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Acetaminophen prodrugs. I. Synthesis, physicochemical properties, and analgesic activity.
Carbonate and carboxylic acid ester prodrugs of acetaminophen were prepared. As expected, they had lower water solubilities and higher oil/water partition coefficients than acetaminophen itself. AtExpand
Enhancement of gastrointestinal absorption of a quaternary ammonium compound by trichloroacetate.
The hypothesis that ion-pair formation and transport across the lipid gastrointestinal barrier is an important mechanism for drug absorption has been examined using a quaternary ammonium compound,Expand
A simple rocking apparatus has been constructed for routine determination of distribution coefficients. With this apparatus, up to 36 two-phase samples in cylindrical tubes are equilibrated byExpand
Colorimetric assay procedure for dissolution studies of meprobamate formulations.
A colorimetric analytical procedure applicable to N—H-containing compounds was employed in dissolution studies of meprobamate formulations. The method, which can be applied directly to the aqueousExpand
4-acetamidophenyl 2,2,2-trichlorethyl carbonate synthesis, physical properties, and in vitro hydrolysis.
A trichloroethyl carbonate prodrug ester of acetaminophen has been made by reacting acetaminophen with trichloroethyl chloroformate. It is a virtually tasteless crystalline compound retaining theExpand
Acetaminophen prodrugs. II. Effect of structure and enzyme source on enzymatic and nonenzymatic hydrolysis of carbonate esters.
Hydrolysis rates are reported for acetaminophen prodrugs with the structure CH 3 CONH-ϕ-OCOOR at pH 7.4 in phosphate buffer alone or containing 1% human plasma or serum from several animal species.Expand
Carbonate ester prodrugs of salicylic acid. Synthesis, solubility characteristics, in vitro enzymatic hydrolysis rates, and blood levels of total salicylate following oral administration to dogs.
The methods of synthesis, solubilities, and partition coefficients for the ethyl-, butyl-,hexyl-, and 2,2,2-trichloroethylcarbonate esters of salicylic acid are reported. The solubility andExpand
Encapsulation of clomacran phosphate [2-chloro-9[3-(dimethylamino) propyl]acridan phosphate] I. Effect of flowability of powder blends, lot-to-lot variability, and concentration of active ingredient
Abstract A correlation has been shown to exist between the flow properties of clomacran phosphate powder blends and capsule fill weight variation when an automatic capsule-filling machine is used.AExpand
Hydrolysis of 4-acetamidophenyl 2,2,2-trichloroethyl carbonate by esterolytic enzymes from various sources.
Hydrolysis rates were determined for ATC in pH 7.4 phosphate buffer containing human plasma from a number of individuals; human plasma treated and stored in various ways; several Cohn fractions ofExpand
Heating and cooling rate coefficients and related factors affecting procedures for tablet shelf life prediction
Data are presented for the heating and cooling rate coefficients of tablets under the usual conditions of exaggerated temperature hot air oven stability studies. The interrelationships of tabletExpand