Immediate release formulations and dosage forms of gamma-hydroxybutyrate
The present invention provides a solid immediate release dosage form adapted for oral administration of GHB. The solid immediate release dosage form includes an immediate release formulation comprising a relatively high weight-percentage of GHB with a bioavailability similar to that of a liquid GHB dosage form.
1. An immediate release compressed tablet for oral delivery of GHB, the tablet comprising:
GHB in an amount of about 90-98% by weight;
at least one binder in an amount of about 1-5% by weight;
at least one lubricant in an amount of about 1-5% by weight; and
wherein the tablet releases at least 90% of the GHB contained therein within a period of less than one hour after administration.
2. The compressed tablet of claim 1 , wherein the at least one binder is selected from at least one of hydroxypropyl cellulose, ethylcellulose, hydroxypropyl methylcellulose, polyvinyl alcohol, hydroxyethyl cellulose, povidone, copovidone, pregelatinized starch, dextrin, gelatin, maltodextrin, starch, zein, acacia, alginic acid, carbomers (cross-linked polyacrylates), polymethacrylates, sodium carboxymethylcellulose, guar gum, hydrogenated vegetable oil (type 1), methylcellulose, magnesium aluminum silicate, and sodium alginate.
3. The compressed tablet of claim 1 , wherein the at least one lubricant is selected from at least one of magnesium stearate, stearic acid, calcium stearate, hydrogenated castor oil, hydrogenated vegetable oil, light mineral oil, magnesium stearate, mineral oil, polyethylene glycol, sodium benzoate, sodium stearyl fumarate, and zinc stearate.
4. The compressed tablet of claim 1 , further comprising at least one surfactant, wherein the tablet comprises:
GHB in an amount of about 90-97.5% by weight;
at least one binder in an amount of about 1-4% by weight;
at least one lubricant in an amount of about 1-4% by weight; and
at least one surfactant in an amount of about 0.5-2.0% by weight.
5. The immediate release dosage form of claim 4 , wherein the immediate release formulation is prepared as a solid dosage form comprising an immediate release tablet and the immediate release tablet releases at least 90% of the GHB contained therein within a period of less than one hour after administration.
6. The compressed tablet of claim 4 , wherein the at least one surfactant is selected from at least one of docusate sodium (dioctyl sulfosuccinate sodium salt), sodium lauryl sulfate, a polyoxyethylene alkyl ether, a polyoxyethylene stearate, a poloxamer, a polysorbate, a sorbitan ester, and glyceryl monooleate.
7. An immediate release compressed tablet for oral delivery of a pharmaceutically acceptable salt of GHB, the tablet comprising:
about 90-98% by weight of a pharmaceutically acceptable salt of GHB selected from sodium oxybate and calcium oxybate;
at least one binder in an amount of about 1-5% by weight;
at least one lubricant in an amount of about 1-5% by weight; and
wherein the tablet releases at least 90% of the pharmaceutically acceptable salt of GHB contained therein within a period of less than one hour after administration.
8. The compressed tablet of claim 7 , wherein the at least one binder is selected from at least one of hydroxypropyl cellulose, ethylcellulose, hydroxypropyl methylcellulose, polyvinyl alcohol, hydroxyethyl cellulose, povidone, copovidone, pregelatinized starch, dextrin, gelatin, maltodextrin, starch, zein, acacia, alginic acid, carbomers (cross-linked polyacrylates), polymethacrylates, sodium carboxymethylcellulose, guar gum, hydrogenated vegetable oil (type 1), methylcellulose, magnesium aluminum silicate, and sodium alginate.
9. The compressed tablet of claim 7 , wherein the at least one lubricant is selected from at least one of magnesium stearate, stearic acid, calcium stearate, hydrogenated castor oil, hydrogenated vegetable oil, light mineral oil, magnesium stearate, mineral oil, polyethylene glycol, sodium benzoate, sodium stearyl fumarate, and zinc stearate.
10. The compressed tablet of claim 7 , further comprising at least one surfactant, wherein the tablet comprises:
about 90-97.5% by weight of a pharmaceutically acceptable salt of GHB selected from sodium oxybate and calcium oxybate;
at least one binder in an amount of about 1-4% by weight;
at least one lubricant in an amount of about 1-4% by weight; and
at least one surfactant in an amount of about 0.5-2.0% by weight.
11. The compressed tablet of claim 10 , wherein the at least one surfactant is selected from at least one of docusate sodium (dioctyl sulfosuccinate sodium salt), sodium lauryl sulfate, a polyoxyethylene alkyl ether, a polyoxyethylene stearate, a poloxamer, a polysorbate, a sorbitan ester, and glyceryl monooleate.
12. The compressed tablet of claim 7 , wherein the tablet releases at least 90% of the pharmaceutically acceptable salt of GHB contained therein within a period of less than one hour after administration.
13. The immediate release dosage form of claim 10 , wherein the immediate release formulation is prepared as a solid dosage form comprising an immediate release tablet and the immediate release tablet releases at least 90% of the pharmaceutically acceptable salt of GHB contained therein within a period of less than one hour after administration.
14. A method for treating an individual afflicted with cataplexy and excessive daytime sleepiness associated with narcolepsy, restless leg syndrome, essential tremor, fibromyalgia, or chronic fatigue syndrome, the method comprising:
administering an immediate release formulation for oral delivery of sodium oxybate, the immediate release formulation comprising:
sodium oxybate in an amount of about 90-98% by weight;
at least one binder in an amount of about 1-5% by weight;
at least one lubricant in an amount of about 1-5% by weight; and
wherein the immediate release dosage form releases at least 90% of the GHB contained therein within a period of less than one hour after administration.
15. The method of claim 14 , wherein the at least one binder is selected from at least one of hydroxypropyl cellulose, ethylcellulose, hydroxypropyl methylcellulose, polyvinyl alcohol, hydroxyethyl cellulose, povidone, copovidone, pregelatinized starch, dextrin, gelatin, maltodextrin, starch, zein, acacia, alginic acid, carbomers (cross-linked polyacrylates), polymethacrylates, sodium carboxymethylcellulose, guar gum, hydrogenated vegetable oil (type 1), methylcellulose, magnesium aluminum silicate, and sodium alginate.
16. The method of claim 14 , wherein the at least one lubricant is selected from at least one of magnesium stearate, stearic acid, calcium stearate, hydrogenated castor oil, hydrogenated vegetable oil, light mineral oil, magnesium stearate, mineral oil, polyethylene glycol, sodium benzoate, sodium stearyl fumarate, and zinc stearate.
17. The method of claim 14 , wherein the immediate release formulation comprises:
GHB in an amount of about 90-97.5% by weight;
at least one binder in an amount of about 1-4% by weight;
at least one lubricant in an amount of about 1-4% by weight; and
at least one surfactant in an amount of about 0.5-2.0% by weight.
18. The method of claim 17 , wherein the at least one surfactant is selected from at least one of docusate sodium (dioctyl sulfosuccinate sodium salt), sodium lauryl sulfate, a polyoxyethyelene alkyl ether, a polyoxyethylene stearate, a polaxamer, a polysorbate, a sorbitan ester, and glyceryl monooleate.
19. The method of claim 14 , wherein the immediate release formulation is prepared as a solid dosage form comprising an immediate release tablet and the immediate release tablet releases at least 90% of the GHB contained therein within a period of less than one hour after administration.