Coated hydralazine hydrochloride beads for sustained release after oral administration.
Hydralazine hydrochloride is an antihypertensive used alone or in combination with isosorbide nitrate for the treatment of congestive heart failure. Since control of blood pressure should be continuous, sustained release delivery of this drug is considered therapeutically beneficial. Core beads for oral administration of this drug were prepared by extrusion-spheronization. Using experimental design to define the coat that was applied, the core beads were coated using a fluid bed coater to different coat thickness with combinations of two commercially available products dissolved in a hydroalcoholic solvent. The coat is a film with a combination of ethylcellulose and hydroxypropylcellulose that can provide desirable release profiles. Visually spherical and rugged bead products were obtained. Two products were identified that exhibited essentially a zero order release profile following a 2-h lag time with release of greater than 70% of the drug over the next 10 h in simulated intestinal fluid.
Philadelphia College of Pharmacy, University of the Sciences, 600 43rd Street, Philadelphia, PA 19104, USA.
M Akhlaq
MA
Mughal
Kalyan K
KK
Saripella
Chahinaz
C
Kouba
Zafar
Z
Iqbal
Steven H
SH
Neau
D000284:Administration, Oral; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000032:analysis / Q000737:chemistry*; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D055598:Chemical Phenomena; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000032:analysis / Q000737:chemistry; D004339:Drug Compounding; D005750:Gastric Juice / Q000737:chemistry; D006801:Humans; D006830:Hydralazine / Q000008:administration & dosage / Q000032:analysis / Q000737:chemistry*; D007700:Kinetics; D008863:Microspheres; D010189:Pancreatic Juice / Q000737:chemistry; D016062:Porosity; D015203:Reproducibility of Results; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013223:Statistics as Topic; D013499:Surface Properties; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000032:analysis / Q000737:chemistry*
D000959:Antihypertensive Agents; D003692:Delayed-Action Preparations; D012997:Solvents; D014665:Vasodilator Agents; D006830:Hydralazine; C013517:ethyl cellulose; D002482:Cellulose; C008079:hydroxypropylcellulose