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abstract & commentary
Synopsis: The bioequivalence of a proprietary liquid dapsone preparation and commercially available dapsone tablets makes dapsone available to children and others who are unable to ingest tablets.
Source: Mirochnick M, et al. Bioequivalence of a propylene glycol-based liquid dapsone preparation and dapsone tablets. Am J Health Syst Pharm. 2000;57(19):1775-1777.
In a bioequivalence study, 12 adult volunteers received dapsone doses (either in liquid or tablet form) with 8 ounces of water 1-2 hours after breakfast. Each volunteer initially received a 100-mg dose of a propylene glycol-based liquid preparation of dapsone with blood sampling before each dose and up to 96 hours after administration of each dose. This was repeated in each individual 2 weeks later with a 100-mg dapsone tablet.
The area under the concentration-vs.-time curve and maximum serum concentration for the 2 formulations met the specifications for bioequivalence. While the time to maximum serum concentration tended to be lower for the liquid preparation, it was not significant. Both preparations could be used interchangeably.
Comment by Thomas g. Schleis, MS, RPh
Dapsone is a versatile agent that has been used in the areas of infectious diseases, immunology, and dermatology (see Table). Its use as a prophylactic agent for Pneumocystis carinii pneumonia (PCP), either alone or with pyrimethamine, or as treatment of PCP in combination with trimethoprim is well documented.1-3 Advances in the treatment of pediatric HIV and oncology patients have resulted in a higher population of children at risk for PCP, and a pediatric formulation of dapsone would be desirable for those patients that cannot tolerate trimethoprim-sulfamethoxazole, which is a first-line agent for PCP prophylaxis. Previous liquid formulations of dapsone either demonstrated poor bioavailability or did not have adequate stability information available.4,5
This new preparation, which is available for compassionate use in patients who cannot tolerate trimethoprim-sulfamethoxazole, is an advance in treating the pediatric population. Once FDA approved and released, it will also be useful in administering to those patients who are not able to swallow tablets.
1. Podzamczer D, et al. Intermittent trimethoprim-sulfamethoxazole compared with dapsone-pyrimethamine for the simultaneous primary prophylaxis of pneumocystis pneumonia and toxoplasmosis in patients infected with HIV. Ann Intern Med. 1995;122:755-761.
2. Centers for Disease Control and Prevention. 1999 USPHS/ISDA guidelines for the prevention of opportunist infections in patients infected with human immunodeficiency virus. MMWR Morb Mortal Wkly Rep. 1999;48:1-66.
3. Masur H. Prevention and treatment of pneumocystis pneumonia. N Engl J Med. 1992;327:1853-1860.
4. Mirochnick M, et al. Pharmacokinetics of dapsone in children. J Pediatr. 1993;122:806-809.
5. Gatti G, et al. Pharmacokinetics of dapsone in human immunodeficiency virus-infected children. Antimicrob Agents Chemother. 1995;39:1101-1106.