Orally disintegrating tablet formulation for enhanced bioavailability
In some aspects of the present invention is a formulation comprising a solid dispersion or intimate mixture of a poorly water soluble drug and an ionic polymer surprisingly exhibiting fast disintegration of tablet.
1. An orally disintegrating tablet comprising:
an amorphous solid dispersion comprising a hot-melt extrudate comprising a poorly water soluble drug and an ionic polymer,
wherein the poorly water soluble drug is selected from the group consisting of: megestrol, ziprasidone, eszopiclone, sumatriptan, and pharmaceutically acceptable salts thereof, and wherein the ionic polymer is selected from the group consisting of:
a copolymer of methacrylic acid, ethyl acrylate, and methyl methacrylate;
hypromellose acetate succinate; and
a copolymer of dimethylaminoethyl methacrylate, butyl methacrylate, and methyl methacrylate; and
wherein the ionic polymer is present in an amount of at least 45% by weight of the amorphous solid dispersion,
wherein the poorly water soluble drug and the ionic polymer are present in a drug-to-polymer weight ratio of between 20:80 and 40:60,
wherein the amount of poorly water soluble drug in amorphous form is present in the amount of at least 80% by weight of the poorly water soluble drug, and
wherein the tablet disintegrates in water within 40 seconds.
2. The orally disintegrating tablet of claim 1 , wherein the poorly water soluble drug is megestrol or a pharmaceutically acceptable salt thereof.
3. The orally disintegrating tablet of claim 1 , wherein an amount of the ionic polymer is at least about 55% by weight of said dispersion.
4. The orally disintegrating tablet of claim 1 , wherein an amount of the ionic polymer is at least about 65% by weight of said dispersion.
5. The orally disintegrating tablet of claim 1 , wherein the poorly water soluble drug is ziprasidone or a pharmaceutically acceptable salt thereof.
6. The orally disintegrating tablet of claim 1 , wherein the poorly water soluble drug is eszopiclone or a pharmaceutically acceptable salt thereof.
7. The orally disintegrating tablet of claim 1 , wherein the poorly water soluble drug is sumatriptan or a pharmaceutically acceptable salt thereof.
8. The orally disintegrating tablet of claim 1 , wherein the poorly water soluble drug and the ionic polymer are present in a drug-to-polymer weight ratio of 20:80, and wherein the tablet disintegrates within 40 seconds.
9. The orally disintegrating tablet of claim 1 , wherein the poorly water soluble drug and the ionic polymer are present in a drug-to-polymer weight ratio of 40:60, and wherein the tablet disintegrates within 30 seconds.