Journal of Pharmaceutical Sciences p. 942 - 945 (1991)
Update date:2022-08-18
Topics:
ElSohly
Stanford
Harland
Hikal
Walker
Little Jr.
Rider
Jones
Oral administration of Δ-9-tetrahydrocannabinal (Δ9-THC) was shown to result in low and erratic bioavailability, while the drug showed no bioavailability from various suppository formulations. Δ9-THC-Hemisuccinate was formulated as a prodrug for Δ9-THC in suppositories using Witepsol H15 base. The bioavailability of Δ9-THC from this formulation was evaluated in monkeys. The plasma levels of Δ9-THC and its metabolite 11-nor-Δ9-THC-9-COOH were determined using GC/MS analysis. The calculated bioavailability of Δ9-THC from this formulation was found to be 13.5%. Non-compartmental analysis of the plasma concentration data using statistical moments showed the mean residence time (MRT) for Δ9-THC in the body to be 3 h following iv administration of Δ9-THC or its hemisuccinate ester (3.4 and 2.7 h, respectively), as compared with 5.8 h following rectal administration of the Δ9-THC hemisuccinate. The observed rectal bioavailability of Δ9-THC from suppositories containing the hemisuccinate ester as a prodrug is of significant importance in developing an alternative approach to oral administration of the drug.
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