Neosaxitoxin combination formulations for prolonged local anesthesia
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A01N-043/40
A61K-031/445
A61K-031/519
A61K-031/137
A61K-031/52
출원번호
US-0331983
(2014-07-15)
등록번호
US-8975281
(2015-03-10)
발명자
/ 주소
Berde, Charles
Kohane, Daniel S.
출원인 / 주소
The Children's Medical Center Corporation
대리인 / 주소
Pabst Patent Group LLP
인용정보
피인용 횟수 :
0인용 특허 :
35
초록▼
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 epinephri
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.
대표청구항▼
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,
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. 2. The method of claim 1 wherein the human is awake. 3. The method of claim 1 comprising administrating a high volume of a formulation of between 0.5 and 1.8 ml/kg for children, comprising Bupivacaine in a concentration range between 0.1% (1 mg/ml) and 0.25% (2.5 mg/ml), giving a total systemic bupivacaine dose of no more than 2.5 mg/kg;NeoSTX in a concentration range from 0.1 mcg/ml-1 mcg/ml, giving a total systemic dose of 0.05-1.5 mcg/kg, andEpinephrine in a concentration range between 2 mcg/ml (1:500,000) and 10 mcg/ml (1:100,000). 4. The method of claim 3 comprising administering an effective amount by infiltration of multiple layers of a large surgical wound for a full-length open laparotomy, thoraco-abdominal incision, or flank incision in a child in need thereof. 5. The method of claim 3 comprising administering an effective amount for esophago-gastrectomy, nephrectomy, or large abdominal cancer surgeries in a child in need thereof. 6. The method of claim 3 comprising administering an effective amount for wound infiltration for total hip replacement or total knee replacement in a child in need thereof. 7. The method of claim 1 for medium volume use of 15 to 50 ml comprising providing a formulation containing Bupivacaine in a concentration range of 0.125%-0.3% (1.25-3 mg/ml), giving a systemic dose of no more than 2 mg/kg in children,NeOSTX in a concentration range from 0.2-2 mcg/ml, giving a systemic dose of 0.1-1.5 mcg/kg in children, andEpinephrine in a concentration range from 0-10 mcg/ml (<1:100,000). 8. The method of claim 7 comprising administering an effective amount for peripheral nerve blocks or plexus blocks. 9. The method of claim 7 comprising administering an effective amount for infiltration. 10. The method of claim 7 comprising administering an effective amount for shoulder, hand or arm surgery, infiltration or ilio-inguinal/ilio-hypogastric blocks for inguinal hernia repair, penile block for hypospadias repair, femoral block for total knee replacement or anterior cruciate ligament repair, intercostal nerve blocks for open chest surgery, or femoral and sciatic nerve blocks for leg amputation or foot and ankle surgery. 11. The method of claim 10 comprising performing a femoral nerve block, lumbar plexus block or lower volume sciatic block. 12. The method of claim 7 comprising administering the formulation to provide anesthesia for surgery for periods of between 3 and 12 hours, analgesia after surgery for at least 24 hours, and recovery from motor block to permit some strength in limb movement within 24 to 48 hours after administration.
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