High Concentration Formulations of Opioids and Opioid Derivatives
First Claim
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1. A pharmaceutical formulation comprising:
- an aqueous solvent comprising a low molecular weight carboxylic acid or salt thereof; and
a drug selected from fentanyl and sufentanil;
wherein the drug is present in the formulation at a concentration of at least 100 mg/ml.
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Abstract
The present invention provides opioid formulations suitable for long-term delivery to a subject. The formulation of the invention comprises an opioid or opioid derivative (e.g., morphine, hydromorphone, fentanyl or a fentanyl congener), and an aqueous solvent comprising a low molecular weight carboxylic acid (e.g., C2-4, C2-7). The invention thus provides for formulations comprising morphine, hydromorphone, fentanyl or fentanyl congeners in concentrations significantly in excess of conventional aqueous formulations, e.g., on the order about 2-fold to about 10,000-fold greater than conventional formulations, e.g., currently commercially available formulations.
107 Citations
31 Claims
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1. A pharmaceutical formulation comprising:
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an aqueous solvent comprising a low molecular weight carboxylic acid or salt thereof; and a drug selected from fentanyl and sufentanil;
wherein the drug is present in the formulation at a concentration of at least 100 mg/ml. - View Dependent Claims (2, 3, 4, 5, 8, 9, 25, 29)
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6-7. -7. (canceled)
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10. A pharmaceutical formulation comprising:
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an aqueous solvent comprising a low molecular weight carboxylic acid or salt thereof; and a drug selected from fentanyl and sufentanil;
wherein the molar ratio of carboxylic acid or carboxylic acid salt to drug in the formulation is greater than 1. - View Dependent Claims (11, 12, 13, 14, 16, 17, 27, 30)
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15. (canceled)
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18. A pharmaceutical formulation comprising:
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an aqueous solvent comprising a low molecular weight carboxylic acid or salt thereof; and an opioid or opioid derivative;
wherein the opioid or opioid derivative is present in the formulation at a concentration of at least 100 mg/ml. - View Dependent Claims (19, 20, 21, 22, 24, 28, 31)
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23. (canceled)
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26. (canceled)
Specification