Tamper-resistant pharmaceutical compositions of opioids and other drugs
Inventors
Rariy, Roman V. • Fleming, Alison • Hirsh, Jane C. • Saim, Said • Varanasi, Ravi K.
Assignees
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Publication Number
US-10004729-B2
Publication Date
2018-06-26
Expiration Date
Abstract
Tamper-resistant pharmaceutical compositions have been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opioids. The tamper-resistant compositions retard the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is passes through the GI tract.
Core Innovation
The invention provides a tamper resistant pharmaceutical composition comprising a plurality of substantially spherical solid particles. Each particle comprises one or more drugs prone to abuse, one or more waxes or wax-like substances, and one or more fatty acids, with the particles having a median particle size (D(0.5)) between about 200 microns and about 400 microns.
The composition is configured so that, after oral administration as directed, a therapeutically effective amount of drug is released over a period of 6-24 hours. The drug is oxycodone or a pharmaceutically acceptable salt thereof, and the molar ratio of fatty acid to drug is about 6:1 to about 15:1.
The composition maintains a slow release of drug even if the particles are crushed with a mortar and pestle and snorted. The invention also encompasses a method of treating pain by administering a therapeutically effective amount of the same tamper resistant pharmaceutical composition to a human subject in need thereof.
Claims Coverage
The partial content includes two independent claims. The inventive subject matter centers on substantially spherical tamper resistant particles containing an abuse-prone drug with waxes or wax-like substances and fatty acids, specified particle size and fatty acid-to-drug ratio, 6-24 hour oral release, and maintained slow release after crushing and snorting; a second claim applies the composition to pain treatment.
Tamper resistant spherical particle composition with waxes and fatty acids
A tamper resistant pharmaceutical composition comprising a plurality of substantially spherical solid particles, each particle comprising one or more drugs prone to abuse, one or more waxes or wax-like substances, and one or more fatty acids, with a median particle size (D(0.5)) between about 200 microns and about 400 microns and a molar ratio of fatty acid to drug of about 6:1 to about 15:1, wherein the drug is oxycodone or a pharmaceutically acceptable salt thereof and a therapeutically effective amount of drug is released over 6-24 hours after oral administration as directed, maintaining slow release even if the particles are crushed with a mortar and pestle and snorted.
Method of treating pain using the tamper resistant composition
A method of treating pain comprising administering to a human subject in need thereof a therapeutically effective amount of a tamper resistant pharmaceutical composition comprising a plurality of substantially spherical particles, each particle comprising one or more drugs prone to abuse, one or more waxes or wax-like substances, and one or more fatty acids, with a median particle size (D(0.5)) between about 200 microns and about 400 microns, a molar ratio of fatty acid to drug of about 6:1 to about 15:1, wherein the drug is oxycodone or a pharmaceutically acceptable salt thereof, with therapeutically effective drug release over 6-24 hours after oral administration as directed, and maintaining slow release even if the particles are crushed with a mortar and pestle and snorted.
The independent claims cover the tamper resistant oral formulation defined by substantially spherical particles containing an abuse-prone drug, waxes or wax-like substances, and fatty acids, with specified size and molar ratio parameters, and the corresponding pain-treatment method.
Stated Advantages
Provides slow release of oxycodone over 6-24 hours after oral administration as directed.
Maintains slow release of drug even if the particles are crushed with a mortar and pestle and snorted.
Documented Applications
Treating pain by administering a human subject a therapeutically effective amount of the tamper resistant pharmaceutical composition.
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