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Publication Number
US-10716784-B2
Publication Date
2020-07-21
Expiration Date
Abstract
This application describes compounds, compositions, pharmaceutical compositions that can be used in the treatment of, for example, pain and pain related disorders.
Core Innovation
The invention relates to pharmaceutical compositions for treating pain that combine dextromethorphan, or a pharmaceutically acceptable salt thereof, with quinidine, or a pharmaceutically acceptable salt thereof, and an opioid agonist selected from morphine, or a pharmaceutically acceptable salt thereof. The described dosage forms use a defined ratio of dextromethorphan to quinidine to morphine, with the ratio about 1:1:1.
The document further describes dosage form concepts in which dextromethorphan and quinidine are formulated together with morphine for pain treatment, including oral dosage forms and concepts of simultaneous administration. The compositions are described using weight-based component ratios such as opioid:dextromethorphan about 1:1 and opioid:quinidine about 1:0.1 to about 1:1, and tri-component ratios about 1:1:0.1 to about 1:1:1.
The background and disclosure address pain treatment in the context of tolerance, dependence, and withdrawal symptoms, and discuss risk evaluation mitigation strategy avoidance. Purported outcomes include lower effective opioid amount, fewer side effects, increased opioid bioavailability to the brain, longer duration of analgesia, and lower incidence of tolerance, including tri-combination effects compared with two-component combinations.
Claims Coverage
The independent claims are directed to three composition or dosage-form frameworks for treating pain, each centered on the same core active ingredients and an about 1:1:1 ratio. Across the independent claims, the inventive features comprise dextromethorphan with quinidine with morphine, each optionally as pharmaceutically acceptable salts, and the about 1:1:1 dextromethorphan:quinidine:morphine ratio, plus the dosage-form context of treating pain.
Dextromethorphan, quinidine, and morphine at about 1:1:1 ratio for pain treatment
A dosage form for treating pain consisting of dextromethorphan, quinidine, and morphine, each optionally as a pharmaceutically acceptable salt, wherein the ratio of dextromethorphan to quinidine to morphine is about 1:1:1.
Essentials composition of dextromethorphan, quinidine, and morphine at about 1:1:1 ratio
A dosage form for treating pain consisting essentially of dextromethorphan, quinidine, and morphine, each optionally as a pharmaceutically acceptable salt, wherein the ratio of dextromethorphan to quinidine to morphine is about 1:1:1.
Active ingredients set of dextromethorphan, quinidine, and morphine at about 1:1:1 plus excipients
A dosage form for treating pain comprising active ingredients that consist of dextromethorphan, quinidine, and morphine, each optionally as a pharmaceutically acceptable salt, wherein the dextromethorphan to quinidine to morphine is about 1:1:1, and pharmaceutical acceptable excipients.
Overall, the claim coverage centers on pain-treating dosage forms that include dextromethorphan, quinidine, and morphine in an about 1:1:1 ratio; one independent claim specifies the composition as consisting, another as consisting essentially of, and another additionally recites pharmaceutical acceptable excipients.
Stated Advantages
Lower effective opioid amount.
Fewer side effects.
Increased opioid bioavailability to the brain.
Longer duration of analgesia.
Lower incidence of tolerance.
Documented Applications
Treating pain by administering the claimed pharmaceutical dosage forms to a subject.
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