Alkaline phosphatase formulations
The present invention provides, in part, formulations comprising an alkaline phosphatase (AP)-based agent. Particularly, modified-release powder formulations comprising an AP-based agent are provided which release a substantial amount of the AP-based agent in the intestines. Therapeutic uses of the formulations are also provided.
1. A formulation comprising an alkaline phosphatase (AP), being in the form of a tablet, comprising:
about 1-10% by weight AP,
about 80-95% by weight polymer, wherein the polymer is hypromellose acetate succinate (HPMCAS),
about 1-10% by weight buffer,
about 0.01-0.1% by weight zinc,
about 0.1-1% by weight magnesium stearate, and
about 1-10% by weight protein stabilizer,
wherein the formulation is compressible and releases the AP in the intestines.
2. The formulation of claim 1 , wherein the AP is released in the small intestine.
3. The formulation of claim 1 , wherein the AP is released in the large intestine.
4. The formulation of claim 1 , wherein the tablet transforms into a gel in the presence of stomach acid.
5. The formulation of claim 1 , wherein the tablet further comprises a poly(methacrylic acid, methylmethacrylate) polymer.
6. The formulation of claim 1 , wherein the tablet comprises:
about 5% by weight AP,
about 87% by weight polymer, wherein the polymer is hypromellose acetate succinate (HPMCAS),
about 2% by weight buffer;
about 0.05% by weight zinc;
about 0.5% by weight magnesium stearate; and
about 5% by weight protein stabilizer.
7. The formulation of claim 1 , wherein the tablet comprises:
5% by weight AP,
87.45% by weight polymer, wherein the polymer is hypromellose acetate succinate (HPMCAS),
2% by weight buffer;
0.06% by weight zinc;
0.49% by weight magnesium stearate; and
5% by weight protein stabilizer.