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Composition containing levodopa and borneol, and application thereof

A technology of levodopa and composition, which is applied in the field of compositions containing levodopa and borneol, can solve problems affecting the effect of treatment, and achieve the effects of reducing drug dosage, prolonging drug action time, and increasing concentration

Inactive Publication Date: 2012-01-18
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The amount passing through the blood-brain barrier directly affects the amount of levodopa converted into dopamine in the brain, thereby affecting the therapeutic effect
At present, borneol or its derivatives or pharmacologically acceptable salts of these compounds are used in combination with levodopa for simultaneous, separate or sequential use in the treatment of disorders requiring restoration of dopamine function, particularly Parkinson's disease and Drugs for restless legs syndrome have not been reported

Method used

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  • Composition containing levodopa and borneol, and application thereof
  • Composition containing levodopa and borneol, and application thereof
  • Composition containing levodopa and borneol, and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Effect of different ratios of borneol and levodopa on the content of levodopa in cerebrospinal fluid in embodiment 1SD rats

[0030] Animals: In this study, ordinary SD rats (six groups in total, 12 rats in each group, weighing 200-250 g, half male and half male) were used in this study. They were adaptively raised in the laboratory for one week, and their behavior was observed.

[0031] Drug handling:

[0032] Levodopa: suspend the levodopa (416mg / kg) crude drug in PEG-400, and administer it orally with a volume of 1ml / 100g by intragastric administration.

[0033] Composition of levodopa and borneol (high dose): Grind borneol (600 mg / kg) into a fine powder, pass through a 100 mesh (aperture 0.15 mm) sieve, and then dissolve the powder in PEG-400 (polyethylene glycol-400) In, and levodopa (416mg / kg) crude drug is suspended in this solution, use oral administration with the volume of 1ml / 100g by gavage method.

[0034] Levodopa and borneol composition (medium dose): bo...

Embodiment 2

[0044] The influence of embodiment 2 borneol on levodopa cerebrospinal fluid pharmacokinetics

[0045] Drug handling:

[0046] Levodopa: suspend the levodopa (416mg / kg) crude drug in PEG-400, and administer it orally with a volume of 1ml / 100g by intragastric administration.

[0047] Composition of levodopa and borneol: grind borneol (300mg / kg) into a fine powder, pass through a 100 mesh (aperture 0.15 mm) sieve, then dissolve the powder in PEG-400, and mix levodopa (416mg / kg) The crude drug is suspended in this solution, and administered orally with a volume of 1ml / 100g by intragastric method.

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Abstract

The invention discloses a composition containing levodopa and borneol, and the application thereof. The composition comprises the levodopa and the borneol which have the mass ratio of 300:1-1:300. The composition can lead the concentration of the levodopa in the head to be increased by blood brain barrier, thus prolonging the maintaining time of the effective concentration of the levodopa in the head, reducing the peripheral concentration of the levodopa, and lowering the toxic and side effect. When being used for preparing the medicine for treating parkinson disease or restless Legs syndrome, the composition has little toxic and side effect and remarkable treatment effect, and is suitable for wide clinical application.

Description

technical field [0001] The invention relates to the field of pharmaceutical compositions, in particular to a composition containing levodopa and borneol and an application thereof. Background technique [0002] Parkinson's disease is a neurodegenerative disease involving different areas of the brain, especially the "stantia nigra", using dopamine as a neurotransmitter, resulting in slow, progressive disorders of movement, the main symptoms being bradykinesia, muscle stiffness, resting tremor and Postural instability, usually confirmed by a favorable response to pharmacologic therapy. Pharmacological treatment is based on the use of selegemide, anticholinergics, adamantanes, dopaminergic agonists, ergot alkaloids, levodopa, COMT (catecholamine-O-methyltransferase) inhibitors. [0003] Current drug therapy for Parkinson's disease is based on restoring dopamine function. Dopamine cannot pass the blood-brain barrier and therefore cannot be used to treat Parkinson's disease. Its...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/198A61K31/045A61P25/16A61P25/14
Inventor 李明亚周毅生冼嘉雯
Owner GUANGDONG PHARMA UNIV
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