium hydroxide as a methylating reagent, a small amount of water decomposed phenobarbital and interfered with the quantitative analysis. Thus, both the sample and the methylating reagent must be sufficiently dehydrated to att...

journal_title：Journal of pharmaceutical sciences

authors： Kurata K,Takeuchi M,Yoshida K

更新日期：1979-09-01 00:00:00

abstract：:Acute experiments were performed on overnight fasted chloralose-urethan anesthetized dogs, cats, rabbits, and rats. Under these conditions, somatostatin practically abolished gastric contractions and decreased GI tonus in all species examined. The canine duodenum, jejunum, and ileum exhibited only a contractile respon...

journal_title：Journal of pharmaceutical sciences

authors： Tansy MF,Martin JS,Landin WE,Kendall FM

更新日期：1979-09-01 00:00:00

abstract：:The effects of aspirin on 14C-pirprofen disposition in the rat were studied. An oral 60-mg/kg dose of aspirin significantly reduced plasma radioactivity during the 1--8-hr interval after an intravenous 5-mg/kg injection of 14C-pirprofen. The aspirin-treated group had only 69% as much area under the radioactivity curve...

journal_title：Journal of pharmaceutical sciences

authors： Thompson TA,Borman CH,Goodblatt RS,Roth WJ 3rd

更新日期：1979-08-01 00:00:00