COMPOSITIONS COMPRISING METHYLPHENIDATE-PRODRUGS, PROCESSES OF MAKING AND USING THE SAME
The present technology is directed to d-threo-methylphenidate conjugates and a composition comprising d-threomethylphenidate conjugated to nicotinoyl-L-serine, or salt thereof. The present technology also relates to a composition comprising at least one conjugate of d-methylphenidate having at least two or more chiral centers. The composition is optically active. The present technology additionally relates to oral formulations and pharmaceutical kits comprising at least one d-threo-methylphenidate conjugate.
1 . A method of treating a patient having Attention Deficit Hyperactivity Disorder (ADHD), comprising orally administering to the patient a pharmaceutically effective amount of a composition comprising serdexmethylphenidate and dexmethylphenidate in an amount of 26.1 mg serdexmethylphenidate and 5.2 mg dexmethylphenidate.
2 . The method of claim 1 , wherein the serdexmethylphenidate has the following structure
3 . The method of claim 1 , wherein the serdexmethylphenidate is in the form of serdexmethylphenidate chloride, and wherein the 26.1 mg serdexmethylphenidate is equivalent to 28 mg serdexmethylphenidate chloride.
4 . The method of claim 3 , wherein the serdexmethylphenidate chloride has the following structure
5 . The method of claim 1 , wherein the dexmethylphenidate is in the form of dexmethylphenidate hydrochloride, and wherein the 5.2 mg dexmethylphenidate is equivalent to 6 mg dexmethylphenidate hydrochloride.
6 . The method of claim 1 , wherein the combined molar does of serdexmethylphenidate and dexmethylphenidate is equivalent to 20 mg of dexmethylphenidate hydrochloride.
7 . The method of claim 6 , wherein the 20 mg of dexmethylphenidate hydrochloride is equivalent to 17.3 mg dexmethylphenidate free base.
8 . The method of claim 1 , wherein the composition is in the form of a capsule or tablet.
9 . The method of claim 8 , wherein the capsule is an immediate release capsule.
10 . The method of claim 8 , wherein the capsule or tablet is contained in a blister pack, roll, or bulk bottle.
11 . The method of claim 8 , wherein the capsule or tablet is administered as a dosage of 1 capsule or tablet every day.
12 . A method of treating a patient having Attention Deficit Hyperactivity Disorder (ADHD), comprising orally administering to the patient a pharmaceutically effective amount of a composition comprising serdexmethylphenidate and dexmethylphenidate in an amount of 39.2 mg serdexmethylphenidate and 7.8 mg dexmethylphenidate.
13 . The method of claim 12 , wherein the serdexmethylphenidate has the following structure
14 . The method of claim 12 , wherein the serdexmethylphenidate is in the form of serdexmethylphenidate chloride, and wherein the 39.2 mg serdexmethylphenidate is equivalent to 42 mg serdexmethylphenidate chloride.
15 . The method of claim 14 , wherein the serdexmethylphenidate chloride has the following structure
16 . The method of claim 12 , wherein the dexmethylphenidate is in the form of dexmethylphenidate hydrochloride, and wherein the 7.8 mg dexmethylphenidate is equivalent to 9 mg dexmethylphenidate hydrochloride.
17 . The method of claim 12 , wherein the combined molar does of serdexmethylphenidate and dexmethylphenidate is equivalent to 30 mg of dexmethylphenidate hydrochloride.
18 . The method of claim 17 , wherein the 30 mg of dexmethylphenidate hydrochloride is equivalent to 25.9 mg dexmethylphenidate free base.
19 . The method of claim 12 , wherein the composition is in the form of a capsule or tablet.
20 . The method of claim 19 , wherein the capsule is an immediate release capsule.
21 . The method of claim 19 , wherein the capsule or tablet is contained in a blister pack, roll, or bulk bottle.
22 . The method of claim 19 , wherein the capsule or tablet is administered as a dosage of 1 capsule or tablet every day.
23 . A method of treating a patient having Attention Deficit Hyperactivity Disorder (ADHD), comprising orally administering to the patient a pharmaceutically effective amount of a composition comprising serdexmethylphenidate and dexmethylphenidate in an amount of 52.3 mg serdexmethylphenidate and 10.4 mg dexmethylphenidate.
24 . The method of claim 23 , wherein the serdexmethylphenidate has the following structure
25 . The method of claim 23 , wherein the serdexmethylphenidate is in the form of serdexmethylphenidate chloride, and wherein the 52.3 mg serdexmethylphenidate is equivalent to 56 mg serdexmethylphenidate chloride.
26 . The method of claim 25 , wherein the serdexmethylphenidate chloride has the following structure
27 . The method of claim 23 wherein the dexmethylphenidate is in the form of dexmethylphenidate hydrochloride, and wherein the 10.4 mg dexmethylphenidate is equivalent to 12 mg dexmethylphenidate hydrochloride.
28 . The method of claim 23 , wherein the combined molar does of serdexmethylphenidate and dexmethylphenidate is equivalent to 40 mg of dexmethylphenidate hydrochloride.
29 . The method of claim 28 , wherein the 40 mg of dexmethylphenidate hydrochloride is equivalent to 34.6 mg dexmethylphenidate free base.
30 . The method of claim 23 , wherein the composition is in the form of a capsule or tablet.
31 . The method of claim 30 , wherein the capsule is an immediate release capsule.
32 . The method of claim 30 , wherein the capsule or tablet is contained in a blister pack roll, or bulk bottle.
33 . The method of claim 30 , wherein the capsule or tablet is administered as a dosage of 1 capsule or tablet every day.