Pramipexole nanocrystal transdermal gel and preparation method thereof

A pramipexole and nanocrystal technology, applied in the field of medicine, can solve the problems of low solubility, limit the amount of drug transdermal penetration, etc., and achieve the effects of good biocompatibility, improved drug compliance, and convenient operation.

Inactive Publication Date: 2017-12-26
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Pramipexole has good fat solubility, but its solubility in water is low, which greatly limits the transdermal penetration of the drug

Method used

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  • Pramipexole nanocrystal transdermal gel and preparation method thereof
  • Pramipexole nanocrystal transdermal gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Weigh 0.5% (w / v) Tween 80 and dissolve it in deionized water, stir to obtain a stabilizer solution, then weigh 2.0% (w / v) pramipexole to disperse in the above stabilizer solution, and ultrasonically disperse to obtain pramipexole Coarse suspension. Then, the pramipexole nanocrystals can be obtained by stirring for 4 hours at a rotational speed of 800 r / min by media grinding method. Carbomer 980 (1.0%, w / w) of the prescribed amount is dispersed on the surface of pramipexole nanocrystals, fully swelled, a few drops of triethanolamine are added dropwise, the pH is adjusted to 6-7, and the general pramipexole can be prepared by stirring evenly. Laxole nanocrystal transdermal gel. Detected with a laser particle size analyzer, the average particle diameter is 493.6nm, and the polydispersity index is 0.345.

[0029] Franz diffusion cell was used to measure the transdermal penetration rate of the rabbit ear skin, and the skin area of ​​the transdermal diffusion test was 0.71c...

Embodiment 2

[0031] Take by weighing 1.0% (w / v) hydroxypropyl methylcellulose and dissolve it in deionized water, stir to obtain a stabilizer solution, then weigh 1.5% (w / v) pramipexole and disperse it in the above-mentioned stabilizer solution, ultrasonic Disperse to obtain a coarse suspension of pramipexole. Then, the pramipexole nanocrystals can be obtained by stirring for 4 hours at a rotational speed of 800 r / min by media grinding method. Carbomer 980 (1.0%, w / w) of the prescribed amount is dispersed on the surface of pramipexole nanocrystals, fully swelled, a few drops of triethanolamine are added dropwise, the pH is adjusted to 6-7, and the general pramipexole can be prepared by stirring evenly. Laxole nanocrystal transdermal gel. Detected with a laser particle size analyzer, the average particle diameter is 405.2nm, and the polydispersity index is 0.357.

[0032] The Franz diffusion cell was used to measure the percutaneous penetration rate of the rabbit ear skin, and the skin ar...

Embodiment 3

[0034] Weigh 0.2% (w / v) poloxamer 188 and dissolve it in deionized water, stir to obtain a stabilizer solution, then weigh 2.0% (w / v) pramipexole and disperse in the above stabilizer solution, and ultrasonically disperse to obtain Pramipexole coarse suspension. Then, the pramipexole nanocrystals can be obtained by stirring for 4 hours at a rotation speed of 800 r / min by media grinding method. Carbomer 980 (1.0%, w / w) of the prescribed amount is dispersed on the surface of pramipexole nanocrystals, fully swelled, a few drops of triethanolamine are added dropwise, the pH is adjusted to 6-7, and the general pramipexole can be prepared by stirring evenly. Laxole nanocrystal transdermal gel. Detected with a laser particle size analyzer, the average particle diameter is 340.3nm, and the polydispersity index is 0.253.

[0035] The Franz diffusion cell was used to measure the percutaneous penetration rate of the rabbit ear skin, and the skin area of ​​the transdermal diffusion test ...

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Abstract

The invention relates to pramipexole nanocrystal transdermal gel and a preparation method thereof, belonging to the technical field of medicines. Pramipexole nanocrystals with uniform appearances are prepared by virtue of a medium grinding method, and the average particle size of the pramipexole nanocrystals is 200nm-400nm. The transdermal gel is prepared from the pramipexole nanocrystals, so that the transdermal permeation rate of pramipexole is remarkably increased, and pramipexole can permeate into a human body within 3 days at a constant speed. The pramipexole nanocrystal transdermal gel has moderate viscosity, low skin stimulation and good stability and is capable of remarkably improving the medication compliance of patients with Parkinson disease. Meanwhile, the pramipexole nanocrystal transdermal gel further has the advantages that a preparation process is simple, the quality is safe and stable, industrial production is easily realized, and the like.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a pramipexole nanocrystal transdermal gel and a preparation method thereof. Pramipexole nanocrystal transdermal gel can improve the percutaneous penetration properties of the active ingredient pramipexole. Background technique [0002] Parkinson's disease, also known as Parkinson's disease, is a common chronic degenerative disease of the central nervous system in middle-aged and elderly people. The clinical symptoms mainly include motor symptoms such as tremor, muscle rigidity, bradykinesia, and posture and gait instability, as well as non-motor symptoms such as dementia, depression, and psychosis. The current treatment mainly uses drugs to relieve symptoms, commonly used are dopamine receptor agonists, such as levodopa, pramipexole, rotivatin, ropinirole and so on. [0003] Pramipexole, whose chemical name is (S)-2-amino-4,5,6,7-tetrahydro-6-propylaminobenzothiazole, is a new...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/428A61K47/32A61K47/38A61P25/16
CPCA61K31/428A61K9/0014A61K9/06A61K47/32A61K47/38
Inventor 刘建平宋文婷李莹
Owner CHINA PHARM UNIV
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