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Generated: September 22, 2017

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Title: Compositions for inhibiting platelet aggregation
Abstract:The invention is a pharmaceutical composition for intravenous administration to a patient comprising a) a pharmaceutically effective amount of 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid; b) a pharmaceutically acceptable amount of a citrate buffer effective to provide a pH of between about 5 and 7; and c) a pharmaceutically acceptable amount of a tonicity adjusting agent effective to make the formulation substantially isotonic with the osmotic pressure of the biological system of the patient.
Inventor(s): Gelotte; Karl M. (North Wales, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:08/965,922
Patent Claims: 1. An aqueous pharmaceutical composition for intravenous administration to a patient comprising

a) a compound which is 2-(S)-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propi onic acid or a pharmaceutically acceptable salt thereof;

b) a concentration of a citrate buffer buffer effective to provide a pharmaceutically acceptable pH;

c) a concentration of a tonicity adjusting agent effective to make the formulation substantially isotonic with the osmotic pressure of the biological system of the patient.

2. A pharmaceutical composition of claim 1, wherein the compound is 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid, and the concentration of citrate buffer is about 2-20 mM.

3. A composition of claim 2, wherein the concentration of 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid or a salt thereof is about 0.05 to about 0.25 mg/ml.

4. A composition of claim 2, wherein the concentration of 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid is about 0.25 mg/ml, the concentration of citrate buffer is about 10 mM, the concentration of tonicity adjusting agent is sufficient to achieve a solution osmolarity of about 290 mOsmol/L, and the pH is about 6.

5. A composition of claim 3, wherein the concentration of 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid or salt thereof is about 0.05 mg/ml, the concentration of citrate buffer is about 10 mM, the concentration of tonicity adjusting agent is sufficient to achieve a solution osmolarity of about 290 mOsmol/L, and the pH is about 6.

6. A method for inhibiting the aggregation of blood platelets in a mammal, comprising intravenously treating the mammal with a therapeutically effective amount of the composition of claim 2.

7. A method of claim 6 where the mammal is a human.

8. A method for inhibiting the aggregation of blood platelets in a mammal, comprising intravenously treating the mammal with a therapeutically effective amount of the composition of claim 1.

9. A method of claim 8 where the mammal is a human.

10. A composition of claim 1 comprising a concentration of a citrate buffer effective to provide a pH of between about 5 and 7, and a concentration of a tonicity adjusting agent sufficient to achieve a solution osmolarity of between about 50-500 mOsmol/L.

11. A composition of claim 10 comprising about 0.01-0.5 mg/ml of the compound, or a pharmaceutically acceptable salt thereof, about 2-100 mM citrate buffer, and a concentration of a tonicity adjusting agent sufficient to achieve a solution osmolarity of between about 50-500 mOsmol/L.

12. A composition of claim 11 comprising about 2-20 mM citrate buffer, and a concentration of a tonicity adjusting agent sufficient to achieve a solution osmolarity of about 290 mOsmol/L.

13. A composition of claim 1 wherein the compound is 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid or a salt thereof in a concentration of about 0.25 mg/ml, the concentration of citrate buffer is about 10 mM, the concentration of tonicity adjusting agent is sufficient to achieve a solution osmolality of about 316 mOsmol/kg, and the pH is about 6.

14. A composition of claim 1 wherein the compound is 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid or a salt thereof in a concentration of about 0.05 mg/ml, the concentration of citrate buffer is about 10 mM, the concentration of osmolality of about 315 mOsmol/kg, and the pH is about 6.

15. A composition prepared by mixing

a) an amount of 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid hydrochloride salt sufficient to obtain a final solution 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid concentration of between 0.01 mg/ml and 0.5 mg/ml;

b) an amount of sodium citrate and an amount of citric acid sufficient to obtain a final solution pH of between 5 and 7; and

c) an amount of tonicity adjusting agent sufficient to provide solution osmolarity of between about 50 and 500 mOsmol/L.

16. A composition of claim 15, wherein the amount of 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid hydrochloride salt is sufficient to obtain a final solution 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid concentration of between 0.05 mg/ml and 0.25 mg/ml.

17. A composition of claim 15, wherein the amount of sodium citrate and the amount of citric acid is sufficient to obtain a pH of between about 5.8 and 6.2.

18. A composition of claim 15, wherein the amount of tonicity adjusting agent is sufficient to provide solution osmolarity of about 290 mOsmol/L.

19. A composition of claim 15, wherein

a) the amount of 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid hydrochloride salt is sufficient to obtain a final solution 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl}propion ic acid concentration of about 0.05 mg/ml;

b) the amount of sodium citrate and an amount of citric acid is sufficient to obtain a final solution pH of about 6; and

c) the amount of tonicity adjusting agent is sufficient to provide solution osmolarity of about 290 mOsmol/L.

20. A composition of claim 15, wherein

a) the amount of 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid hydrochloride salt is sufficient to obtain a final solution 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid concentration of about 0.25 mg/ml;

b) the amount of sodium citrate and an amount of citric acid is sufficient to obtain a final solution pH of about 6; and

c) the amount of tonicity adjusting agent is sufficient to provide solution osmolarity of about 290 mOsmol/L.

21. A composition prepared by mixing

a) an amount of 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid hydrochloride salt is sufficient to obtain a final solution 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid concentration of about 0.25 mg/ml;

b) an amount of sodium citrate and an amount of citric acid is sufficient to obtain a final solution pH of about 6; and

c) an amount of tonicity adjusting agent is sufficient to provide solution osmolality of about 316 mOsmol/kg.

22. A composition prepared by mixing

a) an amount of 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid hydrochloride salt is sufficient to obtain a final solution 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl}propion ic acid concentration of about 0.05 mg/ml;

b) an amount of sodium citrate and an amount of citric acid is sufficient to obtain a final solution pH of about 6; and

c) an amount of tonicity adjusting agent is sufficient to provide solution osmolality of about 315 mOsmol/kg.
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