Medicinal aerosol compositions with a functionalized polyethyleneglycol excipient
View Patent ↗The invention comprises a medicinal aerosol composition comprising a propellant, an excipient comprising a functionalized polyethyleneglycol, and a drug. The invention also comprises particulate medicinal compositions comprising particles with a mean mass aerodynamic diameter of less than about 10 microns that incorporate an excipient comprising a functionalized polyethyleneglycol.
1. A medicinal aerosol composition comprising:
a propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane, and a mixture thereof;
an excipient comprising a compound of the structure R 1 —(O—CH 2 —CH 2 ) n —X; wherein
X is selected from the group consisting of: —C(O)OH; —S(O 2 )OH; —OS(O 2 )OH; —P(OH) 2 O; —OP(OH) 2 O; —N(R 2 )(R 2 ); —OC(R 2 )(R 2 )—C(O)—Z; —OC(O)—R 2 —C(O)—Z; —O—R 3 —C(O)—Z; and —OC(O)CH(R 3 )—N(R 2 )(R 2 );
Z is selected from —OH; —N(R 2 )(R 2 ); —NH—R 2 —NH—; an amino acid residue; a peptide residue with from 2 to 8 amino acids; or a hydroxy acid;
n is from 1 to 250;
R 1 is methyl or ethyl;
Each R 2 is independently selected from hydrogen or linear, branched, or cyclic hydrocarbon with 1 to 6 carbons; and
R 3 is independently selected from hydrogen or linear, branched, or cyclic hydrocarbon with 1 to 6 carbons, wherein R 2 and R 3 may optionally be connected together to form an alkylene bridge of from 2 to 4 carbons; and
a drug.
2. The medicinal aerosol composition of claim 1 wherein X is —OC(R 2 )(R 2 )—C(O)—Z.
3. The medicinal aerosol composition of claim 2 wherein Z is —OH.
4. The medicinal aerosol composition of claim 2 wherein Z is an amino acid residue selected from the group consisting of glycine, glycineamide, alanine, proline, taurine, and sarcosine.
5. The medicinal aerosol composition of claim 1 wherein n is from 2 to 45.
6. The medicinal aerosol composition of claim 1 wherein the drug, excipient, and propellant form a solution.
7. The medicinal aerosol composition of claim 1 wherein the composition comprises a suspension in the propellant.
8. The medicinal aerosol composition of claim 1 further comprising a polar cosolvent.
9. The medicinal aerosol composition of claim 8 wherein the polar cosolvent is selected from the group consisting of ethanol, isopropanol, and mixtures thereof.
10. The medicinal aerosol composition of claim 1 wherein the molar ratio of excipient to drug is between about 5:1 and 1:5.
11. The medicinal aerosol composition of claim 1 wherein the molar ratio of excipient to drug is about 1:1.