Active Agent Formulations, Methods of Making, and Methods of Use
Stable fenofibrate suspensions are disclosed herein. A fenofibrate composition includes fenofibrate nanoparticles having an average particle size of less than 500 nm, and a particle sequestrant, wherein the average particle size of the nanoparticulate suspension changes by less than 50% after standing at room temperature for 21 or more days.
1 . A fenofibrate composition comprising
fenofibrate nanoparticle suspension having an average particle size of less than 500 nm, and
a particle sequestrant,
wherein the average particle size of the nanoparticulate suspension changes by less than 50% after standing at room temperature for 21 days.
2 . The fenofibrate composition of claim 1 , wherein the average particle size of the nanoparticulate suspension changes by less than 50% after standing at room temperature for 28 days.
3 . The fenofibrate composition of claim 1 , wherein the average particle size of the nanoparticulate suspension changes by less than 50% after standing at room temperature for 59 days.
4 . The fenofibrate composition of claim 1 , wherein the average particle size of the nanoparticulate suspension changes by less than 50% after standing at room temperature for 122 days.
5 . The fenofibrate composition of claim 1 , wherein the average particle size of the nanoparticulate suspension changes by less than 50% after standing at room temperature for 181 days.
6 . The fenofibrate composition of claim 1 , wherein the average particle size of the nanoparticulate suspension changes by less than 50% after standing at room temperature for 194 days.
7 . The fenofibrate composition of claim 1 , wherein the average particle size of the nanoparticulate suspension changes by less than 50% after standing at room temperature for 404 days.
8 . The fenofibrate composition of claim 1 , wherein the particle sequestrant is a pH-sensitive copolymer having both hydrophobic (meth)acrylate units and acid-soluble (meth)acrylate units.
9 . The fenofibrate composition of claim 3 , wherein the particle sequestrant is a butyl methacrylate-(2-dimethylaminoethyl)methacrylate-methyl methacrylate copolymer.
10 . The fenofibrate composition of claim 1 , comprising no added surfactant, phospholipid, or a combination thereof.
11 . The fenofibrate composition of claim 1 , wherein the fenofibrate nanoparticles and the particle sequestrant are disposed on an inert core particle to form a fenofibrate granulate.
12 . A fenofibrate composition comprising
fenofibrate nanoparticle suspension having an average particle size of less than 500 nm, and
a particle sequestrant,
wherein the average particle size of the nanoparticulate suspension is 200 to 500 nm after standing at room temperature for 21 days
13 . The fenofibrate composition of claim 12 , wherein the average particle size of the nanoparticulate suspension is 200 to 500 nm after standing at room temperature for 28 days.
14 . The fenofibrate composition of claim 12 , wherein the average particle size of the nanoparticulate is 200 to 500 nm after standing at room temperature for 59 days.
15 . The fenofibrate composition of claim 12 , wherein the average particle size of the nanoparticulate suspension is 200 to 500 nm after standing at room temperature for 122 days.
16 . The fenofibrate composition of claim 12 , wherein the average particle size of the nanoparticulate suspension is 200 to 500 nm after standing at room temperature for 181 days.
17 . The fenofibrate composition of claim 12 , wherein the average particle size of the nanoparticulate suspension is 200 to 500 nm after standing at room temperature for 194 days.
18 . The fenofibrate composition of claim 12 , wherein the average particle size of the nanoparticulate suspension is 200 to 500 nm after standing at room temperature for 404 days.
19 . The fenofibrate composition of claim 12 , wherein the particle sequestrant is a pH-sensitive copolymer having both hydrophobic (meth)acrylate units and acid-soluble (meth)acrylate units.
20 . The fenofibrate composition of claim 19 , wherein the particle sequestrant is a butyl methacrylate-(2-dimethylaminoethyl)methacrylate-methyl methacrylate copolymer.
21 . The fenofibrate composition of claim 12 , comprising no added surfactant, phospholipid, or a combination thereof.