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Ketorolac tromethamine and Ketoprofen suppositories: release profiles and bioavailability of cocoa butter base formula in rabbits

Author(s):  Zia Hossein, Rashed Suzette F, Quadir Mohammed, Needham Thomas E, Squillante Emilio

Issue:  Sep/Oct 1998 - Parenteral Nutrition Solutions
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Abstract:  Ketorolac tromethamine suppositories (30 mg) and ketoprofen suppositories (50 mg) were made by the fusion method with various bases such as cocoa butter, Witepsol® H15, Witepsol W25, Witepsol W35, Witepsol E75, Suppocire AML and Hydrokote AP5-1. Also, ketorolac tromethamine and ketoprofen suppositories were prepared using Eudragit® L100 and propylene glycol. The release rates for both ketorolac tromethamine and ketoprofen suppositories in Sørensen’s phosphate buffer pH 7.4 were determined and found to be: cocoa butter> Witepsol H15> Witepsol W25> Suppocire AML> Witepsol W35> Hydrokote AP5-1> Witepsol E75. Drugrelease studies showed that ketorolac tromethamine demonstrates faster release profiles from these selected bases in comparison to those seen for ketoprofen. Analysis of the release kinetics for ketorolac tromethamine and ketoprofen from the various bases suggests that a combination of release mechanisms such as melting of the base followed by partitioning of the drug, along with some diffusion of the drug from the base to the dissolution media, seems to be operative in these systems. The absolute bioavailability of the suppository formulation made with ketorolac tromethamine in cocoa butter base was found to be 61% in rabbits.

Related Keywords: Witepsol

Related Categories: PAIN MANAGEMENT, PEER-REVIEWED

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