Process for synthesis and incorporation of nitric oxide donors in macromolecular compositions

Backlog Materiais, Metalurgia Produtos farmacêuticos Química

Process for synthesis and incorporation of nitric oxide donors in macromolecular compositions

NOVELTY – The device for the synthesis of S-nitrosothiols and incorporation of freshly synthesized S-nitrosothiol in biocompatible hydrophilic macromolecular compositions for medical or pharmaceutical applications e.g. stimulation of blood flow, comprises a reaction compartment containing an acid aqueous solution, two storage compartments to enclose separately a nitrosable thiol in the solid form and a nitrite salt in the solid form, and a formulation compartment containing a macromolecular matrix. The macromolecular matrix is either coupled to or uncoupled from the reaction compartment. USE – The device is useful for the synthesis of S-nitrosothiols and incorporation of freshly synthesized S-nitrosothiol in biocompatible hydrophilic macromolecular compositions for medical or pharmaceutical applications such as stimulation of blood flow, blood vessel dilatation, treatment of vascular insufficiencies, treatment of Raynaud’s syndrome, modification of skin pigmentation, promotion and acceleration of skin, muscle, tendon, ligament, mucosa, bone and corneal wound healing, prevention of necrosis, treatment de eczemas and arthritis, systemic lupus erythematosus and cutaneous leishmaniasis (claimed). ADVANTAGE – The device allows effective and economical synthesis of active S-nitrosothiols and their subsequent incorporation in hydrophilic macromolecular compositions immediately before the topical application thus increasing their thermal stability. DETAILED DESCRIPTION – The device for the synthesis of S-nitrosothiols and incorporation of freshly synthesized S-nitrosothiol in biocompatible hydrophilic macromolecular compositions for medical or pharmaceutical applications e.g. stimulation of blood flow, comprises a reaction compartment containing an acid aqueous solution, two storage compartments to enclose separately a nitrosable thiol in the solid form and a nitrite salt in the solid form, and a formulation compartment containing a macromolecular matrix. The macromolecular matrix is either coupled to or uncoupled from the reaction compartment. The formulation promotes: the contact of the nitrosable thiol and nitrite salt with the acid aqueous solution enclosed in the reaction compartment using a first mechanical action thus forming an S-nitrosothiol through an immediate S-nitrosation reaction; and the incorporation of the freshly synthesized S-nitrosothiol to the macromolecular matrix using a second mechanical action thus resulting in a pharmaceutical formulation in the form of viscous solution or hydrogel appropriate useful in topical medical or pharmaceutical applications. The acid aqueous solution is employed in a sufficient amount to dissolve the nitrosable thiol and the nitrite salt, and yield the synthesis of S-nitrosothiol in 1-6 pH range. The reaction compartment encloses water in a sufficient amount to dissolve the acid salt of the nitrosable thiol and the nitrite salt. The amount of nitrite salt is in excess in relation to the molar quantity of the nitrosable thiol. The macromolecular components are already crosslinked or undergo crosslinking by the action of an agent. The resulting formulation is a liquid or a hydrogel, which is appropriate to topical application, and jellifies after contact with the tissue to be treated. The storage and/or formulation compartments comprise agents of conserving, buffering and colorant, dispersing agents and/or metal complexants. An INDEPENDENT CLAIM is included for a formulation presented as a viscous liquid solution with an incorporated S-nitrosothiol. DESCRIPTION OF DRAWING(S) – The figure shows a device for synthesis of S-nitrosothiols. Sections. (1, 2, 3, 4)

Main Application Field

A96 (Medical, dental, veterinary, cosmetic.); B05 (Other organics – aromatics, aliphatic, organo-metallics, compounds whose substituents vary such that they would be classified in several of B01 – B05.); B07 (General – tablets, dispensers, catheters (excluding drainage and angioplasty), encapsulation etc, but not systems for administration of blood or saline or IV feeding etc.); D22 (Sterilising, bandages, dressing and skin protection agents – including sterilising agents (other than for food), sutures, plaster casts, bioactive prostheses, contact lenses, diapers, animal litter, timber, preservatives, disinfectants, bactericidal detergents, deodorants, insect repellent compounds, moth proofers, sheep dip (A61L).)

INVENTORS:

PACHECO OGARI
MOREIRA ROBERTO
SEABRA AMEDEA
SOUZA GABRIELA
OLIVEIRA MARCELO

121_FERIDAS

Patent number: WO2008031182-A1;BR200603802-A;US2009311292-A1

PATENT STATUS:

For information contact Inova Unicamp

FOR ADDITIONAL INFORMATION:

parcerias@inova.unicamp.br

+55 (19) 3521-5207 / 2607

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