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Acetaminophen prodrugs. I. Synthesis, physicochemical properties, and analgesic activity.
TLDR
The results show how the carbonate linkage may be employed to create prodrugs and how it is possible to obtain a series of pharmacologically similar compounds possessing vastly different physicochemical properties.
Enhancement of gastrointestinal absorption of a quaternary ammonium compound by trichloroacetate.
TLDR
Evidence is presented which clearly indicates that TCA, an anion capable of forming a lipid-soluble ion pair with isopropamide, significantly enhances the pharmacologic response of orally administered isoproamide.
DRUG PARTITIONING. I. NONEMULSIFYING METHOD FOR MEASURING DISTRIBUTION COEFFICIENTS.
TLDR
Considerable man hours are saved with some pharmaceutical systems if the rocking method, rather than the usual shake-out method, is used, and results which are in agreement with results from shake- out methods are given.
Colorimetric assay procedure for dissolution studies of meprobamate formulations.
TLDR
A colorimetric analytical procedure applicable to N—H-containing compounds was employed in dissolution studies of meprobamate formulations and gave results comparable to the official GC analytical procedure.
4-acetamidophenyl 2,2,2-trichlorethyl carbonate synthesis, physical properties, and in vitro hydrolysis.
TLDR
It was surmised that following oral administration to animals, a portion of the prodrug may be absorbed intact, but some cleavage may occur before and during absorption from the intestines, since enzymes that hydrolyze it are prevalent in plasma and liver, and the pro drug on entering the blood will be hydrolyzed very rapidly.
Acetaminophen prodrugs. II. Effect of structure and enzyme source on enzymatic and nonenzymatic hydrolysis of carbonate esters.
TLDR
The sera of small rodents were more potent catalysts of the hydrolyses of all types of acetaminophen carbonates than that of other animals or human plasma.
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.
TLDR
The results suggest that the prodrug carbonate esters are as readily absorbed as aspirin despite their different aqueous and lipid solubilities and that all the drugs including aspirin are converted to a common form within 2—3 hr. after oral administration.
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.A
Antacid Properties of Calcium, Magnesium, and Aluminum Salts of Water-Insoluble Aliphatic Acids
The antacid properties of several calcium, magnesium, and aluminum salts of aliphatic acids were studied. A number of the salts showed potential antacid properties in vitro . Of this group calcium
Hydrolysis of 4-acetamidophenyl 2,2,2-trichloroethyl carbonate by esterolytic enzymes from various sources.
TLDR
It was concluded that, following oral administration, ATC would be exposed to many enzymes that are potent catalysts for its hydrolysis, both in the gastrointestinal tract and following absorption and distribution in body tissue.
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