Alza Corporation

Societe De Conseils De Recherches Et D'applications Scientifiques

Other

Peter W Ramwell

Marie L Foegh

Pierre Braquet

Jane E Shaw

Hideo Shio

A method for inhibiting blood vessel blockage in a mammal particularly after a procedure such as angioplasty, an arterial bypass operation or an allograft transplant operation which comprises: administering to a mammal before, during and/or after the procedure an effective blood vessel blockage inhibiting amount of an octapeptide having the formula ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl), or R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; A.sub.3 is CH.sub.2 A.sub.6 (where A.sub.6 is pentafluorophenyl, naphthyl, pyridyl, or phenyl); A.sub.4 is o-, m- or, more preferably, p-substituted X-Phe (where X is a halogen, H, NH.sub.2, NO.sub.2, OH , or C.sub.1-13 alkyl), pentafluoro-Phe, or .beta.-Nal; A.sub.5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile; A.sub.7 is Thr, Trp, or .beta.-Nal (and can be either the D- or L-isomer); and Z is NH.sub.2 or OH; or a pharmaceutically acceptable salt thereof.

Method for inhibiting blood vessel blockage using octapeptide

This invention is directed to the use of thromboxane as an early indicator for coronary artery thrombosis (acute myocardial infarction), and assays for detecting thromboxane B.sub.2 or a metabolite of TXB.sub.2 or TXA.sub.2.

Thromboxane B.sub.2 assay for coronary artery thrombosis

A living tissue or living cell preservation solution comprising an effective amount of a ginkgolide to reduce reperfusion injury in living tissue which has been stored therein and a substance or mixture or substances present in an amount sufficient to produce an osmotic pressure in said solution approximately equal to the osmotic pressure or mammalian cell and a method for preventing or reducing reperfusion injury in transplanted mammalian organs, which comprises contacting an organ prior to reperfusion with an effective amount of a ginkgolide to reduce reperfusion injury in said organ.

Use of ginkgolides to prevent reperfusion injury in organ transplantation

An intrauterine device for administering drug locally to the uterus at a controlled rate for a prolonged period of time is disclosed. The device contains a body of polymer capable of bioeroding in the environment of the uterus over a prolonged period of time. This body has the drug dispersed throughout so that as the body gradually bioerodes, it slowly releases the dispersed drug. In a preferred embodiment, the device releases a uterine contraction-inducing prostaglandin locally to the uterus at a controlled rate over a prolonged period of time.

Intrauterine device that bioerodes in response to the environment of the

Polymeric materials having at least one exposed surface rendered as a release means for platelet aggregation inhibiting agent by serving as a reservoir for release of aggregation inhibiting prostaglandin. The polymeric surface can also be both platelet aggregation agent releasing and non-thrombogenic agent releasing by having together on the polymeric surface an aggregation inhibiting prostaglandin and an anti-coagulant which are easily released from the surface when in close contact with the blood, plasma or platelets.

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McLean, VA, United States of America

Peter W Ramwell