Search PubMed⌕ Search

Biomedical subjects

A Hussain

Publications and source records attributed to A Hussain.

At least 217 records · Page 12Linked to original sources
PubMed1979

Kinetics and mechanism of hydrolysis of 1-(2'-acetoxybenzoyl)-2-deoxy-alpha-D-glucopyranose, a novel aspirin prodrug.

The formation rate of aspirin from the prodrug was determined as a function of the pH, temperature, and dielectric constant of the solvent spectrophotometrically and was confirmed by high-pressure liquid chromatography. Aspirin formation was first order with respect to the prodrug and zero order with respect to the hydroxide-ion concentrations. The hydrolysis rate was independent of buffer concentration but very sensitive to the dielectric constant of the solvents. The half-life for the formation of aspirin at 37 degrees was 7 min. The activation energy for the hydrolysis was 23.7 kcal/mole. The results suggest that the hydrolysis of the prodrug to aspirin proceeds by an SN1-type mechanism.

Aspirin↗
PubMed1979

Cell mediated immunity to bovine rhinovirus type 1 in calves.

Calves experimentally infected with bovine rhinovirus type 1 developed a mild respiratory disease and exhibited a cell mediated immune (CMI) response, as determined by leukocyte migration inhibition (LMI) and lymphocyte blastogenesis tests. The CMI response to the virus was detected by day 3 post-inoculation using direct and indirect LMI tests. It persisted through day 28, with maximal responses occurring between days 4 and 14. Measurement of cellular immunity by blast transformation, however, was not evidenced until day 12. The humoral antibody response was minimal with serum neutralizing titers ranging from 1:4 to 1:16 and this response was not evident until 3 weeks after inoculation.

Animals↗
PubMed1978

Prodrug approaches to enhancement of physicochemical properties of drugs IX: acetaminophen prodrug.

The synthesis, hydrolysis rate, and bioavailability of 1-(p-acetaminophenoxy)-1-ethoxyethane, an acetaminophen prodrug, are described. The prodrug is less soluble than acetaminophen and stable at neutral pH. However, in an acidic environment, the compound cleaves rapidly, generating acetaminophen. When both the prodrug and acetaminophen were administered to dogs in equivalent amounts, the blood acetaminophen levels were comparable.

Acetaminophen↗
PubMed1977

Precautionary note for use of bisulfite in pharmaceutical formulations.

The effect of sodium bisulfite on aspirin hydrolysis was studied at 40 degrees in the pH range of 6.5-7.5. Significant catalytic activity by the sulfite ion was observed. Second-order rate constants were calculated for this catalysis and compared to other buffer species. The sulfite ion was a much more efficient catalyst than acetate, phosphate, or carbonate.

Antioxidants↗
PubMed1976

Prodrug approaches to enhancement of physicochemical properties of drugs IV: novel epinephrine prodrug.

The synthesis and characterization of a prodrug that appears to overcome the problem of inefficient absorption of epinephrine through the lipoidal membranes of the eye are described. The enzymatic rate of regeneration of epinephrine from the prodrug was determined using a rabbit eye homogenate, rabbit plasma, and human plasma. The prodrug had no activity of its own when tested against a guinea pig smooth muscle preparation. Upon enzymatic regeneration of epinephrine from the prodrug, however, the reaction mixture exhibited alpha-adrenergic activity equivalent to that of epinephrine when tested in the same preparation.

Animals↗