DOSAGE FORMS AND METHODS FOR ENANTIOMERICALLY ENRICHED OR PURE BUPROPION
This disclosure relates to dosage forms containing an enantiomerically enriched or pure bupropion such as enantiomeric excess of (S)-bupropion, enantiomerically enriched (S)-bupropion, or enantiomerically pure (S)-bupropion and methods of using these dosage forms. These dosage forms may be administered to human beings in a reduced amount as compared to the amount of racemic bupropion that would be administered in the same situation.
1 . A method of treating a condition that is treatable with racemic bupropion, comprising:
selecting a human being having the condition that is treatable by orally administering a reference dosage form containing a first amount of racemic bupropion at a first dosing frequency; and
orally administering a dosage form containing a second amount of (S)-bupropion that is at least 95% enantiomerically pure at the first dosing frequency to achieve the same therapeutic effect that would be achieved by administering the reference dosage form at the first dosing frequency;
wherein the first dosing frequency is once daily or twice daily; and
wherein the second amount is about 40% to about 60% of the first amount.
2 . The method of claim 1 , wherein the method achieves a C max of (S)-bupropion that is at least 60 ng/mL.
3 . The method of claim 1 , wherein the method is effective in increasing the C max of (S)-bupropion at least 5-fold as compared to the C max of (R)-bupropion that results from administering the same amount of (R)-bupropion to the human being.
4 . The method of claim 1 , wherein the method achieves a C max of (R,R)-hydroxybupropion that is at least about 500 ng/mL in the human being.
5 . The method of claim 1 , wherein the method is effective in increasing the C min of (R,R)-hydroxybupropion at least 3-fold as compared to the C min of (R,R)-hydroxybupropion that results from administering the same amount of (R)-bupropion to the human being.
6 . The method of claim 1 , wherein the dosage form is administered once daily.
7 . The method of claim 1 , wherein the dosage form is administered twice daily.
8 . The method of claim 1 , wherein (R,R)-hydroxybupropion is at least 97% of the total of amount of (R,R)-hydroxybupropion and (S,S)-hydroxybupropion present in the plasma of the human being.
9 . The method of claim 1 , wherein the method achieves a C max of (R,R)-hydroxybupropion that is at least about 500 ng/mL in the human being.
10 . The method of claim 1 , wherein the dosage form is administered for at least 8 consecutive days.
11 . The method of claim 1 , wherein the dosage form is administered for at least 14 consecutive days.
12 . The method of claim 1 , wherein the dosage form is administered for at least 21 consecutive days.
13 . The method of claim 1 , wherein the dosage form contains about 60 mg to about 90 mg of (S)-bupropion.
14 . The method of claim 1 , wherein the dosage form is administered once daily for 1 to 3 consecutive days, then the dosage form is administered twice a day for at least the following 4 to 7 consecutive days, so that the dosage form is administered once daily or twice daily for a total of at least 8 consecutive days.
15 . The method of claim 1 , wherein the dosage form is administered once daily for 1 to 7 consecutive days, then the dosage form is administered twice a day for at least the following 7 consecutive days, so that the dosage form is administered once daily or twice daily for a total of at least 8 consecutive days.
16 . The method of claim 1 , wherein the dosage form contains about 70 mg to about 80 mg of the (S)-bupropion.
17 . A method of treating a condition that is treatable with racemic bupropion, comprising:
selecting a human being having the condition that is treatable by orally administering a reference dosage form containing a first amount of racemic bupropion at a first dosing frequency; and
orally administering a dosage form containing a second amount of (S)-bupropion that is at least 95% enantiomerically pure at the first dosing frequency to achieve the same therapeutic effect that would be achieved by administering the reference dosage form at the first dosing frequency;
wherein the first dosing frequency is once daily or twice daily;
wherein the second amount is about 40% to about 60% of the first amount; and
wherein the method achieves a C max of (S)-bupropion in the human being that is 60 ng/mL to about 140 ng/mL.
18 . The method of claim 1 , wherein the method achieves an AUC 0-12 of (S)-bupropion in the human being that is at least about 400 ng·hr/mL.
19 . The method of claim 1 , wherein the method achieves an AUC 0-12 of (S)-bupropion in the human being that is about 500 ng·hr/mL to about 900 ng·hr/mL.
20 . The method of claim 1 , wherein the dosage form provides sustained release of the (S)-bupropion.
21 . The method of claim 1 , wherein the method achieves a C max of (R,R)-hydroxybupropion in the human being that is at least about 600 ng/mL.
22 . The method of claim 1 , wherein the method achieves an AUC 0-12 of (R,R)-hydroxybupropion in the human being that is at least about 7000 ng·hr/mL.
23 . The method of claim 1 , wherein the method achieves an AUC 0-12 of (R,R)-hydroxybupropion in the human being that is at least about 8000 ng·hr/mL.