Tablet capable of combatting misuse by injection
Inventors
Herry, Catherine • Contamin, Pauline
Assignees
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Publication Number
US-10987309-B2
Publication Date
2021-04-27
Expiration Date
Abstract
The invention relates to an oral pharmaceutical composition in the form of a sustained-release tablet comprising an active ingredient capable of being misused, which composition makes it possible to combat misuse by injection.
Core Innovation
The invention relates to an oral pharmaceutical composition in the form of a sustained-release matrix tablet intended to prevent misuse by injection of an active ingredient likely to be misused for drug addiction purposes. The background problem is misuse of opioid or psychotropic active ingredients for drug addiction purposes, including attempts to extract active ingredient for parenteral use.
The sustained-release matrix tablet uses a defined excipient system that forms a gel when reduced to powder and dissolved in an injectable volume of an aqueous or hydro-alcoholic solution. The matrix includes polyvinyl acetate and polyvinylpyrrolidone combined with xanthan gum and a carbomer, optionally with a pH stabilizing agent comprising citric acid and/or sodium bicarbonate, and at least one anti-adherent agent.
The composition is characterized by gel viscosity and trapping behavior that prevent misuse by injection, by forming a gel that cannot pass through a needle when the composition is reduced to powder and dissolved in an injectable volume of an aqueous or hydro-alcoholic solution. It further aims to preserve sustained active ingredient release over more than 20 hours while limiting active ingredient extraction in an aqueous medium to lower than 25%.
Claims Coverage
The partial content provides one independent claim. The claim includes six main inventive elements defining an oral sustained-release matrix tablet, a specific polymer and gel-forming excipient blend with defined component ranges, a defined carbomer structure, a pH stabilizing agent defined as citric acid and/or sodium bicarbonate, misuse-by-injection prevention via gel trapping with needle passage resistance and extraction limitation, and sustained-release timing together with mechanical yield strength.
Oral sustained-release matrix tablet for misuse prevention
An oral pharmaceutical composition in the form of a sustained-release matrix tablet, the matrix consisting of 10% to 40% by weight of at least one active ingredient likely to be misused for drug addiction purposes.
Defined excipient blend of PVA/PVP, xanthan gum, carbomer, pH stabilizing agent, and anti-adherent agent
A combination comprising 20% to 60% by weight of a mixture of polyvinyl acetate and polyvinylpyrrolidone, 15% to 25% by weight of xanthan gum, 10% to 30% by weight of a carbomer, 1% to 20% by weight of a pH stabilizing agent, and at least one anti-adherent agent.
Carbomer definition as cross-linked acrylic acid polymer
The carbomer is a polymer of acrylic acid of high molecular weight cross-linked with allyl sucrose or allyl ethers of pentaerythritol.
pH stabilizing agent comprises citric acid and/or sodium bicarbonate
The pH stabilizing agent comprises at least one compound chosen from citric acid and sodium bicarbonate.
Gel trapping that resists needle passage and limits aqueous extraction
The combination prevents misuse by injection by forming a gel trapping the active ingredient and having a viscosity such that the gel cannot pass through a needle when the composition is reduced to powder and dissolved in an injectable volume of an aqueous or hydro-alcoholic solution, and such that the amount of active ingredient extracted in an aqueous medium is lower than 25%.
Sustained release over more than 20 hours with yield strength above 6 MPa
The active principle is released over a period of more than 20 hours, and the tablet has a yield strength higher than 6 MPa.
The core inventive coverage is a sustained-release oral matrix tablet with a defined gel-forming excipient blend and a specifically defined carbomer structure. The claim links these composition features to misuse-by-injection prevention by forming a high-viscosity gel that resists needle passage and limits aqueous extraction, while also requiring sustained release for more than 20 hours and tablet yield strength higher than 6 MPa.
Stated Advantages
Prevents misuse by injection by forming a gel that traps the active ingredient and cannot pass through a needle when the composition is reduced to powder and dissolved in an aqueous or hydro-alcoholic solution.
Limits the amount of active ingredient extracted in an aqueous medium to lower than 25%.
Provides active ingredient release over a period of more than 20 hours.
Provides tablet mechanical strength, with yield strength higher than 6 MPa.
Documented Applications
Oral pharmaceutical composition use as a sustained-release matrix tablet for preventing misuse by injection of active ingredients likely to be misused for drug addiction purposes.
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