Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1995-09-18
1999-06-15
MacMillan, Keith D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514330, 514544, 514626, 514817, 424489, 426450, A61K 3116, A61K 31445, A61K 916, A23B 403
Patent
active
059122714
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to a novel pharmaceutical preparation for use as a local anaesthetic for topical administration, to the use of said preparation and to a process for preparing said preparation.
BACKGROUND OF THE INVENTION
EMLA.RTM. cream is the only product on the market giving anaesthesia of intact skin. EMLA.RTM. cream is administered to the skin under occlusion for 60 minutes. In order to obtain faster onset of anaesthesia other local anaesthetic agents and vehicle systems have been tested (Refs. Freeman, et al., Pediatr. Anaesthesia 1993:3, 129). For tetracaine, an old well-known topical anaesthetic agent, there are several patent applications for different formulations, among them a cream and a patch (Refs. Woolfson and McCafferty, WO 88/09169 and Smith & Nephew, EP 0175609 respectively). WO 88/09169 discloses an onset time of approximately 30 minutes for the tetracaine cream and EP 0175609 discloses an onset time of approximately 30-45 minutes for the tetracaine patch. None of these formulations are so far on the market.
PRIOR ART
WO 93/19736 discloses a pharmaceutical composition containing a defined lipid system of at least two lipid components, at least one being amphiphatic and polar and one being non polar, and wherein the active agent is lidocaine. The problem that has been solved according to WO 93/19736 is the considerable difficulties in overcoming the poor bioabsorption of lidocaine.
WO 94/00127 discloses application of lipids and lipid formulations for the treatment of skin and mucous membrane diseases or disorders displaying epidermal hyperproliferation and disruptions of the barrier function.
EP 455528 discloses cosmetic and dermopharmaceutical. compositions containing vesicles of a mixture of phospholipids and glycolipids.
FR 2692781 discloses a cosmetic composition containing sphingomyelin from milk or fish.
JP 05163153 discloses a sphingolipid composition, solving the problem with malodour and discoloration, giving a stable composition during storage. The sphingolipid composition can be used as a cosmetic base and in the field of medicines, e.g. as emulsion. stabilisers, percutaneous promoting agents etc. The lipids are extracted from the brain.
OUTLINE OF THE INVENTION
BRIEF DESCRIPTION OF THE DRAWING
FIG. 1 is a graph showing the solid fat content in the triacylglycerol used, as determined by solid-phase NMR.
We have now surprisingly found that the problem mentioned above, namely to obtain faster onset of anaesthesia, can be solved by the new pharmaceutical preparation according to the present invention. The object of the invention is thus to provide a novel, clinically and pharmaceutically acceptable preparation for dermal pain management.
By using the pharmaceutical preparation according to the invention it is possible to achieve pain relief with a faster onset of anaesthesia than what is possible to achieve with classical topical anaesthetic agents. Another advantage with the pharmaceutical preparation according to the invention is that it is less skin irritating than topical local anaesthetic formulations according to the prior art. Still another advantage is that the hydrolysis of ester compounds such as tetracaine seem to be much slower in the lipid vehicle than in conventional formulations.
The pharmaceutical preparation according to the present invention comprises the following ingredients:
The amount of the local anaesthetic is in the range 1-40%, preferably 5-10%. The amount of the polar lipid is in the range 1-40%, preferably 1-10%. The amount of the triacylglycerol is in the range 60-95%, preferably 50-85%. The amount of water is 0-95%, preferably 0-20%. All percentages are given as the percentage by weight of the total weight of the pharmaceutical preparation.
The local anaesthetic can be selected from tetracaine, lidocaine, prilocaine, mepivacaine, lidocaine/prilocaine, tetracaine/lidocaine, and other local anaesthetics and combinations thereof.
The polar lipid is preferably a sphingolipid. The sphingolipid can be cerami
REFERENCES:
patent: 4610868 (1986-09-01), Fountain et al.
patent: 5635205 (1997-06-01), Nyqvist et al.
Freeman et al., "Topical Anaesthesia of the Skin: A Review," Pediatr. Anaesthesia 3:129-138 (1993).
Jackson et al., "Anesthetics Alter the Lipid Composition of Barley-Root Membranes," Planta 162:415-421 (1984).
Matsuzaki et al ., "Development of a Model Membrane System Using Stratum Corneum Lipids for Estimation of Drug Skin Permeability," Chem. Pharm. Bull. 41:575-579 (1993).
English language abstract of document AL1, WPI accession No. 86-071058/11, Derwent World Patents Index, Dialog file 351, 1986.
English language abstract of document AM1, WPI accession No. 91-327376/45, Derwent World Patents Index, Dialog file 351, 1991.
English language abstract of document AN1, WPI accession No. 94-036989/05, Derwent World Patents Index, Dialog file 351, 1994.
Brodin Arne
Carlsson Anders
Herslof Bengt
Nicklasson Martin
Rydhag Lisbeth
Astra AB
MacMillan Keith D.
Sanzo Michael A.
LandOfFree
Pharmaceutical preparation for pain management does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pharmaceutical preparation for pain management, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pharmaceutical preparation for pain management will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-402888