Use of rotigotine for treating the restless leg syndrome
First Claim
Patent Images
1. Use of (−
- )-5, 6, 7, 8-tetrahydro-6-[propyl [2-(2-thienyl)ethyl]amino]-1-naphtol for the treatment of Restless Leg Syndrome.
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Abstract
This invention relates to the use of rotigotine for the effective treatment of Restless Leg Syndrome (RLS) as well as to a rotigotine-containing transepicutaneous pharmaceutical composition, provided in particular in the form of an acrylate- or silicone-based Transdermal Therapeutic System (TTS) having a surface area of 2.5 to 20 cm2 and containing 0.1 to 3.15 mg/cm2 rotigotine as its active component against the Restless Leg Syndrome, said system leading in the human Restless Leg Syndrome condition to an improvement, compared to a placebo treatment, by 2 or more units on the International Restless Leg Syndrome Study Group (IRLSSG) scale after administration over a period of eight days.
149 Citations
24 Claims
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1. Use of (−
- )-5, 6, 7, 8-tetrahydro-6-[propyl [2-(2-thienyl)ethyl]amino]-1-naphtol for the treatment of Restless Leg Syndrome.
- View Dependent Claims (4)
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2. Use of (−
- )-5, 6, 7, 8-tetrahydro-6-[propyl [2-(2-thienyl)ethyl]amino]-1-naphtol in producing a medication for the transepicutaneous treatment of the Restless Leg Syndrome.
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3. Use of (−
- )-5, 6, 7, 8-tetrahydro-6-[propyl [2-(2-thienyl)ethyl]amino]-1-naphtol in producing a transdermal therapeutic system (TTS).
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5. Transdermal therapeutic system comprising a backing that is inert relative to the components of the matrix, a self-adhesive matrix layer containing (−
- )-5, 6, 7, 8-tetrahydro-6-[propyl [2-(2-thienyl)ethyl]amino]-1-naphtol, and a protective film that is to be removed prior to use, characterized in that the matrix
a) includes as a substrate a non-aqueous, acrylate- or silicon-based polymer adhesive, b) has a solubility of ≧
5% (g/g) for its free base (−
)-5, 6, 7, 8-tetrahydro-6-[propyl [2-(2-thienyl)ethyl]amino]-1-naphtol, andc) contains the free base (−
)-5, 6, 7, 8-tetrahydro-6-[propyl [2-(2-thienyl)ethyl]amino]-1-naphtol in an effective quantity. - View Dependent Claims (6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16)
- )-5, 6, 7, 8-tetrahydro-6-[propyl [2-(2-thienyl)ethyl]amino]-1-naphtol, and a protective film that is to be removed prior to use, characterized in that the matrix
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17. Method for producing a transdermal therapeutic system, encompassing the following procedural steps:
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i) Mixing of a suspension of (−
)-5, 6, 7, 8-tetrahydro-6-[propyl [2-(2-thienyl)ethyl]amino]-1-naphtol hydrochloride in ethanol with an alkaline compound in ethanol for converting the hydrochloride into its free base;
ii) Filtering of the resulting suspension if and as necessary;
iii) Addition of polyvinyl pyrrolidone and an adhesive solution; and
iv) Drying of the product. - View Dependent Claims (18, 19, 20, 21)
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22. Use of a silicone-based transdermal therapeutic system with a surface area of 5 to 20 cm2 and containing 0.1 to 3.15 mg/cm2 rotigotine as its active component, for producing an anti-Restless Leg Syndrome medication which in a human patient afflicted with Restless Leg Syndrome brings about an improvement, compared to a placebo treatment, by 2 or more units on the International Restless Leg Syndrome Study Group (IRLSSG) scale after at least eight days of application.
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23. Method for treating the Restless Leg Syndrome by applying a transdermal therapeutic system having a surface area of 5 to 20 cm2 and containing 0.1 to 3.15 mg/cm2 rotigotine as its active component, on a patient afflicted with that disease, leading to an amelioration of the patient'"'"'s condition by about 2 or more units on the Restless Leg Syndrome Study Group scale, as compared to a placebo treatment, after administration over a time period of 8 days.
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24. Transdermal therapeutic system for treating the Restless Leg Syndrome, having a size of 5 to 20 cm2 and containing in its matrix 0.4 to 0.5 mg/cm2 rotigotine as its active component, said matrix comprising primarily a mixture of at least two amine-resistant silicone-based adhesives.
Specification