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Claims for Patent: 5,733,919

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Claims for Patent: 5,733,919

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 a compound having the formula ##STR1## as 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:08/735,878
Patent Claims: 1. A pharmaceutical composition comprising

a) a pharmaceutically effective amount of a compound having the formula ##STR8## and the pharmaceutically acceptable salts thereof, wherein R.sup.4 is aryl,

C.sub.1-10 alkyl, or

C.sub.1-10 arylalkyl;

R.sup.5 is ##STR9## wherein R.sup.8 is hydroxy or C.sub.1-10 alkyloxy; p is zero or one; and

m is an integer from two to six;

b) a pharmaceutically acceptable amount of a citrate buffer effective to provide a pH of between about 5 and 7; and

c) between about 50-500 milliosmoles of a tonicity adjusting agent.

2. A composition comprising about 0.01-0.5 mg/ml of a compound having the formula ##STR10## and the pharmaceutically acceptable salts thereof, wherein R.sup.4 is aryl,

C.sub.1-10 alkyl, or

C.sub.1-10 arylalkyl;

R.sup.5 is ##STR11## wherein R.sup.8 is hydroxy or C.sub.1-10 alkyloxy; p is zero or one; and

m is an integer from two to six;

about 2-100 mM citrate buffer, between about 50-500 milliosmoles tonicity adjusting agent, and water.

3. A composition of claim 2 comprising about 0.01-0.5 mg/ml of a compound having the formula ##STR12## and the pharmaceutically acceptable salts thereof, wherein R.sup.4 is aryl,

C.sub.1-10 alkyl, or

C.sub.1-10 arylalkyl;

R.sup.5 is ##STR13## wherein R.sup.8 is hydroxy or C.sub.1-10 alkyloxy; p is zero or one; and

m is an integer from two to six;

about 2-20 mM citrate buffer, about 290 milliosmoles tonicity adjusting agent, and water.

4. A pharmaceutical composition of claim 3, wherein the amount of 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid is about 0.05 to about 0.25 mg/ml, and the amount of citrate buffer is about 2-20 mM.

5. A pharmaceutical composition of claim 4, wherein the amount of 2-S-(n-Butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propion ic acid is about 0.25 mg/ml, the amount of citrate buffer is about 10 mM, the amount of tonicity adjusting agent is about 290 milliosmoles, and the pH is about 6.
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