Sensory-specific local anesthesia and prolonged duration local anesthesia
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A01N-037/18
A61K-031/165
C07C-233/00
C07C-235/00
C07C-237/00
C07C-239/00
출원번호
US-0993622
(2009-05-19)
등록번호
US-8609733
(2013-12-17)
국제출원번호
PCT/US2009/044549
(2009-05-19)
§371/§102 date
20101119
(20101119)
국제공개번호
WO2009/143175
(2009-11-26)
발명자
/ 주소
Kohane, Daniel S.
Sagie, Itay
출원인 / 주소
Massachusetts Institute of Technology
대리인 / 주소
Pabst Patent Group LLP
인용정보
피인용 횟수 :
0인용 특허 :
8
초록▼
Combinations of charged local anesthetics with chemical permeation enhancers have been developed to give long duration block which is selective for sensory block over motor block. The duration of block is greatly prolonged by combining the local anesthetic with a permeation enhancer. The selectivity
Combinations of charged local anesthetics with chemical permeation enhancers have been developed to give long duration block which is selective for sensory block over motor block. The duration of block is greatly prolonged by combining the local anesthetic with a permeation enhancer. The selectivity of sensory over motor block is provided by selecting the concentration of the local anesthetic and the permeation enhancer to provide selective permeability of the sensory and motor neurons to the enhancer.
대표청구항▼
1. A method for selective sensory nerve blockade comprising administering a combination of effective amounts of a charged local anesthetic selected from the group consisting of local anesthetics of Formula I: where R1-R5 are independently selected from linear or branched alkyl groups, and a chemica
1. A method for selective sensory nerve blockade comprising administering a combination of effective amounts of a charged local anesthetic selected from the group consisting of local anesthetics of Formula I: where R1-R5 are independently selected from linear or branched alkyl groups, and a chemical permeation enhancer selected from the group consisting of sulfoxide decylmethylsulfoxide (C10MSO); diethylene glycol monoethyl ether, dekaoxyethylene-oleylether, diethylene glycol monomethyl ethers; sodium lauryl sulfate (SLS), sodium octyl sulfate (SOS), dodecyltriethylammonium bromide (DDAB), octyltriethylammonium bromide (OTAB), and polysorbate,in a suitable pharmaceutically acceptable carrier to selectively increase or prolong the duration of sensory block, without affecting motor block. 2. The method of claim 1 wherein the local anesthetic comprises an excipient having a pH rendering the local anesthetic charged. 3. The method of claim 1 further comprising administering the local anesthetic and chemical permeation enhancer with a vasoconstrictor. 4. The method of claim 1 wherein the local anesthetic is selected from the group of QX-314((N-(2,6)dimethylphenylcarbamoylmethyl triethylammonium bromide); and QX-222(2-((2,6-dimethylphenyl)amino)-N,N,N-trimethyl-2-oxoethanaminium). 5. The method of claim 1 wherein the chemical penetration enhancer is sodium lauryl sulfate (SLS), sodium octyl sulfate (SOS), dodecyltriethylammonium bromide (DDAB), or octyltriethylammonium bromide (OTAB). 6. The method of claim 1 wherein the chemical permeation enhancer is selected from the group consisting of polysorbate 80 and polysorbate 20. 7. The method of claim 1 wherein the local anesthetic and chemical permeation enhancer are administered as a bolus dosage unit. 8. The method of claim 1 wherein the local anesthetic and chemical permeation enhancer are administered in a continuous or sustained release formulation. 9. The method of claim 1 wherein the local anesthetic and chemical permeation enhancer are administered in a topical or aerosol formulation. 10. The method of claim 1 wherein the local anesthetic and chemical permeation enhancer is administered by injection. 11. A composition for selective sensory nerve blockade comprising a combination of effective amounts of a charged local anesthetic selected from the group consisting of local anesthetics of Formula I: where R1-R5 are independently selected from linear or branched alkyl groups, and a chemical permeation enhancer selected from the group consisting of sulfoxide decylmethylsulfoxide (C10MSO); diethylene glycol monoethyl ether, dekaoxyethylene-oleylether, diethylene glycol monomethyl ethers; sodium lauryl sulfate (SLS), sodium octyl sulfate (SOS), dodecyltriethylammonium bromide (DDAB), octyltriethylammonium bromide (OTAB), and polysorbate,in a suitable pharmaceutically acceptable carrier to selectively increase or prolong the duration of sensory block, without affecting motor block. 12. The composition of claim 11 wherein the local anesthetic comprises an excipient having a pH rendering the local anesthetic charged. 13. The composition of claim 11 further comprising administering the local anesthetic and chemical permeation enhancer with a vasoconstrictor. 14. The composition of claim 11 wherein the local anesthetic is a selected from the group of QX-314((N-(2,6)dimethylphenylcarbamoylmethyl triethylammonium bromide); and QX-222 (2-((2,6-dimethylphenyl)amino)-N,N,N-trimethyl2-oxoethanaminium). 15. The composition of claim 11 wherein the chemical penetration enhancer is sodium lauryl sulfate (SLS), sodium octyl sulfate (SOS), dodecyltriethylammonium bromide (DDAB), or octyltriethylammonium bromide (OTAB). 16. The composition of claim 11 wherein the chemical permeation enhancer is selected from the group consisting of polysorbate 80 and polysorbate 20. 17. The composition of claim 11 in a bolus dosage unit. 18. The composition of claim 11 in a continuous or sustained release formulation. 19. The composition of claim 11 in a topical or aerosol formulation. 20. The composition of claim 11, wherein the pH of the formulation is from about 3 to about 8. 21. The composition of claim 20, wherein the pH of the composition is about 4.5 to about 7.5. 22. The composition of claim 11, further comprising an effective amount of a site I sodium channel blocker. 23. The composition of claim 22 wherein the site I sodium channel blocker is saxitoxin, decarbamoyl saxitoxin, or neosaxitoxin. 24. The composition of claim 23 wherein the local anesthetic is an amino-amide or amino-ester local anesthetics or derivatives thereof. 25. The composition of claim 23 wherein the site I sodium channel blocker is neosaxitoxin and the local anesthetic is QX-314. 26. The method of claim 1, further comprising administering an effective amount of a site I sodium channel blocker. 27. The method of claim 26, wherein the site I sodium channel blocker is saxitoxin, decarbamoyl saxitoxin, or neosaxitoxin. 28. The method of claim 27 wherein the site I sodium channel blacker is neosaxitoxin and the local anesthetic is QX-314. 29. The method of claim 1 wherein the pH of the composition is from about 3 to about 8. 30. The method of claim 1 wherein the pH is from about 4 to about 7.5.
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이 특허에 인용된 특허 (8)
Kohane Daniel S. ; Berde Charles B. ; Strichartz Gary ; Langer Robert S., Local anesthetic formulations.
Patel Dinesh C. (Murray UT) Chang Yunik (Lakewood NJ), Penetration enhancement with binary system of oleic acid, oleins, and oleyl alcohol with lower alcohols.
Sanders Harold F. (Palo Alto CA) Cheng Yu-Ling (Cupertino CA) Enscore David J. (Saratoga CA) Libicki Shari B. (Palo Alto CA), Transdermal drug composition with dual permeation enhancers.
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