Neosaxitoxin combination formulations for prolonged local anesthesia
First Claim
1. A method of treating or preventing pain in an adult in need thereof comprising administering an effective amount to a human in need thereof of a dosage unit for treatment or prevention of pain in an awake, sedated or anesthetized adult human comprising an effective amount of neosaxitoxin, a local anesthetic selected from the group consisting of bupivacaine, levobupivacaine, tetracaine, and ropivacaine in a concentration range between 0.1% (1 mg/ml) and 0.5% (5 mg/ml), and epinephrine in a concentration range between 2 mcg/ml (1:
- 500,000) and 10 mcg/ml (1;
100,000), to produce a minimum effective concentration at the site of administration to treat or prevent pain or provide local anesthesia.
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Abstract
Since each of the site I sodium channel blockers have a unique activity and cannot be used to extrapolate the same effective dosage for another site I sodium channel blocker, studies were conducted to identify dosages of neosaxitoxin (“NeoSTX”) and bupivacaine, alone or in combination with epinephrine, to provide two to three days of pain relief in humans. Bupivacaine-NeoSTX combinations produce more reliable blockade and longer duration blockade compared to NeoSTX alone. The three-way combination of NeoSTX-bupivacaine-epinephrine produces more prolonged local anesthesia than the two-way combination of NeoSTX-bupivacaine. Addition of epinephrine to this NeoSTX-bupivacaine combination dramatically prolongs the duration of complete blockade to a mechanical stimulus. These results led to development of specific combination dosage formulations.
56 Citations
12 Claims
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1. A method of treating or preventing pain in an adult in need thereof comprising administering an effective amount to a human in need thereof of a dosage unit for treatment or prevention of pain in an awake, sedated or anesthetized adult human comprising an effective amount of neosaxitoxin, a local anesthetic selected from the group consisting of bupivacaine, levobupivacaine, tetracaine, and ropivacaine in a concentration range between 0.1% (1 mg/ml) and 0.5% (5 mg/ml), and epinephrine in a concentration range between 2 mcg/ml (1:
- 500,000) and 10 mcg/ml (1;
100,000), to produce a minimum effective concentration at the site of administration to treat or prevent pain or provide local anesthesia. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
- 500,000) and 10 mcg/ml (1;
Specification