Claims for Patent: 4,258,030

Summary for Patent: 4,258,030

Title:	Urokinase preparation for oral administration
Abstract:	Disclosed is a urokinase preparation for oral administration which is effective for remedy of thrombosis such as cerebral thrombosis and cardiac infarction. This preparation comprises urokinase and, incorporated therein, an enzyme inhibitor.
Inventor(s):	Sasaki; Koji (Omiya, JP), Harada; Yasukazu (Tokyo, JP)
Assignee:	Zeria-Shinyaku Kogyo Kabushiki Kaisha (Tokyo, JP)
Application Number:	06/018,240
Patent Claims:	1. A pharmaceutical composition with antithrombotic action for oral administration comprising an effective amount of urokinase and an effective urokinase stabilizing amount of an enzyme inhibitor which is a trypsin inhibitor extractable from human urine selected from the group consisting of mingin, minginin and urine trypsin inhibitor, together with a pharmaceutical carrier. 2. A pharmaceutical composition with antithrombotic action for oral administration comprising an effective amount of urokinase and an effective urokinase stabilizing amount of an enzyme inhibitor which is soybean trypsin inhibitor, together with a pharmaceutical carrier. 3. A pharmaceutical composition with antithrombotic action for oral administration comprising an effective amount of urokinase and an effective urokinase stabilizing amount of an enzyme inhibitor which is aprotinin, together with a pharmaceutical carrier. 4. A pharmaceutical composition with antithrombotic action for oral administration comprising an effective amount of urokinase and an effective urokinase stabilizing amount of an enzyme inhibitor which is selected from the group consisting of .epsilon.-aminocaproic acid, tranexamic acid, .epsilon.-guanidinocaproic acid, p-amidinobenzoic acid and p-guanidinobenzoic acid, together with a pharmaceutical carrier. 5. The pharmaceutical composition as defined in claims 1 or 2 which comprises a ratio of enzyme inhibitor units to urokinase units of from about 1 to about 4. 6. The pharmaceutical composition as defined in claim 3 which comprises a ratio of aprotinin units per urokinase units of from about 1:500 to 1:50. 7. The pharmaceutical composition as defined in claim 6 wherein the ratio is from about 1:100 to about 1:50. 8. The pharmaceutical composition as defined in claim 4 which comprises an amount of from 2.5 to 250 .mu.g of tranexamic acid per 25 units of urokinase. 9. The pharmaceutical composition as defined in claim 5 which comprises an amount of from about 100 to about 200 units of enzyme inhibitor per 50 units of urokinase. 10. The pharmaceutical composition as defined in claim 1, 2, 3 or 4 which is in the form of capsules or tablets. 11. The pharmaceutical composition as defined in claim 10 which is in the form of capsules or tablets coated wuth an enteric coating.

Details for Patent 4,258,030

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Bayer Healthcare Pharmaceuticals Inc.	TRASYLOL	aprotinin	Injection	020304	December 29, 1993	4,258,030	1999-03-07
Microbix Biosystems Inc.	KINLYTIC	urokinase	For Injection	021846	January 16, 1978	4,258,030	1999-03-07