Neosaxitoxin combination formulations for prolonged local anesthesia
First Claim
1. A method of use comprising administering an effective amount of a dosage unit for treatment or prevention of pain in an awake, sedated or anesthetized human child 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 a human child in need thereof to treat or prevent pain or provide local anesthesia.
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Accused Products
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.
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12 Claims
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1. A method of use comprising administering an effective amount of a dosage unit for treatment or prevention of pain in an awake, sedated or anesthetized human child 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 a human child in need thereof 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