| Title: A TIME-RELEASE DELIVERY MATRIX COMPOSITION AND CORRESPONDING
CONTROLLED-RELEASE COMPOSITION Inventor(s): V. Galiatsatos, L. Alabakovska
Disclosure 236 U.S. Patent 5,676,972
This "broad based" platform invention relates to a composition for use as a
matrix in time and controlled-release compositions. Such compositions utilize an active
ingredient dispersed in a matrix. Active ingredients include, for example, both
pharmaceutical and agricultural agents.
The matrix is a blend of a poly(hydroxyethyl) methacrylate, polyethylene glycol and
time-release extending agent which is a low molecular weight polymer having hydrophilic
and hydrophobic side groups, such as diblock or triblock poly(ethylene oxide
propyleneoxide).
The polymeric matrix composition is a biologically compatible, nontoxic, hydrophilic,
water-soluble blend composition. In addition, the composition, optionally, eliminates the
use of a Dimethyl Sulfoxide (DMSO) solvent which is currently on the Federal Food and Drug
Administrations's list of non-approved substances.
The matrix resin comprises a blend from about 10-90 percent poly(2-hydroxyethyl
methacrylate) or PHEMA, 5-85 percent polyethylene glycol or PEG, and 5-30 percent
poly(ethylene oxide)/poly(propylene oxide) copolymer preferably having 25-80 percent
poly(propylene oxide) repeating units.
One example of a suitable pharmaceutical active ingredient is diltiazem hydrochloride
("DTZ") which is a calcium channel blocking agent used in the treatment of
angina and hypertension. DTZ is sold under the trade name Cardizem (MDL 20, 307A) by
Hoechst Marion Roussel (formerly Marion Merrell Dow).
Examples of suitable agricultural active ingredients are insecticides, pesticides,
herbicides, and fertilizers.
The matrix composition can be optimized for controlled burst and\or sustained release
attributes by manipulating matrix composition and based upon active ingredient(s) and
specific end applications. |
