Pharmaceutical compositions with enhanced performance and improved processability
View Patent ↗The presently disclosed and claimed inventive concept(s) relates to a polymer for enhancing drug performance and improving processability. Specifically, the polymer comprises hydroxypropyl methyl cellulose acetate succinate (HPMC-AS). On the HPMC-AS, the percentage of total succinoyl degree of substitution is less than 12% at C6-OH position and greater than 53% at C3-OH, and the percentage of total acetyl degree of substitution is greater than 32% at C6-OH position.
1. A polymer for enhancing drug performance and improving processability, wherein the polymer is hydroxypropyl methyl cellulose acetate succinate having:
a percentage of a total degree of substitution (DS) of succinoyl less than or equal to 6% at a C6-OH position (%C 6 DS Suc ≦6%) and from 58% to 84% at a C3-OH position (58% <%C 3 DS Suc <84%), and
a percentage of a total DS of acetyl from 33% to 51% at a C6-OH position (33%<%C 6 DS Ac <51%) and from 16% to 20% at the C3-OH position (16%<%C 3 DS Ac <20%).
2. A composition comprising a drug and a polymer, wherein the polymer is hydroxypropyl methyl cellulose acetate succinate having:
a percentage of a total degree of substitution (DS) of succinoyl less than or equal to 6% at a C6-OH position (%C 6 DS Suc ≦6%) and from 58% to 84% at a C3-OH position (58%<%C 3 DS Suc <84%), and
a percentage of a total DS of acetyl from 33% to 51% at a C6-OH position (33%<%C 6 DS Ac <51%) and from 16% to 20% at the C3-OH position (16% <%C 3 DS Ac <20%).
3. The composition of claim 2 , wherein the drug is a low-solubility drug having a solubility equal to or less than about 0.5 mg/mL in an aqueous solution at a pH from 1 to 8.
4. The composition of claim 3 , wherein the composition comprises a solid amorphous dispersion comprising the low-solubility drug and the polymer.
5. The composition of claim 3 , wherein the composition comprises a physical mixture of the low-solubility drug and the polymer.