Patent EA-000628-B1 (EA)
Title: Pharmaceutical compositions containing platelet aggregation inhibitors
Inventor: GELOTTE KARL M
IPC: A61K47/02
Filed: 1996-10-23
Abstract: 1. A pharmaceutical composition for intravenous administration to a patient comprising a) a pharmaceutically effective amount of a compound having the formula   and the pharmaceutically acceptable salts thereof, wherein R<4>is aryl, C1-10 alkyl or C1-10 arylalkyl R<5> is   wherein R<8> is hydroxy or C1-10 alkyloxy; p is zero or one; and m is an integer from two to six; and pharmaceutically acceptable salts thereof; b) a pharmaceutically acceptable amount of a citrate buffer effective to provide a pharmaceutically acceptable pH; 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. 2. A pharmaceutical composition of Claim 1 comprising a) a pharmaceutically effective amount of a compound having the formula   and the pharmaceutically acceptable salts thereof, wherein R<4>is aryl, C1-10 alkyl or C1-10 arylalkyl, R<5> is   wherein R<8> is hydroxy or C1-10 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. 3. A composition of Claim 2 comprising about 0.01 -0.5 mg/ml of a compound having the formula   and the pharmaceutically acceptable salts thereof, wherein R<4>is aryl, C1-10 alkyl or C1-10 arylalkyl R<5> is   wherein R<8> is hydroxy or C1-10 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. 4. A composition of Claim 3 comprising about 0.01-0.5 mg/ml of a compound having the formula   and the pharmaceutically acceptable salts thereof, wherein R<4> is aryl, C1-10 alkyl or C1-10 arylalkyl, R<5> is   wherein R<8> is hydroxy or C1-10 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. 5. A pharmaceutical composition of Claim 4, wherein the compound is 2-S-(n-butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propionic acid. 6. A pharmaceutical composition of Claim 5, wherein the amount of 2-S-(n-butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propionic acid is about 0.05 to about 0.25 mg/ml, and the amount of citrate buffer is about 2-20 mM. 7. A pharmaceutical composition of Claim 6, wherein the amount of 2-S-(n-butylsulfonylamino)-3-[4-(4-(piperidin-4-yl)butyloxy)phenyl]propionic acid is about 0.25 mg/ml, the amount of citrate buffer is about 10 mM, the amount oftonicity adjusting agent is about 290 milliosmoles, and the pH is about 6. 8. A method for inhibiting the aggregation of blood platelets in a mammal, comprising intravenously treating the mammal with a pharmaceutically effective amount of the composition of Claim 1. 9. A method of Claim 8 where the mammal is a human. 10. A method for inhibiting the aggregation of blood platelets in a mammal, comprising intravenously treating the mammal with a pharmaceutically effective amount of the composition of Claim 7. 11. A method of Claim 10 where the mammal is a human.