Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Patent
1994-03-16
1998-10-13
Krass, Frederick
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
424449, 424447, A61F 1302
Patent
active
058208755
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
1. Technical Field
This invention is in the field of medical devices for administering drugs transdermally. More particularly, it concerns a transdermal drug delivery device whose structure and composition is such that the skin flux of the drug varies in a controlled manner over the period of administration, typically from a high flux in the initial stage of administration to a lower flux in the later stage of administration.
2. Background
The efficacy of some systemically acting drugs may be optimized by administering them in a manner that produces therapeutically effective blood levels rapidly. The most common such method of administration is bolus injection. Oral administration, depending upon the ability of the drug to be absorbed into circulation via the gastrointestinal tract, may also afford a rapid onset of therapeutically effective blood levels.
Transdermal drug delivery, while often viewed as an advantageous mode of administration over injection or oral dosing, is not normally considered to be a practical means for achieving high blood levels of drug rapidly. This is because most transdermal devices operate in a manner that results in a significant lag time between placing the device on the skin and realizing the required or desired blood levels.
There are, however, two prior transdermal device designs that have been proposed for providing an initial burst or pulse of drug. The first of these designs is described in U.S. Pat. No. 4,060,084. It involves use of a drug reservoir layer in which the bulk of the drug is contained, an underlying rate-controlling membrane that controls the release rate of the drug from the reservoir, and a basal adhesive layer that is loaded with drug. When this type of device is placed on the skin, the drug in the adhesive migrates rapidly into the skin providing a "burst." The burst is followed by the controlled delivery of drug from the reservoir via the rate-controlling membrane. The second design is described in U.S. Pat. No. 4,698,062. It uses a first reservoir which contains a sufficient amount of the drug to provide a baseline flux over the entire administration period and a second reservoir which contains a permeation enhancer in an amount that is sufficient to provide enhancement only during the beginning of the administration period. With this design, the magnitude and duration of the period of enhanced drug flux is apparently dependent only upon the amount of enhancer contained in the second reservoir and its effect on skin flux. The patent indicates that this pattern of drug release may be achieved with various enhancers including ethanol, n-decylmethylsulfoxide, dimethyl lauramide, and polyethylene glycol monolaurate.
Prior workers have investigated certain aspects of transdermal drug delivery from binary solvent systems. Comfort et al., Proc. J. Intern. Symp. Control. Rel. Bioact. Mater. (1991) 18:297-298, describes the release of nitroglycerin through cadaver skin from solutions of nitroglycerin in mixtures of ethanol and water. Berner et al., J. Pharm. Sciences (1984) 78:402-407, also described the flux of nitroglycerin through skin from ethanol/water solutions. Their studies show that ethanol flux from the solution is a function of the ethanol/water ratio, with a maximum occurring at a ratio of 0.5:1 and that nitroglycerin flux is a linear function of ethanol flux. Kondo et al., Pharmaco. Ber. (1987) 10:587-594 and 743-749, report studies relating to the delivery of nifedipine through an ethylene-vinyl acetate membrane and skin from mixtures of acetone and propylene glycol and/or isopropyl myristate. They observed a transient increase in the flux of nifedipine from such mixtures which they attributed to the evaporation of the acetone from the mixture. They further teach adding polymeric agents to the solution to prevent the nifedipine from precipitating from the solution. Finally, Coldman et al., J. Pharm. Sciences (1969) 58:1098-1102, show that the 16 hour cumulative transdermal delivery of fluocinolide from a binary mixture of isopropyl a
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Beste Russell D.
Fallon Renee A.
Wilson Donald R.
Cygnus Inc.
Krass Frederick
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