In vitro transdermal delivery of atenolol using mouse and guinea pig.

In vitro percutaneous absorption of atenolol was done in order to assess its feasibility for transdermal development across mouse and guinea pig skins using Keshary-Chien type of diffusion cell. Values of diffusion rate (J) and permeability coefficient (Kp) across guinea pig skin were lowered as compared to those in mouse skin. When the concentration of drug in donor compartment was increased a decrease in Kp and increase in J value were observed with both the skins. Under the same conditions, values of J and Kp were lowered for dorsal skin compared to abdominal skin both for mouse and guinea pig. The results suggest that atenolol can be pursued further for transdermal system development.

Toxicity studies with potassium embelate, a new analgesic compound.

Potassium embelate, 2,5-dihydroxy, 3-undecyl-1, 4-benzoquinone, from Embelia ribes Burm. was subjected to toxicity evaluation which included subacute, chronic, reproductive toxicity testing and teratological investigations in laboratory animals (mice, rats and monkeys). The results did not indicate adverse effects suggesting that potassium embelate is a safe compound.

Kinetic fate of potassium embelate, a non-narcotic centrally acting analgesic after oral and intravenous administration.

The pharmacokinetics of oral and intravenous potassium embelate (20 mg/kg) was studied in rats. The results revealed that this compound follows a biexponential kinetic pattern. Absorption was complete (bioavailability 97%) and fast. The disposition half-life is 9.5 h on intravenous and 11 h on oral administration. High concentrations of the drug were found in brain between 0.25 and 2 h, which is in agreement with its pharmacological action. The kidney plays a major role in the excretion of the drug.