Abuse deterrent solid dosage form for immediate release with functional score
View Patent ↗The present disclosure provides an immediate release, abuse deterrent pharmaceutical solid dosage form comprising at least one functional score. In particular, the immediate release, abuse deterrent solid dosage form comprises at least one low molecular weight hydrophilic polymer, at least one high molecular weight hydrophilic polymer, and an effervescent system.
1. A pharmaceutical solid dosage form comprising at least one active pharmaceutical ingredient (API) or a pharmaceutically acceptable salt thereof, at least one low molecular weight hydrophilic polymer, at least one high molecular weight hydrophilic polymer, and an effervescent system, wherein the solid dosage form comprises at least one score, provides immediate release of the API, and breaks into a plurality of particles having an average diameter of greater than about 250 microns rather than a fine powder when crushed, ground, or pulverized, and wherein contact with a suitable solvent leads to formation of a viscous gel.
2. The pharmaceutical solid dosage form of claim 1 , wherein the score is a functional score.
3. The pharmaceutical solid dosage form of claim 1 , wherein the solid dosage form has one score, with the score on either an upper surface or a lower surface.
4. The pharmaceutical solid dosage form of claim 1 , wherein the solid dosage form has two scores, with a first score on an upper surface and a second score on a lower surface.
5. The pharmaceutical solid dosage form of claim 1 , wherein the solid dosage form is a tablet, optionally having an oval shape.
6. The pharmaceutical solid dosage form of claim 1 , wherein the solid dosage form further comprises a film coating.
7. The pharmaceutical solid dosage form of claim 1 , wherein, upon splitting the solid dosage form to yield split solid dosage portions, the split solid dosage portions have a loss of mass of less than about 3.0% and a friability of no more than about 1.0%.
8. The pharmaceutical solid dosage form of claim 7 , wherein the split solid dosage portions have an in vitro dissolution rate of at least about 70% of the API within 45 minutes when measured using an USP approved procedure.
9. The pharmaceutical solid dosage form of claim 7 , wherein the split solid dosage portions have an in vitro dissolution rate of at least about 80% of the API within 30 minutes when measured using an USP approved procedure.
10. The pharmaceutical solid dosage form of claim 1 , wherein the API is an opioid or a combination of an opioid and a non-opioid analgesic.
11. The pharmaceutical solid dosage form of claim 10 , wherein the opioid is oxycodone, oxymorphone, hydrocodone, hydromorphone, codeine, or morphine.
12. The pharmaceutical solid dosage form of claim 1 , wherein the low molecular weight hydrophilic polymer has an average molecular weight of no more than about 250,000 Daltons; the low molecular weight hydrophilic polymer is polyethylene oxide, hydroxypropyl methylcellulose, sodium carboxymethylcellulose, polyethylene glycol, a Poloxamer, or a combination thereof; and the low molecular weight hydrophilic polymer is present in an amount from about 5% to about 50% by weight of the solid dosage form.
13. The pharmaceutical solid dosage form of claim 1 , wherein the high molecular weight hydrophilic polymer has an average molecular weight of at least about 400,000; the high molecular weight hydrophilic polymer is polyethylene oxide, hydroxypropyl cellulose, hydroxypropyl methylcellulose, xanthan gum, or a combination thereof; and the high molecular weight hydrophilic polymer is present in an amount from about 0.1% to about 30% by weight of the solid dosage form.
14. The pharmaceutical solid dosage form of claim 1 , wherein the effervescent system comprises an acid component and a base component; the acid component is an organic acid, an inorganic acid, or a combination thereof; the base component is an alkali metal bicarbonate, an alkaline earth metal bicarbonate, an alkali metal carbonate, an organic carbonate, or a combination thereof; and the effervescent system is present in an amount from about 20% to about 90% by weight of solid dosage form.
15. The pharmaceutical solid dosage form of claim 1 , wherein the solid dosage form is a tablet; the low molecular weight hydrophilic polymer has an average molecular weight of no more than about 250,000 Da and is present in an amount from about 20% to about 40% by weight of the solid dosage form; the high molecular weight hydrophilic polymer has an average molecular weight of at least about 400,000 Da and is present in an amount from about 2% to about 10% by weight of the solid dosage form; the effervescent system comprises an acid component and a base component and is present in an amount from about 50% to about 70% by weight of the solid dosage form; and the API is oxycodone, oxymorphone, hydrocodone, hydromorphone, codeine, or morphine.
16. The pharmaceutical solid dosage form of claim 15 , wherein the low molecular weight hydrophilic polymer is polyethylene oxide, hydroxypropyl methylcellulose, sodium carboxymethylcellulose, polyethylene glycol, a Poloxamer, or a combination thereof; the high molecular weight hydrophilic polymer is polyethylene oxide, hydroxypropyl cellulose, hydroxypropyl methylcellulose, xanthan gum, or a combination thereof; the acid component of the effervescent system is an organic acid; and the base component of the effervescent system is an alkali metal bicarbonate, an alkali metal carbonate, or a combination thereof.
17. The pharmaceutical solid dosage form of claim 16 , wherein the API is oxycodone, oxymorphone, hydrocodone, hydromorphone, codeine, or morphine.
18. The pharmaceutical solid dosage form of claim 17 further comprising a film coating.
19. The pharmaceutical solid dosage form of claim 1 , wherein the suitable solvent is water, an alcohol, an acid, a fruit juice, or a combination thereof.