Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Patent
1996-03-07
1998-09-08
Phelan, D. Gabrielle
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
424449, 424445, A61F 1302
Patent
active
058042148
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE DISCLOSURE
1. Technical Field
This invention relates to transdermal drug delivery.
2. Background Art
1. Monolithic Matrix Delivery Devices.
Transdermal delivery has become an increasingly acceptable mode for administration of prescription and nonprescription drugs, and considerable effort has been expended toward development of transderrnal drug delivery systems. A number of drugs have reached the market in transdermal delivery form, most popularly in the form of an adhesive patch.
Essentially, the methodology of transderrnal drug delivery involves placing the drug on the skin surface and allowing the drug to permeate through the skin. Transdermal delivery devices employ a structure that serves as a reservoir for the drug and that provides for bringing the drug into diffusive communication with the skin surface. In one general type, the structure includes a three-dimensionally stable matrix material having a discrete size and shape; such a structure may be referred to as a "monolithic matrix".
A variety of monolithic matrix formulations have been proposed for use in transdermal delivery systems.
U.S. Pat No. 5,149,538 describes transdermal delivery of opioids using an adhesive matrix prepared from polymers and copolymers of acrylic esters or methacrylic esters and copolymers of acrylic esters or methacrylic esters and other ethylenically-unsaturated monomers. Preferred acrylic adhesives are butyl acrylate, ethyl acrylate, ethyl hexyl acrylate, vinylacetate/ethylene acrylate and mixtures of these.
U.S. Pat No. 4,956,171 describes using sucrose cocoate and methyl laurate for permeation enhancement in transdermal delivery of buprenorphine HCl or hydromorphone HCl, in an adhesive matrix made up of polyacrylic polymers or vinyl acetate-acrylic polymers, and, particularly, a vinyl acetate-acrylic multipolymer solution marketed by Montsanto Co. under the name Gelva.RTM. 788.
German Patent Publications DE 38 43 239 and DE 38 43 238 describe transdermal delivery of physostigmine using a polymer matrix made up, in one example, of an acrylate copolymer of 2-ethylhexyl acrylate, vinyl acetate, and acrylic acid; a methacrylate copolymer of dimethylaminoethyl methacrylate and neutral methacrylic acid esters; and a triglyceride of capryl/caprinacids.
International Application No. PCT/US86/00789(WO 86/06281) describes a pressure-sensitive adhesive tape for transdermal delivery of nitroglycerin, having a pressure-sensitive adhesive coating made up of an acrylic adhesive copolymer including as a major constituent a hydrophobic monomeric acrylic or methacrylic acid ester of a C.sub.4-10 alkyl alcohol; and including a reinforcing monomer selected from acrylic acid, methacrylic acid, C.sub.1-3 alkyl acrylate or methacrylate, acrylamide, methacrylamide, t-butyl acrylamide, diacetone acrylamide, vinyl ether, substituted ethylene, and vinyl ester.
European Patent Publication No. EP 0 481 443 A1 describes a transdermal delivery system having a polymeric matrix made up of a acrylic polymer 7927 79 Rohm-Pharma.
2. Ketorolac tromethamine.
Ketorolac is a pyrrolizine carboxylic acid derivative. Combined with tromethamine, ketorolac forms a salt ("ketorolac tromethamine"), which has greater aqueous solubility than ketorolac. The chemical structure of ketorolac and ketorolac tromethamine are shown below: ##STR1##
Ketorolac tromethamine is a nonsteroidal anti-inflammatory drug useful for short-term management of moderate to severe pain. Ketorolac tromethamine is available via prescription in oral tablet form (10 mg strength) and in intramuscular injection form (30 mg/ml).
Ketorolac tromethamine has a chiral center and is used as a racemate marketed under the name Toradol; the ( -)-S isomer has many times greater analgesic potency than the ( +)-R isomer (A. Guzman et al., 1986). Ketorolac tromethamine is an off-white crystalline powder and has a pK.sub.a value of 3.49. Ketorolac is quite lipophilic with a log PC (partition coefficient) value of 2.72 (Muchowski et al., 1985). Ketorolac tromethamine is extremely stable in
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Nguyen Thuytien N.
Wong Ooi
Cygnus Inc.
Phelan D. Gabrielle
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