Pharmaceutical Compositions Containing Dimethyl Fumarate
OwnerDavid Goldman, Katherine Dawson +1inventors
InventorsDavid Goldman, Katherine Dawson, Ajay Nirula
Life of this patent
Estimating the term…
Abstract
Provided herein are compositions containing compounds, or pharmaceutically acceptable salts, that metabolize to monomethyl fumarate with certain pharmacokinetic parameters and methods for treating, prophylaxis, or amelioration of neurodegenerative diseases including multiple sclerosis using such compositions in a subject, wherein if the compositions contain dimethyl fumarate, the total amount of dimethyl fumarate in the compositions ranges from about 43% w/w to about 95% w/w.
Claims32
A composition comprising dimethyl fumarate and one or more excipients, wherein the total amount of dimethyl fumarate in the composition ranges from about 43% w/w to about 95% w/w.
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
A composition comprising, about 43% w/w to about 95% w/w dimethyl fumarate, a total amount of about 3.5% w/w to about 55% w/w of one or more fillers, a total amount of about 0.2% w/w to about 20% w/w of one or more disintegrants, a total amount of about 0.1% w/w to about 9.0% w/w of one or more glidants, and a total amount of about 0.1% w/w to about 3.0% w/w of one or more lubricants.
(canceled)
(canceled)
A method of making a powder composition comprising combining about 43% w/w to about 95% w/w dimethyl fumarate, a total amount of about 3.5% w/w to about 55% w/w of one or more fillers, a total amount of about 0.2% w/w to about 20% w/w of one or more disintegrants, a total amount of about 0.1% w/w to about 900% w/w of one or more glidants, and a total amount of about 0.1% w/w to about 3.0% w/w of one or more lubricants to form the composition.
A composition comprising dimethyl fumarate and one or more excipients, wherein about 80% or higher of the dimethyl fumarate has a particle size of 250 microns or less.
(canceled)
A capsule comprising microtablets comprising dimethyl fumarate, wherein the total amount of dimethyl fumarate in an uncoated microtablet ranges from about 43% w/w to about 95% w/w.
(canceled)
(canceled)
A method for treating, prophylaxis, or amelioration of multiple sclerosis (MS) comprising orally administering to a subject in need thereof a therapeutically effective amount of dimethyl fumarate (DMF) and an amount of one or more non-steroidal anti-inflammatory drugs effective to reduce flushing.
A method of treating, prophylaxis, or amelioration of multiple sclerosis, comprising administering to a subject in need thereof a composition containing a compound, or a pharmaceutically acceptable salt thereof, that metabolizes to monomethyl fumarate wherein said administering the composition provides one or more of the following pharmacokinetic parameters:
- (a) a mean plasma monomethyl fumarate Tmax of from about 1.5 hours to about 3.5 hours;
- (b) a mean plasma monomethyl fumarate Cmax ranging from about 1.03 mg/L to about 3.4 mg/L;
- (c) a mean plasma monomethyl fumarate AUCoverall ranging from about 4.81 h.mg/L to about 11.2 h.mg/L;
- (d) a mean plasma monomethyl fumarate AUC0-12 ranging from about 2.4 h.mg/L to about 5.5 h.mg/L;
- and (e) a mean AUC0-infinity ranging from about 2.4 h.mg/L to about 5.6 h.mg/L.
(canceled)
Dependencies are inferred from the claim text.