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1. (WO1998051290) LOCAL ANESTHETIC FORMULATIONS COMPRISING A SITE 1 SODIUM CHANNEL BLOCKER COMBINED WITH A SECOND ACTIVE AGENT
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1998/051290 International Application No.: PCT/US1998/009991
Publication Date: 19.11.1998 International Filing Date: 15.05.1998
Chapter 2 Demand Filed: 16.12.1998
IPC:
A61K 9/00 (2006.01) ,A61K 9/16 (2006.01) ,A61K 31/505 (2006.01) ,A61K 31/52 (2006.01) ,A61K 31/55 (2006.01) ,A61K 31/57 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
14
Particulate form, e.g. powders
16
Agglomerates; Granulates; Microbeadlets
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
52
Purines, e.g. adenine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
56
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
57
substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane, progesterone
Applicants:
CHILDREN'S MEDICAL CENTER CORPORATION [US/US]; 300 Longwood Avenue Boston, MA 02115, US
BRIGHAM AND WOMEN'S HOSPITAL, INC. [US/US]; 75 Francis Street Boston, MA 02115, US
Inventors:
KOHANE, Daniel, S.; US
BERDE, Charles, B.; US
STRICHARTZ, Gary, R.; US
LANGER, Robert, S.; US
Agent:
PABST, Patrea, L.; Arnall Golden & Gregory, LLP 2800 One Atlantic Center 1201 West Peachtree Street Atlanta, GA 30309-3450, US
Priority Data:
60/046,16316.05.1997US
60/046,68316.05.1997US
60/046,76116.05.1997US
60/053,46223.07.1997US
Title (EN) LOCAL ANESTHETIC FORMULATIONS COMPRISING A SITE 1 SODIUM CHANNEL BLOCKER COMBINED WITH A SECOND ACTIVE AGENT
(FR) FORMULATIONS ANESTHESIQUES LOCALES
Abstract:
(EN) Combinations of naturally occurring site 1 sodium channel blockers, such as tetrodotoxin (TTX), saxitoxin (STX), decarbamoyl saxitoxin, and neosaxitoxin (referred to jointly herein as 'toxins'), with other agents, have been developed to give long duration block with improved features, including safety and specificity. In one embodiment, duration of block is greatly prolonged by combining a toxin with a local anesthetic, vasoconstrictor, glucocorticoid, and/or adrenergic drugs, both alpha agonists (epinephrine, phenylephrine), beta-blockers (propranalol), and mixed central-peripheral alpha-2 agonists (clonidine), or other agents. In another embodiment, the duration of nerve block from toxin can be greatly enhanced by the inclusion of amphiphilic or lipophilic solvents. In still another embodiment, the effectiveness of these compositions is enhanced by microencapsulation within polymeric carriers, preferably biodegradable synthetic polymeric carriers. Modality specific nerve block can be obtained using combinations of toxin with vanilloids.
(FR) Cette invention se rapporte à des combinaisons d'agents bloquants des canaux sodiques du site 1, tels que la tétrodotoxine (TTX), la saxitoxine (STX), la décarbamyl-saxitoxine et la néosaxitoxine (conjointement ci-après dénommées 'toxines'), ainsi que d'autres agents, lesdites combinaisons ayant été mises au point pour assurer un blocage de longue durée associé à des caractéristiques perfectionnées, telles que la sécurité et la spécificité. Selon une réalisation, on accroît considérablement la durée du blocage en combinant une toxine à un anesthésique local, un vasoconstricteur, un glucocorticoïde et/ou des médicaments adrénergiques, deux alpha agonistes conjoints (l'épinéphrine, la phényléphrine), des bêtabloquants (le propanadol), et des alpha-2 agonistes mélangés des systèmes centraux et périphériques (la clonidine) ou d'autres agents. Selon une autre réalisation, il est possible d'allonger considérablement la durée du blocage nerveux provoqué par une toxine en incluant des solvants amphiphiles ou lipophiles. Dans une autre réalisation, on accroît l'efficacité de ces compositions en procédant à leur microencapsulation au sein de supports polymères, de préférence des supports polymères synthétiques biodégradables. Il est possible de parvenir à un blocage nerveux spécifique au moyen de combinaison de toxines et de vanilloïdes.
Designated States: AU, CA, JP
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
AU1998073890