Percutaneous absorption of Octopirox.

[14C]Octopirox administered to rats by intubation or injection was excreted mostly in the faeces (65-85% of the dose) with smaller amounts (6-19%) in the urine. Blood levels after intubation of Octopirox (4.8 mg/kg body weight) reached a maximum equivalent to 0.137 micrograms/ml at 2 hr and declined to 0.007 micrograms/ml at 48 hr after administration. Tissue levels were low, the greatest was the liver with the equivalent of 3 micrograms Octopirox at 6 hr after intubation. With female rats skin penetration of Octopirox at 1% (v/v) in shampoo without rinsing was 65.1 micrograms/cm2 under non-occlusive conditions for 48 hr. When the skin was rinsed after a 10-min contact, penetration was reduced to 3.4 micrograms/cm2 under occlusive, and 2.0 micrograms/cm2 under non-occlusive conditions. Skin penetration of Octopirox was dependent on duration of contact up to 10 min before rinsing. Penetration at 1% Octopirox increased significantly from 2.4 micrograms/cm2 after 2.5 min exposure to 4.5 micrograms/cm2 after 10 min contact, but there was no further increase in penetration with a 20-min application. Skin penetration and deposition of Octopirox were both proportional to Octopirox concentration between 0.1 and 1% (w/v); skin penetration increased from 0.31 to 3.6 micrograms/cm2 while deposition increased from 0.8 to 7.6 micrograms/cm2. There was no significant difference between the penetration through clipped skin and hairy skin from an application of 1% Octopirox for 5 min followed by rinsing. Under non-occlusive conditions, penetration was 1.5 micrograms/cm2 for both types of skin. Blood levels after topical application (15.4 mg/kg body weight) without rinsing and with occlusion reached the equivalent of 0.32 micrograms/ml at 6 hr. However, when the skin was rinsed and protected with a non-occlusive patch blood levels were reduced to a maximum equivalent to 0.02 micrograms/ml at 1 hr after application. The safety factor estimated for the consumer using a shampoo containing 1% Octopirox is 29,400, so that the possibility of systemic effects due to absorption through the skin is remote.

Infrared spectra and the chain organization of erythrocyte membranes.

Changes in the intensity of the 720 cm(-1) band were followed in the infrared spectra of the human erythrocyte membrane and its total lipid extract, recorded at various temperatures. These changes are interpreted in terms of the configuration of the lipid hydrocarbon chains within the membrane. Effects of temperature, sonication, removal of lipids, and organic solvents on the amide I and II bands, associated with protein conformations, were also studied.

Physicochemical differences between fragments of plasma membrane and endoplasmic reticulum.

Specific turbidities, densities, and refractive indices of fragments of plasma membrane (PM) and endoplasmic reticulum (ER) from Ehrlich ascites carcinoma have been measured. A spherical shell model of specified dimensions and refractive index was established for PM fragments. The ionic composition of the dispersion medium was varied systematically. Increases in Gamma/2 caused increases in the turbidity of both PM and ER suspensions, the greatest effects being observed with Ca(2+) and Mg(2+). In the case of PM this effect is attributable mainly to aggregation, whereas "structural" changes account for most of the turbidity increase with ER. The pH was also varied systematically to obtain pH- density and turbidity profiles and to establish the isoelectric pH of the two membrane types (PM-3.6; ER-4.35). Turbidity was maximum at "isoelectric" pH, which corresponds in each case to the region of minimum charge on the particle surfaces. Both PM and ER show large increases of density at the "isoelectric" pH, but only ER shows substantial structurally based turbidity increase under these conditions. Both PM and ER show operation of electrostatic attractions near "isoelectric" pH. PM has been shown to have ionically distinctive inner and outer surfaces while ER shows no such dissymmetry. The necessary theoretical background for interpretation of turbidity and density measurements is included, as well as a discussion of the limitations of our conclusions and the biological importance of our results.