Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Patent
1996-03-15
1998-05-05
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, 514946, 514947, A61F 1302
Patent
active
057470650
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
This invention relates to the transdermal delivery of biologically active oxybutynin. More particularly, this invention relates to novel methods and compositions for enhancing the percutaneous absorption of oxybutynin when incorporated in transdermal drug delivery systems. More particularly, but without limitation thereto, this invention relates to the transdermal delivery of oxybutynin utilizing a permeation-enhancing mixture of a monoglyceride and a lactate ester. Still more particularly, but without limitation thereto this invention relates to the transdermal delivery of oxybutynin utilizing a permeation-enhancing mixture of a monoglyceride and a lactate ester, wherein the composition contains from 15 to 25 wt % of a monoglyceride or monoglyceride mixture and from 8 to 25 wt % of lactate ester.
BACKGROUND OF THE INVENTION
The transdermal route of parenteral delivery of drugs provides many advantages over other administrative routes, and transdermal systems for delivering a wide variety of drugs or other beneficial agents are described in U.S. Pat. Nos. 3,598,122; 3,598,123; 3,731,683; 3,797,494; 4,031,894; 4,201,211; 4,286,592; 4,314,557; 4,379,454; 4,435,180; 4,559,222; 4,568,343; 4,573,995; 4,588,580; 4,645,502; 4,704,282; 4,788,062; 4,816,258; 4,849,226; 4,908,027; 4,943,435; and 5,004,610. The disclosures of the above patents are incorporated herein by reference.
In many instances, drugs which would appear to be ideal candidates for transdermal delivery are found to have such low permeability through intact skin that they cannot be delivered at therapeutically effective rates from reasonably sized systems.
In an effort to increase skin permeability, it has been proposed to pretreat the skin with various chemicals or to concurrently deliver the drug in the presence of a permeation enhancer. Various materials have been suggested for this purpose, as described in U.S. Pat. Nos. 3,472,931, 3,527,864, 3,896,238, 3,903,256, 3,952,099, 4,046,886, 4,130,643, 4,130,667, 4,299,826, 4,335,115, 4,343,798, 4,379,454, 4,405,616 and 4,746,515, all of which are incorporated herein by reference; British Pat. No. 1,001,949; and Idson, Percutaneous Absorption, J. Pharm. Sci., vol. 64, No. b6, June 1975, pp 901-924 (particularly 919-921).
To be considered useful, a permeation enhancer should have the ability to enhance the permeability of the skin for at least one and preferably a significant number of drugs. More importantly, it should be able to enhance the skin permeability such that the drug delivery rate from a reasonably sized system (preferably 5-50 cm.sup.2) is at therapeutic levels. Additionally, the enhancer, when applied to the skin surface, should be non-toxic, non-irritating on prolonged exposure and under occlusion, and non-sensitizing on repeated exposure. Preferably, it should be capable of delivering drugs without producing topical reactions, burning or tingling sensations.
The present invention greatly increases oxybutynin permeability through the skin, and also reduces the lag time between application of the oxybutynin to the skin and attainment of the desired therapeutic effect.
While it is known in the art to combine permeation enhancers, this invention utilizes a novel combination of a monoglyceride and a lactate ester. Further, the invention utilizes a specific concentration of each of the novel components. The combined effect and, further, specific concentrations of the components produce a significant and surprising improvement over use of either a monoglyceride or a lactate ester alone or the combination in nonspecified concentrations.
Neurogenic bladder disease is a disorder involving loss of control of urination. The major symptoms of this disease are urinary frequency, urinary retention or incontinence. There are two types of lesions that cause a neurogenic bladder. The first, upper motoneuron lesion, leads to hypertonia and hyperreflexia of the bladder, a spastic condition, giving rise to symptoms of urinary frequency and incontinence. The second lesion, a lower
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Tetrahedron Letters No. 20, pp. 1609-1612. Pergamon Pre
Burkoth Terry L.
Gale Robert M.
Lee Eun Soo
Watanabe Tyler
Phelan D. Gabrielle
Rafa Michael J.
Sabatine Paul L.
Stone Steven F.
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