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Use of rotigotine for treatment or prevention of dopaminergic neurone loss

A dopaminergic and useful technology, applied in the field of use of rotigotine for treating or preventing the loss of dopaminergic neurons, can solve the problem that the preventive treatment of Parkinson's disease cannot be guaranteed and the like

Inactive Publication Date: 2007-01-17
UCB SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Parkinson's drugs that are effective only for symptoms do not guarantee an advantage in the preventive treatment of Parkinson's disease because they have no effect on the destruction of dopaminergic cells and on the progression and / or intensity of the disease

Method used

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  • Use of rotigotine for treatment or prevention of dopaminergic neurone loss
  • Use of rotigotine for treatment or prevention of dopaminergic neurone loss
  • Use of rotigotine for treatment or prevention of dopaminergic neurone loss

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0120] Embodiment 1: Rotigotine plaster

[0121] 1.8 g rotigotine (free base) was dissolved in 2.4 g ethanol and 0.4 g Kollidon 90F (dissolved in 1 g ethanol) was added. This mixture was added to a 74% solution of silicone polymer in heptane (8.9 g BioPSA 7-4201 + 8.9 g BIO-PSA 7-4301 [DowComing]). After adding 2.65 g of petroleum ether, the mixture was stirred at 700 rpm for 1 hour in order to obtain a homogeneous dispersion. After layering in polyester, it was dried at 50°C. The final weight of the plaster was 50 g / cm2.

Embodiment 2

[0122] Example 2. Rotigotine depot suspension

[0123] (a) Weigh 1411.2 g of Miglyol 812 into a Duran flask. 14.4 g of Imwitor 312 were added to the Miglyol and heated to 80°C for 30 minutes with stirring. The clear solution was cooled to room temperature and filtered.

[0124] (b) 1188 g of the solution produced in (a) were transferred to a glass laboratory reactor, 12 g of rotigotine were added and homogenized in an Ultraturrax at 10,000 rpm under nitrogen for 10 minutes. The suspension was poured gently into a brown glass bottle while running the Ultraturrax (2,000 rpm).

Embodiment 3

[0125] Example 3: Subacute MPTP Model

[0126] For intoxication purposes, 80 mg / kg of the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydro-pyridine (MPTP) was administered to mice (20 mg / kg in batches at two intervals). hours, groups 3 to 6 in Figures 1 and 2), which can lead to about 50 to 60% of neuron degeneration in the substantia nigra (group 3 in Figures 1 and 2 has the greatest degeneration). Rotigotine was administered daily for 7 days at doses of 0.3, 1 or 3 mg / kg as a so-called "sustained release formulation" (see Example 2) (groups 4 to 6 in Figures 1 and 2). A rotigotine vehicle solution (see Example 2 without rotigotine HCl) was administered to a group of MPTP-treated animals (group 3) and served as reference. Groups 1, 2 and 7 served as controls whereby group 1 received no treatment at all, group 2 was treated with a vehicle solution of MPTP and rotigotine and group 7 received rotigotine alone. Animals were sacrificed on day 8 and their brains were removed and f...

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Abstract

The invention relates to the use of rotigotine or salts thereof and prodrugs for the production of a medicament for the treatment or prevention of dopaminergic cell destruction in diseases which are connected to increased dopaminergic cell destruction. The invention also relates to the use of rotigotine as a medicament for the preventive treatment of Parkinson's disease.

Description

[0001] introduce Background technique [0002] Parkinson's disease arises as a result of chronic, progressive neuronal degeneration, the causes of which are not fully understood. The main symptomatic forms shown clinically are resting tremor, rigidity, bradykinesia and postural instability. [0003] Drugs initially used to relieve motor symptoms were levodopa, dopamine agonists such as rotigotine, pramipexole, bromocriptine, ropinirole, cabergoline, pergolide, apomorphine, and lisuride , anticholinergic drugs, NMDA antagonists, β-blockers, and MAO-B inhibitor selegiline (selegeline) and COMT inhibitor entacapone. Most of these active substances are able to interfere with dopaminergic and / or cholinergic signaling cascades and in this way affect symptomatically the movement disturbances typical of Parkinson's disease. [0004] So far, Parkinson's disease has been treated starting from the main symptoms. If at least two of the four cardinal symptoms (bradykinesia, resting trem...

Claims

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Application Information

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IPC IPC(8): A61K31/381A61P25/16
CPCA61K31/381A61P25/16A61P25/28A61P43/00
Inventor D·谢勒F·德雷森
Owner UCB SA
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