Videomicroscopy techniques for agglomeration studies.
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Excipients↗
Biomedical subjects
J F Stearns
Publications and source records attributed to J F Stearns.
Structural rheology of a model ointment.
A model ointment consisting of white petrolatum, mineral oil and microcrystalline wax was studied using rheology, microscopy and thermal techniques. Rheograms studied over a temperature range of 25-40 degrees C indicated that the overall rheogram shape changed little as the temperature increased. However, two inflections gradually disappeared as the temperature increased. Thermal optical analysis showed that the temperature range over which these inflection disappeared correlated with the melting transition of the components forming the secondary structure. Another series of rheograms obtained from ointments with different combinations of the raw materials showed the rheology of the ointment is primarily controlled by the white petrolatum and mineral oil and that the microcrystalline wax acts to build-up the structure by incorporating itself into the existing white petrolatum structure. Thermal optical analysis of comelts of the raw materials proved that the ointment network structure is essentially a recombination of the naturally occurring components in differing ratios. The knowledge obtained from these studies is applied to a discussion of the thermal and mechanical stresses encountered in the filling operation.
Drug Packaging↗
Inhibition of the fusion-inducing conformational change of influenza hemagglutinin by benzoquinones and hydroquinones.
Influenza hemagglutinin (HA) undergoes a conformational change that is required for viral entry. The rearrangement includes exposure of the fusion peptide, a hydrophobic segment buried in the trimer interface of the native protein. Since fusion peptide release triggers the membrane fusion event crucial for viral replication, inhibition of fusion peptide exposure should prevent infection. We reasoned that small molecules that bind to HA and stabilize its nonfusogenic conformation would block viral activity. A computer-assisted method was used to select putative HA ligands. One of the selected compounds, 4A,5,8,8A-tetrahydro-5,8-methano-1,4-naphthoquinone, prevented the conversion of X31 HA to a conformation recognized by alpha-fusion peptide antisera. Several derivatives of this compound, including both benzoquinones and hydroquinones, also showed inhibition. The most effective compounds tested have IC50S between 1 and 20 microM. Representative compounds also inhibited virus-induced syncytia formation, HA-mediated hemolysis, and viral infectivity in vitro. The inhibitors are attractive leads for the development of antiviral drugs and can serve as probes of the mechanism of the conformational change of HA.
Benzoquinones↗