These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Relative bioavailability of immediate- and sustained-release hydralazine formulations.
    Author: Ludden TM, Rotenberg KS, Ludden LK, Shepherd AM, Woodworth JR.
    Journal: J Pharm Sci; 1988 Dec; 77(12):1026-32. PubMed ID: 3244106.
    Abstract:
    The in vivo performance of hydralazine sustained-release dosage forms prepared using an ethylcellulose-coated drug:resin complex was studied in healthy males who were determined to be slow acetylators. Two studies were performed. The first study (I) compared four different coating levels (6.8, 8.7, 10, and 12%) with an immediate-release tablet and a solution. The second study (II) compared three additional coating levels (4, 5, and 7.8%) to the 6.8% formulation from the first study. Both hydralazine peak blood concentration (Cmax) and area under the blood concentration-time curves (AUC) decreased as the coating level increased [coating level (Cmax, ng/mL; AUC, ng.h/mL): 4% (37; 58), 5% (31; 55), 6.8% (13; 42 and 14; 39); 7.8% (16; 38), 8.7% (11; 34), 10% (7.8; 21), 12% (8.9; 17)]. In Study I both the solution and the immediate-release tablet were administered in two divided doses at 8 a.m. (fasting) and 2 p.m. (post-prandial). There was evidence for decreased bioavailability of unchanged hydralazine after the 2 p.m. doses as compared with the 8 a.m. doses. On the other hand, an assay that measures primarily the pyruvic acid conjugate of hydralazine yielded much higher concentrations after the afternoon dose. The results of these studies indicate that a sustained-release dosage form of hydralazine can be prepared using an ethyl-cellulose coated drug:resin complex and its in vivo characteristics are related to the coating level. Hydralazine bioavailability is influenced by food or recent prior exposure to hydralazine.
    [Abstract] [Full Text] [Related] [New Search]