Immediate release dosage forms of sodium oxybate
View Patent ↗The present invention provides a pharmaceutical composition, presented as a solid unit dosage form adapted for oral administration of sodium oxybate. The preferred unit dosage form is a tablet comprising a relatively high weight-percentage of sodium oxybate, in combination with a relatively small weight-percentage of total excipients. This permits the tablets to contain/deliver a pharmaceutically effective amount, e.g., about 0.5-1.5 g of sodium oxybate in each tablet with a delivery profile similar to that of the liquid form. The tablets are bioequivalent to the liquid form.
1. A compressed tablet of sodium oxybate for oral delivery of 0.5-1.25 g of sodium oxybate comprising 80-95 wt % sodium oxybate; 5-10 wt % compression aid; and 1-50% binder; wherein the tablet is bioequivalent to sodium oxybate oral solution.
2. The compressed tablet of claim 1 , wherein the tablet is coated to 1-10 wt % gain with a film coating.
3. The compressed tablet of claim 1 , wherein the tablet comprises 80-90 wt % sodium oxybate.
4. The compressed tablet of claim 1 , wherein the tablet does not contain a super-disintegrant.
5. The compressed tablet of claim 1 , wherein the tablet further comprises 0.1-10 wt % of a surfactant.
6. An immediate release unit dosage form comprising an about 0.5-1.5 g compressed tablet comprising 80-95 wt-% sodium oxybate; about 2.5-7.5 wt-% microcrystalline cellulose and about 0.25-2.5 wt-% surfactant, wherein at least 90% of the sodium oxybate is released from the tablet within one hour from exposure of the tablet to an aqueous medium.
7. The unit dosage form of claim 6 , wherein the tablet is coated with a water resistant coating.
8. The unit dosage form of claim 6 , wherein the surfactant is an ionic surfactant.
9. The unit dosage form of claim 6 , further comprising a minor but effective amount of at least one of a second binder, a disintegrant, a glidant and a lubricant.
10. The unit dosage form of claim 9 , further comprising about 0.5-5 wt-% polyvinylpyrrolidone.
11. The unit dosage form of claim 9 , further comprising about 2.5-7.5 wt-% pregelatinized starch.
12. The unit dosage form of claim 9 , further comprising about 0.1-0.75 wt-% silicon dioxide.
13. The unit dosage form of claim 9 , further comprising magnesium stearate.
14. A therapeutic method for treating a human afflicted with narcolepsy, restless leg syndrome, essential tremor, fibromyalgia, or chronic fatigue syndrome by orally administering to said human an effective amount of a unit dosage form of claim 6 .
15. A method for preparing the tablet of claim 1 by granulating a water-free composition comprising the sodium oxybate, the compression and the binder; and compressing the granulated composition to yield said tablet.
16. The method of claim 15 further comprising coating said tablet with a water resistant coating.
17. The method of claim 16 wherein the coating comprises PVA and lecithin.
18. A compressed tablet of an oxybate salt for oral delivery of 0.5-1.25 g of oxybate salt comprising 80-95 wt % oxybate salt; 5-10 wt % compression aid; and 1-50% binder; wherein the tablet is bioequivalent to sodium oxybate oral solution.
19. The tablet of claim 18 wherein the oxybate salt is selected from the group consisting of potassium oxybate, calcium oxybate, lithium oxybate and magnesium oxybate.