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Influence of Dielectric Constant of the Base on the Release of Acetaminophen from Suppositories

1979; Taylor & Francis; Volume: 5; Issue: 5 Linguagem: Inglês

10.3109/03639047909069239

1520-5762

S. Stavchansky, M. Garabédian, Peng Wu, A. Martin,

Analytical Chemistry and Chromatography

The dielectric constant of various polyethylene glycol suppository bases (vehicles) was investigated in relation to the release of acetaminophen as measured by dissolution. Bioavailability of the drug from the bases was also studied in the rectum of beagle dogs. Blood samples were removed at appropriate time intervals and the acetaminophen analyzed by an improved GLC method. A solubility study of acetaminophen in dioxane-water mixtures indicated that maximum solubility of the drug occured at a dielectric constant of about 14. The bioavailability results in dogs showed minimum release of drug in bases of dielectric constants near 14 and increased release characteristics in bases farther removed from this dielectric constant. The results suggest that vehicles with lower solubility for the drug tend be release acetaminophen readily and provide improved bioavailability.