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Method for treatment of Parkinson's disease

一种帕金森病、组合物的技术，应用在帕金森病的治疗领域，能够解决没有提供帕金森病最佳治疗等问题

Inactive Publication Date: 2015-12-30
NEURODERM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, the various formulations disclosed do not provide optimal treatment of Parkinson's disease due to still relatively high levels of side effects and fluctuations in levodopa blood levels

Method used

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  • Method for treatment of Parkinson's disease
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  • Method for treatment of Parkinson's disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Example 1. Preparation of solutions / formulations for subcutaneous administration

[0063] A. A 2% carbidopa solution / formulation was prepared by adding a pre-warmed 0.1% sodium bisulfite solution to carbidopa [ASSIAL Ltd.]. Arginine (Merck) was added to obtain a final molar ratio of CD(carbidopa):Arg(arginine) of 1:1.2. The mixture was stirred at 60 °C until complete dissolution was obtained. Heating was stopped and the preparation was allowed to cool to RT; pH of 8.5. The solution was filtered through a sterile 0.22 μM PVDF membrane.

[0064] B. Prepare a 10% tolcapone solution / formulation as follows: by adding the corresponding amount of H 2 O was added to tolcapone (Synfine Research), a solution containing 10% tolcapone was prepared and arginine was added slowly with stirring to obtain a final molar ratio of 1:1. Stir the mixture until complete dissolution is obtained. After cooling, the pH of the solution was 7.8.

[0065] C. A solution containing 10% entacapo...

Embodiment 2

[0070] Embodiment 2. preparation preparation process

[0071] Levodopa (LD) and carbidopa (CD) formulations can be prepared as follows. However, as shown in Table A, the method of preparation has a significant impact on the final physical and chemical stability of the composition.

[0072] Method 1 (L-Arg solution) . L-Arg and Na-Bis (sodium bisulfate) were dissolved in water. The solution was added to the LD and CD powders. The mixture was heated and stirred at 75 °C for 13 min until complete dissolution. The LD / CD solution was kept at RT for 10 min to cool down.

[0073] Method 2 (all powders together) . All powders (LD, CD and L-Arg) were weighed and water containing Na-Bis was added. The suspension was heated and stirred at 75 °C for 13 min until completely dissolved. The LD / CD solution was kept at RT for 10 min to cool down.

[0074] Method 3 (same as 2 but without Na-Bis preheat) . All powders (LD, CD and L-Arg) were weighed together and water was added. ...

Embodiment 3

[0087] Example 3. Effect of arginine on the long-term stability of levodopa and levodopa / carbidopa compositions

[0088] Prepare liquid formulations with levodopa, carbidopa and arginine using the procedure outlined in Example 2, and compare studies prepared with different concentrations of arginine, and / or amino sugars (e.g. meglumine) , and / or sugar (eg dextrose), and / or base (NaOH), or other basic amino acids (eg lysine, histidine) formulations. The results are shown in Table B.

[0089] Form B

[0090]

[0091] * Lys - lysine; His - histidine; Arg - arginine; Dex - dextrose; Meg - methylglumine; NA - not available.

[0092] Table B shows that arginine forms stable solutions with high concentrations of levodopa and carbidopa (>2.5%) at molar ratios <1:2.5, whereas with other basic amino acids, LD Not even soluble. At molar ratios of LD / CD to arginine of 1:<2, solutions have no long-term stability unless meglumine or another counterion is used, and meglumine can be u...

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Abstract

The present invention provides a method for treatment of a neurological or movement disorder, e.g., Parkinson's disease, in an individual in need thereof, by parenteral administration of a composition comprising carbidopa and levopoda, or pharmaceutically acceptable salts thereof, and concomitant oral administration of a catechol-O-methyl transferase (COMT) inhibitor, e.g., entacapone or tolcapone.

Description

technical field [0001] The present invention provides for the treatment of e.g. Parkinson's by parenteral administration of levodopa and carbidopa with concomitant oral administration of COMT inhibitors such as entacapone and tolcapone approach to neurological or motor disorders such as disease. Background technique [0002] Parkinson's disease is a degenerative condition characterized by decreased concentrations of the neurotransmitter dopamine in the brain. Levodopa (L-dopa or L-3,4-dihydroxyphenylalanine), the immediate metabolic precursor of dopamine, unlike dopamine, is able to cross the blood-brain barrier and is most commonly used to restore brain concentration of dopamine in . For the past 40 years, levodopa has been the most effective therapy for Parkinson's disease. [0003] However, even with the best current standard of care, levodopa has a short half-life in plasma, resulting in pulsatile dopamine stimulation. Thus, for some patients long-term treatment is c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/121A61K31/198A61K31/277A61P25/16
CPCA61K31/121A61K31/198A61K31/277A61P25/16A61P43/00A61K2300/00A61K9/0053A61K31/195A61K9/0019
Inventor 奥伦·亚柯比-泽维
Owner NEURODERM
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