This technology is available from Temarex Corporation.



Inventor(s): D. Smith, W. Rao

Disclosure 275 U.S. Patent not yet issued

This invention generally relates to biodegradable polymers useful as carriers of pharmaceutical compounds and as degradation agents. More specifically, the present invention relates to biodegradable, water-soluble polyester resins, preferably a poly(butanediol spermate) (PBS) compound, containing derivatized secondary amine groups capable of carrying pharmaceutical compounds such as nitric oxide (NO).

This innovation addresses industry's need for a readily degradable, biocompatible, "high" molecular weight polymer capable of site-specific and controlled delivery of a pharmaceutical compound within an organism.

Currently, biodegradable polymers are one of the most common types of carriers used in controlled drug delivery systems. In regards to prior art "low" molecular weight polymers must be chemically manipulated to prevent their absorption into the bloodstream because quick absorption can cause cytotoxicity. Also, "low" molecular weight polymers tend to degrade quickly, thus inhibiting their ability to provide controlled delivery over a significant period of time. At the other end of the continuium, "High" molecular weight carriers are also known. However, these carriers tend to take a long time to degrade and be cleared from the body. This innovation overcomes the limitations of these low and high molecular weight polymer systems.

Several objectives that this invention addresses are: (a) a carrier that is capable of delivering and releasing a biologically active moiety or other agent to a site-specific area within the body; (b) a carrier that releases a pharmaceutical compound then quickly biodegrades, at various pH levels following release, into biologically inert and naturally occurring compounds found within the biological systems of mammals and then readily removed from the body without accumulation; (c) a compound that has numerous amine sites in the backbone for derivatization; (d) a compound that can be inserted into a polymer to facilitate the degradation of the polymer; (e) a method for controlling the rate of pharmaceutical release by the amount of pharmaceutical loading; (f) a method of controlling the rate of degradation by the amount of pharmaceutical loading.

Suitable pharmaceutical compounds envisioned are those that can react with secondary amine groups and can be loaded onto the carrier such as amino acids, peptides, proteins, enzyme inhibitors, nucleic acids, and other naturally occurring products. A particularly preferred pharmaceutical is NO which has many biological effects, and its site-specific delivery has many uses including, for example, vasodilation and suppression of an immune response to an implant.

Other applications suitable for the present invention include: (a) incorporation into a cross-linked, urine absorbing polymer, such as a polysaccharide, thereby rendering soluble an otherwise insoluble polymer, such as found in a diaper (i.e. make toilet flushable) or hospital bed mats; (b) disposable garments, mats\runners, dust clothes and the like (i.e. medical, industrial, etc.); (c) synthetic supports for the growth of cells for artificial organs; (d) coatings on medical devices.



Inventor(s): D.J. Smith, D.C. Roselle

Disclosure 274 U.S. Patent not yet issued

This invention relates to novel composition of matter for pharmaceutical use comprising molecules capable of delivering nitric oxide (NO) to specific sites with the body. The molecules are lipophilic, biodegradable, biocompatable, and preferably degrade into naturally occurring products.

Also provided is a method for synthesizing such compositions, as well as a method of using such compositions in pharmaceutical applications.

The NO donor molecules of the present invention are in improvement over the existing art by delivering such NO donor molecules to specific sites within the body.

NO donor molecules of the present invention can be used in a multitude of pharmaceutical uses wherein the delivery of NO is desired in human and animal species. Some site specific areas capable of being treated with NO are bronchial airways, stomach, internal organs as well as artificial or synthetic grafts, FDA approved medical devices via use of atomizers, tablets, topical creams or ointments.



Inventor(s): D. Smith, D. Chakravarthy, L. Keefer

Disclosure 233-CIP U.S. Patent 5,691,423

A polymeric composition capable of releasing nitric oxide, in a controlled manner for effective dosing, comprises a polysaccharide including a nitric-oxide releasing N2O2- functional group bound to the polymer; pharmaceutical compositions including the polymeric composition; and methods for treating biological disorders in which dosage with nitric oxide is beneficial.

The composition can be used as is and\or incorporated into implants, injectables, condoms, prosthesis coatings, patches, and the like for use in a wide variety of medical applications such as pulmonary disorders, impotence in men (i.e. male erectile dysfunction), reduce clotting.