IMMEDIATE RELEASE FORMULATIONS OF d-LYSERGIC ACID DIETHYLAMIDE FOR THERAPEUTIC APPLICATIONS
A solid oral immediate release formulation of LSD, including LSD contained within a dosage form of a capsule, tablet, or orally disintegrating tablet. A method of making a solid oral immediate release formulation of LSD as a free base or in a salt form by granulation, including moisture-activated dry granulation or dry blending. A method of treating an individual, by administering a solid oral immediate release formulation of LSD and treating the individual.
1 . A composition of a solid oral immediate release formulation of LSD, comprising LSD contained within an immediate release dosage form chosen from the group consisting of a capsule, tablet, and orally disintegrating tablet, wherein said composition is produced by a method chosen from the group consisting of granulation and dry blending.
2 . The composition of claim 1 , wherein said LSD is in a form chosen from free base and salt and wherein said LSD is present in an amount of 0.01-1 mg.
3 . The composition of claim 2 , wherein said LSD is in a salt form and the salt is chosen from the group consisting of hydrochloride, hydrobromide, maleate, tartrate, citrate, phosphate, fumarate, sulfate, mesylate, acetate, and oxalate.
4 . The composition of claim 1 , wherein said composition is produced by granulation and further including a filler chosen from the group consisting of lactose, mannitol, dicalcium phosphate, calcium sulfate, starch, cellulose, kaolin, sodium chloride, sorbitol, trehalose, and sucrose, a binder chosen from the group consisting of acacia gum, hydroxypropyl methylcellulose, hydroxypropyl cellulose, tragacanth, polyvinyl pyrrolidone (PVP), and starch, an absorbent chosen from the group consisting of croscarmellose sodium, starch, mesoporous silicon dioxide, and microcrystalline cellulose, a disintegrant chosen from the group consisting of croscarmellose sodium, starch, microcrystalline cellulose, crospovidone, and sodium starch glycolate, a glidant chosen from the group consisting of magnesium stearate and colloidal silicon dioxide, a lubricant chosen from the group consisting of magnesium stearate, sodium stearyl fumarate, polyethylene glycol (PEG), polyoxyethylene stearates, lauryl sulphate salts, talc, glyceryl behenate, stearic acid, glyceryl palmitostearate, calcium stearate, and hydrogenated vegetable oils.
5 . The composition of claim 1 , wherein said composition is produced by granulation and further including an agent for adjusting pH chosen from the group consisting of citrate, phosphate, acetate, sodium hydroxide, and hydrochloric acid.
6 . The composition of claim 1 , wherein said composition is produced by granulation and further including an antioxidant chosen from the group consisting of ascorbic acid, butylated hydroxyanisole (BHA), and butylated hydroxytoluene (BHT).
7 . The composition of claim 1 , wherein said composition is produced by granulation and further including a photostabilization agent, a permeation enhancer chosen from the group consisting of sulphoxides, azones, pyrrolidones, alcohols, alkanols, glycols, surfactants, and terpenes, and coloring agents, sweeteners, and flavoring agents.
8 . The composition of claim 1 , wherein said composition is produced by dry blending and further including a filler chosen from the group consisting of lactose, mannitol, dicalcium phosphate, calcium sulfate, starch, cellulose, kaolin, sodium chloride, sorbitol, and sucrose, a glidant chosen from the group consisting of magnesium stearate and colloidal silicon dioxide, a dry binder of microcrystalline cellulose, and a disintegrant chosen from the group consisting of croscarmellose sodium, starch, microcrystalline cellulose, crospovidone, and sodium starch glycolate.
9 . A method of making a solid oral immediate release formulation of LSD, including the steps of:
granulating LSD with excipients of fillers, absorbents, binders, disintegrants, lubricants, and/or glidants; and
encapsulating or compressing to form a tablet of a solid oral immediate release formulation of LSD.
10 . The method of claim 9 , wherein said granulating step is further defined as moisture activated dry granulation and includes charging powders of LSD, binders, and fillers to a closed container which contains mixing/blending components, wetting the powders with a binder solution/suspension while mixing allowing for particle cohesion and granule growth, and adding fillers, glidants, disintegrants, and lubricants.
11 . The method of claim 9 , wherein the LSD is in a form chosen from free base and salt.
12 . The method of claim 9 , wherein the filler is chosen from the group consisting of lactose, mannitol, dicalcium phosphate, calcium sulfate, starch, cellulose, kaolin, sodium chloride, sorbitol, trehalose, and sucrose, wherein the binder is chosen from the group consisting of acacia gum, hydroxypropyl methylcellulose, hydroxypropyl cellulose, tragacanth, polyvinyl pyrrolidone (PVP), and starch, wherein the absorbent is chosen from the group consisting of croscarmellose sodium, starch, mesoporous silicon dioxide, and microcrystalline cellulose, wherein the disintegrant is chosen from the group consisting of croscarmellose sodium, starch, microcrystalline cellulose, crospovidone, and sodium starch glycolate, and wherein the glidant is chosen from the group consisting of magnesium stearate and colloidal silicon dioxide.
13 . The method of claim 10 , wherein the lubricant is chosen from the group consisting of magnesium stearate, sodium stearyl fumarate, polyethylene glycol (PEG), polyoxyethylene stearates, lauryl sulphate salts, talc, glyceryl behenate, stearic acid, glyceryl palmitostearate, calcium stearate, and hydrogenated vegetable oils.
14 . The method of claim 9 , wherein the LSD is in a salt form and the salt is chosen from the group consisting of hydrochloride, hydrobromide, maleate, tartrate, citrate, phosphate, fumarate, sulfate, mesylate, acetate, and oxalate.
15 . A method of making a solid oral immediate release formulation of LSD by dry blending, including the steps of:
blending LSD minimally with filler excipients and additionally a disintegrant, dry binder, glidant and lubricant; and
a forming step chosen from the group consisting of directly compressing to form a tablet or orally disintegrating tablet (ODT) of a solid oral immediate release formulation of LSD and encapsulating to form a solid oral immediate release formulation of LSD.
16 . The method of claim 15 , wherein the filler is chosen from the group consisting of lactose, mannitol, dicalcium phosphate, calcium sulfate, starch, cellulose, kaolin, sodium chloride, sorbitol, trehalose, and sucrose, wherein the dry binder is microcrystalline cellulose, wherein the disintegrant is chosen from the group consisting of croscarmellose sodium, starch, microcrystalline cellulose, crospovidone, and sodium starch glycolate, wherein the glidant is chosen from the group consisting of magnesium stearate and colloidal silicon dioxide, and wherein the lubricant is chosen from the group consisting of magnesium stearate, sodium stearyl fumarate, polyethylene glycol (PEG), polyoxyethylene stearates, lauryl sulphate salts, talc, glyceryl behenate, stearic acid, glyceryl palmitostearate, calcium stearate, and hydrogenated vegetable oils.
17 . The method of claim 15 , wherein the LSD is in a form chosen from free base and salt.
18 . The method of claim 15 , wherein the LSD is in a salt form and the salt is chosen from the group consisting of hydrochloride, hydrobromide, maleate, tartrate, citrate, phosphate, fumarate, sulfate, mesylate, acetate, and oxalate.