abstract：:Eighteen healthy adult volunteers completed an open-label, four-way crossover study designed to determine the bioequivalency of 160-mg cibenzoline [2-(2,2-diphenylcyclopropyl)-4,5-dihydro-1H-imidazole] capsules and tablets, their relative bioavailability compared with an oral solution of the drug, as well as the absol...

journal_title：Journal of pharmaceutical sciences

authors： Massarella J,Silvestri T,Lin A

更新日期：1986-09-01 00:00:00

abstract：:In this paper we describe the synthesis and characterization of magnetic microcapsules, intended for use in vivo, and which contain polyethyleneimine nucleophilic targets capable of trapping electrophilic carcinogens. The microcapsules, 15-50 microns in diameter, consist of a semipermeable cross-linked nylon membrane ...

journal_title：Journal of pharmaceutical sciences

authors： Povey AC,Bartsch H,Nixon JR,O'Neill IK

更新日期：1986-09-01 00:00:00

abstract：:Various novel diesters of pilocarpic acid were synthesized and evaluated as prodrug forms for pilocarpine with the aim of improving the ocular delivery characteristics of the drug. The pilocarpic acid monoesters previously studied cyclized spontaneously to pilocarpine in aqueous solution and although they showed enhan...

journal_title：Journal of pharmaceutical sciences

authors： Bundgaard H,Falch E,Larsen C,Mosher GL,Mikkelson TJ

更新日期：1986-08-01 00:00:00

abstract：:The pharmacokinetic profiles of cimetropium bromide, after either intravenous injection of 10 mg or oral ingestion of 200 mg, were determined in eight healthy volunteers. After intravenous administration, the plasma levels and urinary excretion indicated that the drug is distributed and eliminated at a rapid rate (ter...

journal_title：Journal of pharmaceutical sciences

authors： Imbimbo BP,Daniotti S,Vidi A,Foschi D,Saporiti F,Ferrante L

更新日期：1986-07-01 00:00:00

abstract：:A simple enzyme immunoassay for the determination of captopril was developed. A specific antibody for captopril was produced in rabbits that were immunized with a hapten-bovine immunoglobulin G conjugate, which was prepared by using 4-(maleimidomethyl)cyclohexane carboxylic acid as a spacer group. The limit of detecti...

journal_title：Journal of pharmaceutical sciences

authors： Kinoshita H,Nakamaru R,Tanaka S,Tohira Y,Sawada M

更新日期：1986-07-01 00:00:00

abstract：:High yields of potential glycol metabolites of p-synephrine, epinephrine, octopamine, and normacromerine can be obtained from the readily available monosubstituted and disubstituted acetophenones. The general procedure involves alpha-bromination followed by displacement with acetate ion and reduction with lithium alum...

journal_title：Journal of pharmaceutical sciences

authors： Holshouser MH,Kolb M

更新日期：1986-06-01 00:00:00

abstract：:Aqueous solutions of several ionizable substances were stored in plastic infusion bags and the sorption of the substances monitored with time. The substances used were p-nitrophenol, p-toluidine, warfarin sodium [3-(alpha-acetonylbenzyl)-4-hydroxycoumarin sodium salt] and trifluoperazine hydrochloride (10-[3-(4-methyl...

journal_title：Journal of pharmaceutical sciences

authors： Kowaluk EA,Roberts MS,Polack AE

更新日期：1986-06-01 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：:The single-dose pharmacokinetics and bioavailability of three ketoconazole formulations were evaluated using HPLC in five healthy human volunteers and six male mongrel dogs. The human volunteers received 400 mg po of ketoconazole as tablet (Ktab) and solution (Ksol) formulations. The dogs received 400 mg po of Ktab an...

journal_title：Journal of pharmaceutical sciences

authors： Baxter JG,Brass C,Schentag JJ,Slaughter RL

更新日期：1986-05-01 00:00:00

abstract：:Sodium salicylate improves the rectal absorption of drugs which exhibit molecular self-association; it is suggested that salicylate may improve drug bioavailability by altering the drug self-association pattern. Methylene blue was chosen as a model molecule for investigating the interference of salicylate with drugs u...

journal_title：Journal of pharmaceutical sciences

authors： Touitou E,Fisher P

更新日期：1986-04-01 00:00:00

abstract：:A randomized, two-way, crossover study was performed on 18 normal volunteers to assess the influence of food on the bioavailability of lisinopril, (1-[N2-[(S)-1-carboxy-3-phenylpropyl]-L-lysyl]-L-proline), a long-acting nonsulfhydryl angiotensin converting enzyme inhibitor. A single, 20-mg oral dose of lisinopril was ...

journal_title：Journal of pharmaceutical sciences

authors： Mojaverian P,Rocci ML Jr,Vlasses PH,Hoholick C,Clementi RA,Ferguson RK

更新日期：1986-04-01 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：:Allopurinol exhibits good bioavailability (78-90%) after administration of oral dosage forms to humans and rabbits; however, it is not absorbed rectally from any of the dosage forms to any significant extent. Oral administration of allopurinol in a polyethylene glycol suspension, to which allopurinol may be reversibly...

journal_title：Journal of pharmaceutical sciences

authors： Patel VS,Kramer WG

更新日期：1986-03-01 00:00:00

abstract：:The pKa values of benzoic acid, p-methylbenzoic, and p-aminobenzoic acid (PABA) were determined by potentiometric titration in mixtures of 0-0.5 volume fractions of various cosolvents and water. The differences between the aqueous and semiaqueous pKa values were similar for the three solutes at a particular cosolvent-...

journal_title：Journal of pharmaceutical sciences

authors： Rubino JT,Berryhill WS

更新日期：1986-02-01 00:00:00

abstract：:In an attempt to explain the triamterene stone diathesis, we studied the excretion and solubility of triamterene, 1, and its metabolite, the sulfate ester of the hydroxy derivative of triamterene, 3. The urinary excretion pattern and metabolism in stone formers was the same as in other chronic users of triamterene or ...

journal_title：Journal of pharmaceutical sciences

authors： Sörgel F,Ettinger B,Benet LZ

更新日期：1986-02-01 00:00:00

abstract：:A potentiometric study of lithium complexation with tyramine, dopamine, norepinephrine, and 5-hydroxytryptamine was undertaken using monovalent cationic selective and pH glass electrodes. The conditional stability constants for the lithium catecholamine complexes were calculated for a range of pH values from direct po...

journal_title：Journal of pharmaceutical sciences

authors： Sandmann BJ,Luk HT

更新日期：1986-01-01 00:00:00

abstract：:Solubility values of a selected group of nonsteroidal anti-inflammatory drugs have been determined in water and 1-octanol as a function of temperature. Thermodynamic functions of dissolution and partition have been calculated and discussed with respect to various physical parameters of each solute and the two solvents...

journal_title：Journal of pharmaceutical sciences

authors： Fini A,Laus M,Orienti I,Zecchi V

更新日期：1986-01-01 00:00:00

abstract：:It is shown, using oxalic acid dihydrate as a model, that nonisothermal recrystallization of powders gives rise to particle size distributions which approach log-normality in many cases. The number of particles formed is, primarily, a function of the nucleation rate constants and the particle size distribution, i.e., ...

journal_title：Journal of pharmaceutical sciences

authors： Carstensen JT,Rodriguez-Hornedo N

更新日期：1985-12-01 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 distribution conditions in oil-water emulsions prepared by emulsifying a 1:1 eutectic mixture of lidocaine and prilocaine with a nonionic surfactant in water were studied by membrane and gel filtration methods. In this system, the local anesthetics are considered to be freely dissolved, surfactant solubilized, and...

journal_title：Journal of pharmaceutical sciences

authors： Nyqvist-Mayer AA,Brodin AF,Frank SG

更新日期：1985-11-01 00:00:00

abstract：:1-[4-(2-Cyclopropylmethoxyethyl)phenoxy]-3-[1-p-(bromoacetamidophe nyl) -2-methyl-2-propylamine]-2-propranol (8), which is a derivative of the beta 1-adrenergic agent betaxolol, was synthesized. Compound 8 showed less potent beta-adrenergic blocking activity than betaxolol in an in vitro test with guinea pig tracheal ...

journal_title：Journal of pharmaceutical sciences

authors： Amlaiky N,Leclerc G

更新日期：1985-10-01 00:00:00

abstract：:A model for estimating in vivo skin permeability coefficients for finite doses is presented. The ratio of the maximum value of the excretion rate to the steady-state flux is a function of the thickness of the applied vehicle and the vehicle-skin partition coefficient. The decay rate of the excretion is a function of s...

journal_title：Journal of pharmaceutical sciences

authors： Cooper ER,Berner B

更新日期：1985-10-01 00:00:00

abstract：:Gepirone hydrochloride, an investigational anxiolytic drug, was found to have at least three polymorphic forms which melted at 180 degrees C (I), 212 degrees C (II), and 200 degrees C (III). Thermal analytical studies showed that forms I and II were an enantiotropic pair, as were forms I and III. Form III was monotrop...

journal_title：Journal of pharmaceutical sciences

authors： Behme RJ,Brooke D,Farney RF,Kensler TT

更新日期：1985-10-01 00:00:00

abstract：:The mechanism of drug loading in cross-linked polymers was studied by X-ray photoelectron spectroscopy (XPS). This gave the atomic composition of the surface layers of the loaded polymeric particles so that the exact location of the drug molecules could be identified. Three different lots of popcorn crospovidone and a...

journal_title：Journal of pharmaceutical sciences

authors： Carli F,Garbassi F

更新日期：1985-09-01 00:00:00

abstract：:[7-3H]Tetracycline and [carbonyl-14C]rafoxanide were injected intravenously into anesthetized controls and rats in which experimental fascioliasis had been induced by 20 Fasciola hepatica metacercariae. The biliary excretion (1 and 3 h, respectively) of the radioactivity consisted of approximately 4% of the administer...

journal_title：Journal of pharmaceutical sciences

authors： Galtier P,Larrieu G,Franc M

更新日期：1985-09-01 00:00:00

abstract：:The reaction of chlorthalidone with methanol to give the corresponding methyl ether was investigated. The kinetics are pseudo-first-order in chlorthalidone, but the observed pseudo-first-order rate constants show an unexpected dependence on the initial chlorthalidone concentration, attributable to the presence of trac...

journal_title：Journal of pharmaceutical sciences

authors： Pandit NK,Hinderliter JS

更新日期：1985-08-01 00:00:00

abstract：:Coralyne analogues, isomers, and related alkaloids were examined as inhibitors of reverse transcriptase of RNA tumor viruses in the presence of polyriboadenylic acid-oligodeoxythymidylic acid (Poly rA.oligo dT), polydeoxyadenylic acid-oligodeoxythymidylic acid (Poly dA.oligo dT), polyribocytidylic acid-oligodeoxyguany...

journal_title：Journal of pharmaceutical sciences

authors： Sethi ML

更新日期：1985-08-01 00:00:00

abstract：:Mathematical models were determined relating preservative concentration and D values (decimal reduction times at 25 degrees C; pH 6.9-7.1) against Escherichia coli in aqueous medium. Preservatives investigated were 2-bromo-2-nitro-1,3-propanediol (Bronopol), N-(hydroxymethyl)-N-(1,3-dihydroxymethyl-2, 5-dioxo-4-imidaz...

journal_title：Journal of pharmaceutical sciences

authors： Hurwitz SJ,McCarthy TJ

更新日期：1985-08-01 00:00:00

abstract：:The pharmacokinetics of drug delivery from transdermal controlled-release devices consisting of (a) a membrane plus a reservoir or (b) a monolithic slab are examined. For the period when the devices act as if the drug reservoir were infinite, simple relationships for the steady-state slope and time lag are derived and...

journal_title：Journal of pharmaceutical sciences

authors： Berner B

更新日期：1985-07-01 00:00:00

abstract：:6-Amino-2-mercapto-5-methylpyrimidine-4-carboxylic acid proved to be a potent hypolipidemic agent in rodents at the low dose of 20 mg/kg/d. The agent effectively reduced the liver enzyme activities required for the synthesis of triglycerides and cholesterol. Lower lipid levels in tissue were observed in mice but not i...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Cocolas GH,Murthy AR,Rhyne KA,Knowles M

更新日期：1985-07-01 00:00:00

abstract：:The pharmacokinetics of atropine in three healthy male volunteers after intravenous administration of 1.35 and 2.15 mg of the drug was determined. Pharmacodynamic effects of atropine were measured simultaneously. All the data were fitted to a novel integrated kinetic-dynamic model. Plasma concentrations of atropine an...

journal_title：Journal of pharmaceutical sciences

authors： Hinderling PH,Gundert-Remy U,Schmidlin O

更新日期：1985-07-01 00:00:00

abstract：:A stability-indicating reversed-phase high-performance liquid chromatographic method using a refractive index detector is described for the determination of propylene carbonate in pharmaceutical formulations. Good precision and accuracy of the method was demonstrated using an aqueous formulation. This method is also a...

journal_title：Journal of pharmaceutical sciences

authors： Cheng H,Gadde RR

更新日期：1985-06-01 00:00:00

abstract：:There is a need to identify suitable blends of solvents to dissolve drugs. Empirical approaches, such as trial-and-error and response surface, require several solubility measurements. In this study the UNIFAC method was used to predict solubility in highly nonideal multicomponent systems in which only the solute entha...

journal_title：Journal of pharmaceutical sciences

authors： Ochsner AB,Sokoloski TD

更新日期：1985-06-01 00:00:00

abstract：:The purpose of this study was to evaluate the cardiovascular effects of two potential beta-hydroxylase inhibitors, a dithiocarbamate and a thiourea derivative of d-amphetamine, 1 and 2, respectively. These compounds when given intravenously elicited a significant dose-dependent depressor effect in normotensive rats an...

journal_title：Journal of pharmaceutical sciences

authors： Venugopalan CS,Jenkins HJ

更新日期：1985-06-01 00:00:00

abstract：:An equation was developed which enables blood level data to be utilized for determining whether or not the first-order absorption and elimination rate constants are equal in the one-compartment open model. This equation was tested using simulated data with excellent results. ...

journal_title：Journal of pharmaceutical sciences

authors： Macheras PE

更新日期：1985-05-01 00:00:00

abstract：:Hydroxypropyl cellulose films were prepared by compression molding of three different lots of hydroxypropyl cellulose powder at 149 degrees C, 188 degrees C, and 232 degrees C. Rectangular pieces were cut from these films and viscosity average molecular weight (Mv), degree of orientation, and rate of dissolution were ...

journal_title：Journal of pharmaceutical sciences

authors： Grabowski LA,Bondi JV,Harwood RJ

更新日期：1985-05-01 00:00:00

abstract：:A program is described that permits iterative least-squares nonlinear regression fitting of polyexponential curves using the Hewlett Packard HP 41 CV programmable calculator. The program enables the analysis of pharmacokinetic drug level profiles with a high degree of precision. Up to 15 data pairs can be used, and in...

journal_title：Journal of pharmaceutical sciences

authors： Thornhill DP,Schwerzel E

更新日期：1985-05-01 00:00:00

abstract：:It is shown that tricalcium phosphate follows a simple Heckel relationship in pressures of usual tablet compression, only if a density of 1.92 g/mL is used. This coincides with the density obtained by wet pycnometry, whereas the crystallographical density is 3.1 g/mL. The interpretation is that some of the pore space ...

journal_title：Journal of pharmaceutical sciences

authors： Hou XP,Carstensen JT

更新日期：1985-04-01 00:00:00

abstract：:Bioadhesive polymers that bind to the gastric mucin or epithelial cell surface are useful in drug delivery for the purposes of (a) retaining a dosage from in the GI tract and (b) increasing the intimacy and duration of contact of drug with the absorbing membrane. Polycarbophil has previously been shown to have bioadhe...

journal_title：Journal of pharmaceutical sciences

authors： Longer MA,Ch'ng HS,Robinson JR

更新日期：1985-04-01 00:00:00

abstract：:A stability-indicating high-performance liquid chromatographic assay has been used to investigate the stability of solutions of melphalan under conditions that pertain to setting up in vitro chemosensitivity assays. Melphalan (1 and 20 micrograms/mL) was found to be 30% more stable in 150 mM NaCl solution (normal sali...

journal_title：Journal of pharmaceutical sciences

authors： Bosanquet AG

更新日期：1985-03-01 00:00:00