High concentration local anesthetic formulations
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/167
A61K-031/245
A61K-031/445
A61K-031/47
A61K-009/00
A61K-009/06
출원번호
US-0401088
(2012-02-21)
등록번호
US-9370500
(2016-06-21)
발명자
/ 주소
Campbell, James N.
Michaelis, Arthur F.
출원인 / 주소
Centrexion Therapeutics Corporation
대리인 / 주소
Goodwin Procter LLP
인용정보
피인용 횟수 :
0인용 특허 :
35
초록▼
A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effe
A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effective in the painful area or immediately adjacent areas, to ameliorate or eliminate the pain. High concentration of local anesthetic in solution in the carrier is used to drive rapid release and uptake of the drug. Relief is typically obtained for a period of several hours.
대표청구항▼
1. A method of treating pain, comprising topically administering an effective amount of a formulation to a site in need thereof to treat the pain, wherein the formulation comprises a free base caine alkaloid local anesthetic in an amount of about 40% by weight of the formulation,the formulation is a
1. A method of treating pain, comprising topically administering an effective amount of a formulation to a site in need thereof to treat the pain, wherein the formulation comprises a free base caine alkaloid local anesthetic in an amount of about 40% by weight of the formulation,the formulation is a non-aqueous gel,the free base caine alkaloid local anesthetic is lidocaine free base, andthe free base caine alkaloid local anesthetic is released into the skin for at least three hours to provide pain relief at or near the site of administration without systemic toxicity. 2. The method of claim 1 providing an initial burst release within two hours of administration. 3. The method of claim 1 providing an initial burst release within four hours of administration. 4. The method of claim 1 providing an initial burst release within six hours of administration. 5. The method of claim 1 providing an initial burst release within eight hours of administration. 6. The method of claim 1 providing an initial burst release within twelve hours of administration. 7. The method of claim 1 for administration to wounds, abrasions, or burns. 8. The method of claim 1, wherein the local anesthetic is lidocaine free base in a gel comprising propylene glycol, dehydrated alcohol, isopropyl myristate, diethylene glycol monoethyl ether, and hydroxypropylcellulose. 9. The method of claim 8, wherein the concentration of propylene glycol is from about 1% to about 20% w/w, the concentration of dehydrated alcohol is about 18.80% w/w, the concentration of isopropyl myristate is about 10% w/w, the concentration of diethylene glycol monoethyl ether is about 10% w/w and hydroxypropyl cellulose is about 1.2%. 10. The method of claim 9, wherein the local anesthetic is lidocaine free base in a gel comprising about 20% w/w propylene glycol. 11. The method of claim 10, wherein the local anesthetic is lidocaine free base in a gel comprising 20% w/w propylene glycol, 18.80% w/w dehydrated alcohol, 10% w/w isopropyl myristate, 10% w/w diethylene glycol monoethyl ether and 1.2% w/w hydroxypropylcellulose. 12. The method of claim 1 wherein the free base caine alkaloid local anesthetic is present in an amount of 40% by weight of the formulation. 13. The method of claim 1 wherein the formulation comprises diglycol monoethyl ether and propylene glycol. 14. The method of claim 13 wherein the formulation comprises ethanol and hydroxypropyl cellulose. 15. The method of claim 14 wherein the formulation comprises isopropyl myristate. 16. The method of claim 14 wherein the formulation comprises dimethyl isosorbide. 17. The method of claim 1 wherein the formulation is a gel containing 40% w/w lidocaine free base, 20% w/w diglycol monoethyl ether, 10% w/w propylene glycol, 10% w/w dimethyl isosorbide, 18.80% w/w ethanol, and 1.2% w/w hydroxypropyl cellulose. 18. The method of claim 1 wherein the formulation is a gel containing 40% w/w lidocaine free base, 10% w/w isopropyl myristate, 10% w/w diglycol monoethyl ether, 20% w/w propylene glycol, 18.80% w/w ethanol, and 1.2% w/w hydroxypropyl cellulose. 19. The method of claim 1, wherein the pain is neuropathic pain. 20. The method of claim 17, wherein the pain is neuropathic pain. 21. The method of claim 18, wherein the pain is neuropathic pain. 22. The method of claim 14, wherein the pain is neuropathic pain. 23. The method of claim 15, wherein the pain is neuropathic pain. 24. The method of claim 16, wherein the pain is neuropathic pain. 25. The method of claim 19, wherein the method comprises topically administering the formulation to a wound. 26. The method of claim 20, wherein the method comprises topically administering the formulation to a wound. 27. The method of claim 21, wherein the method comprises topically administering the formulation to a wound. 28. The method of claim 22, wherein the method comprises topically administering the formulation to a wound. 29. The method of claim 23, wherein the method comprises topically administering the formulation to a wound. 30. The method of claim 1, wherein the pain is non-neuropathic pain. 31. The method of claim 15, wherein the pain is non-neuropathic pain. 32. The method of claim 16, wherein the pain is non-neuropathic pain.
연구과제 타임라인
LOADING...
LOADING...
LOADING...
LOADING...
LOADING...
이 특허에 인용된 특허 (35)
Richard R. Jackson ; John N. Williams, Anesthetizing plastics, drug delivery plastics, and related medical products, systems and methods.
Kanios David P. ; Gentile Joseph A. ; Mantelle Juan A. ; Sablotsky Steven, Compositions and methods for topical administration of pharmaceutically active agents.
Caldwell Larry J. (4146 Cranford Cir. San Jose CA 95124) Galer Bradley Stuart (7409 Woodlawn Ave. NE Seattle WA 98115), Method for treating headache pain with topical local anesthetic compositions.
Miranda Jesus (Miami FL) Sablotsky Steven (Miami FL), Solubility parameter based drug delivery system and method for altering drug saturation concentration.
Miranda Jesus (Miami FL) Sablotsky Steven (Miami FL), Solubility parameter based drug delivery system and method for altering drug saturation concentration.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.