Guar gum-based sustained release diltiazem.
OBJECTIVE
This study was performed to examine the use of guar gum to sustain the release of diltiazem under in vitro and in vivo conditions.


METHODS
Guar gum tablet formulations were prepared and evaluated under a variety of in vitro dissolution conditions. The formulations, along with Dilacor XR, were administered to a group eight fasted, healthy volunteers in a four period crossover study.


RESULTS
Varying the lot of guar gum as well as using guar from different suppliers had little effect on diltiazem dissolution. Also, dissolution of diltiazem from guar gum tablets was essentially independent of stir speed under normal conditions (USP Apparatus II) The stability of guar-based formulations under stressed conditions (40 degrees C/75% relative humidity for 3 months) was also established. All four formulations gave similar plasma concentrations over time in the healthy volunteers pharmacokinetic study.


CONCLUSIONS
Guar gum-based matrix tablets represent a simple and economical alternative to existing diltiazem sustained release dosage forms.
CIBUS Pharmaceutical, Inc., Menlo Park, California 94026-1226, USA.
S A
SA
Altaf
K
K
Yu
J
J
Parasrampuria
D R
DR
Friend
D000959:Antihypertensive Agents / Q000008:administration & dosage*; D004110:Diltiazem / Q000008:administration & dosage*; D004337:Drug Carriers; D005685:Galactans / Q000737:chemistry; D006244:Hardness; D006801:Humans; D006813:Humidity; D006863:Hydrogen-Ion Concentration; D008351:Mannans / Q000737:chemistry; D010316:Particle Size; D053149:Plant Gums; D012016:Reference Values; D012995:Solubility
D000959:Antihypertensive Agents; D004337:Drug Carriers; D005685:Galactans; D008351:Mannans; D053149:Plant Gums; C007894:guar gum; D004110:Diltiazem